CNS Li Vasopressin (HTN) Aminoglutethimide Trilostane (paresthesia) Mitotane Heart Li Vasopressin (HTN) TH Agonists Metyrapone (HTN) Metformin TZD

Lung Blockers Liver PTU Ketoconazole SU's (amide; uride; izide; iride) TZD (troglitazones) Chol Methimazole S'statin (g-stone) GI Somatostatin Ketoconazole Metyrapone Tilostane Mitotane -Glycosidase Inhibitors - Acarbose; Miglitol Nausea / Vomit Renal SU's (amide; uride; izide; iride) Metformin (lactic acidosis) Acyclovir K+ Spironolactone Amiloride Hydrochlorothiazide Ca2+ Thiazides Heme (bleed) Spironolactone Ketoconazole GnRH (HA fx) Hemolytic Anemia Ribavirin Megaloblastic Anemia Zodovudine Skin Iodine (eruption) Aminoglutethimide (rash) Thyroid (itis) Amiodarone IFN / IL-2 Steroids/Adrenal Cortex GI S.E.'s

Neuro S.E.'s

PENICILLINS PCN G (IV Form; Acid labile) 1/2 Life = 30 minutes PCN V (oral; Acid stabile)

INDICATIONS PCN G = Strep pneumonia PCN V = Grp A Strep (pharyngitis) Spirochetes (syphilis)

PCNase-RESISTANT PCN's Nasty Nafcillin (I.V.) Methy (messy) Methicillin (I.V.) Oxacillin (Oral; I.V.) Ox Dicloxacillin (Oral) Clocks SA AMINO-PCN's Amoxicillin + Clavulanic acid Ampicillin + Clavulanic acid

Staph aureus Sepsis; IE; Cellulitis = Nastycillin Nasty Messy Ox Clocks Staph aureus Knocks it out!! Gram(+) - All Gram(-) Rods Bronchitis; Sinusitis UTI's

MECHANISM OF ACTION Bactericidal Rx enters bacteria through porin A 1) Activates autolytic enzymes A 2) Inhibits transpeptidase (PBP) A No cross-linkage of cell wall A 3) Inhibits cell wall synthesis A Osmotic lysis of bacteria Inhibits cell wall synthesis

SIDE EFFECTS / TOXICITY Hypersensitivity Rash Anaphylaxis Hemolytic Anemia; Neutropenia Widespread PCN Resistance: -lactamase cleavage of ring Methicillin = I.S. nephritis Meth Messes w/ Neph

Inhibits cell wall synthesis

Hypersensitivity Rash (Ampicillin) Colitis (Ampy-crampy; Colicky-amoxy) Clavulanic Acid --> Diarrhea

CA competitively inhibits -lactamase HELPS kill entero's H Flu; E. Coli; List.; Prot.; Salm. TICARCILLIN Pseudomonas auruginosa PIPERACILLIN Gram(-) Rods CARBINICILLIN Totally pseudo, dude. "Toke the Pipe and Carb" + hit of Acid! Add Clavulanic acid CEPHALOSPORINS 1st Generation Cephalexin Alex is in Cephalothin Alice is in Cefazolin Us all in 2nd Generation Cefuroxime Fur ox Cefotetan Teets [use an] Cefoxitin Ox tin 3rd Generation Ceftriaxone (oral) - AX 'em!! Cefotaxime - TAX 'em!! Ceftazidime - TAZ 'em!! Cefoperazone - Opera will kill too!! 4th Generation Cefepine 1st Generation Proteus E. coli Klebsiella 2nd Generation H. Flu Enterobacter Neisseria

Inhibits cell wall synthesis

Hypersensitivity Rash Clavulanic Acid --> Diarrhea

Inhibits cell wall synthesis

Hypersensitivity Rash Granulocytopenia I.S. Nephritis Fn Group A-glycosides + Cephalosporin

Proteus E. coli Klebsiella Serratia

-Lactamase Cuts here

3rd Generation X-BBB - Bacterial Meningitis Gram(-) serious infections Gonorrhea (ceftriaxone) 4th Generation Pseudomonas & Gram(+)

Resistance: -lactamase cleavage of ring MRSA Enterococci

1st = Pro Colie Klub 2nd = Pro Colie Klub+Sarra, Homo, Nice Aunt 3rd = Serious bunch 4th = Pseudo Inhibits cell wall synthesis Non-toxic (usually) GI Sx's (occasional) Peaceful Tree: Ok w/ Aminoglycosides Non-toxic (usually) Aerobic (GNR's) Inhibits cell wall synthesis Cilistatin - Dihydropeptidase Dihydropeptidase (renal enzyme) A Metabolizes and inactivates imipenem Seizures Skin rash GI distress

MONOBACTAMS Aztreonam -Lactamase resistant Synergistic with Aminoglycosides CARBAPENEMS

Only Aerobic GNR's Klebsiella P. auruginosa Serratia

Everything!!!

Imipenem + Cilastatin I'm A Pen = X all bugs out Hydrolized by Dihydropeptidase Cilastatin inhibits above enzyme Most powerful bug drug out there Meropenem Not hydrolized by Dihydropeptidase -Lactamase resistant

Lactam Rings
VANCOMYCIN Glycopeptide (poorly absorbed) "Vanc" the deaf red-neck cowboy A Kills Staph aureus and gut bugs Gram(+) Staph aureus C. difficile Vancomycin Resistance Enterococci (plasma mediated) Bactericidal Binds to D-analyl-D-analine A Inhibits peptidoglycan synthesis A Inhibits cell wall synthesis Poorly absorbed A Remains in gut and attacks GI bugs Nephrotoxicity when used in combo Tx Vancomycin + aminoglycoside Red Neck Syndrome / Rash Rapid infusion A HA release Ototoxicity Resistance: D-ala <-- D-lac; Affinity

Cell Wall Inhibitors

AMINOGLYCOSIDES "G-TANKS" w/ 30-ott Ammo

INDICATIONS Aerobic GNR's (severe) Aerobes! (amine-O2-glycosides) Amp-Gent Combo Tx!!

Gentomycin Tobramycin Amikacin Netilmicin Kanamycin Streptomycin

Ineffective Anaerobes Streptoccoci H. Flu Neomycin (topical; not well-absorbed) Syphilis The American Gent, Toby Strips "Neti" in the Kan TETRACYCLINES

MECHANISM OF ACTION Bactericidal O2 Required for uptake (aerobic orgs) Aerobic organism produces metabs' A Alters membrane potential A Allows uptake of Rx A Rx binds to 30S Ribosome A Protein synthesis Blocks initiation Misreading Early termination Syngergistic with -Lactams

SIDE EFFECTS / TOXICITY Nephrotoxic Ototoxic Teratogen Grenade goes off A Deaf Hits kidney Resistance: Modification of: Acetylation Adenylation Phosphorylation

Tet Offensive Dz's Bacteriostatic STD's - Chlamydia; Ureaplasma Binds 30S Ribosome subunit Malaria - P. falciparum (doxy) Minocycline A Inhibits protein synthesis Tick-borne - Rickettsia; Lyme Doxycycline (take w/ food; fecal elim) A Aminoacyl-tRNA attachment Diarrhea - Vibrio cholera Demeclocyline Tetracyclines Acne Don't Take With Bio-Rx - B. anthracis Milk Ellas - Pasteurella, etc. "Mine Doxy Demands 4 Tetes" (pups) Antacids A Takes care of multiple diseases Fe2+ containing substances No Milk!

Deposited in growing bones A Stains teeth gray-brown to yellow Inhibits bone growth in children Fanconi syndrome when expired Photosensitivity Think of newborn pups Sharp gray-brown teeth Shut eyes (photosensitive) Resistance: Uptake Export

MACROLIDES Azithromycin Clarithromycin Erythromycin Dirithromycin "Big Mac ACED his women" Panting = lung infection Thrusting = STD's

Gram (+) Cocci Streptoccoci Px's w/ PCN Mycoplasma (#1 for CAP) Legionella (#1) Chlamydia Neisseria CAP Etiology Mycoplasma Strep pneumonia Chlamydia

Bacteriostatic Binds 50S (23S rRNA) A Inhibits protein synthesis 50c Big Mac

Eosinophilia GI Nausea; Vomiting; Ab cramps Metallic taste (Clarithromycin) Cholestatic hepatitis (Erythromycin) Eat a Big Mac A GI upset + cholestatic hep Cardiac Arrhythmia (E'mycin + Terf) Resistance: Methylation of rRNA

CHLORAMPHENICOL "Clears a meningitis Call" Only as alternative to: PCN's Cephalosporins (3rd gen) Tetracycline in pregnancy

Meningitis H. Flu N. meningitis S. pneumonia Anaerobes Bacteroides fragilis

Bacteriostatic Binds 50S peptidyl transferase A Inhibits peptide bond formation A Inhibits protein synthesis

BM toxicity Anemia (reversible) Aplastic anemia (irreversible) Pancytopenia Gray Baby Syndrome Glucuronidation Death Resistance: Modification of acetylation GI Causes Pseudomembranous C. Fever P. colitis Resistance Methylated rRNA -->no Rx binding Myalgias Arthralgias Phlebitis Resistance Methylated rRNA -->no Rx binding

CLINDAMYCIN

Anaerobes Clostridium Cleans my sin[ister anaerobes] Bacteroides Gunshot Clindamycin = Diaphragm O2 bugs Aminoglycosides Metronidazole = Diaphragm O2 bugs Clindamycin Aspiration pneumonia STREPTOGRAMMINS Dalfopristin (Streptogrammin A) Quinupristin (Streptogrammin B)

Bacteriostatic Binds 50S ribosomal subunit A Inhibits peptide bond formation A Inhibits protein synthesis 50c for Linda

Streptococci Bacteriostatic Binds 50S Ribosome subunit Staphylococci Enterococcus faecium (bact-static) A Inhibits protein synthesis Not E. Faecalis Bacteriocidal Strep A = Near site of Microlides Strep B = Overlaps with Microlides A Used together = synergistic A Bacteriocidal

RNA Inhibitors

SULFANOMIDES - SMX Rotten eggs (oral) Porto-Potty (urinary excretion)

INDICATIONS MECHANISM OF ACTION TMP-S[MX] Bacteriostatic Tree (respiratory) Dihydropteroate Synthase Mouth - GI tract A Folate synthesis Pee - UTI; Urethritis; Prostatitis A Purine synthesis (bacterial) Syndrome Dz's - Toxo; PCP; I. Bella A DNA synthesis (bacterial) A Growth All Bacteria Nocardia Chlamydia Malaria Burns (silver sulfadiazine) UTI's

SIDE EFFECTS / TOXICITY Displaces protein-bound Rx's (Warfarin) S.E. = Rare (common w/ AIDS Px's) Hypersensitivity Nephrotoxicity; Kernicterus (infants) Hemolysis (if G6PD deficiency) Blood / WBC abnormalities Sulfanamide Resistance Altered target (plasmid-mediated) Uptake: Impermeability to Rx PABA synthesis

PABA antimetabolite TRIMETHOPRIM - TMP TMP + SMX Combo Tx 20-100x potency of sulfa DHFR (dihydrofolate reductase) TMP-S[MX] Tree (respiratory) - PCP Mouth - GI tract (shig.; salm.) Pee - UTI (recurrent); Urethritis Syndrome - Toxo; PCP; I. Bella Bacteriostatic Dihydrofolate Reductase Inhibitor A Folate synthesis TrimethopRim = Reductase Sulfanomide = Synthase BM Suppression Megaloblastic anemia Leukopenia; Granulocytopenia TMP = Treats Marrow Poorly Tx: Folinic acid

