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Clinical Pharmacology
Module 1. Autonomic Nervous System
• Chapter 1: Functions of Autonomic Nervous System
• Chapter 2: Adrenergic Drugs
• Chapter 3: Cholinergic Drugs
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1
Autonomic Nervous System
Nervous System
Cholinergic Adrenergic
Functions of ANS
• The autonomic nervous system controls involuntary body functions. The ANS is
composed of two divisions.
• Sympathetic (adregenic) system
• Parasympathetic (cholinergic) system
1-1
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• Glandular activity
• Hormonal activity
• Ensure that the body operates in optimum range
1-2
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AUTONOMIC SOMATIC
Sympathetic innervation Sympathetic Parasympathetic
of adrenal medulla
Preganglionic
neuron
Ganglionic
transmitter
Adrenal medulla
Postganglionic
neurons
Adrenergic
Adrenergic Muscarinic
receptor Nicotinic
receptor receptor
receptor
Effector organs Striated Muscle
1-3
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2
Adrenergic Drugs
There are four types of adrenergic receptors. These are alpha1 and alpha2 and βeta1
and βeta2. Alpha receptors are located mainly in the blood vessels and pupils. Βeta1
receptors are in the heart and βeta2 receptors are mainly in the lungs, skeletal muscles
and uterus.
Adrenergic Drugs
2-1
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Adrenergic receptors
ᾳ Receptors ᾳ2 Receptors
Located on vascular smooth muscle of the skin Located in presynaptic nerve terminals,
and splanchnic regions, the gastrointestinal platelets, fat cells and the walls of the GI tract
(GI) and bladder sphincters, and the radial Often produce inhibition (eg. Relaxation or
muscle of the iris. dilation)
Produce excitation (eg. Contraction or Mechanism of action: inhibition of adenylate
constriction). cyclase and decrease in cyclic adenosine
Equally sensitive to norepinephrine and Monophosphate (c AMP).
epinephrine, but only norepinephrine is
Present in concentrations that are high enough
to activate ᾳ receptors.
Mechanism of action: formation of inositol
1,4,5-triphosphate (IP3) and increase in
Intracellular (Ca2+).
ẞ1 Receptors ẞ2 Receptors
Located in the sinoatrial (SA) node, Located on vascular smooth muscle of skeletal
atrioventricular (AV) node, and ventricular muscle, bronchial smooth muscle, and In the
muscle of the heart. walls of the GI tract and bladder.
produce excitation (eg. Increase heart rate, Produce relaxation (eg. Dilation of vascular
increase conduction velocity, increase smooth muscle, dilation of bronchioles,
Contractility). Relaxation of the bladder wall).
Sensitive to both norepinephrine and More sensitive to epinephrine than to
epinephrine and more sensitive than the ᾳ1 norepinephrine.
Receptors. More sensitive to epinephrine than the ᾳ1
Mechanism of action: activation of adenylate receptors. For example, when small amounts
cyclase and production of c AMP. of epinephrine are released from the adrenal
medulla, Vasodilation (ẞ2) occurs; when larger
amounts of epinephrine are released from the
Adrenal medulla, vasoconstriction (ᾳ1) occurs.
Mechanism of actions: same as for ẞ1
receptors.
Important Concept!
• Alpha1. peripheral vascular constrictors (blood vessels)
• Alpha2. inhibitory receptor act on norepinephrine in brain
• Beta1. Increase HR, Conduction, Contraction on heart, ↑Renin secretion
• Beta2. Branchodilators in lung, relaxation of bladder detrussors, vasodilator in skeletol muscles.
2-2
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α1agonists
• Phenylephrine
• Pseudoephedrine
• Ephedrine
• Methoxamine
• Xylometazoline
2-3
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β 2 agonist
2-5
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Epinephrine (adrenaline)
Dopamine
Mechanism. Act on D1, D2, D3, D4, D5, and mixed α1and α2, β1, β2 agonist. Activate
alpha and beta adrenergic receptor. At higher doses it causes vasoconstriction by
activating alpha receptor, whereas at lower dose, it stimulates beta receptor. In
addition, D1 and D2 dopaminergic receptor, occur in the mesenteric and renal vascular
beds where binding of dopamine produces vasodilation.
Major affects
• Has +ve inotropic and +ve chronotropic effects
• Dilates renal arterioles by increasing blood flow to kidney
• Dopamine is drug of choice for shock given by continuous infusion.
2-6
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Adrenergic Antagonist
Adrenergic antagonist
α1 antagonist α2 antagonist
α1 antagonists
α2antagonist
2-7
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α1 & α2 antagonists
α1 & α2 antagonist
Beta Blockers
Beta Blockers
Nonselective (β 1 & β2) Cardioselective β1, β2 & α1 blockers Partial agonist &
(β 1 only) antagonist
• Propranolol • Esmolol • Labetalol • Acebutolol
• Pindolol • Metoprolol • Carvedilol • Pindolol
• Nadolol • Acebutolol • Oxprenolol
• Timolol • Atenolol
• Levobutolol • Bisoprolol
2-8
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Side effects
• Bradycardia, heart blockage
• Bronchospasm (avoid non selective in asthma)
• Avoid beta blockers in peripheral vascular disease such as Raynaud’s phenomenon
and intermittent claudication however carveidilol and labetalol can be tried.
• CAUTION in congestive heart failure and left ventricular dysfunction.
Pharmacokinetics
• Propanolol is the best absorbed with food but consistency is the most important
factor.
• Metoprolol is best taken with meals
• These drugs shoukd be taken at about same time everyday.
• Beta blockers that have first pass metabolism propanolol and timolol
• Beta blockers that have no biotransformation atenolol.
• Beta blockers that have alpha blockade effect; labetalol and carveidilol
• Beta blockers that acts as membrane stabilizer is propanolol.
Beta-blockers therapeutic uses.
• Propranolol is used for hypertension, angina, post MI, migraine, essential tremor,
performance anxiety, Hyperthyroidism (acute-thyroid storm).
• Timolol is used for chronic treatment of open angle glaucoma. hypertension, post
MI, and migraine.
• Pindolol used for hypertension
• Cardioselective, metaprolol, atenolol, esmolol and acebutolol used to treat for
hypertension, angina and tachycardias.
Tips
• Drugs that have +ve inotropic and +ve chronotropic effect is dopamine and
epinephrine
• Inotropic is force of contraction (+ve increase in force of contraction)
• Chronotropic isheart rate (+ve increase in heart rate)
• Drugs that have +ve inotropic and –ve chronotropics is digoxin
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Pheochromacytoma: Type of adrenal gland cancer, can cause uncontrolled blood pressure. Can cause
uncontrolled tachycardia, and increase heart rate and palpitation
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3
Cholinergic Drugs
The parasympathetic (cholinergic) system slows the heart, constricts the pupil, and
stimulates the GI tract and aids in digestion and elimination. Drugs with a cholinergic
effect will produce similar effects. A cholinergic effect may be direct acting drugs
occupy the cholinergic receptor. Indirect acting drugs inhibit the activity of
cholinesterase, an enzyme that breaks down acetylcholine. By preventing the
breakdown of acetylcholine, there is an accumulation of acetylcholine allowing
increased parasympathetic effects.
Cholinergic
Cholinesterase
Acetylcholine -------------> Acetyl + Choline
3-1
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Pilocarpine
Mechanism. A cholinergic agent most often used to treat
glaucoma since it produces a reduction in intraocular
pressure.
Side effects. Cramps, diarrhea, and increased gastric
acid. May cause bradycardia, flushing and a fall in blood
pressure, bronchoconstriction causing difficulty in
breathing, sweating and salivation.
3-3
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Muscarinic antagonist
Muscarinic antagonists
Anticholinergic • Atropine, ipratropium, tiotropium, scopolamine, benztropine
drugs • tropicamide, glycopyrrolate, and trihexyphenidyl.
Pharmacological • ↓ in salivation cause dry mouth (xerostomia).
actions • ↓ intestinal secretion cause constipation
• Increase HR cause tachycardia
• Mydriasis cause pupil dilatation
• Relaxation of detrussor muscle cause urinary retention.
3-4
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NMJ blockers
These agents are used for surgical patients to relax the muscles during surgery.
Pharmacological actions. Blocks the cholinergic transmission between motor nerve and
nicotinic receptors. Antagonizes (non depolarizing type) and agonist (polarizing) the
effect of acetycholine.
3-5
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Myastenia gravis. This disease is a disorder of skeletal (voluntary striated) muscle due to
excessive cholinesterase or lack of acetylcholine (ACh). It is characterized by increasing
fatigue and muscle weakness; some cases are mild, some are severe. Death usually
occurs due to respiratory depression.
Urinary retention is the inability to empty the bladder. It can be due to a number of
conditions such as old age, prolonged surgery, tumours, distended bladder without
voiding for long periods, exposure to cold or anemia.
3-6
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4
Antihypertensive Drugs
This chapter review antihypertensive drugs such as angiotensin converting enzyme inhibitors (ACEi),
Angiotensin receptor blockers (ARBs), beta blockers, alpha1 blockers, calcium channel blockers (CCBs) and
vasodilators mechanism of action, major therapeutic use, side effects, pharmacokinetics, dosage forms
and instructions for counseling.
ACE Inhibitors
B P
Angiotensin I Angiotensin II
Bradykinin
ACE I
Na & H2O levels
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Pharmacological actions
ACE inhibitors block the angiotensin converting enzyme that cleaves angiotensin I to
form, angiotensin II. The angiotensin II is potent vasoconstrictor. It also decreases
the secretion of aldosterone resulting in decreased sodium and water retention.
Therapeutic use: 1ST line to treat heart failure, diabetes nephropathy, post MI ,
uncomplicated hypertension, and pre-hypertensive patient, LVH (left ventricular
heart failure) and prior CVA/TIA (cardiovascular attacks/transient ischemic attacks)
& in renal disease
Pharmacokinetics
• DIs. NSAID’s can reduce the effect of captopril. Diuretics can cause rapid fall of blood
pressure with captopril.
• High fat meals may reduce absorption of quinapril. Food does not affect the other
drugs in this class.
• Captopril should be taken one hour before meals. Dosage captopril is taken bid or
tid due to short half life.
• Call doctor ASAP if you experience swelling of the face, eyes, lips, tongue, arms, or legs, or if you have
difficulty breathing or swallowing (symptoms of angioedema).
• In case of cause cough symptoms contact doctor to change the medication to ARBs.
Pharmacological actions
• Angiotensin binds to its own receptors are found on vascular muscle and in the
adrenals. Stimulation leads to vasoconstriction and release of aldosterone in the
adrenal gland. It blocks aldosterone secretion
• Losartan has moderate uricosuric effects and may be useful in patients with gout or
hyperuricemia who require antihypertensive therapy.
Side effects. Less dry cough (cough associated with ACEi does appear with these drugs),
bradykinin causes vasodilation of arterioles and venules results ↓TPR, less dry cough.
Dizziness, hypotension(syncope), renal dysfunction (reversible renal failure),
hyperkalemia and angioedema.
Contraindications. Pregnancy (renal fetal toxicity), and bilateral renal artery stenosis
(stenosis, abnormal narrowing of passage or opening, such blood vessels or heart valve).
Direct Renin inhibitors. Aliskiren 150 mg once daily. Takes 4 weeks to 6 wks realize maximum
antihypertensive effect.
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Side effects. Diarrhea, the incidence of dry cough, and hyperkalemia is low compared with
ACEi.
Avoid use in pregnancy.
β-blockers
Beta-blockers are used to treat hypertension and angina. These drugs act by slowing
the heartbeat, which results in lowered blood pressure since blood pressure is affected
by the heart rate and peripheral resistance. Beta-blockers are categorized into 4 types
based on their action on sympathetic receptors beta1, beta2, alpha1, and alpha2 action.
Beta Blockers
Pharmacological actions
• β 1 decrease heart rate
• β 2 bronchoconstriction
• Peripheral vasoconstriction (Increase TPR)—β 2
• ↓ Na/water retention
• β 2 ↓ glycogenolysis (glycogen glucose) and gluconeogenesis.
• ↓ glucagon secretions
• Blocks the effect of isoproterenol
Therapeutic use. Beta-blockers are used to treat hypertension and angina. Because of
its action on the lining of arteries, propranolol is also used migraines and it highest lipid
soluble beta blocker.
Abrupt discontinuation may cause rebound hypertension. Labetelol & carvedilol may
cause orthostatic hypotension due to partial alpha blockade.
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α1 blockers
In addition to being used for hypertension these drugs cause the muscles (sphincter) of
the bladder neck and prostate to relax, thereby making it easier for patients to urinate
thus also used for benign prostatic hyperplasia.
Alpha 2 agonist used to treat hypertension are centrally acting agents, which act directly
in the brain to change the signals send to the heart and blood vessels.
Pharmacological actions
• Decrease central adrenergic outflow.
• α2 receptors have inhibitory action on epinephrine and NE.
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• Bradycardia (little)
Side effects. Clonidine may cause severe rebound hypertension, decrease lipolysis,
decrease insulin secretions, and sexual dysfunction. Methyldopa has cardiovascular,
bradycardia, orthostatic hypotension, blood related hemolytic anemia,
thrombocytopenia and bone marrow depression. The GI related include dry mouth,
nausea, and diarrhea.
Clonidine. Don’t discontinue abruptly, reduce dose over 2 to 3 days to reduce sever
hypertension.
Clonidine comes as transdermal patch TT1 (release 0.1 mg/24 h), TT2 (0.2 mg 24/h). TT3
(0.3 mg/24 h). Pruritus and rash at the site of transdermal patch.
α 1 antagonist α 2 agonist
Indication Hypertension, Benign Prostatic Hypertension and Treat withdrawal symptoms in
Hypertrophy (BPH or enlarged recovering drug and alcohol abusers (clonidine)
prostate).
DIURETICS
Diuretics also known as water pills.
Mannitol
"Distal convoluted "Ascending "Collecting duct" Urea
tubule" loop" Spironolactone "proximal"
Triamterene
Chlorothiazide Furosemide Acetazolamide
Amiloride
Hydrochlorothiazide Ethacrynic acid Dorzolamide
Chlothalidone Bemetanide
Thiazide Diuretics
B.P.
Loop Diuretics
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Potassium sparing
Osmotic Diuretics
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Vasodilators
Vasodilators
Important Concepts!
Preload. Volume of blood that fills the ventricle during diastole.
After load. The pressure that must overcome for the heart to pump blood into
the arterial system.
Decrease more diastolic blood pressure than systolic blood pressure
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Vasodilators cause the smooth muscle in blood vessels to relax. Relaxed or dilated
blood vessels allow more blood to flow through, causing a reduction in blood pressure
by decreasing peripheral resistance. As vasodilators work, the blood vessels become
dilated causing a drop in pressure because there is less blood volume to fill the vessel.
The body can compensate for this by retaining enough fluid to fill the blood vessel
sufficiently to raise the blood pressure again.
Hydralazine and minoxidil are direct vasodilators not usually used a sole therapy for high
blood pressure, as their effect is usually short lived when administered alone.
Side effects: flushing and headache
Pharmacological action
• Vasodilators reduce excessive preload and after load.
• Elevated after load causes the heart to work harder to pump blood into arterial
system.
• Dilation of venous blood vessels leads to decrease in cardiac preload by increasing
venous capacitance.
• In arteries dilators reduce systemic arteriole resistance and decrease after load.
Minoxidil
Sodium Nitroprusside
Mechanism • Dilates both resistance and capacitance vessels.
• Nitroprusside when come in contact with red blood cells produces
nitric oxide (NO), which then stimulates guanylate cyclase.
Therapeutic Drug of choice for hypertensive crisis.
use
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Diazoxide
Hydralazine
Ca2+CHANNEL BLOCKERS
These agents are used to treat hypertension and are effective in treating angina as well.
All muscles, including the smooth muscle of the blood vessels, require calcium in order
to contract. If the CCB block the entrance of the calcium into the muscle, the muscle will
not contract. This will allow the muscle to relax and subsequently reduce the blood
pressure. Other therapeutic uses angina, migraine, and antiarrhythmic.
Nondihydropyridine
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• Diltiazem hydrochloride
• Verapamil hydrochloride
Mechanism
• Verapamil similar to beta blockers in effect
• Verapamil can
cause
bradycardia
• The effect on
heart is graded
from higher to
lower.
Verapamil>Diltiazem>Nifedipine
• Verapamil-avoid using in CHF (cause -ve inotropic effect)
and constipation
Dihydropyridine
• Nifedipine
• Felodipine
• Amlodipine
• Nicardipine
Side effects
• Flushing, headache
• Profound low blood pressure
• Swelling of legs and feet.
• constipation and stomach upset.
• If ankle edema (swelling) of legs and feet occurs, a diuretic
may be added to the regimen.
The most common SEs dizziness, hypotension, headache, peripheral and pulmonary
edema.
Duration of action ranges 4-8 hrs.
Verapamil 4hr (TID to QID)
Diltiazem 6-8hrs (TID to QID)
Nifedipine 4-8hrs (TID to QID)
Nicaradipine 6-8hrs (TID to QID)
Amlodipine 24hr once Daily
Dihydropyridines
Adalat, Adalat XL
Mechanism A calcium blocker which interfere with conduction of signals in
the muscles of the heart and vessels.
Therapeutic use
Given regularly to prevent angina attacks. Reduce high blood
pressure and is often helpful in improving circulation to the limbs
in disorders such as Raynaud’s disease.
Side Effects Blood pressure will fall too low’ and sometimes causes heart
rhythm.
Tachycardia, flushing, headache, dizziness, orthostatic
hypotension, and edema.
Amlodipine
Mechanism A calcium blocker which interfere with the conduction of signals
in the muscles of heart and vessels.
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Therapeutic use Angina and chest pain. Can be safely used by asthmatic and non-
insulin-dependent diabetic.
Side Effects May cause mild to moderate leg and ankle swelling (arterial). and
hypotension.
Non dihydropyridines
Tips
Tips
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5
Antihyperlipedemic Drugs
Classification of antihyperlipidemic drugs
HMG-CoA reductase inh. Nicotinic acid Bile acid Fibric acid Cholesterol
sequesterants derivatives Absorption
inhibitors
Lovastatin Niacin
Simvastatin Act at liver Cholestyramine Gemfibrozil
Pravastatin Ezetimibe
Cholestipol Clofibrate
Fluvastatin Act at GIT Fenofibrate
Atorvastatin Compete with bile salts
Rosuvastatin prevents reabsorption
Increased intracellular cholestrol results from LDL catabolism inhibits the activity of 3-
hydroxy-3-methyl glutaryl-coenzyme A (HMG-CoA) reductase, the rate limiting enzyme
for intracellular cholesterol biosynthesis.
