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NMJ blockers Non-depolarizing eye and face first, respiratory last bronchoconstrict and hypotension
tubocurarine
vecuronium
atracurium
Depolarizing - succinylcholine metab’d by plasma cholinesterase
Parasympathetic
Agonists Synthetic choline esters
carbachol no hydrolysis by AChE
bethanechol no hydrolysis by AChE
methacholine small hydrolysis by AChE
Drug mechanism of action side effects
Muscarinic agonists
muscarine
pilocarpine
Nicotinic agonists – nicotine
Indirect agonists inhib AChE
edrophonium short acting, reversible
neostigmine medium acting, reversible
physostigmine medium acting, reversible
pyridostigmine long acting, reversible
organophosphates irreversible
Sympathetic
α – Adrenergic receptors Agonists effects of stimulation:
NE not used clinically vasoconstriction
phenylephrine mydiasis radial mm in eye
methoxamine ejaculation
metaraminol has both direct and indirect effects stim of pilomotor mm
clonidine α2-selective partial agonist
guanabenz, guanfacine α2-selective
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Drug mechanism of action side effects
Antagonists
ergot alkaloids
phentolamine reversible
phenoxybenzamine irreversible
prazosin α1-selective
terazosin α1-selective
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Drug mechanism of action side effects
CNS/Neurologic
Antiparkinson
drugs that replete dopamine Levdopa prodrug
Carbidopa inhib Lev→DA conversion in periphery
Entacapone COMT inhib (prolongs DA ½ life)
Stimulants
drugs affecting catechol amphetamine
neurons methamphetamine
ephedrine
methylphenidate (Ritalin)
cocaine
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Drug mechanism of action side effects
ETOH naltrexone opioid antag
acamprosate glutamate antag
disulfiram aldehyde dehydrogenase inhib
Anti-epileptics
Na channel inactivators phenytoin inactivates rapid firing Na channel arrhythmias
fosphenytoin prodrug of phenytoin, less toxic
carbamazepine prolongs inactivation of Na diplopia
lamotrigine
tobrimate
valproate liver, GI, no use w/phenobarb
Unknown GABApentin
Psychiatric
Anti-psychotics
typical reserpine parkinsonism, tardive dyskinesia
chlorpromazine (after prolonged use), sedation,
thioridazine anti-cholinergic
haloperidol
domperidone
thiothixine
benzotropine
trihexyphenidyl
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Drug mechanism of action side effects
atypical clozapine not as many extra-pyramidal
olanzapine effects, weight gain
risperidone
aripiprazole
Anxiolytics
Anxiety Benzodiazepines GABA inhibs, can not OD dependence
alprazolam short acting
diazepam intermediate acting
lorazapam long acting
triazolam
5HT/NE uptake inhibs
SSRI
SNRI
imimpramine
venalfixine
Buspirone
Herbal
kava kava + diazepam = coma
valerian
Insomnia Benzodiazepines
Flurazepam
Temazepam
Non-benzos
zolpidem (ambien)
Barbituates sedative
pentobarbital ½ life – 18-48h
phenobarbitol ½ life – 4 days
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Drug mechanism of action side effects
Anti-depressants
Depression TCA’s low therapeutic index, dry mouth,
Tertiary amines inhibit 5HT uptake, muscarinic & dizziness, constipation, tachy,
Imipramine α-1 antags orthostatic HTN
Amitryptiline
Secondary amines inhibit NE uptake, muscarinic &
Desipramine α-1 antags
Nortryptiline
MAOIs MAO-A – NE and DA neurons,
Phenalzine non-selective MAOI involved in tyramine metab in gut
Tranylcypromide MAO-B – 5HT neurons
deprenyl MAO-B but non-selective at dose
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Drug mechanism of action side effects
Cardiovascular
Atherosclerosis
Statins Lovastatin HMG Co-A reductase inhib which upregs GI upset, muscle ache, hepatitis
Fluvastatin LDL receptors
Atorvastatin
Pravastatin
Simvastatin
Antithrombosis
Anticoagulants heparin stims antithrombin III which binds
thrombin
fondaparinaux sulfate binds to ATIII selective inhib of FX/Xa
warfarin (coumadin) vitK analog – competive inhibitor
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Drug mechanism of action side effects
Thrombolytics streptokinase convert plasminogen → plasmin contraindicated in pxs w/strep inf
TPA (alteplase & retaplase)
urokinase
anistrplase
Anti-arrhythmics
Class I – Na channel Class Ia incr ARP and AP sudden death arrhythmias
quinidine
procainamide
Class Ib – lidocaine raise threshold and prolong RRP pro-arrhythmic (not as bad)
Class Ic – flecainide raise threshold and slow conduction sudden death arrythmias
Class III – K channel amiodarone block DRK channels + Class I, II, and IV
soltalol block DRK channels + Class II torsades de pointed (ventr tachy)
Cardiac glycosides
Digitalis glycosides digoxin
digitoxin
digoxin immune Fab
Bipyridines milnirone
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Drug mechanism of action side effects
β1 agonist dobutamine
Anti-hypertensives
Central acting clonidine stimulates central α2
guanbenz
methyldopa
Diuretics
Osmotic mannitol
urea
Nitrodilators nitroglycerin
isosorbide dinitrate
nitric oxide
nitroprusside
ARBs losartan
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Drug mechanism of action side effects
GI Drugs
Control of gastric acidity