FLUOROQUINOLONES Quinolone Nalidixic acid Fluoroquinolones Ciprofloxacin Sparfloxacin Mortifloxacin Enoxacin Ofloxacin Norfloxacin Gatifloxacin

Aerobic GNR's UTI's Pseudomonas - Cipro Neisseria Gram (+)

Bactericidal DNA gyrase (Topoisomerase II) A Inhibits DNA synthesis

S.E.'s Uncommon - Rare

To See Pro Sparing Mortifies Enough Olfs of the North Gate

Tendonitis & Tendon ruptures Fluoroquinolones hurts Olfs are Gyrating (dancing) so much they Attachments to your bones Hurt their tendons Headache; Dizzy GI Upset GI Upset Headaches; Dizziness Superinfections Rash

Fluoroquinolone Resistance Mutation --> DNA gyrase / T.I. Alcohol! A Disulfiram-like reaction with alcohol Headache On the metro: No drinking alcohol! Metallic taste (of train water) GI Upset (from motion)

METRONIDAZOLE

Anaerobes Bacteroides fragilis Clindamycin = Diaphragm O2 bugs Clostridium difficile Metronidazole = Diaphragm O2 bugs Protozoa Giardia (flagellate) Entamoeba Gardnerella vaginalis Trichomonas (flagellate) Gee your aunt's guard tricked me to get on the metro 3X Tx (H, pylori) Metro + Amoxicillin + Bismuth Tetracycline + PPI + Bismuth POLYMIXINS / POLYPEPTIDES Polymixin B Polymixin E Colistin Resistant Gram (-)

Bactericidal Forms toxic metabolites in cell wall A Alters cell membrane e-potential Kills bugs in GI tract lumen

Cationic, basic proteins A Act like detergents A Bind to cell membrane A Disrupt osmotic integrity

Neurotoxicity Acute renal tubular necrosis Polymixin Resistance Proteus Serratia Impermeable cell walls A Rx cannot reach target

MISC. ANTIBIOTICS

ISONIAZID - INH

INDICATIONS TB Solo prophylaxis

MECHANISM OF ACTION Mycolic acid synthesis

SIDE EFFECTS / TOXICITY Neurotoxicity (Tx = Pyridoxine [B6]) Hepatotoxicity SLE-like syndrome Hemolysis (if G6PD) INH = Injures Neurons and Hepatocytes

RIFAMPIN 4 R's RNA polymerase inhibitor Revs up microsomal P450 Red/orange body fluids Resistance (rapid) if used alone

M. TB; M. avian Leprosy

DNA-dependent RNA polymerase

Hepatotoxic (P450)

Always used in combo with other Rx's Meningococcal prophylaxis H. Flu B prophylaxis

TB DRUGS

SIDE EFFECTS / TOXICITY

Colitis (Ampy-crampy; Colicky-amoxy)

Peaceful Tree: Ok w/ Aminoglycosides

Lactam Rings
Nephrotoxicity when used in combo Tx

Resistance: D-ala <-- D-lac; Affinity

Cell Wall Inhibitors

SIDE EFFECTS / TOXICITY

Cholestatic hepatitis (Erythromycin)

Methylated rRNA -->no Rx binding

Methylated rRNA -->no Rx binding

RNA Inhibitors

SIDE EFFECTS / TOXICITY Displaces protein-bound Rx's (Warfarin) S.E. = Rare (common w/ AIDS Px's)

Altered target (plasmid-mediated)

Disulfiram-like reaction with alcohol

MISC. ANTIBIOTICS

SIDE EFFECTS / TOXICITY

INH = Injures Neurons and Hepatocytes

TB DRUGS

INDICATIONS BACTERIAL PROPHYLAXIS Rifampin (1st line); Minocycline Ceftriaxone PCN G TMP/SMX TMP/SMX (1st line); Pentamidine Fluconazole Meningococcal Gonorrhea Syphilis Recurrent UTI's PCP Crypto prophylaxis / management

MECHANISM OF ACTION

SIDE EFFECTS / TOXICITY

ANAEROBES PCN + Clavulanic Acid Cephalosporins (2nd Gen) Imipenem Chloramphenical Clindamycin Metronidazole Ofloxacin PSEUDOMONAS Ticarcillin Pipercillin Carbenicillin Cephalosporins (3rd Gen) Imipenem Aztreonam Quinolones (Cipro) Aminoglycosides - Gent; Tobra; Amik

GRAM (+) TOUGHIES Vancomycin Ampicillin Imipenem MRSA; Staph; Enteros Enteros Enteros

Tough Bug Drugs

SIDE EFFECTS / TOXICITY

Tough Bug Drugs

AMPHOTERICIN B I.V. Not absorbed IM or orally Cross BBB t1/2 = 1 day Intrathecal Fungal meningites (rare)

INDICATIONS Systemic Mycoses Cryptococcus Blastomyces Coccidioides Aspergillus Histoplasma Candida albicans Mucor mycoses

MECHANISM OF ACTION Binds to membrane ergosterols >> Chol. A Forms pore in fungal cell membrane A Permeability & leakage of e'lytes A Homeostasis A Cell death "AmphoTears holes in membranes"

SIDE EFFECTS / TOXICITY "Ampho-terrible" Fever; Chills = Shake & Bake (44%) Nausea; Vomiting; Ab. pain; Anorexia Phlebitis (common) Heparin controls this S.E. Anemia (common) Nephrotoxicity (common) Monitor K+, Mg++, BUN, CRE, A-B K+emia

NYSTATIN Swish and swallow

Oral Candidiasis

Binds to membrane ergosterols >> Chol. A Forms pore in fungal cell membrane A Permeability A Homeostasis A Cell death Hormone synthesis inhibition A Gynecomastia (Keto) Liver dysfunction (via P450) Fever; Chills Nausea; Anorexia Combo Tx - Anti-HA A Q-T interval prolongation A Torsade de Pointes Voriconazole Visual disturbances (30min after Tx) A Warn Px's if driving,etc. Resistance Related to efflux pump Deposits in kertin-containing tissues Teratogenic / Carcinogenic CNS: Headaches; Confusion Warfarin metabolism

IMIDAZOLE DERIVATIVES Itraconazole Ketocanazole (No Amp B!) Fluconazole (X-BBB) Clotrimazole Voriconazole Miconazole (topical) H2 acids or antacids absorption Liver metabolism

#1 Itraconazole > Ketocanazole C14 demethylase inhibitors (via P450) Blastomycoses A Ergosterol & FA synthesis in wall Cociidioides A Permeability & leakage of e'lytes Histoplasma A Homeostasis Candidiasis (mucocutaneous) A Cell death Hypercortisolism Fluconazole Cryptococcal meningitis (L. term) Crypto prophylaxis (AIDS) Candida albicans Voriconazole / Itraconazole Aspergillosis!! Clotrimazole / Miconazole Dermatophytosis Microtubule function A Mitosis

GRISEOFULVIN Oral Tx Grizzlies are full of ringworm & tinea CASPOFUNGIN IV only Renal excretion Liver metabolism No P450 Highly protein bound 5-FLUORO-CYTOSINE - 5-FC Combo Tx (mostly) 5-FC + Ampho B

Superficial infections Dermatophytes Tinea Ringworm

Grizzlies interfere with might! (mitosis) Aspergillosis In amphotericin intolerant Px's Candidiasis Disseminated Inhibits Beta(1-3) glucan synthesis A Fungal cell wall disruption Well-tolerated HA release possible

Chromomycosis Candida Aspergillosis Cryptococcal

RX entry into yeast cell (cytosine permease) A 5-FC --> 5-FU (via cytosine deaminase) A 5-FU inhibits transcription of RNA A Blocks tymidylate synthetase A Stops DNA synthesis

BM suppression (#1 problem) Diarrhea (10%) Watch renal failure Px's Resistance Loss of permease or deaminase Crypto

Anti-Fungal Rx's

SIDE EFFECTS / TOXICITY

Nausea; Vomiting; Ab. pain; Anorexia

Monitor K+, Mg++, BUN, CRE, A-B

Visual disturbances (30min after Tx)

Anti-Fungal Rx's

IVERMECTIN "rIVER blindness" "rIVER es muy ancho"

INDICATIONS Onchocerciasis (River blindness) Black flies A Fibrous nodules A Lizard skin

MECHANISM OF ACTION Kills microfilariae Microfilariae from leaving uteri of worms

SIDE EFFECTS / TOXICITY

MEBENDAZOLE THIOBENDAZOLE "Bendy, like worms" PYRANTEL PAMOATE

Nematode / Roundworm Whipworm Pinworm

Paralyzes worm A Passes out stool

Giant roundworm (Ascaris) Pinworm (Enterobius) "Pray tell, PAM ATE a GIANT WORM!!"Hookworm (Necator/Ancylostoma) Toe rash --> Lung --> GI Fe2+ def. Anemia; Wt. Loss PRAZIQUANTEL Cysticercosis Schistosomiasis (flukes) Praze tha Lord: Paragonimus "Christ's Sister Schisto Clonorchis is a Paragon Clone" All tapeworms NICLOSAMIDE "Nickle = es-toad / Tapeworm" Toad with nickle tape A Making a "teeny lata" Cestode (tapeworm) D. latum Hymenolepsis nana Taenia solium (#2 Rx)

Broad spectrum antiparasitic

Mitochondrial Ox-Phos GLU uptake by parasite

PENTAVALENT ANTIMONY "Leechman is Anti-Money" ie he will leech off you

Leishmania

CHLOROQUINE QUININE MEFLOQUINE

PRIMAQUINE Prima Viva Ova!!

Malaria (chloroquine) vivax ovale malariae Quinine (if chloro-resistant) Tx = Artemethol for severe P. falc. Malara (latent hypnozoite--liver) Plasmodium vivax Plasmodium ovale

Human resistance to Vivax & Falciparim Vivax = Duffy a + b Falcip: SSD-->rupture-->infxn

P. falciparum = Aggressive A 30% of RBC's Mefloquine resistant Chloroquine resistant Quinine resistant Chloroquine resistant Hemolysis in G6PD GI upset

Exo-RBC cycle: vivax; ovale A Liver

METRONIDAZOLE Sitting on the METRO gives you Diarrhea Vadge infections

Giardia Entameba histolytica Gardnerella vaginalis Trichomonas (nasty vadge discharge) "Gee-ur Aunt's Guard Tricked me to get on the metro"

Metallic taste

PENTAMIDINE I'm all Pent up I might die [AIDS PCP]

Prophylaxis: Pneumocystis carinii pneumonio

NIFURTIMOX

Chagas Dz (Trypanosoma cruzi)

SURAMIN " I Sure Am Sleepy; I might trip"

Sleeping sickness (African tryp) Tripanosomiasis (tsetse fly)

Antiparasitics

SIDE EFFECTS / TOXICITY

Antiparasitics

INDICATIONS Influenza A (prophylaxis) Parkinson's Dz Don't ask "a man to dine" with you if: Rubella He has A Flu (sneeze on your dish) He's got Parkinson's (throw food) He's dizzy, ataxic, slurring AMANTADINE Rimantidine = derivative w/ few S.E.'s ZANAMIVIR Zanamivir (inhaled) Oseltamivir (oral) RIBAVIRIN Ribavirin is rabid RSV (RibaVirin) Eats the IMP Rabid and bloody (hemolytic) ACYCLOVIR A cycle of Di-p --> Tri-p --> DNA Zovirax ACV Valacyclovir (pro-drug) FAMCYCLOVIR Zovirax ACV Valacyclovir (pro-drug) HSV VZV EBV Prophylaxis (compromised Px's) Influenza Virus A Influenza Virus B Asthmatics (use Oseltamivir) RSV

MECHANISM OF ACTION Viral penetration / uncoating

SIDE EFFECTS / TOXICITY CNS Ataxia Dizziness Slurred speech

Influenza Neuraminidase

Bronchoconstriction (asthma) A Use Oseltamivir, not Zanamivir

IMP dehydrogenase A Synthesis of guanine nucleotides

Hemolytic anemia Teratogen (severe)!!