Statins
Generic Name Trade Name Generic Name Trade Name Generic Name Trade Name
Atorvastatin LIPITOR Fluvastatin LESCOL Simvastatin ZOCOR
Lovastatin MEVACOR Pravastatin PRAVACHOL Rosuvastatin CRESTOR
Acetyl CoA
HMG CoA
HMG CoA Statins
Reductase
Mevalonic acid
Cholesterol
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Statin
Atorvastatin Fluvastatin Lovastatin Pravastatin Rosuvastatin Simvastatin
Metabolizing CYP3A4 CYP2C9 CYP3A4 not known CYP2C9 CYP3A4
Enzyme (s)
Grapefruit juice Avoid Avoid Avoid
Take Anytime At night At night At night
Food With or With or With or With or With or With or
without after after without without without
Statins (A= atorvastatin, L=lovasatin, F=fluvastatin, S = simvastatin, P = pravastatin); FLS = take at bed time (night); ALS = avoid
grapefruit juice (because grape fruit juice inhibit CYP 3A4); ALS = avoid grapefruit juice (substrate CYP3A4); FLS = take at bedtime; FL
= take with food; A = any time of the day; PF = can taken with grapefruit juice; P = least drug interaction
Pregnacy. All statins are contraindicated to use in pregnancy, breast feeding, and children.
Monitoring. LFT, evaluate liver function and measure serum transaminases and creatin
kinase CK-MM.
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Therapeutic use. Decrease TG levels, LDL levels and increase HDL levels (moderately).
Very useful in treatment of hypertriglyceridemia in diabetic patients. Prophylaxis for
coronary heart disease and cerebrovascular diseases.
Side effects. Mild GI disturbances. Drug may cause excretion of cholesterol into the bile
leading to cholelithiasis. If tested discontinue the drug. Lithiasis predispose gallstone
formation.
Drug Interactions. Combination with statins may lead to myopathies, or rhabdomyolysis.
Contrainidcations. Sever hepatic and renal dysfunction, potentiates warfarin activity.
Preexisting gall bladder disease.
Monitoring. At 3, 6 and 12 mo, and yearly liver function test. Creatinin kinase complete
blood count, and renal function test.
Pharmacokinetics. Fibrates renally eliminated. Thus no hepatotoxicity. Need dose
adjustment in renal disease.
• Fibrates decrease serum uric levels (uricosuric effect) in normal patients and
hyperuricemic patients.
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Antihyperlipidemics
Elimination Food LFT CK- Uric Tips
MM acid
Atorvastatin Biliary (feces) +
Fluvastatin Biliary (feces) +
Lovastatin Biliary (feces) With +
food
Pravastatin Biliary (feces) +
Rosuvastatin Biliary (feces) +
Simvastatin Biliary (feces) +
Niacin Biliary (feces) + + Avoid in uncontrolled diabetics
Least likely used combination niacin + statin
Fibrates Renal/Biliary LFT/ Good for lowering TG
(feces) RFT Monitor CK, CBC, liver and renal function
Ezetamibe Statin+ezetamibe
Fibrate+ezetamibe
Resins hepatic LFT Monitor LFT and TG
• Pravastatin not extensively metabolized by CYP450. Can be taken with grapefruit juice.
• Should not be used in patients with active liver disease. (statins & niacin)
Resins (Bileacidsequestrant)
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Ezetimibe
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6
Nitrates and Nitroglycerin
Nitrates are antianginal agents. The most common complications associated with
coronary artery disease includes angina pectoris, MI, post MI, ischemic stroke.
Insuficient supply of oxygen to heart can lead to ischemic conditions.
Nitrates
Nitrates
Pharmacological action
6-1
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Nitroglycerin
Mechanism • Vascular smooth muscle relaxation.
Action • Two major effects "dilation of the large veins (resulting of
pooling blood in veins this reduces preload and decrease work of
heart.
• Dilates coronary vasculature, providing increased blood supply
to the heart muscles.
Side effects • The most common side effect is headache. Higher doses,
Postural hypotension, facial flushing and tachycardia.
Thiocyanate
Nitroprusside Cyanide (toxic) (nontoxic)
Thiosulfate
6-2
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Tips
Write the correct number (s) of the drug(s) that corresponds to the question.
• Nitroglycerin spray storage and administration (room temperature until expiry)
• Nitrates should be avoided taking with (1,4, and 7 )
• What is active moiety of nitrates (2 )
• Nitroglycerin is chemically classified as ( 5 )
• What drugs effective in MI prevention and treatment ( 12 )
• What drugs should be avoided in MI (verapamil and diltiazem)
• It can cause tolerance, to avoid tolerance use nitrate free period. (nitroglycerin
patches)
• Act as irreversible antiplatelet drug in MI prophylaxis ( ASA)
• It is used for only 6 months after opening bottle: Light sensitive amber glass and
metal cap: Hygroscopic: dispense in same container; discard cotton (nitroglycerin SL)
• Use until expiry, do not shake, prime it. (nitroglycerin SL spray pump)
6-3
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• Nitrates Increase nitrites Increase nitric oxide (NO) vascular smooth muscle
relaxation
• Angina is a clinical syndrome characterized by discomfort in the chest, jaw, shoulder,
back and arms.
• Which is usually aggravated by exertion or stress and relieved by nitroglycerine.
• The following Coronary Vasodilators nitrates are used in treatment of angina:
Nitroglycerin, Isosorbide dinitrate, Isosorbide-5-mononitrate.
• ASA = Analgesics, Antipyretics, Antiinflammatory, Antiplatelets
6-4
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7
Cardiac Glycosides. Digoxin
Cardiac Glycosides
Question Alerts!
Digoxin is?
+ve inotropic (force of contraction)
-ve chronotropic (heart rate)
Vagomimetic
7-1
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Pharmacyprep.com Cardiac Glycosides: Digoxin
Pharmacological
action
Therapeutic use CHF, Atrial fibrillation, protects ventricles
Side effects 1st sign: GI effects: Nausea, vomiting, diarrhea, blurry yellow vision, scotoma.
CVS: Arrhythmias, ventricular tachycardia
CNS: visual disturbances (blurred vision)
Bioavailability • 75% bioavailability, 20-40% protein bound
• T1/2 = 40 hr
• Urinary excretion
Monitor • Patient should understand the importance of follow up
laboratory test for this medication.
• Pulse, ECG and Adjust the dose with renal failure patients.
7-2
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Pharmacyprep.com Cardiac Glycosides: Digoxin
Digitalis toxicity
Digitalis toxicity Toxicities of digoxin increased by renal failure (decrease excretion)
hypokalemia, or hyperkalemia (potentiates drug effect)
Predisposing factors Hypothyroidism, hypoxia, renal failure and myocarditis also predisposing factors for
digitalis toxicities.
Digitalis toxicity Digitalis toxicity can be managed by discontinue digoxin, monitor blood
Management potassium levels. Sever tachycardia may require the use of Fractionated
antibodies (FAB antibodies). Which bind to inactive digoxin.
Antidote Digifab
Drugs that may cause digitalis toxicity
Drugs that ↑ digoxin levels Drugs that ↓K+ levels
Amiodarone Thiazides
Verapamil Loop diuretics
Erythromycin Corticosteroids
Tetracyclin
Quinidine
Digitalis toxicity symptoms are severe nausea vomiting, anorexia, muscular weakness,
bradycardia, and ventricular premature contractions. Severe toxic symptoms include
blurred vision, disorientation, diarrhea, ventricular tachycardia, AV blockade which
progress to ventricular fibrillation.
Tips
7-3
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www.PharmacyPrep.Com Antiarrhythmic drugs
8
Anti Arrhythmic Drugs
Antiarrhythmic Drugs Classification
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Electrocardiograph Wave Forms. The electrical activity occurs during depolarization and
repolarization transmitted through electrode attached to the body and transformed by
an electrocardiograph into series of waveforms.
• P Wave. indicated atrial depolarization
• PR INTERVAL. indicates the spread of impulse from the atria to the purkinje fibers.
• QRS Complex. indicates ventricular depolarization
• ST Segments. indicates phase 2 of the action potential, the absolute refractory
period.
• T Wave. shows phase 3 of the action potential ventricular repolarization.
• Q-T Interval. Mechanical contraction of the ventricles (Torse de pointes)
• U wave. Caused by hypokalemia.
ArrhythmiasTreatment
• Flecainide
Pharmacological action: Very effective on slowing phase 0 depolarization
Little effect on repolarization
Therapeutic use • Indicated to treat VA
Class II • Propranolol
Beta blockers • Atenolol
• Timolol
Pharmacological action: Competitively block catecholamine induced
stimulation of Beta receptor thereby Suppress phase IV depolarization
Therapeutic use • Indicated to treat AT, SVT, VT, VA
Class III • Amiodarone blue skin, photosensitivity, photophobia
K+ channel • Bretylium
blockers • Sotalol
Mechanism • Prolong Phase III repolarization (Prolong QT interval)Torose de
pointes
• Indicated to treat VA
Class III agent’s blocks potassium channels and thus diminish the outward
potassium current during repolarization of cardiac cells.
Class IV • Verapamil
Ca2+ channel • Diltiazem
blockers • Nifedipine
Pharmacological action: Shortens action potential
Therapeutic use • Indicated to treat SVA, VA
Digoxin • Pharmacological action: Effects vagotonic response (vegomimetic)
thereby increases AV nodal refractoriness.
• It is contraindicated in ventricular fibrillation.
• Ventricular tachycardia may result from digitalis toxicities
Therapeutic use • Indicated to treat SVA (atrial arrhythmias).
• Contraindicated in ventricular arrhythmias
Quinidine
Pharmacological Acts on Na+, K+ and alpha & beta blocker action Amiodarone is
action structurally related to thyroxine, and it contains iodine.
Therapeutic use DOC antiarrhythmic & recommended in more severe LVD & if CI with
beta blockers.
IV Amiodarone effective in terminating VT, more so in preventing
recurrence. Most effective for treatment in electrical storm
Usually used as an empiric therapy.
Side effects SE of amiodarone are due to its long halflife (13 to 103 days)
"4Ps" Respiratory. irreversible Pulmonary damage, including intererstitial
pneumonitis. Respiratory muscle impairment (due to amiodarone
Pulmonary
deposits into lungs).
Peripheral T4-T3
GI. Nausea, anorexia, constipation, hepatitis and cirrhosis.
Pigmentation
Hypothyroidism or hyperthyroidism. Amiodarone inhibit Peripheral
Phototoxicities
conversion of T4 to T3 (due to similarity amiodarone structure with
hepatotoxicity
thyroid hormone structure).
Amiodarone deposits in skin cause bluish tinge skin color
(pigmentation), corneal deposits cause blurred vision, hepatic toxicity,
optic neuritis, erectile dysfunction, and photophobia.
8-5
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Tips
8-6
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9
Anticoagulants
Anticoagulants
LMWH
Heparin Vit K antagonist 10:2 Factor 10a Inh Others
Enoxaparin
Catalyzes the Warfarin Fandaparinaux Direct thrombin inh
Dalteparin
inhibition of (indirect) Dabigatran (Pradaxa)
Tinzaparin
thrombin 3 Rivaroxaban
Nadroparin
(direct)
Apixaban
Heparin sodium
Question Alerts!
1) What is freely available in
blood?
9-1
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Warfarin
Mechanism • Vitamin K antagonist producing their anticoagulant effect by interfering
with cyclic interconversion of vitamin K and it 2,3-epoxide (vitamin K
epoxide).
• Inhibition of vitamin K-dependent proteins or clotting factors 2, 7, 9
and 10.
Therapeutic • Anticoagulant used to prevent blood clots, mainly in areas where blood
flow is slowest, particularly in the leg and pelvic veins.
Drug-Drug • A wide variety of drugs, such as ASA, barbiturates, oral contraceptives,
interactions cimetidine, diuretics, certain laxatives, certain depressants, and certain
antibiotics interact with warfarin, either by increasing or decreasing the
anti clotting effect.
Side Effects • Bleeding, purple toe syndrome, and skin necrosis
Monitoring • Prothrombin time (PT) ratio and international normalized ratio (INR)
are performed daily upon starting warfarin.
• Oral anticoagulant therapy warfarin INR should be between 2 to 3
Antidote • Vitamin K
9-3
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Warfarin
Chronic alcohol
Vitamin K epoxide reductase Barbiturates
Rifampin
Vitamin K VitaminK epoxide Vitamin K
Polypeptides Dark green vegetables
Spinach
O COO- Cheddar cheese
O
HOOC NH2 CO2 HOOC NH2 Cabbage
Ginseng
Precursor of clotting Factors Active Clotting Factors
Sulfonylureas
II, VII, IX, X II, VII, IX, X
Edema
Hypothyroidism
↓INR Cholestyramine
Penicillin (high doses)
Warfarin Nafcillin
Oral contraceptives
inactivation of
fators IIa, IXa, Xa,
XIa, XIIa, XIIIa.
Antidote Protamin sulfate. Vitamin K,
This works by acid phytanadione
base
neutralization.
Site of In vitro, In vivo In vivo only (liver) or
action Intrinsic and extrinsic pathway
extrinsic only.
Onset of Faster (minutes) Longer half life Slower (half life 6 to
action 8 hours)
Pregnancy Yes LMWH do not cross placenta NO (Terotogenic)
alternate to hep
Renal Can be use in <30 Renally cleared and first Safe in renal
ml/min CrCl order kinestics. Avoid <30
ml/min CrCl.
monitor aPTT No monitoring. predictable INR
dose response relationship.
AVOID Safe. No dose CrCl <30 ml/min CrCl <15 ml/min CrCl <30 ml/min
adjustment require
CrCl/dose 110 mg; 30-49, >25 ml/min , check age, (30-49) 15 mg od
>65yo,↑risk factor for weight, SrCr (>50), 20 mg od
bleeding.
D-L interaction PT and INR effective to aPTT, Thrombin Time PT, INR and aPTT are PT, aPTT, Heptest.
assess anticoagulant (TT), Ecarin clotting little affection. Not influenced but none is used
effect. time (ECT). If necessary useful in assessing to assess. PT (not INR) may
test are used to assess anticoagulant effect be used excess
anticoagulant.*** anticoagulant activity.
Antidote Vitamin K NO available NOT available Not available
• * St. John wort strong induce of both CPY3A4, P-gp may lead to reduced drug plasma concentration.
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• Grapefruit juice is only a moderate CYP 3A4 inhibitor, therefore grapefruit juice consumption is not
expected to be clinically relevant.
• ***To assess dabigatran anticoagulant activity PT (INR is NOT useful and should not be used for this
purpose.
Tips
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10
Antiplatelet Drugs
Antiplatelet drugs
Clopidogrel ASA
Abciximab
Prasugrel
Eptifibatide
Ticlopidine
Tirofiban
Platelets are the elements of blood cells, tend to clump together. The antiplatelet drugs
interfere with the coagulation by inhibiting platelet aggregation. Heart attacks and
strokes occur when a blood clot that forms in a narrowed portion of an artery blood
flow and cuts off the supply of oxygen and nutrients to the tissue that lies beyond the
site of the clot.
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Clopidogrel and ticlopidine given those who do not tolerate ASA. Interact with
glycoprotein IIb/IIIa (a fibrinogen receptor) resulting in an inhibition of the fibrinogen to
form aggregated plug.
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Storage • Store at room temperature. Dispense in light-resistant containers.
conditions Blister packs should not be exposed to light.
Dosage • The recommended dose is 250 mg twice daily with food.
Pharmacokine • Ticlopidine should be taken with meals to minimize GI intolerance.
tics Clopidogrel hepatic elimination, renal dose adjustment is not
necessary.
Eptifibatide and tirofiban. Indicated for unstable angina, NSTEMI and cutaneous
coronary procedure.
Miscellaneous
Epeprostenol is prostacyclin, PGI2, PGX, a bicyclic oxidative prostaglandin metabolites of
arachidonic acid with potent vasodilatory and antiplatelet aggregation properties. .
Tips
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11
Thrombolytic Drugs
Thrombolytic are used to dissolve already been formed thrombus,
as in conditions such as deep vein thrombosis, acute stroke, acute
pulmonary embolism and acute myocardial infarction. Question Alerts!
Thrombolytics are
used for the treatment
Thrombolytic Drugs of stroke, MI, and DVT,
PE
VIIa
Blood
IX X
Xa X
Prothrombin (II) Thrombin IIa
Thrombolytics:
Streptokinase XII
Urokinase
Alteplase
Fibrinogen
Catalyzation
XIIa
Streptokinase
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Monitoring • Don’t give second streptokinase within 6 months of the first
treatment.
Urokinase
Mechanism It is an enzyme with the ability to directly degrade fibrin and
fibrinogen.
Two-chain serine protease obtained from cultured human kidney
cell.
Therapeutic use Coronary artery thrombosis, Pulmonary embolism (PE).
Side effects Allergic reactions may lead to bronchospasm and skin rash
Anistreplase
Tips
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12
Antidepressants
Classification of Antidepressants
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Mechanism. SSRI selectively block the prejuntional neuronal reuptake pumps in the CNS
that terminate serotonin transmission thus increase activity on serotonin receptors.
SSRIs onset of action is 4 to 6 wks for the treatment of depression symptoms.
Side effects
• GI. Nausea (most common), dry mouth, somnolence and sweating. ↑ risk of GI
bleeding. Constipation
• CNS. Headache, insomnia, nervousness, and fatigue. Sexual dysfunction (orgasmic
delay).
Serotonin syndrome. The serotonin syndrome may occur if the SSRI are combined with
MAOi, SSRI and TCA.
Serotonin syndrome is an acute condition due to increase serotonin levels and develops
within minutes to hours (typically within 6 hours) after starting a medication, increasing
the dose of a medication, or overdosing.
Serotonin syndrome occurs with the following agents. All SSRIs, mirtazapine,
venlafaxine and moclobemide. The syndrome is possible when these agents are
combined with each other, MAOi, lithium, meperidine, pentazocine, and
dextromethorphan.