PPIs omeprazole irreversible proton pump inhibs nausea and diarrhea
lansoprazole
labeprazole
pantoprazole
esomeprazole
H2R antagonists cimetidine inhibs GS protein needed to activate pump p450 inhib, nausea, ↑ prolactin
ranitidine
famotidine
nizatidine
Prostaglandin analog misoprostol stims Gi which inhibs proton pump diarrhea, uterine contractions
Anti-emetics
5HT3R antagonists odansetron
granisetron
dolasetron
Antihistamines cyclizine
hydroxyzine
promethazine
diphenhydramine
Anticholinergics scopolamine
dronabinol
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Drug mechanism of action side effects
Prokinetics
Cholinergic agonists carbechol ACh is main NT for GI motility lots of global side effects
bethanechol
IBS
5HT4R agonist tegaserod
Diarrhea
Intraluminal fiber
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Drug mechanism of action side effects
IBD
5 aminosalicylates sulfasalazine
Immunosuppression 6-mercaptopurine
methotrexate inhibs DHFR
cyclosporine
Respiratory
Asthma
β2 agonists albuterol short acting tachy and tremor
salmeterol long acting
Leukotriene inhibs zileuton inhib Arach Acid → Leuko – 5-lipox inhib not for acute
zafirlukast LTD4 R antag
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Drug mechanism of action side effects
Endocrine
Osteoporosis
Ca and Vit D supplements
ERT
SERM raloxifene agonist on bones, antag on breasts
tamoxifen
Thiazolidinediones pioglitazone ↑↑ glucose uptake peripherally via PPARγ edema and weight gain
rioglitazone activation, ↓ gluconeo in liver
Sulfonylureas and glinides nateglinide insulin secretagogues, stimulate beta cell hypoglycemia
repaglinide production of insulin
meglitinide
glipizide
Alpha-glucosidase inhibs acarbose delay absorption of carbs and so moderate flatulence and incr LFTs
miglitol post prandial spike
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Drug mechanism of action side effects
Hyperlipidemia
Statins see above lower LDL
Fibrates see above lower TGs and incr HDL + statin = rhabdomyalisis
Anti-obesity
Adrenergic dexamphetamine
phentermine
Antibiotics
Nucleic acid inhibs
sulfamethoxazole bacteriostatic PABA analog kernicterus,p450 inhib,crystalluria
chloamphenicol 50s, serious infections, incl CNS aplastic anemia and p450 inhib
metronudazole anaerobes
Anti-fungals
Amphoteracin B complex w/sterols results in apoptosis nephro, cardio, and neurotoxic
Flucytosine fungal uracil analog; chain termin bone marrw suppr, alopecia, GItox
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Drug mechanism of action side effects
Anti-parasitics
Entamoeba, giardia, trich metronidazole
Anti-virals
Influenza amantadine flu A by blocking M2 so no uncoating paranoia, depression
neuramidase inhibs prevent cleave of sialic acid-virus no exit
zanamivir inhaled can be prob for asthmatics
oseltamavir oral
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Drug mechanism of action side effects
Analgesics and Anesthetics
Opioids opioid work on three receptors in CNS:
Endogenous endorphins µ – analges,euphor,resp depr,miosis,constp
enkephalins κ – analges, sedation, dysphoria, miosis
dynorphins δ - analgesia
Synthetic fentanyl µ
methadone µ long ½ life(resp dep after 2-3days)
pentazacine agonist κ δ antag µ δ
hydrocodone
meperidine µ + MAOIs = severe resp depression
Chronic pain
Non-opioid NSAIDs
Opioid Full agonist
fentanyl µ
hydromorphone µ
heroin µκδ
morphine µκδ
methadone µ
meperidine µ
Partial agonist
buprenorphine µ
oxycodone µ
hydrocodone µ
codeine µ
propoxyphene µ
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Drug mechanism of action side effects
Adjuvant Muscle relaxants
cyclobenaprine
methocarbamol
diazepam
baclofen
anti-convulsants – see above
local anesthetics – see below
anti-depressants – see above
Local anesthetics
Ester linked cocaine metabolized by blood = short ½ life; if arrythmias, euphoria
procaine administer w/epi, vasoconstr prevents
benzocaine blood from reaching site and incr ½ life
tetracaine
General anesthetics
Inhalational halothane hepatitis, malign hyperthermia
enflurane
isoflurane
desflurane
sevoflurane
nitrous oxide
Injectable/IV propofol
ketamine NMDA-R antag, dissociative anesthesia bad dreams
barbiturates – thiopental
benzodiazapenes
midazolam
diazepam
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Drug mechanism of action side effects
lorazepam
Immunosuppression
Prototype mediators thromboxanes
prostacyclin (PGI2)
prostaglandin E2
leukotrienes
histamine
IL-1
IL-2
TNF
NSAIDs
Non-specific aspirin
acetaminophen
ibuprofen
naproxen
piroxicam
etodolac
nabumetone
endomethacin
COX-2 celecoxib
Immunosuppressive
Cytotoxic methotrexate Inhibit prod of immune system cells
azathioprine
cyclophosphamide
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Drug mechanism of action side effects
Chemotherapy
Cell cycle nonspecific
Alkylating agents cyclophosphamide alkylate DNA, cause DNA cross-linking carcinogenic
nitrourea
cisplatin renal
Antibiotics (except bleo) anthracyclines intercalate DNA, breaks via Topo II cardiac, carcinogenic
doxorubicin
daunorubicin
dactinomycin intercalate DNA, inhib RNA synth
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