Phosphorylated by viral thymidine kinase A Diphosphate --> Triphosphate (active) A Competes w/ Deoxyguanose TRFP A Viral HSV DNA polymerase A DNA synthesis

Delerium Tremor Nephrotoxicity Resistance: CMV

HSV-1 (labialis) Potent inhibitor of HBV DNA P-ase Denavir cream (oral) A Nucleoside Analogue HSV-2 A Deacylated + oxidized in liver Acute (3x/day) A Converted to Pencyclovir Recurrent; Suppression (2x/day) A Taken up by infected cells VZV (3x/day) A Phosphorylated by viral TK HBV A Affinity for P-ase

Rarely side effects Headache; Nausea

GANCICLOVIR "C MoVe the GAN GAN (kankan)"

CMV

Phosphorylated by viral thymidine kinase A Viral CMV DNA polymerase

Leukopenia; Thrombocytopenia Nephrotoxicity Toxicity: Ganciclovir > Acyclovir

DHPG (dihydroxy-2-propoxymethyl guanine) GCV Ctyovene Valgancyclovir (pro-drug) FOSCARNET IV only Pyrophosphate analog (Foscarnet) Foscavir Use when Ganciclovir fails Binds to pyrophosphate binding site CMV A Viral CMV DNA polymerase CMV retinitis in immunocomrpomised No need for phosphorylation

GCSF: G'cyle stim. Factor

E'lytes Thrombophlebitis

INTERFERONS Glycoproteins from Leukocytes

HBV (chronic) HBC (cronic) Kaposi's Sarcoma

Viral RNA and DNA synthesis

Neutropenia

Antivirals

SIDE EFFECTS / TOXICITY

Antivirals

BETHANECHOL "Bet you it's In the colin (retention)" CARBACHOL PILOCARPINE

INDICATIONS MECHANISM OF ACTION Ileus (Post-op / Neuro) Cholinergic Agonist Urinary Retention (Post-op / Neuro) Activates bowel + bladder smooth muscle

SIDE EFFECTS / TOXICITY

Glaucoma

Cholinergic Agonist Activates ciliary muscle of eye (open angle) Activates Pupillary sphincter (narrow angle) DIRECT AGONISTS

NEOSTIGMINE Oral; Injection

PYRIDOSTIGMINE Oral Injection EDROPHONIUM

Myesthenia gravis Carbamylation of Anticholinesterase Ileus (Post-op / Neuro) A ACh -Esterase Urinary Retention (Post-op / Neuro) A Ach (endogenous) Antidote - NMJ blockade Myesthenia gravis Carbamylation of Anticholinesterase A ACh -Esterase A Ach (endogenous) A Strength Dx of Myesthenia gravis Anticholinesterase / Cholinesterase inhibitor ie v. short acting A Ach (endogenous)

PHYSOSTIGMINE Eye drops Ointment Physo for my Eyes, Oh! ECHOTHIOPHATE "Echothio = Echo in my eye, Oh!" Demelarium Isoflurophate PRALIDOXIME

Glaucoma (crosses BBB) Atropine overdose "Eyes are 'fizzing' from pressure" Glaucoma Esotropia (X-eyed)

Anticholinesterase / Cholinesterase inhibitor A Ach (endogenous)

Anticholinesterase / Cholinesterase inhibitor A Ach (endogenous) INDIRECT AGONISTS ACh-Esterase Regenerator

Antidote - ACh-Esterase Toxicity Antidote - Pesticides; Nerve gas Diarrhea Pray + Lie = Doxology of DUMBBELLS Urination Miosis Injection Bronchospasm Bradycardia Excitation of skeletal muscle Lacrimation Sweating Salivation

ACh-E ANTIDOTE ATROPINE "A troop blocking SLUD" Mad as a hatter; Hot as a hare Dry as a bone; Blind as a bat HEXAMETHONIUM Salivation Lacrimation Urination Defecation Muscarinic Antagonist Dilate pupil Secretions (Acid; Airway) GI Motility Tx organophosphate poisoning Nicotinic Antagonist Ganglionic blocker ANTIMUSCARINICS - R-BLOCK BENZTROPINE Parkinson's "Park the Benz - Slowly and smoothly" Tx Sx's of Reserpine; Haloperidol SCOPOLAMINE Motion Sickness Pupil Dilator Anti-Muscarinic Anti-Dyskinetic (Stiffness) Anti-Muscarinic ANTIMUSCARINICS - CNS HOMATROPINE Pupil Dilator Anti-Muscarinic Uveitis Post-synechiae (iris sticks to cornea) Pupil Dilator Anti-Muscarinic Uveitis Post-synechiae (iris sticks to cornea) Asthma COPD Anti-Muscarinic Bronchodilator ANTIMUSCARINICS - LUNG Mydriasis Cycloplegia Mydriasis Cycloplegia ANTIMUSCARINICS - EYE Red as a beat - Temperature; Pulse Hot as a hare - Temperature; Pulse Dry as a bone - Dry mouth / Flushed Mad as a hatter - Disorientation Blind as a bat - Cycloplegia; Mydriasis

TROPICAMIDE Eye drops Ointment IPRATROPIUM Inhalant

Cholinergics

SUCCINYLCHOLINE It "sucks" to be paralyzed

INDICATIONS Muscle paralysis in: Surgery Mechanical ventilation

MECHANISM OF ACTION Neuromuscular blockade (depolarizing) Phase I - Prolonged depolarization Antidote = None Phase II - Repolarized, but blocked Antidote = Neostigmine

SIDE EFFECTS / TOXICITY

X-CUR-X Tubocurarine Atracurium Mivacurium Pancuronium Vecuronium Rapacuronium

Muscle paralysis in: Surgery Mechanical ventilation

Neuromuscular blockade (non-depolarizing) Antidote = Neostigmine; Edrophonium Pyridostigmine

NEUROMUSCULAR BLOCKADE Halothane + Succinylcholine Ca2+ release from SR of skeletal muscle A Malignant hyperthermia "Gets Dan to Lean (relax from rigidity)" Antipsychotic Rx (Phenothiazines) A Neuroleptic Malignant Syndrome DANTROLENE

NM Blockade

EPINEPHRINE Epidemic: It gets all the receptors NOREPINEPHRINE

INDICATIONS Anaphylaxis Asthma Hypotension Glaucoma (open angle) Hypotension

MECHANISM OF ACTION Agonist (direct) 1; 2; 1; 2

SIDE EFFECTS / TOXICITY

Agonist (direct) 1; 2; 1

Renal perfusion

Near-Epidemic: Almost gets all receptors But it be too (2) weak ISOPROTERENOL Iso = Equal; Erenol = Agonist DOPAMINE DOPA = DD DOBUTAMINE X-BU-X = 2 > 1 CATECHOLAMINES AMPHETAMINE Aderol EPHEDRINE Eep! Head run Head run = head:snot; dick:urine Pseudophed PHENYLEPHRINE NE ADD Obesity Narcolepsy Nasal Congestion Urinary incontinence Hypotension Agonist (indirect) Releases stored catecholamines A 1; 2; 1; 2 Agonist (indirect) Releases stored catecholamines A 1; 2; 1; 2 A Constricts (no fluid flow) CATECHOLAMINES Hypotension Nasal Congestion Eye exam (Pupil dilator) Agonist (direct) 1 > 2 AGONIST ALBUTEROL TERBUTALINE X-BU-X = 2 > 1 AGONIST COCAINE Local anesthesia Re-Uptake of Chatecholamine A Agonist (indirect) Agonist (central) A Central adrenergic outflow "Clones NE" (fakes presynaptic-R's) OTHER 1 2 Vasoconstriction Tachycardia; Arrhythmias Asthma Agonist (direct) 2 > 1 Shock Heart failure Agonist (direct) 2 > 1 Shock (DA --> Renal perfusion) Heart failure AV Block (rare use) Agonist (direct) 1 = 2 No effects Agonist (direct) D1 = D2; > >

CLONIDINE -METHYLDOPA

B.V. B.V. Pre-Synaptic

Vasoconstriction Vasoconstriction NE Release - (-) Feedback HR Bronchodilation

1 2

Heart Bronchial Smooth M. Skeletal M. Arterioles

??

Sympathomimetics

PHENOXYBENZAMINE "Pheno = Pheo" PHENTOLAMINE "Phento = Pheo" X-ZOSINS Zosin - Sauce In; HTN Prazosin Terazosin Doxazosin YOHIMBINE

INDICATIONS Pheochromocytoma - HTN

MECHANISM OF ACTION Non-Selective Blocker Irreversible

SIDE EFFECTS / TOXICITY Irreversible Orthostatic Hypo-TN Reflex tachycardia Reversible Orthostatic Hypo-TN Reflex tachycardia 1st-Dose Orthostatic Hypo-TN Dizziness Headache

Pheochromocytoma - HTN

Non-Selective Blocker Reversible 1-Selective Blocker

HTN BPH urinary retention

Impotence (controversial)

2-Selective Blocker

Arrhythmias (no (-) feedback)

-BLOCKERS

-BLOCKERS (X-OLOL) Non-Selective Blockers Propranolol Pindolol Timolol Nadolol Labetalol 1-Selective Blockers Atenolol Betaxolol "A BEAM of 1's" Esmolol Acebutolol Metoprolol

HTN Angina pectoris MI SVT (propranolol; esmolol) CHF Glaucoma

CO; Renin secretion HR; Contractility --> O2 demand HR; Contractility --> O2 demand; Death AV conduction velocity Progression to CHF Secretion of aqueous humor

Impotence Asthma exacerbation Bradycardia; AV block; CHF CNS: Sedation; Sleep; Diabetics

-BLOCKERS

Sympathetic Blockers

SIDE EFFECTS / TOXICITY

DIRECT AGONISTS

INDIRECT AGONISTS

ACh-E ANTIDOTE Red as a beat - Temperature; Pulse Hot as a hare - Temperature; Pulse Dry as a bone - Dry mouth / Flushed Blind as a bat - Cycloplegia; Mydriasis

ANTIMUSCARINICS - R-BLOCK

ANTIMUSCARINICS - CNS

ANTIMUSCARINICS - EYE

ANTIMUSCARINICS - LUNG

Cholinergics

SIDE EFFECTS / TOXICITY

NEUROMUSCULAR BLOCKADE

NM Blockade

SIDE EFFECTS / TOXICITY

CATECHOLAMINES

CATECHOLAMINES

AGONIST

AGONIST

OTHER

Sympathomimetics

SIDE EFFECTS / TOXICITY

-BLOCKERS

-BLOCKERS

Sympathetic Blockers

BARBITURATES (BARBITALS) Phenobarbital Pentobarbital Thiopental Secobarbital BENZODIAZEPINES (EPAMS) Diazepam Lorazepam Temazepam Chlordiazepoxide Short-Acting Triazolam like "TOM's thumb" Oxazepam Tri = three Midazolam Frequency Frenzodiazepines (FREquent) ANTIPSYCHOTICS "Clears thy halo fluff, Psycho!" Chlorpromazine Thioridazine Haloperidol Fluphenazine ATYPICAL ANTIPSYCHOTICS Olanzapine Clozapine Risperidone LITHIUM O lands! A Close! A respite!