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Tricyclic Antidepressants
Generic Brand Name Dose/Dosage form Tips
Name
Amitriptyline generics 10mg, 25mg, 50mg, 75mg,
100mg, 150mg tab, 10mg/ml inj.
clomipramine Anafranil
(generics)
desipramine Norpramin
(generics)
doxepin Sinequan 10mg, 25mg, 50mg, 75mg,
(generics) 100mg, 150mg cap
10mg/ml oral conc
imipramine Tofranil (generics)
maprotiline Generics
nortriptyline Aventyl (generics) 10mg, 25mg, 50mg, 75mg cap
10mg/5ml soln
trazodone Desyrel (generics) 50mg, 100mg, 150 mg, 300 mg
tab
trimipramine Surmontil
(generics)
Overdose symptoms.
• Mydriasis
• Nausea
• Constipation
• Confusion, sedation
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• Sleepiness
• Palpitation (tachycardia)
• Dizziness
• Dry mouth
• Blurred vision
• Fever
• Overdose treatment. Contact physician immediately if any over dose symptoms
appears.
Contraindications. Avoid combining with MAOi and SSRI
MonoaminooxidaseInhibitors
The monoamine oxidase inhibitors (MAOis) were the first class of compounds used to
treat depression. Patients, taking these drugs, must monitor their diet for tyramine, an
amino acid present in many foods that are fermented, aged or smoked. There are a
number of foods containing tyramine and some drugs must be avoided. Monoamine
oxidase is an enzyme, which inactivates the neurotransmitters, epinephrine,
norepinephrine and dopamine. These drugs inhibit the destruction of these brain
chemicals, which leads to increased concentrations of these neurotransmitters, which
may account for their antidepressant activity.
Generic Name Brand Name
phenelzine Nardil
tranylcypromine Parnate
.
MAO Inhibitors Phenelzine , and tranylcypromine
Mechanism • Irreversibly Monoamine oxidase inhibitors, permitting
neurotransmitter to escape degradation and therefore to
both accumulate within. Inhibit both MAO A and MAO B . Blocks
deamination in brain biogenic amines.
• Clorgyline. MAO A selective
• Selegiline. MAO B selective (used as antiparkinson drug)
Therapeutic use • Antidepressant, anti anxiety and narcolepsy
Side effects CVS. Orthostatic hypotension, tachycardia, arrhythmias, and
stroke.
CNS. Insomnia, CNS stimulations
Weight gain
Sexual dysfunction
Anticholinergic SEs less than TCA
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Trazadone SNRI. SEs. Sedation, drowsiness, N&V, headache, dry mouth, priapism
rarely associated with serotonin syndrome. May be combine with SSRIs
Lithium
Lithium toxicity
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Lithium is narrow therapeutic index. Drug serum levels >1.5 mEq/L associated with
lithium toxicity. These symptoms includes Cerebral symptoms. Drowsiness, in
coordination, dizziness, blurred vision, confusion. Autonomic symptoms. Tremors,
Change in heart rate or rhythm, fluid retention and CNS like seizures.
Initial Onset SEs Lithium Long term SEs Lithium Toxicity (Serum > 1.5 mEq/L)
N&V, GI upset, Dry mouth, Fine hand tremors Coarse hand tremor
Fine hand tremor, sedation Weight gain Muscle twitching
Muscle weakness Hypothyroidism Vomiting, severe drowsiness, confusion,
Polydypsia acne, psoriasis nystagmus, seizure,
Polyuria rash, alopecia Ataxia, cogwheel rigidity, coma, death
Nocturia Decreased libido
Arrhythmia: Non specific T-
wave changes, Nephrotoxicity
Nephrogenic
Monitor. Li, Na, Serum TSH, CBC, weight, CrCl (No LFT)
Antidepressant Summary
SSRIs • Most anorexic: Fluoxetine
• Most nauseating: Fluvoxamine
• Most weight gain: Mirtazapine
• Citalopram SE: Somnolence
• All SSRIs have common SE: Nausea
• Antidepressants with Less sexual dysfunction are Bupropion, Mirtazapine,
moclobemide
TCAs • Less hypotensive TCA; Nortriptyline
• Most Anticholinergic and sedative TCA; Amitriptyline
• Least sedative of TCA –Nortriptyline
• Less anticholinergic TCA—Nortriptyline
• Take medication daily
• Antidepressants must be taken for two to four weeks for a noticeable effect
• Continue to take medication even if you are feeling better
• Do not stop taking the antidepressant without checking with the physician
Tips
• A substance found commonly in fermented foods which can be toxic when MAO
inhibitors are used→ Tyramine
• MAO is classified as → Enzyme
• Renal dysfunction and dehydration → Increase lithium toxicity
• Lithium toxicity symptoms --> drowsiness, dizziness, confusion, blurred vision
change in heart rate.
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13
Benzodiazepine and Barbiturates
Benzodiazepines
Benzodiazepine are minor tranquilizers are used to treat insomnia, epilepsy and anxiety.
Short acting Half life (H) Intermediate acting Half life Long acting Half life
Oxazepam 8 Clonazepam 34
Nitrazepam
Low hangover effect High hangover effect
Short half life Long half life
Faster withdrawal Slower withdrawal
symptoms symptoms
Benzodaizepines bind to specific, high affinity site in cell membrane, which are separate
from but adjacent to the receptor for GABA. The benzodiazepine receptor found only in
the CNS and their location parallels that of GABA neurons. The binding of
benzodiazepines enhances the affinity of GABA receptor for this neurotransmitter.
resulting in opening of adjacent chloride channel, in turn results in hyperpolarization
and inhibition neuronal firing.
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Benzodiazepine pharmacokinetics
• Short acting. Triazolam, midazolam (shortest half life). Short acing benzodiazepine.
have no phase I metabolism, or extra hepatic metabolism.
Other sedatives
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Zaleplon
• Short half life 1 hours. Headache. most common
• Reduce sleep latency, used in initial treatment.
• Act on benzodiazepine receptors. No anticonvulsant and muscle relaxant activity.
Zopiclone (Immovane)
• No anticonvulsant and muscle relaxant activity. Short half life 5 hours. Bitter metallic
taste and bad breath.
• Confusion is most common in elderly, do not accumulate, may cause less withdrawal
effects and less rebound insomnia. Less tolerance, minimal additive effect with
alcohol.
Zolpidem (Ambien)
• It is not a benzodiazepine. It is has no anticonvulsant properties, it does not have
muscle relaxing properties.
• Elimination half life is 3 hours
• SEs: NIGHTmares, Dizziness Agitation, GI upset, Headache.
Barbiturates
Barbiturates are used much less commonly than before. They are effective only for a
few weeks since they alter the length of time spent in R.E.M. sleep. They should only be
used for short-term therapy as sedative or hypnotics. Tuinal (a combination of
secobarbital and amobarbital), and secobarbital are reportable controlled drugs.
Phenobarbital is used to control seizure disorders, often in combination with primidone
and/or phenytoin.
Short acting
Amobarbital Long action
Ultra-short action
Secobarbital Phenobarbital
Thiopental
Pentobarbital
• Phenobarbitals: Long acting
• Amobarbital: short acting
• Butabarbital : short acting
• Pentobarbital : short acting
• Secobarbital: short acting
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Miscellaneous
Non-barbiturate Chloralhydrate
sedatives Alcohol
Antihistamine
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Buspirone
Chloralhydrate Tri chlorinated derivative of acetaldehyde
Antihistamine Doxylamine and other antihistamine are used as OTC treatment of
sleep disorders
Hydroxyzine
Mechanism H1 antihistamine with antiemetic activity
Therapeutic use Antihistamine, Antiemetic, Anxiety, Sedation prior to dental
procedure, Insomnia
Advantages Low tendency of habituation thus it is useful for anxiety in-patient
who a history of drug abuses.
Buspirone Buspirone acts on 5HT1a receptors and D2 receptors causes minimal
sedation, least addiction liability.
Disadvantage. slow onset of action
Advantage. Less interference with motor functions (helpful in
elderly).
Ethanol Ethanol is metabolized in liver, first to acetaldehyde by alcohol
dehydrogenase and acetate by aldehyde dehydrogenase. Ethanol has
sedative and antianxiety effect.
Ethanol
Alcohol dehydrogenase
Acetic acid
Tips
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14
CNS Stimulants
These drugs have a stimulating effect on the CNS. Psychomotor stimulants are used to
treat children hyperactivity and attention deficit disorder. As a side effect, they decrease
appetite and for many years were used as appetite suppressants. Addiction and abuse
were side effects of taking these drugs.
These drugs are also used to treat narcolepsy, a condition where the patient lapses into
momentary sleep while sitting. This may occur as many as 20 times a day and is
dangerous if it were to happen while the patient is driving or operating machinery.
CNS Stimulants
• Methylxanthines
• Cocaine • Phencyclidine (PCP)
• Nicotine • Lysergic acid (LSD)
• Amphetamines • Tetrahydrocannabinol (THC) or
dronabinol (Marijuana) (POT)
• Methylphenidate
• Sativex (pain reliever spray)
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Amphetamine
Methylphenidate
Tips
TRUE OR FALSE
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15
Anti Psychotic Drugs
The antipsychotic agents are classed as major tranquilizers and are used to help people
with schizophrenia and other psychoses (major mental disorders). Psychotics symptoms
can be categorized as positive and negative symptoms. Positive. hallucination,
delusions, agitation, disorganized behavior. Negative. social withdrawal or isolation.
Cognitive: memory, judgment, and thinking.
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perphenazine generics
prochlorperazine
Stemetil (generics)
trifluoperazine generics
Second generation antipsychotics
quetiapine Seroquel Usual: 600 mg/day
nd
Olanzapine Usual: 10 mg im. If necessary 2
Zyprexa, Oral tab, Zyprexa im dose of 5–10 mg im may be given
injection, Zyprexa Zydis OD is 2 h after first injection
rapid dissolving tab.
Clozapine Inhibit D 2 , 5HT 2 , D 1-5 , Usual: 300–600 mg/day po
Clozaril, generics Max: 900 mg/day, Divided in 1–3
and H 1 , M, alpha 1-2 doses/day
Side effects
• CNS. extra pyramidal symptoms such as akathisia, tardive dyskinesia, acute dystonia
and parkinsonism. Alteration of temperature regulating mechanism (poikilothermy).
• CVS. Postural hypotension, and reflex tachycardia.
• Other. Sexual dysfunction and anticholinergic.
• Haloperidol with lorazepam im for acute phase, SEs EPS, QT c prolongation. DOC for
+ve symptoms delirium.
• Pimozide: SEs QT c prolongation with dose 8 mg/day (avoid use with sertraline).
• Haloperidol and phenothiazines have high TD, due to high effect on M-receptors
• Chlorpromazine; SEs QT c prolongation, cholestatic jaundice <1%, ~Seizures <1%
Side effects
• Significantly reduced risk of EPS (acute dystonia, parkinsonism, akathisia and tardive
dyskinesia) than typical.
• Weight gain (greatest), hyperlipidemia, ↑ glucose abnormalities (diabetes).
Risperidone
• MOA. Inhibits D 2 and 5HT 2 , also has relatively high affinity at histamine H 1 and
adrenergic alpha 1 and alpha 2
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Quetiapine
MOA. Most effectively binds 5HT 2a , H 1 , alpha 1 . alpha 2 in brain and has low affinity
to D 2 receptors.
• Least EPS
SEs. Hyperlipidemia, ↑triglycerides (17%), ↑ cholesterol (11%), hypothyroidism,
akathisia>2%, and diabetes.
Ziprasidone. Agonist of 5HT 1A and moderate inhibition of synaptic reuptake of 5HT and
NE. Thus ziprasidone has potential efficacy in –ve symptoms and depression.
Aripiprazole. partial agonist at 5HT 1a and D 2 receptors. Thus has potential efficacy in –ve
symptoms and depression. Available oral single daily dose. Taken with or without food.
• D 2 inhibitory effect effective produce more pharmacological benefit to treat positive
symptoms.
• 5HT 2A inhibitory effect effective in producing more pharmacological benefit to treat
negative symptoms.
Ziprasidone + +
Aripiprazole + +
Ziprasidone. moderate 5HT and NE reuptake inh.
Antipsychotics
Bp/ BG LFT BMI WBC TG/ Q-T others
pulse TC
Clozapine + ++ + +++ + + Cardio toxicity, Sedation, weight gain,
hypersalivation. (least anticholinergic)
Risperidone + + +++ + + Akathisia, Mild sedation
Olanzapine ++ + +++ + Sedation, weight gain
Quetiapine + + + +++ + Sedation
Ziprasidone ++ Sedation, insomnia, nausea
ECG Weight neutral
Paliperidone Insomnia
Aripiprazole + Insomnia & sedation, dose dependant somnolence,
weight neutral
Haloperidol +
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Tips
TRUE OR FALSE
• Least extra pyramidal symptoms clozapine, quetiapine (True/False)
• Highest EPS haloperidol, fluphenazine (True/False)
• A patient experiencing hallucination high potency haloperidol, fluphenazine
(True/False)
• 1st generation 4 to 8 weeks no response, change to 2nd generation. (true/false)
• Schizophrenia is characterized by long standing paranoid delusion. (true/false)
• 2nd generation drugs treatments covers +ve and -ve symptoms (True/False)
• Schizophrenia is characterized by hallucination, social withdrawal etc.
(True/False)
• Metoclopramide and chlorpromazine is low potency 1st generation
antipsychotic (True/False)
• Tardive dyskinesia is caused by antipsychotic drugs side effects (True/False)
• Tardive dyskinesia symptoms involuntary movement trunk, neck, and jaws
(True/False)
• For resistance schizophrenia drug of choice clozapine (True/False)
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16
Antiepileptic Drugs
Antiepileptic drugs by mechanism of action
Felbamate
Phenobarbital Carbamazepine Ethosuximide
Topiramate
Primidone Phenytoin
Fosphenytoin
Diazepam Lamotrigine
Vigabatrin
Topiramate Valproate
Tiagabine Valproic acid
Gabapentin?
After each depolarization, Na+ channel adopt an inactive state and remain refractory
to reopening for a period of time. While channels are unable to open rapid repetitive
firing is diminished, and spread of electrical seizure to adjacent cells is suppressed.
Seizure. Abnormal or burst electrical discharge from local areas and spread around the
brain adjacent areas. Condition like hypoxia, uremia, bacterial meningitis, genetic
predisposition and drugs such as cocaine, penicillin G, and anticholinergics can produce
seizure. Withdrawal from chronic use of alcohol, barbiturates, benzodiazepines and
most anti seizure medication can also lead to seizures.
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Carbamazepine
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Phenytoin
Phenytoin decreases the sodium content of nerve in the brain and thereby decreases
the hyperexcitability of the cells that are involved in initiating seizures.
Phenobarbital
Clobazam
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Ethosuximide
Mechanism Analog of GABA, however, this do not act as GABA mimetic and
does not block Na ion channel. May encourage production of or
discourage degradation of GABA.
Therapeutic use Partial seizures, and trigeminal neuralgia and neuropathic pain.
Side effects When initiating therapy CNS. somnolence, sedation, fatigue,
dizziness vision problems and ataxia.
Advantage Safe, well tolerated, not metabolized, can be used in liver failure,
No interaction with oral contraceptives pills.
Disadvantage Not for generalized seizure. Administration with aluminum,
magnesium antacid may ↓ bioavailability.
Tips Very expensive at high doses, best used as “add on drug”.
Lamotrigine
Mechanism Inhibit glutamate and aspartate release and blocks sodium channels
and prevents repetitive firing.
Therapeutic Anticonvulsant
use
Side effects Dose dependant rash. CNS. Somnolence, dizziness, insomnia
Advantage Broad spectrum, no enzyme induction, some patients more “alert”.
Disadvantage Metabolism inhibited by valproic acid.
Only available in oral form
Comment Very expensive at high doses
Topiramate
(glutamate).
Side Effects Cognitive dysfunction, headache, kidney stones and weight loss.
Management Limit use
Advantage Broad spectrum, safe, few drug interaction, weight loss
Disadvantage ↓ efficacy of OCPs, and expensive.
Valproic Acid
Valproic acid and divalproex are related chemicals. Divalproex is a mixture of valproic
acid and sodium valproate. In the body they are metabolized to separate compounds,
and both exert anticonvulsant effects.
Pregnancy
Patient taking antiepileptic drugs phenytoin, CBZ, and valproic acid should take folic acid
supplements.
Antiepileptic Drugs
Serum Elimination LFT Rash Fever BMI Folic acid
level
Carbamazepine + hepatic + + + ↓absorptio
n
Phenytoin + hepatic + + + ↓absorptio <0.45 mg
n
Valproic acid + hepatic +++ + +
Lamotrigine 90% hepatic +++ Dose related
↑ dose 125 mg % excreted rash
gradually unchanged
Ethosuccimide hepatic
Clobazam hepatic
Gabapentin >90%renal
eliminated
Pregabalin
Topiramate 5-70% renal red eye,
glaucoma (↑IOP),
kidney stones.
Vigabatrin 90% renal
Phenobarbital ↓absorptio
n
• Folic acid ↓absorption can cause deficiency. In pregnancy this can lead to Spina bifida. Vitamin K is
routinely given to all new born at delivery to prevent hemorrhagic disease.
• If skin rashes occurs contact your physician immediately.
Tips
TRUE OR FALSE
• Carbamazepine interferes with thyroid function test (True/False)
• Phenobarbital and phenytoin stimulates CYP 3A4 (True/False)
• Avoid phenytoin and carbamazepine in absences seizure (True/False)
• Phenytoin have gingival hyperplasia and nystagmus side effects (True/False)
• Gingival hyperplasia associated with phenytoin is treated by mouth hygiene and
chlorohexidine oral rinse. (True/False)
• Chlorhexidine is used for treatment of gingival hyperplasia (True/False)
• Carbamazepine, phenytoin, clonazepam are used for partial seizures (True/False)
• Gabapentin, and valproic acid, have no interaction with oral contraceptives
(True/False)
• Topiramate cause weight loss (True/False)
• Gabapentin has least drug interactions, specially with oral contraceptive pills
(True/False)
• Phenytoin available as iv (92%), capsules (92%), suspension (100%) and chewable
(100%) (True/False)
• Carbamazepine available as IR tabs and SR tabs (True/False)
• Clobazam is a benzodiazepine has high tolerance (True/False)
• Gabapentin and lamotrigine GABA analogs (True/False)
• Xerostomia is dry mouth (True/False)
• Sialorrhea excessive saliva (True/False)
• Vigabatrin + carbamazepine and phenytoin are used for partial seizures (True/False)
• Phenytoin blood levels monitored for 10 to 20 mcg/ml (True/False)
• List the monitoring parameters for phenytoin.-->blood levels
• Nystagmus is rapid eye movement (True/False)
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17
Dementia
Dementia is a declined in mental ability that usually progresses slowly, in which
memory, thinking, judgment, and ability to pay attention and learn is impaired, and
personality may deteriorate.
