INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY

BETHANECHOL Ileus (Post-op / Neuro) Cholinergic Agonist

Urinary Retention (Post-op / Neuro) Activates bowel + bladder smooth muscle
"Bet you it's In the colin (retention)"

CARBACHOL Glaucoma Cholinergic Agonist

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

NEOSTIGMINE Myesthenia gravis Carbamylation of Anticholinesterase

Oral; Injection Ileus (Post-op / Neuro) $ ≠ACh -Esterase
Urinary Retention (Post-op / Neuro) $ ↑Ach (endogenous)
Antidote - NMJ blockade
PYRIDOSTIGMINE Myesthenia gravis Carbamylation of Anticholinesterase
Oral $ ≠ACh -Esterase
Injection $ ↑Ach (endogenous)
$ ↑Strength
EDROPHONIUM Dx of Myesthenia gravis Anticholinesterase / Cholinesterase inhibitor
ie v. short acting $ ↑Ach (endogenous)

PHYSOSTIGMINE Glaucoma (crosses BBB) Anticholinesterase / Cholinesterase inhibitor

Eye drops Atropine overdose $ ↑Ach (endogenous)
Ointment
Physo for my Eyes, Oh! "Eyes are 'fizzing' from pressure"

ECHOTHIOPHATE Glaucoma Anticholinesterase / Cholinesterase inhibitor

"Echothio = Echo in my eye, Oh!" Esotropia (X-eyed) $ ↑Ach (endogenous)
Demelarium
Isoflurophate INDIRECT AGONISTS

PRALIDOXIME Antidote - ACh-Esterase Toxicity ACh-Esterase Regenerator

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

ATROPINE Salivation Muscarinic Antagonist Red as a beat - ↑Temperature; Pulse

Lacrimation Dilate pupil Hot as a hare - ↑Temperature; Pulse
"A troop blocking SLUD" Urination ↓Secretions (Acid; Airway) Dry as a bone - Dry mouth / Flushed
Mad as a hatter; Hot as a hare Defecation ↓GI Motility Mad as a hatter - Disorientation
Dry as a bone; Blind as a bat Tx organophosphate poisoning Blind as a bat - Cycloplegia; Mydriasis

HEXAMETHONIUM Nicotinic Antagonist

Ganglionic blocker
ANTIMUSCARINICS - R-BLOCK

BENZTROPINE Parkinson's Anti-Muscarinic

"Park the Benz - Slowly and smoothly" Tx Sx's of Reserpine; Haloperidol Anti-Dyskinetic (↓Stiffness)

SCOPOLAMINE Motion Sickness Anti-Muscarinic

Pupil Dilator
ANTIMUSCARINICS - CNS

HOMATROPINE Pupil Dilator Anti-Muscarinic Mydriasis

Uveitis Cycloplegia
Post-synechiae (iris sticks to cornea)
TROPICAMIDE Pupil Dilator Anti-Muscarinic Mydriasis
Eye drops Uveitis Cycloplegia
Ointment Post-synechiae (iris sticks to cornea) ANTIMUSCARINICS - EYE

IPRATROPIUM Asthma Anti-Muscarinic

Inhalant COPD Bronchodilator
ANTIMUSCARINICS - LUNG

Cholinergics
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
SUCCINYLCHOLINE Muscle paralysis in: Neuromuscular blockade (depolarizing)
Surgery Phase I - Prolonged depolarization
It "sucks" to be paralyzed Mechanical ventilation Antidote = None
Phase II - Repolarized, but blocked
Antidote = Neostigmine

X-CUR-X Muscle paralysis in: Neuromuscular blockade (non-depolarizing)

Surgery Antidote = Neostigmine; Edrophonium
Tubocurarine Mechanical ventilation Pyridostigmine
Atracurium
Mivacurium
Pancuronium
Vecuronium
Rapacuronium
NEUROMUSCULAR BLOCKADE

DANTROLENE Halothane + Succinylcholine ≠Ca2+ release from SR of skeletal muscle

$ Malignant hyperthermia
"Gets Dan to Lean (relax from rigidity)" Antipsychotic Rx (Phenothiazines)
$ Neuroleptic Malignant Syndrome

NM Blockade
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
EPINEPHRINE Anaphylaxis Agonist (direct)
Asthma α1; α2; β1; β2
Epidemic: It gets all the receptors Hypotension
Glaucoma (open angle)
NOREPINEPHRINE Hypotension Agonist (direct) ↓Renal perfusion
α1; α2; β1
Near-Epidemic: Almost gets all receptors
But it be too (β2) weak

ISOPROTERENOL AV Block (rare use) Agonist (direct)