INDICATIONS Sedative Anxiety Seizures Insomnia Anesthesia induction (thiopental) Porphyria Anxiety Spasticity Status epilepticus (diazepam) Detoxification (delerium tremens) Insomnia

MECHANISM OF ACTION Cl- channel open duration A Neuronal firing A GABAa facilitator Barbiturates DURATion of Cl- ch.

SIDE EFFECTS / TOXICITY Dependence CNS depression w/ alcohol --> Death Cyt. P450 - Rx interactions

Cl- channel open duration A Neuronal firing A GABAa facilitator

Sedation Dependence CNS depression w/ alcohol --> Death Benzo's < Barb's in CNS depression ie respiratory depression Overdose Tx = Flumazenil

Flumazenil (overdose Tx) GABA-r (competitive antagonist)

Schizophrenia (excess DA) Psychosis

D2-r

Neuroleptic Malignant Syndrome Rigidity; Autonomic instability; Hyperreflex Tardive dyskiniesia Dystopnia (4 hrs) Stereotyped oral-facial mvnts (chr. use) A Akinesia (4 days) A Akathisia (3 wks) A Tardive dyskinesia (4 mos) Schizophrenia - (+) & (-) Sx's OCD (olanzapine) Anxiety (olanzapine) Depression (olanzapine) Bipolar affective disorder Acute manic events (relapse) Mood stabilizer ??PIP Cascade?? 5HT2-r's + DA-r's Fewer extrapyramidal S.E.'s Clozapine = agranulocytosis (monitor)

Sedation; Extrapyramidal S.E.'s Endocrine S.E.'s Muscarinic-r's; HA-r's; -r's

Tremor Hypothyroidism Polyuria (ADH antagonist) Teratogen / Toxic!

TRICYCLIC ANTIDEPRESSANT (IPRAMINE; TRIPTYLINE) Nortriptyline (2') Doxepin Clomipramine Amitriptyline (3') Imipramine Desipramine SSRI's Fluoxetine Sertraline Paroxetine Citalopram HETEROCYCLICS Mirtazapine Buproprion Venlafaxine Trazodone Heterosexuals "Mirt & Bupee Vem la pra Tranzar" Holy trinity / TRI-C Nor tripping Doxology Clomping Am I Desciple

Depression Bed wetting (imipramine) OCD (clomipramine)

NE & SE reuptake

Sedation -Blocking S.E.'s Anticholinergic S.E.'s TRI - C's Convulsions Coma Cardiotoxicity (arrhythmias) 3' > 2' (Amitriptyline > Nortriptyline) Desipramine is least sedating SSRI's < TCA's CNS - Anxiety; Insomnia; Tremor Nausea; Vomiting Serotonin Syndrome w/ MAOI's Hyperthermia; Rigidity; CV collapse

Depression

SE reuptake (serotonin-specific) 2-3 wks for effect

Major depressive disorders Depression; Depression; Smoking cessation Depression; Anxiety disorder Depression; 2 Antagonist --> NE & SE release; 5HT2-r antogonist Cholesterol; Appetite Sedation; ??? Tachycardia; Dry mouth; Psychosis DA & SE reuptake; 5HT2-r antagonist Anxiety; Agitation; Headache; Insomnia SE reuptake Sedation; Nausea; Priapism; HypoTN

CNS Rx's

MOA INHIBITORS (GENERAL) Phenylzine Tranylcypromine MAO-B INHIBITOR Selegiline (Deprenyl)

INDICATIONS Atypical depressions Depression + Psychosis Depression + Phobias Anxiety Hypochondriasis Parkinson's adjuvant Rx L-DOPA + Selegiline

MECHANISM OF ACTION Monoamine Oxidase Inhibition A Degredation of monamines

SIDE EFFECTS / TOXICITY MAO I + Tyramine + Meperidine A HTN crisis CNS stimulation SSRI's; -Agonists Enhances L-DOPA S.E.'s

MAO-B selective inhibition A DA availability

L-DOPA + CARBIDOPA

Parkinson's

L-DOPA L-DOPA crosses BBB A Dopa decarboxylase conversion A DA (in brain) Carbidopa Dopa decarboxylase in periphery A S.E.'s; Bioavailability of DA in brain

Arrhythmias (from periferal conversion) Dyskinesias

OPIOID ANALGESICS

Pain Opioid-r Agonists Cough (dextromethorphan) mu = morphine "MMM, Dexter Fenan's Code is Heroin" Diarrhea (loperamide; diphenoxylate) delta = enkephalin Acute pulmonary edema kappa = dynorphin Morphine Withdrawal (methadone) Modulate synaptic transmission Meperidine Methadone Dextromethorphan Fentanyl Codeine Heroin SUMATRIPTAN Acute migraine Cluster headache attacks I assume a trip and you 5HiT your head A Headaches; Migraines Prinzmetal's Angina; CAD ONDANSETRON "On Dan it runs (vomit)" Vomiting (control) Post-op vomit control Cancer Tx vomit control 5-HT1d Agonist 1/2 life < 2 hrs

Addiction CNS depression Respiratory distress Pinpoint pupils Constipation Toxicity Antidote Naloxone Naltrexone

Chest discomfort Mild tingling

5-HT3 Antagonist A Central-acting anti-emetic

Headache Diarrhea

CNS Rx's

PHENYTOIN "Fee Na+ To In" Na+ has a fee to enter so it can't

INDICATIONS Grand mal seizures

MECHANISM OF ACTION Na+ Channels (use-dependent)

SIDE EFFECTS / TOXICITY Nystagmus; Diploplia Ataxia; Peripheral neuropathy Lethargy; Megaloblastic Anemia (B12) Gingival hyperplasia Hirsutism Teratogenic - Fetal hydantoin syndrome

CNS Rx's

SIDE EFFECTS / TOXICITY CNS depression w/ alcohol --> Death

CNS depression w/ alcohol --> Death Benzo's < Barb's in CNS depression

Clozapine = agranulocytosis (monitor)

Hyperthermia; Rigidity; CV collapse

Anxiety; Agitation; Headache; Insomnia Sedation; Nausea; Priapism; HypoTN

CNS Rx's

SIDE EFFECTS / TOXICITY

Arrhythmias (from periferal conversion)

CNS Rx's

SIDE EFFECTS / TOXICITY Lethargy; Megaloblastic Anemia (B12)

Teratogenic - Fetal hydantoin syndrome

CNS Rx's

ACETAZOLAMIDE "Aceta acidifies"

INDICATIONS Glaucoma Alkalosis (metabolic; urinary) Altitude sickness

MECHANISM OF ACTION Carbonic anhydrase in PCT A NaHCO3 diureses A HCO3 excretion

SIDE EFFECTS / TOXICITY Acidosis (hyperchloremic metabolic) Neuropathy NH3 toxicity Sulfa allergy "Aceta acidifies"

FUROSEMIDE Sulfonamide loop diuretic

Edema (CHF; Cirrhosis; Pulm) HTN Ca2+-emia

Na+ / K+ / 2Cl- Cotransporter in TAL A Hypertonicity of medulla A Concentration of urine A Diuresis / Dilute urine A Na+ to DT --> K+ swapping A K+-emia A Ca2+ excretion --> Ca2+-emia

K+-emia Ca2+-emia Ototoxicity I.S. Nephritis Allergy (sulfa) Gout Dehydration K+-emia Ca2+-emia Ototoxicity I.S. Nephritis Dehydration No uricemia (no gout) No sulfa allergies K+ metabolic alkalosis Na+emia Ca2+emia GLU HyperGLUC Lipids Uricemia Sulfa allergy K+emia Endocrine effects - gynecomastia Blocks ALD --> backflow

ETHACRYNIC ACID Phenoxyacetic acid derivative Not sulfonamide "Ferocious Etha cryin" cuz she got sulfa allergies HYDROCHLOROTHIAZIDE Thiazide diuretic

Na+ / K+ / 2Cl- Cotransporter in TAL A Hypertonicity of medulla A Concentration of urine A Diuresis / Dilute urine NOTE: A Na+ to DT --> K+ swapping Diuresis in Px's w/ sulfa allergies A K+-emia A Ca2+ excretion --> Ca2+-emia Edema HTN Ca2+-emia HTN CHF Ca2+uria Nephrogenic Diabetes Insipidus NaCl reabsorption in early DT A Diluting capacity of nephron A Ca2+ excretion

K+ SPARING DIURETICS "Try and Sprint A mile" - Km sparing Triamterene Spironolactone Amiloride MANNITOL

ALD K+ Depletion CHF

Competitively binds ALD-r in CCT (Spiro) Na+ channel in CCT (Triam; Amilo)

Shock Drug overdose Intraocular pressure (decreases it) Anuria CHF

Osmotic Diuretic

Pulmonary edema Dehydration

DIURETIC E'LYTE CHANGES Carbonic Anhydrase Inhibitors K+ Sparing Loops Thiazides

URINE NaCl (All) K+ (except K+ sparing) Ca2+ (loops) Ca2+ (thiazides)

BLOOD pH (acidosis) - Carb-A Inhib.; K+ sparing pH (alkalosis) - Loops; Thiazides

Diuretics

INDICATIONS -BLOCKERS 1 Selectivity (heart only) Atenolol Betaxolol Esmolol Acebutolol Metoprolol 1 = 2 Propranolol Pindolol Nadolol Labetalol HTN Angina MI SVT CHF Glaucoma Asthma !Diabetics! CO; Renin HR; Contractility Mortality AV conduction velocity Progression Secretion

MECHANISM OF ACTION
Ca2+ Ca2+ Ca2+ Ca2+ Ca2+ Ca2+ Ca2+

SIDE EFFECTS / TOXICITY Impotence Bronchospasm Bradycardia; AV block Sedation; Sleep alterations TG's and HDL

P cAMP

1
ATP

cAMP A Ca2+ influx A HR, Contractility A Refractory period cGMP A Smooth muscle relaxation A Arterioles > Veins Relaxation A Afterload

HYDRALAZINE "Hydra-relaxing"

HTN (severe) CHF

Nausea; Headache Hypotension; Reflex tachycardia Fluid retention SLE-like syndrome Hydra (H2O-retention)

ACE INHIBITORS Captopril Enalapril Lisinopril Angiotensin II-R Antagonist Losartan (no cough S.E.)