• Risk factors of Alzheimer’s disease family history, age, and CVD.
• Symptoms of Alzheimer’s disease? Slurred speech, reduced cognitive functions,
reduce sexual function, and decrease in judgment and skills.
Classification of dementia
• Mild. Forgetting daily activities. Example taking medicines, tel. phone number,
finances, paying bills and directions.
• Moderate. Forgetting personal activities bathing, dressing, eating (remember upon
reminders).
• Severe. Forgetting personal activities but cannot recall upon reminders.
• Terminal. Patient must be fed, immobile and mute.
Nonselective Selective
Galanthamine Rivastigmine
Donepezil
(relatively selective)
Donepezil
Mechanism • Centrally active reversible, non competitive. It selective and have
greater affinity for AchEi in brain than periphery. Little or no
hepatotoxicity.
• Reduces the hydrolysis of acetylcholine, increasing the amount
available in the synaptic cleft.
Side effects • GI effects. Nausea, vomiting and diarrhea.
• CNS effects. Fatigue, insomnia, headache
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Rivastigmine
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Tips
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18
Anti-Parkinson’s Drugs
Parkinson's is a condition, which is characterized by muscle tremors at rest, muscle
weakness, emotionless facial expressions, increased sweating and salivation,
disturbances of motion and increased postural balance difficulty. These patients have a
deficiency of the neurotransmitter, dopamine, allowing acetylcholine to dominate.
Benztropine
Peripheral dopa Trihexphenidyl
Entacapone Selegiline Amantadine
decarboxylase
Tolcapone Rasagiline
inhibitor
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3-O-Methyldopa 3-O-Methyldopa
Tolcapone
Entacapone COMT
Tolcapone
Striatal neuron
Carbidopa
Dopamine
Dopamine
D1 and D2 Dopamine
Bromocriptine and
receptors
Pramipexole
Ropinirole
MAO-B
Selegiline
Rasagiline
Dihydroxyphenylacetic
Acid (DOPAC) + H2O2
Levodopa preparations
Mechanism. Levodopa, a dopamine precursor that is converted to dopamine in the
brain by with enzyme dopa decarboxylase, appears to correct akinesia, rigidity and
tremors of Parkinson’s disease by the
formation of dopamine at the nigro
striatial dopaminergic site. Concept!
Side effects. The most common SEs of 1) Wearing off (end dose effect)
levodopa therapy is gastric upset Nausea, 2) On-off motor fluctuation
vomiting, orthostatic hypotension,
dyskinesia, hallucinations, confusion Long
term use of Levodopa/carbidopa therapy can produce mydriasis & precipitation of
glaucoma, melanoma.
Pharmacokinetics. High protein content meals interfere with transport of levodopa into
CNS. Levodopa should be taken on an empty stomach, typically 45 min before a meal
Wearing off. Short duration response or "end dose" effect. The motor complications
include "off periods" of immobility or greater severity of the other parkinsonism
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symptoms and various abnormal movements. This is due to decrease synthesis and
storage of dopamine generated from endogenous or exogenous levodopa.
On-off fluctuations. Most severe form of wearing off effect (abruptly freezes).
Benztropine
Antiviral Agent
Antiviral agent with anti-Parkinson properties. Indicated in drug induced PD because
levodopa will reverse the beneficial effect of the drug.
Side effects: anticholinergic side effects, hallucinations, edema of feet & ankles.
Amantadine (Symmetrel)
COMT inhibitors are used as an adjunct to L-dopa and carbidopa to reduce response
fluctuation.
The dyskinesia or induction of hallucination can be managed by reducing
the dose of levodopa.
Entacapone
Bromocriptine
Pergolide
Pramipexole
Mechanism • Selective D2 receptor agonist.
Therapeuti • Mild to moderate Parkinson’s disease and to manage motor
c use
fluctuation.
Side Effects • Dizziness, insomnia, lightheadedness. Rarely it can cause
hallucinations or dyskinesia. Sudden onset of sleep
Monitoring • Regular monitoring of your Parkinson's symptoms, and report any
changes to the physician.
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The most common side effects of LEVODOPA are nausea, hypotension, and hallucinations. Domperidone
is useful for managing nausea and hypotension.
After 3-5 years of levodopa therapy, patients begin to develop motor fluctuations (“wearing off”, “on-off”)
and dyskinesias. The exact cause of these late side effects is uncertain. Several strategies can be tried in
an attempt to manage motor fluctuations.
Tips
TRUE OR FALSE
• Athetosis is writhing movements, often with alternating postures of the proximal limbs that blend
continuously into a flowing stream of movement.
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19
Anesthetics
Local anesthetics
• Inhibit sensory nerves that carry stimuli to CNS and block nerve fiber conduction
• Ester local anesthetics produce para amino benzoic acid (PABA) as metabolic
product.
General Anesthetics
Inhaled Intravenous
Inhaled anesthetics: Inhaled anesthetic are used to provide general surgical anesthesia
Halothane (Fluothane)
• Halothane is used in pediatric anesthesia. It is infrequently used in adults.
• Side effects. Malignant hyperthermia.
Enflurane
Enflurane is used as an inhalation agent for adults, but is not widely used for pediatric
cases.
Isoflurane.
Isoflurane may be the most widely used inhalation agent.
Nitrous Oxide. With a MAC value of 105%, nitrous oxide, by itself is not suitable or safe
as a sole anesthetic agent. Nitrous oxide is an effective analgesic and nitrous oxide in
combination with thiopental for induction, a skeletal muscle relaxant and
hyperventilation to reduce CO 2 .
Use as an adjunct to other inhalation agents allows reduction in their dosage.
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Ketamine
• Short acting non-barbiturate anesthetic induces a dissociated state in which the
patient appears awake but is unconscious and does not feel pain.
• Causes sedation, immobility, amnesia, and nightmares, and uses hypertension and
increases cardiac output-avoid use in stroke and high blood pressure patients.
• Mainly used for short procedures.
Intravenous
• Intravenous are indicated to induce drowsiness and provide relaxation before the
induction of inhalational general anesthetics.
Propofol
• Sedative or hypnotic
• Used in induction and maintenance of anesthesia
• Fast onset (40 seconds of administration).
• Poor analgesic.
Fentanyl
• Narcotic
• Available as transdermal patch, good analgesic property.
Anesthetic Tips
• Sequence of MAC. Nitrous oxide > Ether > Enflurane >Isoflurane > Halothane
• Isoflurane (Forane), enflurane (Ethrane), sevoflurane (Sevorane, Ultane)
and desflurane (Suprane) are frequently used in adults.
1 Epinephrine 2 Local anesthetics 3 Halothane
4 Chlorprocaine 5 Benzocaine 6 NO 2
7 Butamben 8 Procaine 9 PABA
10 Procainamide 11 Cocaine 12 Local anesthetics
13 Thiopental 14 Tetracaine 15 lidocaine
• Ester type of local anesthetic metabolize to … ( 9 )
• A vasoconstrictor ( 1 )
• Its action is to helps prolong duration of action and decrease systemic SE. ( 1 )
• Topical anesthetic used for canker sores and cold sores, dental pains, and
hemorrhoids. ( 5 )
• Ester type local anesthetic include. (5,8,11,14 )
• Antiarrhythmic drug (Na+ channel blocker) shows action similar to quinidine (10)
• Used as an antiarrhythmic drug and it is an amide type local anesthetic (15)
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20
Opioid Analgesics
Opioids are derived from opium. These are powerful central nervous system drugs that
are used medically to relieve pain. These drugs are used for moderate to severe pain of
trauma, post-surgical pain, pain associated with myocardial infarction and pain of
terminal illness. Physical and psychological dependence (addiction) can occur when
opioids are administered for some time. When tolerance develops, the patient requires
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increasing amounts of drug to treat pain. All opioids are habit forming, however,
titrated doses to treat pain; the risk of addiction is slight.
Opioid analgesics act primarily on the CNS and the intestines. The perception of and
emotional response to pain are modified when opioid analgesics bind with
stereospecific receptors in the CNS. The most studied subtypes of opioid receptors are
mu (μ), delta (δ) and kappa (κ). Pure opioid agonists such as morphine act primarily at
the mu receptor. Mixed agonist-antagonists such as butorphanol, nalbuphine and
pentazocine are most active at the kappa receptor. Buprenorphine is a partial agonist at
the mu receptor and an antagonist at the kappa receptor.
• Tolerance. Need to use the high dose of drug to get the same effects.
• Physical dependency
• psychological dependency (craving, euphoria (feeling good).
• Opioid overdose gives three characteristic symptoms such as pinpoint pupil (due to
increase in cholinergic activity), decrease respiration (hypoxia), constipation, coma
and somnolence.
Therapeutic use:
• Analgesics (moderate to severe pain)
• Antitussive (dextromethorphan, codeine)
• Antidiarrheal (Loperamide)
Side effects
• Constipation (increase GI tone)
• Sedation, drowsiness
• Miosis
Important!
• Respiratory depression Comparison opioids side effect and
• Urinary retention anticholinergic SEs
• Hypotension
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Tips
• Dyspnea is →
• Avoid opioids in head trauma patients
• Morphine active metabolite →
• Analgesic activity of morphine→
• Codeine is metabolized by →
• Patient taking Tylenol # 3 + hydromorphone →
• Methadone is used for →
• Morphine over dose symptoms →
• Which opioids has highest addiction potential →
• In angina pain what opioids is used →
• Drugs used to treat opioids withdrawal symptoms→
• Opioid antagonist→
• A patient developed seizure after initiating opioids therapy, which opioids would
be responsible→
• Opioids least used in→
• Pinpoint pupil is opioids →
• Avoid opioids with MAOI →
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21
Non–Steroidal Anti-
inflammatory Drugs &
Analgesics
• Antipyretic: a drug to reduce fever
• An analgesic: a drug used to relieve pain
• Anti-inflammatory: Drugs that reduce redness and swelling
• Antiplatelet: Prevent platelet aggregation.
ASA
NSAIDs:
*Salicylic acid *Diflunisal *Celecoxib (Celebrex)
*Methylsalicylic *Flurbiprofen *Rofecoxib
*Ibuprofen
*Naproxen
*Indomethacin
*Sulindac
*Piroxicam
*Ketorolac
ASA
enteric coated ASA Entrophen®, diflunisal generics
Novasen®
celecoxib Celebrex® floctafenine Idarac® (generics)
flurbiprofen Ansaid® (generics)
ibuprofen Motrin®, Advil® (generics)
indomethacin Indocid® (generics) ketoprofen Orudis® (generics)
ketorolac Toradol® meloxicam Mobicox®
naproxen Anaprox®, Naprosyn® piroxicam Feldene® (generics)
(generics)
sulindac generics tiaprofenic acid Surgam® (generics)
tolmetin Tolectin®
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• Antiplatelet low dose (60 to 80 mg). Due to permanent action on TxA 2 thus
prevent platelet aggregation
• Analgesia: Moderate dose, may be two tablets (325 mg bid). Due to inhibition of
Cox 1 and Cox 2 (prevent prostaglandin formation).
• Antipyretics. Moderate dose, may be 4 to 8 tablets. Pyrogen increase PGE 2
formation, which is inhibited by ASA
• Anti-inflammatory. Moderate to high dose. Inhibit Cox 2 which is induced during
inflammation.
Tips
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22
Autocoids
Autocoids (local hormones) are chemical mediators that the body releases as a response
to pathogens or noxious substances. Produced in the body and has profound
pharmacological effects. Generally autocoids can characterized as amine type and
endogenous type.
Histamines
• Histamines, the autocoids act on three receptors H 1 , H 2 and H 3 .
• Present: Skin, lymph, and GI tract
• Release = mast cells, basophiles
• Stimuli = Drugs such as opioids (except fentanyl), venoms, trauma, and vancomycin
(red man syndrome).
H 1 receptor activation
• H 1 - typical allergic and anaphylactic response to histamines.
• ↑ Bronchoconstriction
• ↑ Vasodilation (via NO): ↓ B.P
• ↑ Increase capillary permeability
• ↑ Spasmodic contractions of gastrointestinal smooth muscle (GI)
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•
1st generation 3rd generation
• 2nd generation
Diphenhydramine Desloratadine (Aerius)
Dimenhydrinate
Loratadine
Tripelannamine Fexofenadine
Hydroxyzine Cetirizine
Meclizine Terfenadine
Chlorpheniramine
Promethazone
H 1 blockers indications:
• Allergic reactions
• Allergic Rhinitis (hay fever), and runny nose
• Motion sickness
• Nausea and vomiting (in pregnancy)
• Preoperative sedation
• Sleep aid
1st generation
• Usually lipid soluble
• Similar in terms of absorption and distribution
• Good absorption after oral administration distribution with peak plasma
concentration of 1 – 2 hours
• Allows some to go to the blood-brain-barrier especially
• Structural resemblance to histamine
H2 -Receptors Activation
• ↑ Gastric acid secretion and ↑ GI ulcer.
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5HT1(A-G)
• Found in the CNS (inhibitory) and smooth muscles (excitatory or inhibitory).
• 5HT1A partial agonist = Buspirone
• Used as anxiolytics (specially general anxiety disorders)
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Serotonin antagonist
5HT 3 receptor antagonist
5HT 4 agonist
Found in periphery and GI smooth muscles. Thereby these drugs are used in chronic
constipation.
• Cisapride (a benzamide)
• Ttagaseride (indole derivative).
• Ergotamine-serotonin partial agonist: Ergot alkaloids have agonist and antagonist
properties
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Prostaglandin
Physiological functions
Platelet aggregation, Relax bronchial and GI smooth muscles, Relax smooth muscles,
Inhibit gastric acid secretion, Pain, Edema, Inflammation
PGE 1 analogs
• Protection of gastric mucosa
• Vasodilatation
Misoprostol (Cytotec): is used for prevention of NSAID induced GI ulcers.
Chemically it is ecosonides.
Combination products: Naproxen + misoprostol, diclophenac + misoprostol (arthrotec)
Alprostadil
In adults; for the treatment of impotence
Alprostadil (Caverject, Prostin VR pediatrics) is used treating impotence due to erectile
dysfunction.
Alprostadil (prostin VR pediatric) is used for temporary maintenance of a patent ductus
arteriosus when awaiting corrective surgery for congenital heart defects.
Dinoprost, Dinoprostone
• Dinoprostone derovatives Abortificient
• Dinoprostone (prostin E 2 , prepidil, cervidil) are used for their abortifacient effects
and to induce cervical ripening in pregnancy.
PGF 2α analogs
• Uterine and bronchial muscle contraction
• Decrease intraocular pressure
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PGF 2α analogs are selective prostanoid FP receptor, inhibitors that reduce IOP, and
increase outflow of aqueous humor.
• Latanoprost (Xalatan): (Used topically to lower intra ocular pressure in OAG)
• Travoprost (Travatan) : topical ophthalmic drug
• Bimatoprost (Lumigan) : topical ophthalmic drug
• Unoprostone (Rescula) : topical ophthalmic drug
• Carboprost (Hemabate) :abortificient (withdrawn)
• Precautions: Ophthalmic solutions have been reported to cause changes to
pigmented tissue. The changes include the increased pigmentation and growth of
eyelashes and increased pigmentation of iris and periorbital tissue (eyelid). The
increased pigmentation is permanent.
• Latanoprost (Xalatan): Store unopened bottle under refrigeration. Protect from
light. Once opened store bottle in cool place (refrigerate if possible) for up to 6
weeks.
• Bimatoprost (Lumigan): Store at room temperature, no refrigeration necessary
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Prostaglandin
Corticosteroids
Leukotrienes
Lipoxygenase
Prostaglandins G
Hydroperoxidase
PGH2
Dipyridamole
Thromboxane A2
Prostacyclin (PGI2) PGE2 & PGF2
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Leukotrienes
Physiological functions
LTC and LTD antagonists
Play important role in numerous physiological functions.
Slow reacting substance of anaphylaxis.
Heart: Negative inotropic, Smooth muscles chemotaxis (Chemotaxis = movement of cell
in response to the chemical gradient)
GI tract: Neutrophil chemotaxis
Pulmonary (major): Bronchoconstriction, increase permeability, and increase mucus
secretion.
Blood: Chemotactic agent for neutrophils, eosinophils, and modify lymphocyte
proliferation and differentiation.
Two important leukotrienes antagonists: LTC 4 and LTD 4
e.g. Zafirlukast (Accolate) and montelukast (Singulair); Peptid mimetic structure.
Indicated in prophylaxis of asthma.
Zafirlukast (Accolate)
• Therapeutic use: For the prophylaxis and chronic treatment of asthma in adults and
children 12 years of age and older. Side effects include: GI upset, liver dysfunction.
• Take empty stomach to enhance it absorption.
Montelukast (Singulair)
• Similar profile to that of zafirlukast.
• Can be used in children over 2-year age
• Montelukast may be taken without regard of food.
• Available as chewable tablet (once daily in the evening). Administer granules directly
into mouth or mix with teaspoon of cold or room temperature applesauce, carrot,
rice or ice cream. Do not take aspirin or NSAIDs while on this medication.
• Drug of choice for aspirin induced asthma
Abbreviation and Terminology
5HT 5-hydroxy tryptamine LTD Leukotriene d
DHE Dihydroergotamine PGI Prostaglandin I
PGF Prostaglandin F OAG Open angle glaucoma
LTC Leukotriene c IOP Intraocular pressure
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23
Insulin and Antidiabetic Drugs
There are two types of diabetes mellitus, type I and type II. For type I diabetes, patients
need insulin injections. Type I diabetes is known as insulin dependent diabetes mellitus
(IDDM). It usually begins in young people under 40 and of normal weight.
Insulin Mechanism
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Types of insulin are categorized by their onset of action, and these relative positions
hold true for their effectiveness and their duration of action as well. The delayed onset
action of insulin is due to dimmer and hexamer formation, which takes time to
dissociate.