HTN CHF Diabetic Renal Dz

Antiotensin-converting enzyme Angiotensin I ACE AT II A Vasoconstriction Na+/H2O Bradykinin Sympathetics A Renin release (compensatory)

Cough Angio-edema Proteinuria Taste changes HypO-TN Pregnancy problems (fetal renal injury) Rash Increased Renin Lower A-II Hyperkalemia CAPTOPRIL Tachycardia Hypotension "Monday Dz" Tolerance during work week Intolerance on weekends A Tachycardia Dizziness; Headache

NITRATES Nitroglycerin Isosorbide Dinitrate

Angina Edema (pulmonary) Aphrodesiac; Erection enhancer

NO release from smooth muscle A cGMP A Smooth muscle relaxation A Vasodilation (veins > arteries)

GLYCOSIDES Digoxin 75% bioavailability 25% protein-bound t1/2 = 3 days Peed out

CHF Atrial Fib

Na+/K+ ATPase A Na+ I.C. A Na+ / Ca2+ swap

Na+ Na+ K+

Na+

Nausea; Vomiting; Diarrhea Blurry yellow vision (Van Gogh) Arrhythmia Renal Failure A Excretion A Risk for toxicity K+ A Potentiates glycosides --> Toxic!! Quinidine A Clearance of digoxin Antidote = K+; Lidocaine; Pacer; Anti-dig Fab fragments

Ca2+ Ca2+ Ca2+ Ca2+ Ca2+ Na+ Ca2+ Ca2 Na+ Na+ Na+ Na+

Na+ (IC) A Ca2+ (IC) PHOSPHODIESTERASE INHIB

AMP P-DiesterasecAMP

1
ATP

Cardiovascular

CLASS IA Quinidine Amiodarone Procainamide Disopyramide Queen Amy Proclaims Dis Ol' pyramid

INDICATIONS Atrial arrythmias Ventricular arrhythmias

MECHANISM OF ACTION SIDE EFFECTS / TOXICITY Local anasthetics Quinidine: / Conduction Headache; Tinnitus A Slope of phase 4 depolarization Thrombocytopenia A Threshold in abnormal pacemaker cells Torsade de pointes (QT) Slectively depress frequent depolarizers Procainamide: SLE-like syndrome (reversible) K+ Channel A K+ (IC) A Repol. A PR QRS K+ K+ K+ K+ K+ K+ QT
K+ K+

CLASS IB Lidocaine Mexiletine Tocainide CLASS IC Flecainide Encainide Propafenone

Acute ventricular arrhythmias Post-MI Digitalis-induced arrhythmias

AP duration A Affects ischemic or depolarized Ventricula tissue Purkinje tissue

Local anesthetic CNS stimulation/depression Cardiovascular depression

Last resort b/c of toxicities Ventricular Tach / Fib SVT (intractable) No effect on AP duration

Proarrhythmic

CLASS II - -BLOCKERS Esmolol (short acting) Metoprolol Timolol Atenolol Propranolol Esmo Met Tim A 10 Pro

Suppress abnormal pacemakers

caMP; Ca2+ currents A Phase 4 slope A Abnormal pacemakers A PR interval AV Node sensitive

CLASS III - K+ CH. BLOCKERS Sotalol Ibutilide Bretylium Amiodarone

Use when other antiarrythmics fail

AP duration ERP QT interval

Sotalol - Torsade de pointes Ibutilide - Arrhythmias; HypoTN Bretylium Amiodarone - Pulmonary fibrosis Hepatotoxicity Hypo/Hyper-Thyroidism Neuro; Skin; Photoderm Constipation Flushing Edema CHF; AV block; SN dep. Torsades de pointes (bepridil)

CLASS IV Ca2+ CH. BLOCKERS Verapamil Diltiazem

Nodal arrhythmias (ie SVT) Prevention

Affect AV nodal cells A Conduction velocity ERP PR interval

Ca2+ CHANNEL BLOCKERS "Knife Dealt [you] A Vera!!" Nifedipine > Diltiazem > Verapamil Verapamil > Diltiazem > Nifedipine

HTN Angina Arrhythmias

L-type Ca2+ channels (cardiac; smooth m) Cardiac depression A Contractility Peripheral edema Flushing; Dizziness Constipation Smooth muscle: Knife dealt you a vera Heart: Vera dealt a knife

MISCELLANEOUS Adenosine K+ Mg+ #1 Rx for AV nodal arrhythmias Ectopic pacemakers; Digoxin toxicity Torsades de pointes; Digoxin toxicity

Antiarrhythmics

SIDE EFFECTS / TOXICITY Acidosis (hyperchloremic metabolic)

Diuretics

SIDE EFFECTS / TOXICITY

Pregnancy problems (fetal renal injury)

Potentiates glycosides --> Toxic!!

Cardiovascular

SIDE EFFECTS / TOXICITY

Hypo/Hyper-Thyroidism Neuro; Skin; Photoderm

Antiarrhythmics

SILDENAFIL "Sildenafil FILLS the penis"

INDICATIONS Erectile dysfunction

MECHANISM OF ACTION cGMP phosphodiesterase A cGMP A Relaxation of smooth muscle A Corpus Venosum fills with blood A Erection

SIDE EFFECTS / TOXICITY Headache Flushing Dyspepsia Blue-green vision !!Hypotension!! (Heart Px's; Nitrates)

H2 BLOCKERS Cimetidine Ranitidine Famotidine Nizatidine OMEPRAZOLE LANSOPRAZOLE

PUD Gastritis GERD Z-E Syndrome

H2-r (reversible blockage) A H+ production P450 (potent inhibitor)

Anti-androgenic effect (cimetidine) CRE (cimetidine)

PUD Gastritis GERD Z-E Syndrome PUD Cannot work w/ Antacids PPI's; H2 blockers

H+/K+ ATPase in parietal cells (irreversible) A H+ Production in stomach

SUCRALFATE Aluminum sucrose sulfate

Polymerizes in pH (stomach env.) A Binds necrotic peptic ulcer tissue A Barrier to acid, pepsin, and bile

MISOPROSTOL

NSAID-Peptic-Ulcer prevention PGE1 Analog Induce labor A Mucous secretion of GI mucosa Childbearing potential (abortative) GERD PUD pH buffers

Diarrhea

ANTACIDS Al2+ hydroxide Mg2+ hydroxide Ca2+ carbonate

K+ (all) Al2+ hydroxide = Constipation; PO4Mg2+ hydroxide = Diarrhea Ca2+ carbonate = Ca2+; Acid Can affect absorption of other Rx's

GI Rx's

SIDE EFFECTS / TOXICITY

!!Hypotension!! (Heart Px's; Nitrates)

Al2+ hydroxide = Constipation; PO4-

GI Rx's

HEPARIN LMWH Better bioavailability Longer hal-life Subcutaneous w/o lab monitoring Short 1/2 life WARFARIN Coumadin Long 1/2 life

INDICATIONS IMMEDIATE anticoagulation Pulmonary embolism Storke Angina MI DVT Pregnancy = OK Chronic coagulation Hypercoagulable state (prolonged) Follow PT values Pregnancy (X-placenta)

MECHANISM OF ACTION Catalyzes activation of antithrombin III A AT II Activation

SIDE EFFECTS / TOXICITY Bleeding Thrombocytopenia Rx-Rx Interactions Antidote = Protamine sulfate Follow PTT Check aPTT

Antidote = Protamine sulfate (+) charged molecule A Binds HA(-)

carboxylation of Vit K-dependent Factors Bleeding Protein C & S (via vit. K antagonism) Teratogenic Rx-Rx interactions II, VII, IX, X O2 CO2 Vit K NADPH NADP

IIa, VIIa, IXa, Xa NADPH oxidation A Reduced Vit. K A Activation of II, VII, IX, and X "War-far-in hits 2, 7, 9 and 10" ANTICOAGULANTS THROMBOLYTICS Streptokinase Urokinase t-PA (ALTEPLASE) APSAC (anistreplase) THROMBOLYTICS CLOPIDOGREL TICLOPIDINE Use only for Aspirin intolerant Px's ANTIPLATELETS Acute Coronary Syndrome Coronary stenting Prevention of thrombotic stroke ADP pathway A Binding of fibrinogen A Platelet aggregation Neutropenia (ticlopine) Use only for Aspirin intolerant Px's Early MI Plasminogen --> Plasmin (direct/indirect) A Plasmin cleaves thrombin & fibrin Bleeding

Anticoagulants

INDICATIONS BILE ACID RESINS Cholestyramine Colestipol HMG-CoA REDUCTASE INHIB. Simvastatin Atorvastatin Pravastatin Lovastatin Sim the Actor Prays for Love HMG Studios on Statin Island NIACIN

MECHANISM OF ACTION Reuptake of bile acids in lumen A LDL =HDL ~TG HMG CoA Reductase A CE synthesis in liver A LDL HDL TG

SIDE EFFECTS / TOXICITY Px's HATE it!! Tastes bad GI discomfort

$$$ Myositis; Muscle stiffness LFT's (reversible)

Hepatic release of VLDL A LDL HDL TG LPL activity A Breakdown of VLDL --> IDL --> LDL A LDL HDL TG

Flushing; Red face; Tx w/ aspirin

LIPOPROTEIN LIPASE STIM Gemfibrozil Clofibrate

Myositis; Muscle stiffness LFT's

Lipid-Lowering

SIDE EFFECTS / TOXICITY

ANTICOAGULANTS

THROMBOLYTICS

ANTIPLATELETS

Anticoagulants

SIDE EFFECTS / TOXICITY

Lipid-Lowering

METHOTREXATE S Phase antimetabolite

INDICATIONS Leukemias Lymphomas Choriocarcinoma Sarcomas Abortion Ectopic pregnancy Rheumatoid Arthritis Psoriasis Colon CA Solid tumors Basal Cell CA (topical)

MECHANISM OF ACTION Folic acid analog A Dihydrofolate reductase A dTMP A DNA + Protein synthesis

SIDE EFFECTS / TOXICITY Myelosuppresion Reverse w/ Leucovorin or Folinic acid Liver macrovesicular fatty change

5-FU (5-FLUOROURACIL) S Phase antimetabolite Effects as Methotrexate Synergy w/ methotrexate 6-MP (6-MERCAPTOPURINE)

Pyrimidine analog activated --> 5F-dUMP A Complexes to folic acid A Thymidylate synthase A dTMP Purine synthesis Metabolized by xanthine oxidase A Toxicity w/ Allopurinol

Myelosuppresion (not reversible) Photosensitivity

Leukemias Lymphomas (CLL or HD)

BM Liver GI Toxicity w/ Allopurinol

BUSULFAN

CML

Alkylating agent A X-links DNA

Pulmonary fibrosis Pigmentation

CYCLOPHOSPHAMIDE

NITROSOUREAS Carmustine Lomustine Semustine Streptozocin CISPLATIN

Non-Hodgkin's Lymphoma Breast CA Ovarian CA Immunosuppressant Brain tumors Glioblastoma multiforme

Alkylating agent A Liver bioactivation A X-links DNA at guanine N-7 Alkylating agent A Liver bioactivation A X-links DNA X-BBB Alkylating agent (acts like one) A Hydrolysis of Cl- groups A X-links DNA Intercalates DNA strands (non-covalent) A Replication and transcription A Free radical generation A Breakage Intercalates DNA strands A Free radical generation A Strand breaks Topoisomerase II (G2-phase) A Break repair in DNA A Degradation of DNA ???; Triggers apoptosis

Myelosuppression Hemorrhagic cystitis

CNS toxicity Dizziness Ataxia

DOXORUBICIN Adriamycin BLEOMYCIN

Testicular CA Bladder CA Ovary CA Lung CA HD (ABVD) Myelomas Sarcomas Solid Tumors (Breast; Lung; Ovary) Testicular CA Lymphomas

Nephrotoxicity CN VIII Heart Myelosuppression Alopecia Toxic extravasation Pulmonary fibrosis Skin

ETOPOSIDE

Lung CA (Oat cell) Prostate CA Testicular CA #1 Corticoid in CA Tx CLL Hodgkin's (MOPP) Autoimmune Dz's Breast CA

Myelosuppression GI Alopecia Cushing Syndrome; Immunosuppresion Osteoporosis; HTN; Peptic ulcers Cataracts; Acne; GLU; Psychosis Risk of endometrial cancer Hot flashes

PREDNISONE

TAMOXIFEN / RALOXIFENE

Estrogen mixed Agonist / Antagonist A Binding of estrogen to ER+ cells

VINCRISTINE / VINBLASTINE Oncovin / Vincristine

Lymphomas (MOPP) Wilm's tumor Choriocarcinoma

M-phase alkaloid A Binds to tubulin A Polymerization of microtubules A Mitotic spindle formation

Neurotoxicity Areflexia Peripheral neuritis Paralytic ileus BM (Vinblastine BLASTS BM)

PACLITAXEL

Ovarian CA Breast CA

M-phase alkaloid Myelosuppression A Binds to tubulin Hypersensitivity A Hyperstabilizes polymerized microtubles A Mitotic spindle breakdown A Anaphase

Cancer Drugs

SIDE EFFECTS / TOXICITY

Cushing Syndrome; Immunosuppresion

Cancer Drugs

INSULIN

INDICATIONS Diabetes Mellitus K+ (life-threatening) GLU

MECHANISM OF ACTION SIDE EFFECTS / TOXICITY Binds Insulin-R (liver; muscle; adipose) GLU A Tyrosine Kinase activity Allergy (rare) A GLU --> Glycogen (Liver) A Synthesis of glycogen + protein (Muscle) A Tryglyceride storage (Fat) Close K+ channels in -cell membrane A Cell depolarization A Ca2+ influx A Insulin release stimulated Ca2+ / Car release GLU Disulfiram-like effects Glyburide; Glipizide

SULFONYLUREAS

DM II (NIDDM)

So fun you'll race a Car (hyperglycemic) Chlorpropamide Glyburide Glipizide Tolbutamide METFORMIN Oral Biguanide "Metformin = Stops GLU Formin' " GLITAZONES Pioglitazone Rosiglitazone Troglitazone -GLUCOSIDASE INHIBITORS Acarbose Miglitol DM II MonoTx Combo + Above agents DM II MonoTx Combo + Above agents Chlar pool Glide your ride Glip the side [of the] Toll booth GLU

??Unknown?? Gluconeogenesis (liver) A GLU levels

Lactic acidosis

Targe cell response to insulin Glitazone = Lit a zone up (sensitivity) Inestinal brush border -glucosidase A Sugar hydrolysis and absorption A GLU serum levels (post-prandial)

Hepatotoxic (troglitazone) Weight gain Glitazone = Glutton zone --> Wt. Gain!

GI Disturbances

DIABETIC Rx's LEUPROLIDE GnRH Analog / Agonist Infertility (pulsatile) Prostate cancer (continuous) Leuprolide + Flutamide Uterine fibroids Continuous A LH and FSH Burst (transient) Anti-androgen Nausea; Vomiting

Leuprolide = Leutonizing H / Follicle SH PROPYLTHIOURACIL Thio = Thyro FINASTERIDE Anti-androgen Benign Prostastic Hypertrophy Finasteride = Fine ass rubber ball Big prostate = rubber ball in ass Prostate Carcinoma 5-reductase A Testosterone --> Dihydrotestosterone Finasteride = Final steroid (no conversion) Competitive inhibitor of Testosterone-r A Androgens Steroid synthesis Hyperthryoidism TH synthesis coupling T4 --> T3 conversion in periphery Skin rash Aplastic anemia Agranulocytosis

FLUTAMIDE Non-steroidal Anti-androgen KETOCONAZOLE SPIRONOLACTONE Anti-androgen

Polycystic ovarian syndrome (Prevents hirsutism)

Endocrine

INDICATIONS CLOMIPHENE Infertility

MECHANISM OF ACTION Pituitary ER(+) Estrogen agonist (partial) A Prevents (-)feedback A LH & FSH release A Ovulation stimulation Progestin (competitive inhibitor) A Hospitality of uterus for enpregnation

SIDE EFFECTS / TOXICITY Hot flashes Ovarian enlargement Multiple spontaneous pregnancies Visual Heavy vaginal bleeding GI (nausea; vomiting; anorexia) Abdominal pain TG'S Depression Weight Nausea HTN Coagulable state Non-REM sleep Fatigue; Sedation Sleep onset Night wakenings Immunosuppressant

MIFEPRISTONE (RU-486)

Abortifacient

ORAL CONTRACEPTIVES Estrogen Progestins

Contraception Regulation of menses Endometrial & Ovarian CA risk Ectopic pregnancy incidence Pelvic infections < 1% Failure

PROGESTERONE Produced by corpus luteum

Converts endometrium to decidualized state Withdrawal --> Endometrial shedding Maintains pregnancy Myometrial excitability; Uterine relaxation Thick mucus production (inhibits sperm) Temp (-) Feeback (LH; FSH) Competitively Inhibits aldosterone A Ald secretion (compensatory) Menopause (replacement Tx) A Hot flashes Bone loss

ESTROGEN Estradiol (ovary) Estriol (placenta) Aromatizaztion (in blood) Estrogen (Testes) Estradiol > Estione > Estriol (potency) Ovarian & Extraovarian A Estrone (E1) = Estradiol (E2)

Growth of follicle Excessive / Unopposed Estrogen Tx Endometrium proliferation A Risk of endometrial cancer Genitalia development Tx = Progesterone to balance Breast stroma development; Lactation prep Fat distribution (women) REM sleep Protein synthesis and transport (liver) Sleep wake cycle (-) Feedback (FSH) (+) Feedback (LH) Myometrial excitability Estriol Test = tests fetoplacental function Placental Sulfatase deficieny X-linked metabolic Dz in males Post-date pregnancies Labor inducement Estriol in mother DHEA-S in amniotic fluid Wolffian duct differentiation --> Gonads 2' Sex characteristics Growth spurt (puberty) Spermatogenesis Anabolic function A Muscle RBC's Libido Testosterone + 5-reductase A DHT Testosterone / Androstenedione + Aromatase A Estrogen (convertsion in adipose tissue)

Cholesterol (mother) A Pregnenolone (mother; placenta) A DHA sulfate (fetus) A DHA --> E1; E2 (placenta) A 16OH DHA sulfate (fetus --> placenta) A Estriol (E3); (placenta; mother) ANDROGENS Testosterone (testes; adrenal) DHT (prostate; peripheral conversion) Androstenedione (adrenal) DHT > Testosterone > Andro Targets A Skin; Prostate Epididymis; Seminal vesicles Liver; Muscle; Brain hCG in Choriocarcinoma Hydatidiform Mole Finasteride inhibits Test --> DHT

hCG Human Chorionic Gonadotropin Produced by syncytiotrophoblasts A Placenta (2nd & 3rd Tri) LH

Maintains corpus luteum (1st tri.) Stimulates CL secretion A Progesteron Estrogen Relaxin Pregnancy Test hCG(+) < 8 days

hPL Human Placental Lactogen

Anti-insulin effects on mom A Facilitates GLU delivery to fetus

Hormones

OCP's Ethinyl Estradiol Progestine

INDICATIONS Endometriosis

MECHANISM OF ACTION Pseudopreganncy state Menstrual flow PG's in Luteal phase

SIDE EFFECTS / TOXICITY

GnRH AGONISTS Leuprolide Acetate Nafarelin Goserelin

Endometriosis

(-) Feeback on Hypothalamus A Inhibition of GnRH

Hypoestrogenic state (profound) Hot flushes Bone density Costly drug

GnRH ANTAGONISTS Antagonists > Agonists (efficacy) Ganirelix Cetrorelix

Endometriosis

(-) Feeback on Hypothalamus A Inhibition of GnRH

PROGESTINS Norethindrone acetate Medroxyprogesterone Acetate GnRH Analogs ANDROGENS Danazol

Endometriosis

(-) Feeback on Hypothalamus A Inhibition of GnRH

Endometriosis

Antigonadotropic action

Virilization Estrogen deficiency

AROMATASE INHIBITORS

Endometriosis

Androgen --> Estrogen conversion

MIFEPRISTONE

Anti-progestin

Contraceptives

SIDE EFFECTS / TOXICITY

Glitazone = Glutton zone --> Wt. Gain!

DIABETIC Rx's

Endocrine

SIDE EFFECTS / TOXICITY

Excessive / Unopposed Estrogen Tx

Hormones

SIDE EFFECTS / TOXICITY

Contraceptives

PREDNISONE

CYCLOSPORINE

INDICATIONS #1 Corticoid in CA Tx CLL Hodgkin's (MOPP) Autoimmune Dz's Transplant immunosuppression Autoimmune disorders

MECHANISM OF ACTION Phospholipase A2 & COX-2 Expression A LKT's & PG's

SIDE EFFECTS / TOXICITY Cushing Syndrome; Immunosuppresion Osteoporosis; HTN; Peptic ulcers Cataracts; Acne; GLU; Psychosis Binds to peptidyl proline cis-trans isomerase Prone to viral infections A IL-2 synthesis & IL-2-r Prone to lympomas A Diff. & Activation of T Cells Nephrotoxic (Tx = mannitol diuresis) Anti-metabolite derivative of 6-MP A Metabolism & Synthesis of nucleic acid A L'cyte proliferation Antigenic stimulation A Toxic to L'cytes Folic acid analog A Dihydrofolate reductase A dTMP A DNA + Protein synthesis Myelosuppresion Reverse w/ Leucovorin or Folinic acid Liver macrovesicular fatty change

AZOTHIOPRINE

Kidney transplant I-suppression Autoimmune disorders GN Hemolytic Anemia

METHOTREXATE S Phase antimetabolite

Leukemias Lymphomas Choriocarcinoma Sarcomas

DACTINOMYCIN

CYCLOPHOSPHAMIDE

Non-Hodgkin's Lymphoma Breast CA Ovarian CA Immunosuppressant

Alkylating agent A Liver bioactivation A X-links DNA at guanine N-7

Myelosuppression Hemorrhagic cystitis

ANTI-L'CYTIC GLOBULIN Monoclonal anti-T L'cyte Ab's Rh3(D) Ig

TACROLIMUS (FK506) Cyclosporine

Transplant immunosuppression

Binds FK-binding protein A Secretion of cytokines (IL-2; others) A Diff. & Activation of T Cells

GLUCOCORTICOIDS Hydrocortisone Prednisone Triamcinolone Dexamethasone Beclomethasone

Addison's Dz Inflammation Immune suppression Asthma

Phospholipase A2 & COX-2 Expression A LKT's & PG's

Nephrotoxicity Peripheral neuropathy HTN Pleural effusion GLU IMMUNOSUPPRESSANTS Cushing's Syndrome Dorsal fat pads; Turnkal obesity Moon facies Muscle waisting; Osteoporosis Bruising Adrenocortical atrophy

Immunosuppressants

ASPIRIN NSAID

INDICATIONS Anti-pyretic Analgesic Anti-inflammatory Antiplatelet

MECHANISM OF ACTION SIDE EFFECTS / TOXICITY Acetylation action GI ulceration A COX-1 & COX-2 (IRREVersible inhibition)Bleeding A Arachidonic acid --> PGE's Hyperventilation Reye's syndrome Tinnitus (CN VIII)

OTHER NSAIDS Ibuprofen Naproxen Indomethacin

Anti-pyretic Analgesic Anti-inflammatory Antiplatelet

COX-2 INHIBITORS Celecoxib Rofecoxib

Acetylation action GI ulceration A COX-1 & COX-2 (REVersible inhibition) Bleeding A Arachidonic acid --> PGE's Hyperventilation Reye's syndrome Tinnitus (CN VIII) Patent ductus arteriosus (Indomethacin) NSAIDS Rheumatoid arthritis COX-2 (cyclo-oxygenase isoform 2) NO GI ulceration Osteoarthritis A Inflammation Bleeding Pain Hyperventilation A Spares COX-1 Reye's syndrome A OK = GI Mucosa maintenance Tinnitus (CN VIII) COX INHIBITORS

ACETAMINOPHEN

Anti-pyretic Analgesic !!Anti-inflammatory!!