Diabetes: Insulin
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Meglitinides
Sulfonylureas Repaglinide
Neglitinide
st nd
1 Generation 2 Generation 3rd Generation
Chlorpropamide Glyburide Glimepiride
Tolazamide Gliclazide beta and delta extra
Tolbutamide Glipizide pancreatic.
Chlorpropamide
Mechanism • Increased insulin release from beta cells of the pancreas
Therapeutic use • To control hyperglycemia in glyburide-responsive DM of
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Sulfonylureas 2ndGeneration
Repaglinide • Gluconorm
Mechanism • Stimulate release of endogeneous insulin (rapid-acting),
better post-prandial glucose control.
Therapeutic use • Can be used in sulfa allergies
Contraindications • Hypersensitivity, diabetic ketoacidosis (DKA).
Side Effects • Hypoglycemia (less frequent than with sulfonylureas).
Nateglinide
Mechanism Stimulates the release of insulin
Contraindication Type I and pregnancy
Side effects weight gain, hypoglycemia if meal not taken
Drug-Drug Clearance inhibited by ketoconazole, miconazole, and
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Important Concept!
SEs. Lactic acidosis! Increased with alcohol renal and hepatic disease.
Thiozolidine diones
Mechanism Intestinal lipase inhibitor. Blocks the action of stomach and pancreatic
enzymes (lipases) that digest fats, so fats and other fat soluble vitamins
ADEK are not absorb in the body but pass through and excreted in the
feces.
Therapeutic Reduces fats stores and produce weight loss.
use
Drug-Drug Orlistat increases blood levels and toxicity of pravastatin.
interaction
Dose 120 to 360 mg daily
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Incretin hormones. DPP-4 enzyme inactivates GLP-1. Gliptins inhibits DPP-4 and thus
enhances endogenous incretin hormone like GLP-1 peptides.
GLP-1 increase glucose dependant insulin release and decrease level of circulating
glucagon and hepatic glucose production.
DPP-4
GLP-1 -------------> Inactive GLP-1
SEs. N.V, hypoglycemia, weight neutral, upper respiratory tract infections (URI), and
headache.
INCRETIN (GLP-1) ANALOG. LIRAGLUTIDE. EXENATIDE, ARE GLP-1 (glucagon like peptide)
enhancers. INCRETIN HORMONE ANALOG.
Tips
TRUE OR FALSE
• Acarbose mechanism is alpha glucosidase inhibitor (True/False)
• Orlistat mechanism is intestinal lipase inhibitor (True/False)
• Difference between glyburide and glimepiride. glyburide is short acting and
glimepiride is long acting (True/False)
• Antidiabetic drugs taken before or after meals are sulfonylurea, metformin,
glitazones (True/False)
• The most common cause of glaucoma (blindness) is associated with diabetes
mellitus (True/False)
• Insulin works on receptors on cell membrane (True/False)
• The antidiabetic drug that cause side effect of anorexia is metformin (True/False)
• Anticholesterol drug of choice in diabetic patient is fibrates (True/False)
• Metformin monitoring are renal function and liver function tests (True/False)
• Antidiabetic drugs that is not used in type I DM are sulfonylureas and meglitinides
(True/False)
• Glucagon gives hyperglycemia and insulin gives hypoglycemia (True/False)
• Insulin is antidiabetic drug of choice in pregnancy (True/False)
• If patient has admitted in surgical ward and her blood glucose levels high, the drug
of choice is insulin (True/False)
• Metformin monitoring BSL, HbA1C, CrCl, CBC. (T/F )
Abbreviation and Terminology
IDDM Insulin Dependent Diabetes Mellitus HDL High Density Lipoprotein
NIDDM Non Insulin Dependent DM LDL Low Density Lipoprotein
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24
Thyroid Drugs
Thyroid Drugs
Hypothyroids
Hyperthyroid
131
Thioamides: Lugol's solution (10% KI + 5 %I) I
Methimazole
Propylthiouracil (PTU)
Levothyroxine
Methimazole
Iodides
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RadioactiveIodine(I131isomerofiodine)
Tips
• Why is it beneficial to add propranolol to a drug regimen of a patient diagnosed
with hyperthyroidism?→ to decrease heart rate
• What factors changes required dose adjustment in patient using Synthroid?→
age, weight, heart rate and CVD
1 PTU 2 Serum TSH 3 TSH
4 Hyperthyroidism 5 Deiodinase enzyme 6 Calcitonin
7 Hypothyroidism 8 Lugol’s solution 9 Propranolol
• Stimulated by hypercalcemia. ( 6 )
• Secreted from pituitary gland (anterior) (3)
• Monitoring parameter for hypothyroidism. (2 )
• DOC in pregnancy for hyperthyroidism. (1 )
• What condition has the following symptoms; cold intolerance, constipation,
hypertension, bradycardia, and puffy . (7)
• Graves disease, and Plummer disease. (4)
• Myxedema, and Hoshimoto. (7)
• T 4 metabolized to T 3 by what enzyme. (5)
• Its symptom is sweating. (4)
• 10% KI +5% I solution. ( 8)
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25
Gonadal Hormones
And Antagonists
Gonadal Hormones
Ovary
Testes
Testosterone
Estrogen Progesterone
Testosterone
17β-Estradiol Norethindrone Anabolic steroids
Estrone Norgestrol
Norethynodrel
Testosterone Antagonist
Desogestrel
Estrogen antagonist Finasteride
Medroxyprogesterone
Tamoxifen Dutasteride
Clomiphen Cyproterone
Estrogen agonist + Progesterone Nonsteroidal
antagonist (SERM) antagonist Flutamide
Raloxifine Mifepristone Bicalutamide
(RU-486) Nilutamide
Sex hormones
Included in this category are androgens (male sex hormones), estrogens (female sex
hormones) and progestins. These chemicals are needed for the development,
maintenance and function of the sexual organs and are necessary for normal pregnancy
to occur, be maintained and for birth. Clinical Uses for Various Estrogen Preparations
Estrogen
Estrogens are female sex hormones that are used primarily to decrease bone loss and to
treat the symptoms of menopause. Estrogen is used to reduce or prevent osteoporosis
in susceptible women. Estrogens decrease the frequency and severity of hot flashes as
well as the dryness in the vagina that many post-menopausal women experience.
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Antiestrogens
Tamoxifen
SelectiveEstrogenReceptorModulator(SERM)
Raloxifene
Reduces bone resorption thereby decrease bone turnover.
• Exhibit estrogen like (agonist) effect on bones and lipid metabolism. Exhibit estrogen
antagonist action on uterine and breast tissues.
• Therapeutic use in prevention of osteoporosis.
Progesterone
Progestins are female sex hormones that may be used with estrogens in oral
contraceptive pills, hormone replacement therapy, and treat menstrual irregularities,
and as cancer treatment.
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Therapeutic use • Major clinical use in contraception, generally used with estrogen.
• Not widely used as alone because of its rapid metabolism results in
low bioavailability.
• Progestins are indicated in uterine bleeding, dysmenorrhea,
suppression of postpartum lactone, and endometrium cancer.
• Endometriosis
Side Effects • Weight gain, edema, and depression. Menstrual irregularities
(breakthrough bleeding, amenorrhea).
• Androgen like progestins can increase LDL and HDL ratio cholesterol,
weight gain and edema. Hirsutism, and acne can cause
thrombophlebitis (inflammation of wall of vein).
Antiprogestins-Mifepristone
use once a month when progestin levels are high (Prostaglandin E1 and
misoprostol orally after single dose of mifepristone effectively terminates
the gestation.
Side Effects Uterine bleeding, and possibility of incomplete abortion.
Androgens
Testosterone is the androgen that leads to the development of male secondary sexual
characteristics and maintains the male reproductive system.
Androgens are used to treat delayed puberty in males who do not develop normal
testicular function. They are also used illegally by athletes to build muscle mass. They
are very dangerous when used for this as they may lead to aggressive behavior, and may
cause liver and or brain tumors and death.
Androgens Danazol
Nandrolone and oxandrolone
Stanozolol
Fluoxymesterone
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Antiandrogens.Finasteride
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26
Adrenal Corticosteroids
Glucocorticoids and mineral corticoids
Generic brand Generic Brand
Cortisone Cortone Triamcilone
Hydrocortisone A-hydroCort, Ala-Cort, Methylprednisolone Depo-Medrol, Medralone
Betamethasone Diprosone, Diprolene Ketoconazole Nizoral Shampoo, Nizoral,
Beclomethasone Beconase, Qvar , Spironolactone Aldactone, Spirono
Prednisolone AK-Pred, Econopred, Mifepristone Mifeprex
Prednisone Deltasone, Predone, Sterapred, Metyrapone Metopirone
Aminoglutethimide Aminoglutethimide
The adrenal hormones, or corticosteroids, are drugs with powerful anti-inflammatory
effects. These are used for replacement therapy in conditions such as, Addison’s
disease, a condition of adrenal insufficiency. In replacement therapy, the adverse effects
are minimal since hormones are being replaced and are not added to those already in
the body. Corticosteroids are used for their anti-inflammatory, antiallergic and
antistress effects. Prednisone is used as replacement therapy and also for its anti
inflammatory effects in many conditions, such as arthritis, allergies and asthma.
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0.5% • Flunisolide
• Medium potency. Betamethasone benzoate • Triamcinolone
(0.025), Triamcinolone 0.025 to 0.1 • Fluticasone
• Low potency. dexamethasone, • Mometasone (quick onset, more local
hydrocortisone absorption and lowest systemic absorption,
consequently fewest systemic SEs).
Glucocorticoids
Short acting (8- • Hydrocortisone
12 hour) • Cortisone
Intermediate • Prednisone
acting (18-36 • Prednisolone
hours) • Methylprednisolone
• Triamcilone
Long acting (1- • Betamethasone
3 days) • Dexamethasone
• Paramethasone
Mechanism • For anti-inflammatory corticoids: Glucocorticoids effects on the
distribution, concentration, and function of leukocytes. These
include decrease in concentration of lymphocytes T and B cells)
and increase in concentration of neutrophils.
• Decrease basophils, eosinophils and monocytes, and inhibition of
the ability of leukocyte and macrophages to responds mitogen and
antigen.
• The above Inhibitory response also results in reduce the amount of
histamine release from basophils to inhibit kinins.
Side Effects • High doses stimulate gastric acid and pepsin production and may
cause peptic ulcers.
• Chronic use causes sever bone loss (Due to decrease in calcium)
and myopathy leads to weakness
• Concentration of topical Glucocorticoids depends on site of use on
the body.
Drug and Food • Take with food.Should not be stopped suddenly, taper off or
interactions gradually decrease dose.
• Diabetic drugs: glyburide, chlorpropamide, glipizide, tolbutamide,
and tolzamide. Can rise blood sugar noticeably. Monitor blood
sugar levels
Therapeutic • To treat severe allergic reaction
use • To treat chronic ulcerative colitis
• To treat nephrotic syndrome and renal diseases
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Tips
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27
Oral Contraceptives
Oral contraceptives (birth control pills) are combinations of estrogen and progestins or
progestins only.
Mechanism
• The biological activity of OCs can result from the estrogen and/or progestin
component.
• Prevention of ovulation, alteration of cervical mucus and alteration of
endometrial lining.
• Provide (-) ve feedback to the pituitary gland resulting in suppression of FSH and
LH release from pituitary thus prevents the development and maturation of the
follicle egg, resulting in the prevention of ovulation.
• Stop the pituitary gland from producing LH in order to prevent egg release.
• Make the uterine lining inhospitable to a fertilized egg.
• Partially limit the sperm's ability to fertilize the egg.
• Thicken the cervical mucus to hinder sperm movement (although this effect may
not be key to preventing pregnancy).
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Oral contraceptives
Biphasic. The amount of estrogen is fixed through out the cycle but the amount of
progestin varies (low in the first half and high in the last half).
Triphasic. Low doses of both hormones with minimal effects. The amount of both
estrogen and progestin varies through the cycle in different ratios.
Progestin only
Mechanism of Action. Alteration of cervical mucus, alteration of the endometrium to
inhibit implantation decreased side effects does not suppress the hypothalamus and the
pituitary to the same extent as the combination preparation thus low pregnancy
prevention rate increase in breakthrough bleeding.
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Side effects due to excess estrogen Side effects due to estrogen deficiency
Nausea and vomiting, dizziness Nervousness
Fluid retention; edema Dyspareunia (painful intercourse)
Bloatedness Vaginitis
Enlargement and tenderness of the breast Vaginal bleeding
Chloasma (skin pigmentation) Oligomenorrhea
Leg cramps
Alteration in cornea
Visual changes, headaches
Hypertension
Venous thrombosis
Pulmonary embolism
Depression
Side effects due to excess progestin Side effects due to progestin deficiency
Increase appetite Dysmenorrhea
Weight gain Decrease breast size
Oily skin and scalp Heavy menstrual flow with clots
Acne
Depression
Vaginitis
Increase hair growth
Miss pills Miss one pill. Take as soon as you remember and take usual pill next day.
This means that you might take two pills in a day.
• Miss two pills in a row.
• First two weeks. Take two pills the day you remember and two pills
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next day. Then take one pill until you finish pack.
• Use back up method of birth control, if you have sex in next seven
days of missing pill.
• Third week. Safely dispose remained pills and start new pack same
day. (If you’re on Sunday start schedule continue one pill until
Sunday). You may not have periods this month. If you miss two
periods in a row call doctor.
Emergency
Levonorgestrel 0.75 mg per dose (Plan B) or minipill or morning after pill.
Contracepti
ves
Progestin only. Very effective within 24 hrs and can be used up to 5 days
unprotected sex.
• Contains 2 pills (use 2nd pill after 12 hours of 1st pill).
• To treat nausea and vomiting associated with this pill can be treated
by dimenhydrinate.
Side effects Nausea (23.1%), vomiting (5%), dizziness, and fatigue and also progestins
side effects.
Tips
• Oral contraceptive that are used for the treatment of ACNE include Dian 35, and
Alesse. Diane 35 approved for acne only. (True/False)
• If missed one contraceptive pill? →Double dose next day
• Plan B is used for emergency contraception→ this should be used immediately
after unprotected intercourse.
• The most common side effect of plan B is nausea & vomiting (True/False)
• Absolute contraindications of OCP are pregnancy, CAD, DVT, breast cancer,
genital bleeding, uncontrolled BP, liver cirrhosis. (True/False)
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28
Osteoarthritis
Acetaminophen Betamethasone Synovial Fluid Replacement
Nonsteroidal Anti- Cortisone acetate Hylan G-F 20
inflammatory Drug Dexamethasone Hyaluronic acid sodium
Dexamethasone sodium Sodium hyaluronate
Methyl prednisolone acetate
Topical Pain relievers Prednisolone
Capsaicin Triamcinolone
Methyl salicylate Triamcinolone diacetate
Diclofenac
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Acetaminophen
• Dose of acetaminophen for arthritis 650 mg Q4 to 6h maximum 4 g.
• No cross allergy with NSAID, ASA and Cox-II inhibitors.
• SEs. Rash and at high dose hepatotoxicity.
• Antidote is N-acetyl cysteine, should be administered with 8 hours of overdose
(binds to benzoquinoneimine reactive metabolite).
• Overdose. 7 to 10 g daily refer to poison control centre. Overdose 10 to 13 g daily
dose is lethal.
• 3 drinks/day alcohol ↑ increase risk of hepatotoxicity. Warfarin anticoagulant effect
is ↑>2 g is used.
• MO. AST and ALT elevated.
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NSAIDs. Diclofenac(IR,SR),etodolac,sulindac,pyroxicam,meloxicam,tenoxicam,ibuprfe
n,naproxen,ASA,diflunisal
• Avoid NSAIDS and COX II in ASA allergies. However acetaminophen can be used.
• Avoid concomitant use of 2 NSAIDs.
• Past history of GI ulcers, and avoid in CrCl <50 ml/min.
• ASA anticoagulant effect currently using warfarin avoid in age over 65 years due to
increase risk of GI bleeding and renal disease.
• All NSAIDs CI in severe renal disease (CrCl <30 ml/min) since NSAIDs can cause renal
failure.
• All NSAIDS can increase blood pressure and worsen pre-existing BP.
At initiating NSAIDs patient should be assessed for gastrointestinal, cardiovascular (MI,
stroke, fluid retention, hypertension) and renal risk factors and should be monitored for
toxicities.
Elderly patients, history of GI ulcers, cardiovascular disease patient taking long term
NSAID should be combined with PPI or misoprostol. (Diclofenac+misoprostol,
naproxen+esomeprazole)
Avoid NSAIDs including cox2 inh. If history of peptic ulcer disease, cardiovascular risk
factors, renal failure (CrCl <30), heart failure or asthma.
Topical NSAIDs
Diclofenac topical and Methyl salicylates
• For external use only, approved for treatment regiment not more than 3 months
duration (continuous or intermittent).
• SEs. skin dryness or irritation, hypersensitivity, serious GI toxicity has
NOT been reported.
• Note. Patient with GI ulcers history should avoid NSAIDs, Cox-II, anticoagulants, and
corticosteroids.
• Methyl salicylate. May increase warfarin anticoagulant effect. Avoid contact with
eye and mucous membrane.
Cox-2 inhibitors
Celecoxib
• Usual dose do not appear to have antiplatelets action.
• Contraindicated in sulfa allergy.
• Avoid in patient with serious heart diseases like congestive heart failure. Cox2 can
exacerbate hypertension, and promote edema.
The risk of increased cardiovascular events can occur with Celecoxib.
Avoid in pts history of MI, stroke, serious heart diseases, chest pain, CHF.
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Lumiracoxib (Prexig). Withdrawn due to CHF risk and fetal hepatotoxicity can get by
special access program of health Canada.
Steroids
Intra articular injections. Methyl prednisone.
• Maximum 3 injections/joint/year. Minimize activity for 3 days after injection benefit
last 4-6 weeks inexpensive, safe and effective therapy for individual joints for esp.
hip, and knee).
Systemic corticosteroids
• Systemic corticosteroids are generally not use for OA. Local (intra articular) may be
used in case of signs of inflammation (minimum in OA) but take to max 3 injections
per year per joint (knee joint).
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Opioids
Morphine
• Lidocaine potential enhancement of opioids effect
• Oxycodone IR5-10 mg QID for short for acting formulations
Tips
• Risk factors for renal toxicity associated with NSAIDs and COX II inhibitors include
volume depletion, diabetes, age, and cirrhosis.