COX (CNS mostly) - Reversible Inactivated peripherally

Hepatic necrosis (overdose) Glutathione depletion A Toxic adducts in liver

NSAIDS & COX

SIDE EFFECTS / TOXICITY Cushing Syndrome; Immunosuppresion

IMMUNOSUPPRESSANTS

Immunosuppressants

SIDE EFFECTS / TOXICITY

NSAIDS

COX INHIBITORS

NSAIDS & COX

INDICATIONS INHALED ANESTHETICS Halothane (hepatotoxic) Enflurane (convulsant) Isoflurane Sevoflurane Methoxyflurance (nephrotoxic) Nitrous oxide I.V. ANESTHETICS BARBITURATES Thiopental Sedative Anxiety Seizures Insomnia Porphyria Anesthesia induction Endoscopy (#1 Rx) Anxiety Spasticity Status epilepticus (diazepam) Detoxification (delerium tremens) Insomnia Anesthesia induction (thiopental) Short surgical procedures

MECHANISM OF ACTION Inhaled Lipid solubility = Potency = 1 / MAC Blood solubility = Rapid induction

SIDE EFFECTS / TOXICITY Heart depression Respiratory depression Nausea; Vomiting CNS blood flow Hepatotoxicity (halothane) Nephrotoxicity (methoxyflurane) Convulsant (enflurane)

Cl- channel open duration A Neuronal firing A GABAa facilitator Barbiturates DURATion of Cl- ch. Lipid solubility --> X-BBB Cl- channel open duration A Neuronal firing A GABAa facilitator

Dependence CNS depression w/ alcohol --> Death Cyt. P450 - Rx interactions

BENZODIAZEPINES (EPAMS) Short-Acting Triazolam Oxazepam Midazolam

Post-operative respiratory distress Amnesia Sedation Dependence CNS depression w/ alcohol --> Death Benzo's < Barb's in CNS depression ie respiratory depression Overdose Tx = Flumazenil

Flumazenil (overdose Tx) GABA-r (competitive antagonist)

OPIOID ANALGESICS Morphine Fentanyl

Anesthesia induction

Opioid-r Agonists mu = morphine delta = enkephalin Pain kappa = dynorphin Cough (dextromethorphan) Modulate synaptic transmission Diarrhea (loperamide; diphenoxylate) Acute pulmonary edema Withdrawal (methadone)

Addiction CNS depression Respiratory distress Pinpoint pupils Constipation Toxicity Antidote Naloxone Naltrexone Disorientation Hallucinations Bad dreams Less post-op S.E. than thiopental

KETAMINE PCP analog PROPOFOL

Dissociative anesthetic Cardiovascular stimulant CNS blood flow Anesthesia induction (RAPID) Short procedures Local pain numbing Na+ channels (via inner channel receptors) Minor surgical procedures A Action potential conduction Anesthetic + Epinephrine (v. const.) A Pain signal Spinal anesthesia A Small fibers > Large fibers A Myelanted > Unmyelinated Infected (acidic) tissue A Pain > Temp. > Touch > Pressure Charged anesthetics cannot X A More anesthetic needed 3' Amines penetrate membrane A Bind to channel-r's on inner side

LOCAL ANESTHETICS Esters Progaine Cocaine Tetracaine Amides Lidocaine Bupivacaine

Allergies to Esters A Give Amides CNS excitation Cardiovascular toxicity (bupivacaine) HTN Arrhythmias (cocaine)

Anesthetics

SIDE EFFECTS / TOXICITY

CNS depression w/ alcohol --> Death

CNS depression w/ alcohol --> Death Benzo's < Barb's in CNS depression

Cardiovascular toxicity (bupivacaine)

Anesthetics

MECHANISM OF ACTION PARKINSON'S Benz SLAB Dopamine Agonists Bromocriptine (partial DA agonist) Amantadine (DA release) L-Dopa / Carbidopa MAO Inhibitors Selegiline (selective MAO B inhibitor) Anti-Muscarinic Benztropine (improves tremors) MOTION SICKNESS Scopolamine

SIDE EFFECTS / TOXICITY

ENCEPHALOPATHY Lactulose Neomycin Growth of GI bacteria Ammonia forming bacteria in GI Ototoxicity Neurotoxicity Nephrotoxicity

COMA Airway (protect) Breathing (assist) Circulation (assist) Dextrose (and thiamine; Naloxone IV) DON'T Tx (in that order) Dextrose O2 Naloxone Thiamine Rule Out Infections Trauma Seizure Carbon Monoxoide Overdose / Opioids Metabolic disturbance Alcohol

CNS Rx

MECHANISM OF ACTION EYE EXAM (PUPIL DILATION) Atropine Homatropine Tropicamide GLAUCOMA "ABCD P" -Agonists Epinephrine Brimonidine -Blockers Timolol Betaxolol Carteolol Cholinomimetics Pilocarpine Carbachol Physostigmine Echothiophate Diuretics Acetazolamide Dorzalamide Brinzolamide Prostaglandins Latanoprost Outflow of aqueous humor Secretion of aqueous humor Anti-Muscarinic Anti-Muscarinic Anti-Muscarinic

SIDE EFFECTS / TOXICITY

Mydriasis + Stinging (epi) Closed-angle glaucoma (epi) No pupillary or vision changes (brimo) No pupillary or vision changes

Ciliary muscle contraction A Opening of trabecular meshwork A Outflow of aqueous humor HCO3- (via carbonic anhydrase) A Secretion of aqueous humor Outflow of aqueous humor

Miosis Cyclospasm

No pupillary or vision changes

Iris darkening (browning)

Eye Rx

MECHANISM OF ACTION CHF -Blockers Progression to CHF

SIDE EFFECTS / TOXICITY

ANGINA -Blockers HR; Contractility --> O2 demand

MI -Blockers HR; Contractility --> O2 demand

HTN -Blockers CO; Renin secretion

SVT -Blockers AV conduction velocity

Heart Rx

MECHANISM OF ACTION ASTHMA Isoproterenol Albuterol Salmeterol Theophylline Acute attack Long-acting Agonist (non-specific) A Relaxes bronchial smooth muscle 2 Agonist (acute attack) A Relaxes bronchial smooth muscle 2 Agonist (acute attack) A Relaxes bronchial smooth muscle Phosphodiesterase A Hydrolysis of cAMP A Bronchodilation Muscarinic (competitive antagonist) A Bronchoconstriction Release of Mast cell mediators Inactivates NF-B A Synthesis of Cytokines (TNF- & other cytokines) 5-Lipoxygenase A Arachidonic acid --> LKT's LKT-r's HR

SIDE EFFECTS / TOXICITY

Arrhythmia Tremor Narrow TI Cardiotoxicity Neurotoxicity

Ipratropium Cromolyn Corticosteroids Beclomethasone Prednisone Zileuton Zafirlukast Prophylaxis only

Rare S.E.

Lung Rx

MECHANISM OF ACTION CHRONIC HBV Immunolo-Tx IFN- (high dose) Nucleoside Analogs Lamivudine Adefovir Tenofovir Deoxyguanosine analog Entecavir Interfere before it's too LATE CHRONIC HCV Immunolo-Tx IFN- (high dose) Nucleoside Analogs Ribavirin PRIMARY BILIARY CIRRHOSIS Immunomodulator Methotrexate Biliary Product (Brown Bear) Ursodeoxycholic acid Cholchicine Antibiotics BindS membrane-R's A Viral replication; Prolif; Phago. Incorporates into viral DNA Priming; R-transcriptase; RNAse DNA polymerase; Chaperone

SIDE EFFECTS / TOXICITY

Adefovir = Renal tubular injury

BindS membrane-R's A Viral replication; Prolif; Phago. Enhances IFN; ??Mechanism

Folic Acid antagonist A DNA synthesis --> Apoptosis

Nausea; BM Suppression Hepatotoxic; Tx = Glucovorin to reverse

ASCITES Diuretics Furosemide Spironolactone Spontaneous Bacterial Peritonitis Cephalosporins Quinolones

VARICEAL BLEED Non-Selective -Blockers Propanolol Naldolol Nitrates Somatostatin Analogs Octreotide (#1 Emergency bleed Rx) Vasopressin Angiotensin II Inhibitors

Non-Selective -Blockers Splanchnic vasoconstriction Heart rate and CO Vasodilator Inhibits Serotonin, Gastrin, VIP release A Vasodilation A Splanchnic Constriction A Portal HTN

Indications Hypersensitivity; HypoTN Cardio shock, block, bradycardia Indications: Hypotension

GI Rx

MECHANISM OF ACTION ENDOMETRIOSIS Estrogen antagonists NSAIDS Danazol (Androgens) Oral contraceptives Mifepristone (anti-progestins) Aromatase Inhibitors E.C. Matrix Modulators Immunotherapy WILSON'S DISEASE Copper Chelators D-PCN Trientine Copper Absorption Reducers Zinc Acetate Tetrathiomolybdate Trientine Weaker chelator of copper? Zinc Acetate E'cytes metallothionein production Binds Copper > Zinc A Traps copper inside enterocytes Enterocyte sloughing A Copper eliminated in stools Does not chelate copper from tissues

SIDE EFFECTS / TOXICITY

D-PCN Hypersensitivity; Rash Proteinuria Blood dyscrasias Anorexia; Nausea; Vomiting Trientine Less SE's than D-PCN Zinc Acetate Well-tolerated Non-specific epigastric irritation Pancreatitis Hot flashes Atrophy of Vagina Osteroporosis CAD HAVOC

MENOPAUSE Estrogen GnRH FSH; LH

estrogen production w/ Ovarian follicles with age Age of onset = 51 yrs old Early onset in smokers

DIABETES INSULIN To Tx DM K+ (life-threatening) GLU SULFONYLUREAS To Tx DM II (NIDDM) So fun you'll race a Car (hyperglycemic) Chlorpropamide Chlar pool Glyburide Glide your ride Glipizide Glip the side [of the] Tolbutamide Toll booth METFORMIN To Tx GLU Oral Biguanide "Metformin = Stops GLU Formin' " GLITAZONES DM II MonoTx Combo+Above Rx's Pioglitazone Rosiglitazone Troglitazone -GLUCOSIDASE INHIBITORS Acarbose Miglitol DM II MonoTx Combo+Above Rx's Targe cell response to insulin Hepatotoxic (troglitazone) Weight gain Binds Insulin-R (liver; muscle; adipose) GLU A Tyrosine Kinase activity Allergy (rare) A GLU --> Glycogen (Liver) A Synthesis of glycogen + protein (Muscle) A Tryglyceride storage (Fat) Close K+ channels in -cell membrane A Cell depolarization A Ca2+ influx A Insulin release stimulated Ca2+ / Car release GLU Disulfiram-like effects Glyburide; Glipizide

??Unknown?? Gluconeogenesis (liver) A GLU levels

Lactic acidosis

Glitazone = Lit a zone up (sensitivity) Inestinal brush border -glucosidase A Sugar hydrolysis and absorption A GLU serum levels (post-prandial)

Glitazone = Glutton zone --> Wt. Gain!