• Counseling of Capsaicin Do not apply on open wounds, cuts, and eyes. Wash
your hand after applies. Do not apply on large areas.
• Osteoarthritis recommended? Weight bearing exercise (walk, run, jog, jump,
light lifting).
• Glucosamine/chondritin? Increase synovial fluid
• Viscous supplement hyluronic acid are? Long acting than steroids.
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29
Disease Modifying Antirheumatic Drugs
DMARD’s Drug Name Trade Drug Name Trade Name
Name
Cytotoxics Methotrexate Azathioprine
Gold preparations Aurothioglucose
Sodium aurothioglucose
Other DMARDs Cyclosporine Neoral Sulfasalazine Salazoprin
Hydroxychloroquine sulfate Penicillamine Cuprimine
Leflunomide Arava Tacrolimus
Minocycline
Biological Adalimumab Humira Etanercept Embrel
response Anakinra Kineret Infliximab Remicade
modifiers
A chronic inflammatory disease with frequent acute attacks. The immune system is
involved in attacking the joints and surrounding structures such as muscle tendons and
most other connective tissue. There is inflammation of the synovial membrane.
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Etanercept. Binds to the tumor necrosis factor (TNF alpha and beta).
• Given SC weekly 4 times, it is self injection.
• Side effects. Most common respiratory tract infections.
• Rituximab (Rituxan). B lymphocytes depletor.
• Abatacept (Orencia). T cell co-stimulation inhibitors
• Anakinra (Kinaret). Interleukin-1 (IL-1) receptor inhibitors.
• Toclizumab (Acterma). Interleukin-6 (IL-6) inhibitors.
Methotrexate
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• Renal failure
• Pulmonary toxicities (pneumonitis) in children
• Susceptible to infections (P. carinii)
Dose • Starting 7.5 to 15 mg po Q wk. Increase by 2.5 to 5 mg Q 2-4 wk.
Maximum 25 mg/wk. Maintenance dose 7.5 to 20 mg po, sc or IM
Q wk (single dose if tolerated or divided in 2 or 3 doses Q12h).
• Effectiveness seen after 2 or 6 weeks and administered PO, IM, SC
• If GI upset occurs start 2.5 mg (12 h after) 2.5 mg (12 h after) 2.5
mg
• Methotrexate weekly doses 20 to 25 mg (orally or parenteral) for at
least three months.
• Concurrent use of folic acid reduces oral ulcers side effect. Alcohol
restriction may minimize hepatotoxicity.
Dihydropteroic acid
Dihydrofolic acid
THF cofactors
Therapeutic • Refractory RA
use • Mechanism cytotoxic agent that suppress T-cell activity
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Hydroxychloroquine
Sulfasalazine
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syndrome)
• Skin: facial edema,
• Gastrointestinal: hepatitis, pancreatitis
• Nervous System: smell and taste disorders
Dose • PO or rectally
Pharmacokinetics • About 20% of sulfasalazine is absorbed in the small intestine
after oral administration
Contraindications • In patients with hypersensitivity to component of the product,
sulfonamides, or salicylates. In patients in whom acute
asthmatic attacks, urticaria, rhinitis or other allergic
manifestations are precipitated by ASA or other nonsteroidal
anti-inflammatory agents. Fatal anaphylactic reactions have
occurred in such individuals.
• In patients with intestinal and urinary obstructions.
• In patients with porphyria, as these drugs have been reported
to precipitate an acute attack.
• Infants under 2 year age
Allergies • If allergic to the following drug avoid sulphasalazine
• ASA, Furosemide, Thiazide diuretics, Carbonic anhydrase
inhibitors, Sulfonamides, sulfapyridine and Sulfonylureas
Counseling • Discolors urine and may color skin orange yellow.
• May permanently stain soft lenses
• Take drug after meals to reduce GI distress and to facilitate
passage into intestine.
Leflunomide (Arava)
Cyclosporine(Neoral)
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Minocycline
D-penicillamine
Gold sodiumthiomalate
use
Side Effects • Most common
• Skin rashes
• Proteinuria (after IM admin.)
• Nitritoid reaction (low blood pressure and syncope after
injections)
• Pruritis (pruriginous), dermatitis
• Angioedema
• Thrombocytopenia
• Aplastic anemia
• Diarrhea
• Stomatitis
• Proteinuria
Post dose • Arthralgia, flushing, hypotension
reactions
Tips
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TRUE OR FALSE
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30
Gout and Hyperuricemia
Drugs to treat gout and hyperuricemia
Acute gout attacks are treated by anti-inflammatory drugs like NSAIDS (Indomethacin),
colchicine and corticosteroids. However, chronic hyperurecemia is treated by
antihyperuricemic agents like allopurinol, sulfinpyrazone and probenecid.
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Indomethacin
Colchicine
Probenecid
Mechanism • Uric acid is both actively secreted and actively reabsorbed in the
kidney. Probenecid partially inhibits both the active secretion and
the active reabsorption.
• Uricosuric agents are weak acids that compete with uric acid, in
the S2 segment of the proximal renal tubule, for reabsorption by
weak acid mechanism
Therapeutic use • hyperuricemia
Side effects • Before using probenecid check to see that the patient is not a
high excreter of uric acid, otherwise the use of drug may
precipitate uric acid crystals in the kidney
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Sulfinpyrazone
Allopurinol(Zyloprim)
Tips
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31
Osteoporosis
Osteoporosis Treatment
Alendronate Raloxifene
Etidronate Calcium carbonate Teriparatide hydrochloride
Risedronate Calcium gluconate
Pomidronate
Screening
• All post menopausal women and men over 50 yr age.
• Bone mineral density testing for >65 yr age and high risk based on major risk factor.
• Height loss >4 cm total or >2 cm in 1 yr
• Steroid use >3 mo
Diagnosis
• Bone mineral density (BMD) scan using Dual Energy X-ray Absorptiometry (DEXA)
machine.
• Portable ultrasound
• X-ray
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Calcium Supplements. A study shows 61% of adults with osteoporosis did not take
calcium supplements. Inadequate intake of calcium and vitamin increase risk of
osteoporosis.
• Calcium carbonate (40% elemental calcium)
• Calcium phosphate or Tricalcium phosphate or tribasic (39%)
• Calcium chloride (27%)
• Calcium citrate (21%)
• Calcium lactate (13%)
• Calcium gluconate (9.3%)
Calcium carbonate provides most calcium because it has highest elemental calcium,
some products of calcium carbonate are obtained from oyster example O-Calcium.
calcium gluconate has least elemental calcium.
Calcium Drug Interactions. Acid suppressing agents such as H2RAs and proton pump
inhibitors may reduce phosphate binding capacity of calcium carbonate by increasing
gastric pH. Calcium acetate is better absorbed in alkaline pH. Calcium interaction
interact with drug such as thyroxin, tetracycline, quinolones, and bisphosphonates.
Bisphosphonates
Side Effects • Diarrhea, nausea, altered taste, abdominal pain, nighttime leg cramps.
Esophageal ulcers especially if not taken properly. Bisphosphonates
have NO known impact on cardiovascular diseases, or breast or
endometrial cancer.
• Osteomalacia (etidronate only).
Dose
and • Take first thing in the morning empty stomach and take with plenty of
administration water.
• Do not lie down for 30 to 45 min after medications (stay upright).
• Calcium supplements should be at least separated by 2 hours before or
after.
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Alendronate
• Alendronate increase bone mass of all skeleton, and reduces non vertebral fracture
or decrease vertebral fractures or all fracture (including hip).
• Available dosage forms 5 mg, 10 mg, 35 mg, 40 mg, and 70 mg once weekly.
Fosavance 70mg + 2800IU vitamin D QWK, and 70 mg + 5600IU vitamin D QWK.
• Prevention of osteoporosis in postmenopausal women once 5 mg daily.
• Treatment of osteoporosis in women 10 mg once daily or 70 mg tablet once weekly.
• Take empty stomach, 1st in the morning. Do not lie down 30-40 min.
Etidronate
• Increase bone density and secondary prevention of vertebral fractures.
• Etidornate and calcium is used in cyclical therapy to increase bone density
and prevents vertebral fracture . Etidronate 400 mg/day for 14 days than
76 days calcium 500 mg supplements. Calcium supplements are avoided during the 2
weeks of cycle etidronate.
• Calcium is taken between the cycles of etidronate.
• Etidronate has lowest anti resorptive activity.
Risedronate.
• It is almost same as alendronate. Risedronate has highest anti resorptive activity and
than alendronate.
• Risedronate available dosage forms 5 mg/day or 35 mg once weekly, 75 mg two
consecutive weeks for 1 mo. or 150 mg Q month.
• Take at least 30 min before the first food, beverage, or medication. NOT lie down
for 30 min after taking.
• SEs. Esophageal ulceration, night leg cramps, GI symptoms taste changes.
Raloxifene
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Calcitonin salmon
Calcitonin is a hormone secreted from thyroid gland. Hypercalcemia stimulates the
production of calcitonin from thyroid gland. Calcitonin hormone helps bone formation
by transporting Ca from blood to bones.
Mechanism. Directly effect on osteoclast and decrease bone resorption through direct
effect.
Two products are available. Miacalcin 200 IU/day intranasally once daily. Common SEs is
nasal irritation. Calcimar, caltine 50 to 100 IU sc/day or Q 2nd day or 5 days/wk. Not
approved for osteoporosis.
Tips
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32
Asthma and COPD
Leukotriene antagonists
Muscarinic Methyl
β2 agonist xanthene Corticosteroids Mast cell stabilizers
antagonist Leukotriene
Steroid avoiders
receptors antagonist
Theophylline (Steroid sparing)
Cromolyn sodium
Aminophylline
Nedocromil
Ipratropium (short acting) Zafirlukast
Tiotropium (long acting) Montelukast
Inhaled corticosteroids aerosol (ICS)
Fluticasone, beclomethasone, budesonide
oral. prednisone or prednisolone
iv. hydrocortisone, methyl prednisolone
Short acting (Rescue)
Albuterol (salbutamol)
Terbutaline Long acting (Maintenance)
Formoterol (full agonist), quick onset
Salmeterol (partial agonist)
Formoterol fumarate dihydrate (Oxeze)
Asthma is inflammatory disease that triggers by following factors (factors that increase
Triggers. Early asthmatic response. Symptoms only (i.e. bronchoconstriction).
Cold air, exercise, emotional stress, pets (cats, dogs), environments and non adherence.
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Bronchodilators
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ShortactingBronchodilators (SABA)
Long actingBronchodilators(LABA)
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and diuretics.
Corticosteroids
Side effects • Oral thrush (candidiasis) and hoarseness. Can be reduced by rinsing
mouth or using spacer or aerochamber.
• Spacers or aerochamber reduces systemic side effects and reduces
thrush.
• Nasal sprays. Systemic absorption is minimal and side effects are
localized nasal irritation, nosebleed, sore throat, hoarseness, rarely
candidiasis.
Recommendation • To reduce corticoids side effects rinse and gargle mouth after
inhalations.
Combination Adviar. Salmeterol (LABA) + Fluticasone
products Symbicort. Formoterol (LABA) + Budesonide
Prednisone/Prednisolone
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Therapeutic use • Skin diseases, rheumatic disorders, and certain blood disorders.
Side effects • Long-term treatment with high doses can cause fluid retention,
indigestion, diabetes, hypertension and acne.
Drug-Drug • It may increase the adverse effects of diuretics.
interaction
Recommendation • Prolonged systemic use can lead to such adverse effects as
diabetes, glaucoma, cataracts, and fragile bones, and may retard
growth in children.
• Dosages are usually tailored to minimize these effects.
Fluticasone
Budesonide
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Beclomethasone
Anticholinergics
Ipratropium Atrovent
Mechanism An anticholinergic bronchodilator that relaxes the muscles. surrounding
the bronchioles. Have longer effect but slower onset.
Therapeutic use Anticholinergics are effective bronchodilators and have low lipid soluble
and poor transport across membrane (does not cross blood brain barrier).
Side effects Anticholinergic
Leukotriene inhibitors
Zafirlukast • Accolate
Mechanism • Inhibitors of LTC4 and LTD4 receptors. Steroid sparing properties (Instead
increasing steroid dose LTRA are added.
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Monitoring Periodic checks on blood levels are require especially the serum level.
Theophylline are contraindicated in patients with hypersensitivity to
xanthenes compounds. Caution inpatient with peptic ulcers and seizure
diseases.
Factors that Increase theophylline clearance (decrease levels) in age 1 to 9 years, high
alter protein diet, smoking (tobacco, marijuana), fever, drugs such as
theophylline carbamazepine, phenobarbital, phenytoin and rifampin.
clearance
Decrease theophylline clearance (increase levels) in age (elderly, infants,
under 6 months age, premature neonates), CHF, fatty food, high
carbohydrate diet, liver dysfunction and drugs such as oral contraceptives,
non selective beta blockers, CCBs, macrolide antibiotics (erythro and
clarithromycin) , clindamycin, fluroquinolones (ciprofloxacin) , zafirlukast,
and allopurinol.
CHRONIC BRONCHITIS is an inflammation of the airways in the lungs that causes lungs to
produce excessive amounts of mucus (phlegm). This reduces the flow of air to the lungs.
Onset age 45 years. The major risk factors are smoking (80-90%), family history,
occupational exposures to certain ducts and fumes, air pollution, second hand smoke
and asthma.
SABD
SAAC Ipratropium
SABA Salbutamol
Terbutaline
LABD
LAAC Glycopyrronium
Tiotropium
Aclidinium
LABA Formoterol
Salmeterol
Indacaterol
Combinations Salbutamol + ipratropium
Drug used for the treatment of COPD. Beta adrenergic agonists, corticosteroids,
ipratropium, and theophylline.
Patients with COPD, antibiotic or oral corticosteroid therapy in last 3 months use, a class
of antibiotic, which was not previously prescribed. Antibiotic therapy to treat chronic
bronchitis. Azithromycin, doxycycline, amoxicillin and quinolones. Do not use
erythromycin.
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Tips
• Theophylline inhibit activity of Phosphodiesterase (PDE) induction (True/False)
• Leukotrienes are chemical derivatives of arachidonic acid(True/False)
• Leukotrienes are produced from arachidonic acid by catalyzed by lipoxigenase
(True/False)
• Long term use of oral corticosteroids may cause osteoporosis, diabetes, Cushing
syndrome, susceptible to infections (True/False)
• Leukotriene antagonist act on LTC4 and LTD4 (True/False)
• Drug of choice for aspirin induced asthma LTRAs(True/False)
• Patient has COPD and pneumonia, what is drug of choice penicillin's doxycycline,
azithromycin(True/False).
• Oral contraceptive effect on theophylline decrease clearance of
theophylline(True/False)
• Dry cough is caused by accumulation of bradykinin(True/False)
• What is differentiating symptoms of asthma from COPD wheezing in asthma
• Smoking is very high risk factor for COPD(True/False)
• What asthma devices do not require shaking powder dose inhalers(True/False)
• Asthma exacerbations are NOT triggered by warm air(True/False)
• Obstruction of airways in lungs is referred as COPD (True/False)
• Permanent enlargement of alveoli is referred as emphysema (True/False)
• Highest clearance of theophylline in which age group 1 to 9 yrs(True/False)
• When can we use leukotriene receptor inhibitors to avoid or minimize use of
steroids (True/False)
• What is important to counsel in patient using steroid inhalers --> rinse mouth after
each use
• Histamines are released from mast cells and basophile(True/False)
• What kinds of changes can you expect to see in aminophylline solutions exposed to
air? --> crystal formation of theophylline
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33
Anticancer Drugs and Chemotherapy
Question Alerts!
Action of DNA
Examples of antimetabolites
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Cell cycle phase specific drugs. More active against cells that are specific phase of cycle.
• G 1 phase. L-aspraginase and prednisone
• S phase. Methotrexate, 6-thioguanine, cytarabine
• G 2 specific. Bleomycin and etoposide
• M phase. Vincristine vinblastine, and peclitaxol
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Alkylating agents. Act by alkylating DNA. The most common site of alkylation
is N-7 position of guanine. The alkylating agent appear to be the most
effective on G 1 or S phase.
Highly reactive agent can alkylate or bind covalently with cellular components of DNA.
Cyclophosphamide
Antimetabolites.
Antimetabolites prevents the biosynthesis of normal cellular metabolites.
Inhibits essential components of cell synthesis by competing with the natural substrate
for enzyme involved in synthesis of cell components.
Mercaptopurine (6-MP)
Dactinomycin
Mechlorethamine
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Paclitaxel (Taxol)
Chemotherapy
The treatment of cancer with drugs is called chemotherapy. Antineoplastic drugs, also
referred to as chemotherapeutic agents, are drugs that are used to treat cancer.
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• Skin.
• Alopecia, dry skin, nail changes, pigmentation (melanoma), and xerostomia.
• Alopecia is the loss of hair. Drug that causes alopecia is doxorubicin, daunorubicin,
cyclophosphamide, vincristine, and paclitaxel.
• Vessicant agents includes dactinomycin, doxorubicin, mechlorethamine, mitomycin,
vincristine, and vinblastine.
• Hair re-growth occurs after 1 to 2 months after stopping chemotherapy.
• Xerostomia. Dry mouth is one of the most common complications associated with
radiation therapy. Reversible after 6 to 12 months of therapy.
• Can be managed by sugar free hard candy, chewing sugar free gum stimulates
salivation. Ice chips, sugarless candies, and commercially available saliva substitute
or cholinergic agonist (Pilocarpine 5 mg tab).
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Cardiotoxicity
• Risk of congestive heart failure (CHF), commonly seen with (anthracyclines)
doxorubicin, daunorubicin, epirubicin, mitoxantrone and trastuzumab.
• 5-FU, capecitabine can cause coronary spasms, or myocardial ischemia mimicking a
myocardial infarction (avoid in known coronary artery disease patients).
• Cardio toxicity can prevented or lessens by using cardio protective agent
dexrazoxane. Use of dexrazoxane (500 mg/m2) 30 min prior to administration of
doxorubicin protects against cardiomyopathy.
Neurotoxicity
• Common with vinca alkaloids such as vincristine, vinblastine, cytarabines,
methotrexate (very little), 5FU, and interferon alpha.
• Peripheral neuropathies associated with vincristine, peclitaxel can cause peresthesia
(numbness and tingling, pin feeling) can occur with vincristine, which often appears
within few weeks of therapy.
• High dose of cytarabin may produce cerebllar toxicity that manifest initially as loss of
eye hand coordination and progress to coma.
• Fludrabine cause severe neurotoxicity.
• Caramustine and other alkylating agents cause little or no neurotoxicity.
GI toxicity
Mucositis is generalized burning, and pain on the ventral surface of tongue. Floor of
tongue, mouth looks erythromatus.
Stomatitis is generalized inflammation of oral mucosa.
• Mucositis common with doxorubicin, methotrexate, 5-fluorouracil, actinomycin,
bleomycin and capecitabine.
• Recommend mouth hygiene, xylocaine, viscous sucralfate, nystatin, sodium
bicarbonate, for severe cases peliformin (growth factor) can be used. Avoid alcohol,
antihistamine, steroids, and spicy food.
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• Mucositis treatment and prevention. Topical anesthetics for small ulcers apply
benzocaine in orabase. For generalized mucositis topical rinses like viscous
lidocaine, or dyclonine 0.5 or 1%.
• Corticosteroid provides anti-inflammatory action.
• Capsaicin. Produces burning and pain and ultimately desensitizes pain.
• Sucralfate suspension may provide benefit by coating.
• For localized effect use benzocain in orabase.
• Mucositis prevention. Chlorhexidine gluconate 0.12%, may reduce severity
and frequency of mucositis infections.
Hepatotoxicity
Nephropathy
Methotrexate may precipitate in kidney. Monitor elevate BUN and electrolyte
abnormalities: Cisplatin and streptozocin. Amifostine may be used to protect the kidney
from the nephrotoxicity associated with cisplatin.
Sexual dysfunction
Cyclophosphamide, melphalan, and procarbazine associated with significant infertility in
men and women.
Hemorrhagic cystitis
It is a bladder toxicity that is seen most commonly after administration of
cyclophosphamide and ifosfamide.
• These drugs produce a metabolite called acrolein. This cause chemical irritation in
bladder mucosa, resulting in bleeding.
• Hemorrhagic cystitis caused by acrolein can be prevented by excessive hydration
and subsequent frequent urination. The other method is by administering
uroprotecting agent called MESNA, which bind acrolein and prevent from contacting
the bladder mucosa.
Pulmonary toxicity
• Pneumonitis, pulmonary fibrosis commonly seen with bleomycin, carmustine,
cyclophosphamide, mitomycin, methotrexate, and vinca alkaloids.
• Symptoms of pulmonary toxicity includes SOB, non-productive cough, and rarely low
grade fever.
• The most common with bleomycin, mitomycin, and carmustine.
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Tips
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34
Gastrointestinal Drugs
GI Drugs
Antacids
Types of antacids
• Aluminum hydroxide. SEs. Constipation
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Combined preparations
• Antacids combined with alginates or foaming agents.
• Alginates are intended to float on the content of the stomach to produce a
neutralizing layer to subdue acid that can otherwise rise into esophagus, causing
heartburn.
• Simethicone is antiflatulent agents are intended to relieve flatulence.
Drug interactions with antacids. Tetracycline chelation with bi and trivalent ions,
thereby this can reduce absorption of tetracycline. Antacids decrease absorption of
fluroquinolones, bisphosphonates, and thyroid hormones, by complexation.
Rosuvastatin, gabapentin, levodopa. Antacids increase absorption of levodopa
Ketoconazole and PPIs. The antifungal ketoconazole require acidic medium for
absorption. Concomitant use of antacids can reduce absorption of ketoconazole.
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Drug Clopidogrel are potent inhibitors of CYP2C19 and PPIs are substrate
interactions of CYP2C19. Thus avoid combination of PPI and clopidogrel.
Pantoprazole has weak interaction, and can be combined.
Taken 30 min before food. May ↓ bioavailability of iron salts,
digoxin, ketoconazole, ↓ theophylline levels.
H2receptor antagonists
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Zollinger-Ellison syndrome.
Side effects Gynecomastia. elevation of prolactin (cimetidine.
Headaches. famotidine and ranitidine, hematologic abnormalities
Decreased hepatic microsomal metabolism of some drugs like
cimetidine, which decreases the metabolism of warfarin, theophylline,
diazepam and phenytoin.
Diarrhea, constipation, fatigue, confusion, cardiac effects
Side effects are more common in elderly and decrease renal function
patients.
Tips Nizatidine is preferable used in elderly and renal disorder patients
Cimetidine and famotidine are now available without prescription in
some countries for the treatment of dyspepsia (2 weeks supply).
Drug Cimetidine: Increases the effects of anticoagulants. Inhibit CYP 3A4
interactions metabolism, thereby inhibit metabolism of warfarin, phenytoin,
theophylline.
Sucralfate binds to the ulcer site by forming a viscid sticky gel that coats the ulcer site
and acts as a protecting.
BismuthCompounds
GERD
• Mild GERD, relief of symptoms is with antacids, alginates or non-prescription
strength H 2 RA.
• Severe GERD. PPI are the drug of choice. Use PPI for 2 to 4 weeks.
• The goal is to raise the intragastric pH 4 during periods when reflux is likely to occur.
Peptic ulcers. The common cause of ulcers are due to H. pylori infection or drug induced.
• Gastric ulcers. Due to reflux since has weak pyloric sphincter
• Duodenal ulcers. Excessive secretion HCl from parietal cells
• Acute stress ulcers (Curling’s ulcer) can cause tumors.
• Pathologic acid-hypersecretory states is Zollinger-Ellison syndrome
Tips
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35
Drugs in Renal Diseases
Approximate renal dysfunction
Creatinine clearance range 80 to 120 mL/min and renal disease <50% renal elimination.
Rate of excretion = rate of filtration + rate of secretion - rate of reabsorption.
Nephrotoxic Drugs. Potential to worsen renal function if patient renal function is CrCl
(<0.5 mL/s/70kg).
A female 60 yr old, body weight 70 kg, patient SrCr is 100. Doctor wants to
prescribed nitrofurantoin. Doctor wants to know if suitable to prescribe?
All Aminoglycosides
The nephrotoxicity is acute tubular necrosis.
• Dose will remain same
• Intervals are increased
• 2 to 5 hours half life.
• Eliminate after 10 to 20 days thereby this give post dose antibiotic effect.
• Serum creatinine concentration is monitored frequently every 2 to 4 days.
Drugs needed monitor their therapeutic range. Serum dose concentration monitoring
(SDCM). may help guide dose adjustment.
• Lithium 0.5 to 1.5 mEq/L
• Valproic acid50 to 100 mg/L
• Procainamide4 to 10 mg/L
• Carbamazepine 4 to 12 mg/L
• Quinidine 2 to 6 mg/L
• Vancomycin
• Theophylline
• Aminoglycosides
• Phenytoin
• Cyclosporine
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Tips
• Oliguria: Urine output <400 mL/day
• BUN/Creatinine ratio, normally 10/1.
• Renal azotemia is uremia
• Pylonephritis is? Pelvic inflammation or infections
In renal disease patient what happens to half life of drug and steady state
concentration?
ko
Css = ko = rate of infusion
CL
CL = total body clearance
DL = loading dose
DL = Css x Vd
DM = maintenance dose
Vd = volume of distribution
DM = Css x CL x τ
τ = dosing intervals
ko
Css =
VdK
K el = 0.693/ t 1/2
CL T = V d x (0.693/t 1/2 )
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36
Immunomodulators
Immunomodulators
Immunosuppressants Immunostimulants
Drugs Antibodies
Glucocorticosteroids
Prednisone Lymphokine Colony stimulating
Aldesleukin Interferons factors (CSF)
Prednisolone
Inteferon-α-2a Filgrastim,
Interferon-β-1b Sargramostim
Anti-TNF α agents Interferon-y-1b
Etanercept
Thalidomide
Cytotoxic agents
Azthioprine
Cyclophosphamide
Methotrexate
Enzyme inhibitors
Mycophenolate mofetil
Leflunomide
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Immunosupressant antibiotics
• Cyclosporin. Indicated for organ transplant rejection, rheumatoid arthritis and as
anticancer drug.
Cytotoxic drugs
Methotrexate. Indicated for the treatment of cancer, rheumatoid arthritis and psoriasis.
Immunostimulants
• Indicated for the treatment of
• Anemia
• Thrombocytopenia
• Neutropenia
• Bone marrow depression (myelosupression)
• Immunodeficiencies such as HIV.
Interferons
Indicated for viral infection like hepatitis B and C and multiple sclerosis.
• The most common SE interferon is flu like symptoms.
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37
Ophthalmic Drugs
Agonist Antagonist
Agonist Antagonist Gives mydriosis by
Pilocarpine * Atropine
Gives Miosis
radial muscle
Gives miosis
By spincter muscle
Tropicamides
* contraction
contraction Gives mydriosis
Nonselective Selective
Phenylephrine Timolol Betaxolol
Brimonidine
Psedoephedrine
Xylometazoline
Epinephrine
Propine
Question Alerts!
Mechanism in glaucoma for
Glaucoma
1) Timolol
• Is due to increase intraocular pressure (IOP)
2) Dorzolamide
• Due to closing of schlem canal
3) latanoprost
• Due to increase in aquous humor
4) epinephrine
• Treatment
• Use medications that gives miosis or mydriosis
• Medication that gives mydriosis open schlem canal
Cholinergic drugs
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Cholinergic antagonist
• Atropine is plant Belladona atropa product. It is tertiary amine, it enters, where it
acts as an M receptor antagonist.
• Pharmacological effects at higher doses Mydriasis and cyclopegia (paralysed
accommodation ciliary muscles), hyperthermia, tachycardia, sedation, urinary
retention, constipation, behavioral excitation, and hallucinations.
• Tropicamide: Indicated ophthalmology ocular exams (topical).
Beta blockers
• Timolol and betaxalol. They decrease IOP by inhibiting formation of aqueous humor.
• Decrease aquous humor formation by acting on NE at celiary epithelium.
• Timolol is non selective beta blockers and betaxalol is selective beta 1 blocker.
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Ophthalmic Lubrication
Ophthalmic lubrication
Carbopol 940
for Artificial eye
Carboxymethylcellulose (CMC)
Tyloxapol
Dextran 70/hydroxypropyl
methylcellulose Enzymatic preparations;
Glycerin Opthalmic antiobiotics Chymotrypsin
Hydroxypropyl cellulose Fusidic acid and polysporin Ophthalmic surgical implant;
Hydroxypropyl methylcellulose Opthalmic antivirals. Idoxuridine Gelatin, absorbable film
(HPMC) Viscoelastic preparations;
Hypromellose Sodium hyaluronate
Polyethylene glycol Prostaglandin PGF2α analog
Polysorbate 80 "prost"
Polyvinyl alcohol
Sodium hyaluronate
Viscosity enhancer. Increase tear retention time and help to protect ocular surface.
examples. CMC, HPMC, polyvinyl alcohol, propylene glycol, and hydroxypropyl-guar.
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Tips
• Glaucoma is two types: Open angle glaucoma (95%), close angle glaucoma (5%)
• Open angle glaucoma: Fluid drains too slowly from anterior chamber. Pressure
gradually rises (increase IOP), almost always in both eyes, causes optic nerve
damage. If not treated, can lead to blindness. DOC Timolol
• Emergencies of open angle glaucoma Pilocarpine
• Close angle glaucoma sudden attacks of increased pressure, usually in one eye (T/F)
• Diabetic retinopathy leading cause of blindness, affects the retina. The best way to
prevent is control diabetic condition (T/F)
• Drugs that cause dilation of pupil are Mydriatic
• Blind spot is also known as Optic disk
• When light rays come to a focus behind the retina, the eye is characterized as
Hypermetropic
• The part of the eye that related to focus of eye is Lens
• Tropicamide indicated in ophthalmology ocular exams (topical).
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38
Antimicrobials
Antibiotics classifications
Strep categorized as
Non hemolytic: S. viridans
Hemolytic
Group A (Strep. pyogenes) (GAS)
Group B (Strep. pneumonia)
Group C
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Beta-Lactamase Inhibitors
• Clavulanate
• Sulbactam
• Tazobactam
Clavulanic acid
• Beta-lactamase inhibitors such as clavulanic acid can be combined with sensitive
Beta-lactams to yield an active combination with resistant organisms.
Penicillins • Penicillin G
• Penicillin V
• Methicillin
• Nafcillin
• Oxacillin
• Carbenicillin
• Ticarcillin
• Piperacillin
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Aminopenicillins • Amoxicillin
• Ampicillin
Penicillin G
Mechanism • Cell wall synthesis inhibitors
Therapeutic uses • Gram + ve (all of them), Gram –ve for Neisseria
Side effects Hypersensitive reactions, rash,
• Nausea & Vomiting
• Pseudomembranous colitis
• Intestinal nephritis
Side effects Take empty stomach
management
Drug interactions • Interferes and alters test results for urine and serum protein
levels. It does not interfere with test using bromophenol blue.
• Aminoglycoside causes synergistic effect. Most effective
endocarditis infections.
PenicillinV
Penicillin V
Mechanism • Cell wall synthesis inhibitors
SE management • Give 1 hour before or 2 hour after meals for max absorption.
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Drug interactions • Interferes and alters test results for urine and serum protein
levels. It does not interfere with test using bromophenol blue.
Piperacillinand Carbenicillin
Side Effects
Drug interaction Used combination with β-lactamase inhibitors.
Often mixed with aminoglycoside (not in same IV bag)
Amoxicillin andAmpicillin
Loracarbef
rd
3 generation Cefixime (po) Oral once daily
Contain Cefoperazone Hepatic elimination only, does not get in CNS
methylthiotetraz Cefotaxime (iv) Renal and hepatic elimination. Can penetrate in CSF.
ole side chain. Cefpodoxime
Can cause Ceftazidime (iv) Active against Pseudomonas aeruginosa
hypoprothrombo Ceftriaxone (iv) Longest half life (8 hours). Single dose, it has bile excretion.
nemia and Can be used renal diseases. Good penetration in bone.
bleeding
Cefdinir Oral once daily
problems
Ceftibuten Oral
Gram -ve
th
4 generation Cefepime (iv) Activity is same as 3rd generation, but more resistance to β-
lactamases.
Dose IV and PO
Cephalosporins-3rdGeneration
Clinical use Gram negative only. Reserved for serious infections (bacterial
meningitis).
These drugs can penetrate Cerebrospinal fluids (CSF) thereby it
indicated for bacterial meningitis infections.
Nosocomial infections (hospital acquired infections).
Unknown origin infections Sepsis in immunocompramized
patients.
Dose IV and PO
Cephalosporins- 4thGeneration
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Vancomycin
Mechanism Cell wall synthesis inhibitor. It is unaffected by beta lactamase, thus used in treatment of
penicillin resistant strains. Bactericidal antibiotic against gram +ve.
Therapeutic A very important drug for treating methicillin-resistant Staphylococcus aureas infections
use (MRSA).
Vancomycin is an alternate drug for treating super infection (superbug) by Clostridium
difficile in patients with P. colitis.
Narrow spectrum of activity against Staphylococcus, Streptococcus and Clostridium sp.
(gram + ve bacteria).
Side effects Chills, fever, ototoxicity, and nephrotoxicity (>75% renal elimination). Monitor, renal
function test or Serum drug concentration.
Precautions Rapid administration (infused <1h) causes red man syndrome
(flushing/rash/hypotension). In renal failure patient drug will accumulate.
Dose adjustment is guided by monitoring serum drug concentration.
Dosage iv and oral (oral is used in only treatment of P. colitis) and half life 6 to 8 h.
Amino glycosides
Gentamicin, Streptomycin, Tobramycin, Kanamycin, and Amikacin
Pharmacokinetics
All amino glycosides renally eliminated.
Half-life 2 to 5 hours. Post dose antibiotic effect (PDAE)
• Only kanamycin and neomycin have oral and topical
• Commonly amino glycosides used as IM or IV
• Streptomycin has only IM.
• Pharmacokinetics is not completely understood.
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Gentamicin
Streptomycin
Streptomycin
Uses Gram –ve.
Second line treatment for tuberculosis (mainly streptomycin).
Treatment for plague (streptomycin). Pseudomonas (streptomycin).
Combined with cephalosporin's (2nd and 3rd) to reduce resistance
Side effects Otic nerve toxicity-8th cranial nerve (mainly streptomycin)
Highest ototoxicity and least nephrotoxic.
Tobramycin
Macrolides
Erythromycin (po, parenteral), Clarithromycin (po), Azithromycin (po), and
Telethromycin (po) (ketolides).
SEs. Erythromycin and clarithromycin have severe GI disturbances.
• Pharmacokinetics. All of macrolides hepatically eliminated, except clarithromycin,
which is renally eliminated.
• All macrolides have oral dosage and erythromycin gluceptate and lactobionate is IV.
• Azithromycin has long half-life 68 hours and used single daily doses.
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Clarithromycin
Use Same as erythromycin. H. influenza, Chlamydia, and Legionella
Side Effects Epigastric distress (nausea, vomiting, burning stomach, diarrhea),
renal (azotemia), Liver. Hepatitis (cholestatic hepatitis)
Contraindication Patient with hepatic dysfunction.
Do not refrigerate the reconstituted suspension.Clarithromycin may
increase levels of benzodiazepine, statins (ALS), CBZ, theophylline,
cyclosporins and tacrolimus.
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Azithromycin
Use Less active for Staph. and Strep than erythromycin. Far more active H.
influenza, Moraxella catarrhalis. Mycobacterium avium, except HIV.
Side Effects Epigastric distress (better tolerated than ery &clary). Oral preps has less
nausea and vomiting.
Contraindic in patient with hepatic dysfunction.
ated
Counseling Suspension do not refrigerate.
may increase warfarin effect (clari>azi).
Tetracycline
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Doxycycline
Minocycline
Clindamycin
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Ciprofloxacin
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Ofloxacin
Ofloxacin
Mechanism Inhibits DNA replication of bacterial DNA gyrase
Uses Mainly for E. coli in UTI and STD with exception syphilis.
alternate in gonorrhea
Side effects Hypoglycemia, leukopenia, Neutropenia
Counseling Tell patient to drink fluids liberally.
Separate doses of vitamins, antacids by 2 hours.
Gatifloxacin
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Metronidazole
FolateantagonistSulfaDrugs
Pteridine + PABA
Dihydropteroic acid
Dihydrofolic acid
THF cofactors
Cotrimoxazole(SMX + TMP)
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Cotrimoxazole
Therapeutic Use Chronic treatment of UTI
Gram –ve: H. influenza, Gonorrhea, E. coli, Klebsiella, Salmonella,
shigella sp. and V. cholera.