GI Disturbances

DIABETIC Rx's

Endocrine Rx

MECHANISM OF ACTION GOUT Colchicine Indomethacin (more common) Probenecid Allopurinol Acute Gout Acute Gout Chronic Gout Chronic Gout Depolymerizes microtubules A Lk'cyte chemotaxis & degranulation Absorption of uric acid PCN secretion Xanthing oxidase A Xanthine --> uric acid

SIDE EFFECTS / TOXICITY GI Indomethacin < toxic

CT Dz Rx's

MECHANISM OF ACTION TUBERCULOSIS Rifampin Isoniazid Pyrazinamide Ethambutol Streptomycin Cyclosporine (2nd line Tx) Tx TB before it's RIPE RESPIre BACTERIAL PROPHYLAXIS Meningococcal Gonorrhea Syphilis Recurrent UTI's PCP Combo Tx: RESPIre Prophylaxis Isoniazid - INH used alone

SIDE EFFECTS / TOXICITY Hepatotoxicity (all Rx's)

Rifampin (1st line); Minocycline Ceftriaxone Benzathine PCN G TMP/SMX TMP/SMX (1st line); Pentamidine

HIV Tx - 2Nucleosides + 1Protease Rx initiated at low CD4+ Count < 500 or high viral load Protease Inhibitors Protease enzymes Ritonavir A Viral assembly Amprenavir "When it RAINS it pro's" Indinavir Nelfinavir Saquinavir Reverse Transcriptase Inhibitors Reverser transcriptase Nevirapine A HIV incorporation into host DNA Zidovudine (AZT) "Nevir Efa Delete!" Zalcitabine (ddC) A Non-nucleoside Stavudine (d4T) Abacavir "Get N ZZ (in the) SADDLE and ride reverse" Didanosine (ddI) Delavirdine Lamivudine (3TC) Efavirenz INFLUENZA A VIRUS Amantadine Zanamivir Zany Man fights A Flu CMV CMV = EFG Foscarnet Ganciclovir HSV Target = Viral DNA Polymerase Common in normal and compromised Herpes Simplex Virus (HSV) Varicella Zoster Virus (VZV) Common in immunocompromised Cytomegalovirus (CMV) Key to Abbreviations TK = Thimadine Kinase P-ase = Polymerase RT = Reverse Transcriptase

Nausea; Diarrhea Hyperglycemia Lipid abnormalities Thrombocytopenia (Indinavir) BM Suppression: Neutropenia; Anemia Peripheral neuropathy Lactic acidosis (nucleosides) Rash (non-nucleosides) Megablastic anemia (AZT)

RETROVIRUSES Nucleoside Analogues Cornerstone of 3X Tx for HIV Guidelines Use > 3 drugs against virus Start and stop all drugs at same time Evaluate risk/benefit Simpler regimen = better adherence Nucleoside analogue Target = Viral RT Nucelotide RT inhibitor Target = Viral RT Non-Nucleoside RT Inhibitor (NNRTI) Target = Viral RT Protease Inhibitor Target = Viral Protease Entry Inhibitor Target = Viral Entry

NRTI's Lactic acidosis Severe hepatomegaly with steatosis A May be fatal

Resistance Base-pair mutations in RT

Infectious Dz Rx

SIDE EFFECTS / TOXICITY

CNS Rx

SIDE EFFECTS / TOXICITY

Eye Rx

SIDE EFFECTS / TOXICITY

Heart Rx

SIDE EFFECTS / TOXICITY

Lung Rx

SIDE EFFECTS / TOXICITY

GI Rx

SIDE EFFECTS / TOXICITY

Glitazone = Glutton zone --> Wt. Gain!

DIABETIC Rx's

Endocrine Rx

SIDE EFFECTS / TOXICITY

CT Dz Rx's

SIDE EFFECTS / TOXICITY

Infectious Dz Rx

TETANUS - DTP Clostridium tetani

MECHANISM OF ACTION Vaccine = toxoid treated w/ formaldehyde A Altered virulence Unaltered immunogenicity A 100% effective

DOSAGE Infancy 3 Doses W/ Diphtheria and Pertussis Booster every 10 yrs Wound / Trauma Passive Ab's Active Vaccine

SIDE EFFECTS / TOXICITY Rare Pre-exposed adults A Allergic reaction

DIPHTHERIA - DTP Corynebacterium diphtheriae

Toxoid vaccine DT = Kids dT = Adults (less toxins) DTP > 1 killed bacteria Impure DTaP > 1 purified Ag's of B pertussis P toxoid Filamentous hemagglutinin, etc. Better

Infancy Given with Tetatnus and Pertussis Booster every 10 yrs > 6 mo's 1% mortality < 6mo's of age Given with Tetatnus and Pertussis Recommended > 6 yrs

Toxicity minimal for infants Reactions at injection site (older kids)

PERTUSSIS - DTP Bordetella pertussis Highly contagious

Febrile & local reactions (mild) High fever Convulsions Encephalopathy Serious reactions (DTP) Milder reactions (DTaP)

H. FLU VACCINE Type B (Hib) A Bacterial meningitis

Ab of Hib cap. polysacch. (> 2 yrs old) A Purified PRP A T-L'cyte activation (age limited) > 18-24 months of age A Ab production Conjugate Vaccine (Infants) A PRP conugated to protein carrier A Creates T-L'cyte dependent Ag's that infant can make Ab's to

Purified PRP = > 2 yrs old Conjugate = 2 mo's old

STREP PNEUMONIA #1 cause of bacterial infections Bacteremia URTI Meningitis Pneumonia Bronchitis Otitis media Sinusitis POLIOMYELITIS Poliovirus

CPS's (multivalent) (> 2yrs old) A Purified CPS's of 23 types (~95%) T-independent Ag's ineffective <2yrs old Elderly > 65yrs old; Immunocomp. Underlying Dz Protein-CPS Conjugate (Infants) A 7 valent with 80% serotype coverage A Immunogenic in infants

CPS's (multivalent) (> 2yrs old)

Protein-CPS Conjugate (Infants)

OPV (oral live-attenuated) 3 serotypes 4 dose schedule

OPV (oral live-attenuated) 4 dose schedule Herd immunity

IPV (parenteral, killed) 3 serotypes 4 dose schedule

IPV (parenteral, killed) 4 dose schedule

Vaccines

SIDE EFFECTS / TOXICITY

Reactions at injection site (older kids)

Vaccines

ACTION Anterior Pituitary Releasing Hormones GnRH GHRH LHRH TRH CRH Stimulating Hormones ACTH (cosyntropin) ACTH (corticotropin) FSH TSH hCG HMG Target Hormones GH Somatostatin Somatotropin Prolactin Posterior Pituitary Vasopressin Agonists Vasopressin (ADH) Desmopresssin (DDAVP) Vasopressin Antagonists Oxytocin Dopamine Agonists Bromocriptine Cabergoline

DISEASE

LH, FSH --> Est, Prog, Test GH (G; cAMP) LH --> Prog, Test TSH; Prl ACTH

Hypothalamus; Replacement Tx GH Deficiency

GH Deficiency; RF; Turner; PW Pituitary Dz - Acromegaly

V1 Agonist V2 Agonist Uterine cont.; Milk eject Binds D2-r --> Blocks Prl Binds D2-r --> Blocks Prl

Hypo-TN; Septic shock; GI Bleed DI; Bed wetting; Hemophliacs

Prolactinoma Prolactinoma

Thyroid Thyroxine (T4) Triiodothyronine (T3) Iodide PTU (Propylthiouracil) Parathryroid Hypo-Ca2+ Ca2+ Gluc/Lac/Citrate Thiazied Diuretic Mg2+ Drisdol Dihydrotachysterol (DHT) Calciferol Calcitriol Hydroxyapatite PTH (teriparatide)

Thyroid peroxidase --> T4-->T3 Hyperthyroidism

Ca2+ Supplement Ca2+ Sparing diuretic Mg2+ Supplement Vit D2 Supplement Vitamin D analog Vitamin D analog: 1,25-OHD Vitamin D analog

Osteoporosis Calcitonin (salmon) Alendronate Risedronate Raloxifene Estradiol Paget's Dz Alendronate Risedronate Pamidronate Mithramycin (Caution!) Tiludronate Osteomalacia Vit D (1,25 OHD or DHT) Ca2+ Supplements Phosphate Supplements

Aminobisphosphonate Aminobisphosphonate Selective Estrogen-R Mod.

Bisphosphonate; Resorption Bisphosphonate; Resorption Bisphosphonate; Resorption Bisphosphonate; Resorption Bisphosphonate; Resorption

Pancreas Fast Lispro Aspart IGF-1 Regular Zinc Insulin (Regular) Insulin Zinc Suspension Intermediate Lente Insulin Long Glargine Slow Ultralente insulin Glimepiride Glipizide Glyburide NPH Acarbose Metformin Repaglinide Rosiglitazone Semilente Insulin Tolbutamide

Adrenal Cortex Corticosteroids Hydrocortisone Cortisone Cortisol Prednisone Prednisolone Dexamethasone Mineral Corticoid Fludrocortisone Aldosterone Steroid Genesis Mitotane Ketoconazole Aminoglutethimide Metyrapone Trilostane Kidney Dexomethazone Octreotide K+ Sparing Diuretic Amiloride Spironolactone

Adrenal I; Surgery; Inflammation Short Short Intermediate Intermediate Long 10X Cortisol!! Cushings Adrenotoxic --> Enzymes Multiple enzymes Multiple enzymes 11--hydroxylase 3--Hydroxysteroid dehyd.

TEST: CAH; Adrenal Dz

Suppresses ACTH

1' ALD

Na+ reabsorption in DT / CD 1' ALD p450; ALD-r; Androgen-r 1' ALD; Androgenism

Gonads Testolactone Testosterone Estradiol Ethinyl Estradiol Norgestrel Progesterone Fluoxymesterone Medroxyprogesterone Mestranol Male Dev't Hormones MIS Testosterone Dihydrotestosterone

Anti-mullerian hormone Testicular descent; Wolff duct dev't

S.E. / CONTRA-INDIC.

Suppression Test

Insulin Resistance

Neoplasia; DM; Carpel T

Insulin Resistance

Cardio; CVA; Short t1/2

Anterior Pituitary

Upper GI Sx's Acute phase reaction Caution!

Soft tissue Ca2+

Thyroid / Parathyroid

Unpredictable

Pancreas

Adrenal Insuff; O-Porosis; GH

GI; Neuro; Severe!! GI; Hepatic dysfunction Neuro; Fever; Rash GI; HTN; Acne; Hirsutism GI; Parasthesias

2' Adrenal insufficiency

K+ Gynecomastia; K+

Adrenal Cortex / Kidney

Insulin Resistance

Gonads

ANTIBIOTICS - SITES OF ACTION

Antibacterial Tree

ANTIBIOTICS - SITES OF ACTION

Antibiotics

ANTIVIRALS - SITES OF ACTION

Antivirals

Antibacterial Tree

Antibiotics

Antivirals

INDICATIONS

MECHANISM OF ACTION

SIDE EFFECTS / TOXICITY

TEMPLATE

SIDE EFFECTS / TOXICITY

TEMPLATE