Gram +ve: S. pyogenes (GAS), S. viridans, S. aureus
UTI-Acute, recurrent, chronic.
Upper and lower rasp—chronic bronchitis.
Immunocompromised children P. carinii
Not indicated in infections associated with pseudomonas,
mycoplasma.
Side effects Skin reaction (severe in elderly)
GI. N and V
Blood related: Megaloblastic anemia, Thrombocytopenia,
Leukopenia: The above three effects can be reversed by concurrent
administration of folinic acid.
Hemolytic anemia-G6PD deficiency due to SMX
Counseling Drug is not for IM. Shake oral suspension thoroughly before use
Take oral dose with full glass of water.
With or without food. (food decreases GI side effect)
Store in amber glass of bottle.
Store at room temp until expiry and protect from moisture.
Contraindications Last trimester of Pregnancy, lactation.
Children under 2 months. May cause kernicterus.
Steven-Johnson’s Syndrome (SJS). Rash, skin peeling, and sores on the mucus
membrane. In Steven Johnson’s syndrome, a person has blistering of mucus membrane,
typically in mouth, eyes and vagina. Patchy areas of rash. SJS can occur in all age groups.
Due to "SASPAN" Sulfonylurea, Anticonvulsant (phenytoin, carbamazepine, valproic
acid), Sulfonamide, Penicillin, Allopurinol and NSAIDs. Sulfa drugs including topical sulfa
drugs. Treatment of SJS is cortisone.
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39
Antifungal Agents
Mechanisms of Action and Classification of Antifungal Agents
Antifungal Agents
After cell membrane permeability Block nucleic acid synthesis Disrupt microtubule function
Allylamine Pyrimidine
Azoles Polyene Penicillin
Analog
macrolide derivative
* Terbinafine
antibiotics * Flucytosine
* Naftifine * Griseofulvin
* Amphotericin B
Imidazoles Triazoles *Nystatin
* Ketoconazole * Fluconazole
* Miconazole * Itraconazole
* Clotrimazole
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Amphotericin B
• Fungistic, fungicidal.
Therapeutic use • Widest of any agent, systemic fungal infections; candidiasis;
cryptococcos; blastomycosis; histoplasmosis;
coccodiodomycosis; aspergillosis; sprorotichosis; mycosis;
leishmaniasis.
• Availability. 3% cream/lotion/oral suspension. Not absorbed in
the GIT.
Mechanism • Bind to ergosterol from pores resulting in the leakage of cellular
contents.
Side effects • Very toxic. infusion related fever and chills, anorexia, muscle
pain, and headache.
• Non-infusion related nephrotoxic, hyperkalemia,
hypomagnesaemia, tachycardia, anemia, thrombocytopenia,
arrhythmias, VF, HTN, tachypnea, leukoencephalopathy, dry
skin, skin discoloration, SJS, toxic epidermal necrolysis,
agranulocytosis, jaundice, hemorrhage, sore throat
Contraindication • Allergies
Warning • Apply only to patients with progressive, potentially fatal
infections and should not be used to treat non-serious infection
• Monitor lab test sp. Renal function (frequently), liver function,
serum electrolytes particularly magnesium and potassium,
blood count, Hgb conc. Not use for dosage adjustment.
• Does not penetrate CSF therefore administered intrathecally
Drug interaction • Antineoplastics increase renal toxicity, bronchospasm,
hypotension.
• Corticosteroids/ACTH, increase amphotericin B-induced
hypokalemia, renal toxicity.
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Nystatin
Category • Polyene antibiotic, structurally similar to Amphotericin B, fungicidal,
and fungistatic.
Therapeuti • Active against Candida sp. Primarily use as a topical agent in vaginal
c use and oral candidiasis.
• Not very effective against dermatophytes (Tinea pedis).
Mechanism • Inhibit growth of yeast, binds to sterol in the fungal cell membrane,
increasing permeability and causing leakage of intracellular
components.
Side effects • Irritation e.g. mild digestive upset, nausea & vomiting diarrhea,
cream/vaginal tablet itching, burning, and irritation.
Advantage • Can be use by pregnant women.
Drug
interaction
Precaution • Application of vaginal tablet
Counseling • Nystatin liquid
• Skin ointment or cream.
• Powder. Dust the powder inside shoes and socks.
• Nystatin vaginal tab and cream.
Reference: • CPS 2004 1308-1309
Ketoconazole
Ketoconazole
(Imidazole type)
Therapeutic use • Chronic mucocutaneous candidiasis, systemic and vaginal
candidiasis, Tinea corporis (ringworm), T. cruris (jock itch), T.
pedis (Athlete’s foot), Tinea versicolor (sun fungus),
histoplasmosis, blastomycosis, paracoccidioidomycosis, oral
thrush
• Relative bioavailability: 75 % with meals
• Available as tablet, cream and shampoo
Mechanism • Block the synthesis of ergosterol 14a demethylase in the fungal
CYP 450 complex; hepatic elimination
Side effects • Hormonal effects. Decreased male libido and potency,
gynecomastia, decreased plasma testosterone levels, affects
female menstrual problems, Cardio effects hypertension, fluid
retention.
• GI upset, hepatotoxicity, dizziness, anorexia, Nausea &
vomiting
Contraindication • Hypersensitivity, and teratogenicity.
WARNING • Rebound effect. Apply mild topical corticosteroids in the
morning and ketoconazole at night and gradually decrease
steroid over a period of 2 to 3 weeks. Cross sensitivity.
Precaution • Allergies with imidazoles.
Counselling • Shampoo, 1% or 2%, Cream
References • CPS 2004, 1379-1380
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Fluconazole
Mechanism • Block The Synthesis Of Ergosterol By Inhibit 14A-Demethylase In The
Fungal CYP450 Complex
Therapeutic • Mucocutaneous Candidiasis (Esophageal). Alternative For
use Amphotericin B For Treatment Of Systemic Candidiasis, Cryptococcal
Meningitis, Coccidioidomycosis, Cryptococcosis, HIV Associated
Infections
• Relative Bioavailability 85- 92% With Meals
Side effects • Skin Rash
• GI Effects. Nausea, Vomiting Diarrhea Or commonly Causing GI
Disturbances.
• Liver Effect. Increase liver enzymes, yellowing of the skin, and eyes,
Flu-Like Symptoms,
• CNS. Dizziness, Headache, Exfoliative Skin Reactions, Altered Taste
Buds, Extreme Tiredness, and Seizures.
Drug • Decrease Levels With carbamazepine, H 2 Blockers, INH, Phenytoin.
interaction • Increase Levels Of drugs that substrate of CYP2C9. phenytoin,
warfarin (greatly prolongs PT), and sulfonylureas.
• Less affect CYP3A4 substrates. Anticancer Drugs, Amiodarone,
Benzodiazepine, Cyclosporine, Disopyramide, OCP, Diuretics,
Moxifloxacin, Sotalol, Terfenadine, Quinidine, Valproic Acid,
Thioridazine And Tacrolimus.
Precaution • Decrease elimination of enzyme Inducers Like Rifampin, Allergies To
Fluconazole And Other Antifungals, Irregular Heart Beat, Kidney Or
Heart disease
Reference: • Applied T. Handbook; Chapter. 67, Pp. 67.4 - 67.5
• TC Page 4th Ed Page 1056.
Itraconazole
Warning • Cause CHF; heart attack; irregular heart beat ; lung/ kidney/liver
disease or other serious problems; SOB, coughing up white
phlegm; weakness; excessive tiredness, fast heart beat, swelling
of the feet, ankle or leg; sudden weight gain.
Clotrimazole
Therapeutic use • Yeast infection (Vulvovaginal Candidiasis), skin infections, high
concentration needed in bacterial infection, and athletes foot.
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Miconazole
Category • Broad spectrum fungistatic
Mechanism • Block synthesis of ergosterol by inhibiting 14a-demethylase in
the fungal cytochrome P450 complex; selective inhibition of RNA
& DNA and mucopolysaccharide precursor.
Therapeutic use • Covers both dermatophytes and candidiasis (Advantage Over
Tolnaftate and Nystatin. Also, effective against Tinea infections
by T. pedis, T. cruris, T. corporis, T. versicolor
Side effects • Itching, skin rash, Nausea &vomiting, burning on the site of
application.
Contraindication • Sensitivity to any of the components of Miconazole, not for
children < 2y/o unless directed by a doctor, do not use for the
infection of the nail.
Drug interaction • Anticoagulants, phenytoin, terbinafine, atypical anti-psychotics,
• Cyclosporins and some statins.
Availability • Topical 2%, aerosol powder, 2 % cream, a kit-2% powder 2y/o
and 2% tincture, 2% vaginal cream and 100 and 200 mg vaginal
suppositories.
Application • Aerosol powder
• Cream Apply sparingly, smoothen well and avoid maceration.
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Massage area gently. Athlete’s foot. dry feet, and wear cotton
socks.
Reference • CPS, 2004, page 1246
Tolnaftate
Category • Fungistic, fungicidal
Mechanism • Damage hyphae and stunt mycelial growth in susceptible fungi
Therapeutic use • Jock itch, athlete's foot, ringworm T. pedis, M. canis, Aspergillus
niger, C. albicans, M. gypseum, M. audounii, M. japonicum, T.
rubrum, T, mentagrophytes, T. schonleinii, A. fumigatus
Side effects • Slight irritation, sting (aerosol solution), burning and itching of
athlete's foot and jock itch should decrease with in 2-3 days
Administration • Do not apply dressings, or mix cosmetics or other skin
medications with tolnaftate treatment.
• Powder. Clean and dry affected area. Sprinkle it between toes
and in socks and shoes treated lightly.
• Spray should be shaken well before use. Apply it from a
distance of at least six inches away. Continue treatment until
symptoms disappear. A total of 4 to 6 weeks necessary. Do not
inhale powder, bring close to a hot object or flame
• Cream. Thoroughly clean the infected area. Allow it to dry and
then rub gently the medication until most of it disappears. Use
sufficient quantity to cover the affected area. Wash hands after
application.
• Solution. If it solidifies, dissolve by warming the closed
container in warm water then follow dosage as directed.
Warning • Aerosols: Flammable.
Contraindication • Allergies to tolnaftate or any preservatives, dyes; pregnancy;
children, 2 yo.
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Tips
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40
Anti-Mycobacterial Drugs
Generic Name Trade Name Generic Name Trade Name
Rifampin Rifadin, generics Isoniazid Isoniazid, INH,
Streptomycin generics Rifabutin Mycobutin
Pyrazinamide generics Ethambutol Myambutol
Tuberculosis treatment
• Goal of treatment is must eradicate mycobacterium.
• Important issues in tuberculosis treatment are resistance to drugs.
• Drug of choice for the prophylaxis of tuberculosis --> isoniazid
• Drugs that have lowest resistance is --> Isoniazid, rifampin, streptomycin and
combination of these drugs with pyrazinamide, or ethambutol.
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Tips
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41
Antiviral Drugs
Question Alerts!
1) Examples of herpes virus? HSV1, HSV2, VZV, and EBV
2) Cold sore and keratoconjuntivitis is caused by? HSV1
3) Antiviral drugs for HIV such as NRTIs, NNRTIs, NtRTIs, and protease inhibitors side
effects? Pancreatitis, neuralgia, and cardio toxicities.
4) Hepatitis A is acute and transmitted food & H2O
4) Hepatitis B&C are chronic and transmitted by sexual contact, blood transfusion etc.
5) Seasonal flu is caused by Influenza A & B
Common Viruses
• Herpes virus. HSV 1 , HSV 2 , VZV, EBV
• Hepatitis A, B, C, D, E viruses
• Influenza virus A, B (seasonal flu)
• HIV-AIDS
• Measles, Mumps viruses
• Others; Rabies, Rubella (German measles), Variola, Coxsackie virus
Some Antiviral
• Acyclovir; Cover HSV 1 and 2, VZV. Well tolerated.
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Anti-retroviral therapy
Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Delavirdine mesylate Do not combine within the same NNRTIs class
Efavirenz
Nevirapine
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Abacavir
sulfate
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Tips
1 Zalcitabine 9. Didanosine 17. Tenofavir
2 Erythropeitin 10. Stavudine 18. NRTIs
3 Acyclovir 11. Zidovudine 19. Tenofovir
4 NNRTIs 12. Triflurohexidine 20. Rimantadine
5 Zanamavir 13. Amantadine 21. Oseltamavir
6 Famcyclovir 14. Valacyclovir 22. Hepa A immunization
7 Calamine lotion 15. Flu immunization season 23. Hepa B immunization
8 Antihistamine 16. Oatmeal cream
• Pancreatitis is SEs of what antiviral drugs. (9, 10)
• Peripheral neuropathy is SE of what drugs. (1, 10, 9)
• Didanosine should be avoided with what are the other antiretroviral drugs. (10 )
• October to mid November. (15)
• Treatment of zidovudine induced anemia. (2)
• Drugs of choice to treat HSV 1 and HSV 2 infections. (3)
• Alternate treatment for HSV 1 and HSV 2 . (6, 14)
• Recurrent cold sore treatment. (Abreva )
• Genital herpes can be treated by 5% of what drug. ( 3 )
• Side effects of this drug are bone marrow depression and severe anemia. (11)
• Pancreatitis and neuropathy are side effects of what drug. (9, 10 )
• Peripheral neuropathy is side effect of what drug. (1, 9, 10 )
• What immunization given above for 0, 1 month and 6 month? (23)
• What immunization above given for 1 year old only? ( 22)
• Abacavir (ABC), didanosine (ddl), emtricitabine (FTC), lamivudine (3TC), stavudine (d4T), and
zidovudine (AZT), are examples of what antiviral classification? (NRTI)
• Examples NtRTI (nucleotide Reverse Transcriptase Inhibitor. ( tenofavir (TDF))
• Efavirenz (EFV), Nevirapine (NVP), delavirdine (DLV) and etravirine (TMC-125) are examples
of what drug classification? (NNRTIs)
• Drugs of choice to treat keratoconguntivitis . (trifluridine)
• For influenza A only. (amandatidine)
• Neuroaminidase inhibitors for influenza A and B. (oseltamavir and zanamavir)
• Indicated for influenza A and B. (oseltamavir)
• Herpes simplex virus causes infections of Genital herpes, keratoconjuctivitis, cold sores
• Who should get flu vaccination Patients with respiratory, cardio, DM, HIV, elderly over
65, health care workers, and professionals, patient living in long term care facilities, long
term care workers.
• Who is vector (carrier) of flu Health care workers.
• CD 4 count 100 patient require prophylaxis for Penumocystis carinii Pneumonia
• Flu season in Canada October to April
• Tenofovir (Viread) a nucleotide reverse transcriptase inhibitor (NtRIs) gives --> renal toxicity,
monitor RFT
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42
Anti-Malarial Drugs
Drug Name Trade Name Drug Name Trade Name
Primaquine Radical cure Chloroquine Aralem
Doxycycline Adoxa Pyrimethamine Daraprim
Mefloquine Lariam Atovaquone-proguanil Malarone
Malaria is infection of red blood cells with the single-celled parasite Plasmodium, which
causes fever, an enlarged spleen, and anemia.
Chloroquine is the drug of choice for treatment in a person who has malaria caused by
Plasmodium vivax, Plasmodium ovale, or Plasmodium malariae except in a very few
areas where resistance to chloroquine in people with Plasmodium vivax has been
reported.
Primaquine is added to kill persistent parasites in the liver of a person infected with
Plasmodium vivax or Plasmodium ovale. Before primaquine is given, a blood test is done
to look for a relatively common enzyme deficiency (G6PD deficiency). People with G6PD
deficiency who are given primaquine may have a breakdown of their red blood cells.
Malaria Prevention. N, N-Diethyl-m-toluamide (DEET), 5%, 10%, 15% and 30% should be
applied on the skin before outdoor activities during the main hours of malarial
transmission 30% of DEET may be used in children as young as 2 months of age.
• 30% DEET is effective for four to six hrs.
• Citronella is usually effective for less than 1 hr.
• Avoid eye and mucus membrane.
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DEET 5%
DEET 10%
DEET 15%
DEET 30%
Recommended.
10% DEET for 8 yo. repels for 3 hr
15-30% for adults. repels for 6 hr
Avoid in 1 yo (not used <6 mo), take mosquito nets.
Maximum tid
Apply sparingly exposed skin or/and cloth
Refer to travel clinic
Treatment of malaria
Prophylaxis
P. falciparum Chloroquine
P. malariae Chloroquine
P. vivax Chloroquine + primaquine
P. ovale Chloroquine + primaquine
Chloroquine resistant Mefloquine, Primaquine, Quinine + doxycycline, atovaquone-proguanil.
prophylaxis
Treatment Quinine or mefloquine or pyrimethamine/sulfoxine
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Tips
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43
AnthelminthicDrugs
Question Alerts!
Pinworms treatment and selfcare?
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Mebendazole
• Mechanism. Inhibits microtubule synthesis and glucose uptake in nematodes.
• Clinical Use. Pinworm and whipworm infections.
• Contraindicated in pregnancy.
Pyrantel pamoate
• Mechanism. Depolarizing neuromuscular blocker, which causes paralysis of
nematodes.
• Clinical use: Hookworm infections, pinworm infections, Roundworm.
• Caution: Red color urine, feces, stains on vomiting.
Praziquantel:
• Mechanism: Increase membrane permeability to Ca2+ using muscular contraction
and paralysis of the nematode muscles.
• Clinical Use. Drug of choice for Schistosomiasis, clonorchiasis, and pranomiasis.
Niclosamide:
• Clinical Use: Infections from ingestion of beef, pork, and fish.
Tips
1 Mebanedazole 2 Pyrantel pamoate 3 Praziquantel
4 Niclosamide
• Which antihelmenthic drug can cause red color body fluids, such as urine, saliva etc?
Pyrantel pamoate (2)
• Inhibits microtubule synthesis and glucose uptake in nematodes ( 1 )
• use for infections from ingestion of beef, pork, and fish (4)
• depolarizing neuromuscular blocker, which causes paralysis of nematodes (2)
• it causes red color urine, feces, stains on vomiting ( 2 ).
• increase membrane permeability to Ca2+ using muscular contraction and paralysis of
nematode muscles (3).
• DOC for schistosomiasis, clonorchiasis, and pranomiasis ( 3 ).
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