β1 = β2
Iso = Equal; Erenol = β Agonist ≈No α effects

DOPAMINE Shock (DA --> ↑Renal perfusion) Agonist (direct)

Heart failure D1 = D2; > β > α
DOPA = DDβα

DOBUTAMINE Shock Agonist (direct)

Heart failure β2 > β1
X-BU-X = β2 > β1
CATECHOLAMINES

AMPHETAMINE ADD Agonist (indirect)

Obesity Releases stored catecholamines
Aderol Narcolepsy $ α1; α2; β1; β2

EPHEDRINE Nasal Congestion Agonist (indirect)

Urinary incontinence Releases stored catecholamines
Eep! Head run Hypotension $ α1; α2; β1; β2
Head run = head:snot; dick:urine $ Constricts (no fluid flow)
Pseudophed CATECHOLAMINES

PHENYLEPHRINE Hypotension Agonist (direct)

Nasal Congestion α1 > α2
≈NE Eye exam (Pupil dilator)
α AGONIST

ALBUTEROL Asthma Agonist (direct)

TERBUTALINE β2 > β1

X-BU-X = β2 > β1
β AGONIST

COCAINE Local anesthesia ≠Re-Uptake of Chatecholamine Vasoconstriction

$ Agonist (indirect) Tachycardia; Arrhythmias

CLONIDINE α Agonist (central)

α-METHYLDOPA
$ ↓Central adrenergic outflow
"Clones NE" (fakes presynaptic-R's)
OTHER

α1 B.V. Vasoconstriction

α2 B.V. Vasoconstriction

Pre-Synaptic ≠NE Release - (-) Feedback

β1 Heart ↑HR

β2 Bronchial Bronchodilation
Smooth M.

Skeletal M. ??
Arterioles

Sympathomimetics
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
PHENOXYBENZAMINE Pheochromocytoma - HTN Non-Selective Blocker Irreversible
α Irreversible Orthostatic Hypo-TN
"Pheno = Pheo" Reflex tachycardia

PHENTOLAMINE Pheochromocytoma - HTN Non-Selective Blocker Reversible

α Reversible Orthostatic Hypo-TN
"Phento = Pheo" Reflex tachycardia

X-ZOSINS HTN α1-Selective Blocker 1st-Dose Orthostatic Hypo-TN

BPH urinary retention Dizziness
Zosin - Sauce In; HTN Headache

Prazosin
Terazosin
Doxazosin

YOHIMBINE Impotence (controversial) α2-Selective Blocker Arrhythmias (no (-) feedback)

α-BLOCKERS

β-BLOCKERS (X-OLOL) HTN ↓CO; ↓Renin secretion Impotence

Angina pectoris ↓HR; ↓Contractility --> ↓O2 demand Asthma exacerbation
Non-Selective Blockers MI ↓HR; ↓Contractility --> ↓O2 demand; ↓Death Bradycardia; AV block; CHF
Propranolol SVT (propranolol; esmolol) ↓AV conduction velocity CNS: Sedation; ∆Sleep; ≠Diabetics
Pindolol CHF ↓Progression to CHF
Timolol Glaucoma ↓Secretion of aqueous humor
Nadolol
Labetalol

β1-Selective Blockers
Atenolol
Betaxolol "A BEAM of β1's"
Esmolol
Acebutolol
Metoprolol
β-BLOCKERS

Sympathetic Blockers
≠CNS
Li
Vasopressin (HTN)
Aminoglutethimide
Trilostane (paresthesia)
Mitotane
≠Heart
Li
Vasopressin (HTN)
TH Agonists
Metyrapone (HTN)
Metformin
TZD
≠Lung
β Blockers
≠Liver
PTU
Ketoconazole
SU's (amide; uride; izide; iride)
TZD (troglitazones)

≠Chol
Methimazole
S'statin (g-stone)
≠GI
Somatostatin
Ketoconazole
Metyrapone
Tilostane
Mitotane
α-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
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
PENICILLINS PCN G = Strep pneumonia Bactericidal Hypersensitivity Rash
PCN V = Grp A Strep (pharyngitis) Rx enters bacteria through porin Anaphylaxis
PCN G (IV Form; Acid labile) Spirochetes (syphilis) $ 1) Activates autolytic enzymes Hemolytic Anemia; Neutropenia
1/2 Life = 30 minutes $ 2) Inhibits transpeptidase (PBP)
PCN V (oral; Acid stabile) $ No cross-linkage of cell wall Widespread PCN Resistance:
$ 3) Inhibits cell wall synthesis β-lactamase cleavage of ring
$ Osmotic lysis of bacteria
PCNase-RESISTANT PCN's Staph aureus Inhibits cell wall synthesis Methicillin = I.S. nephritis
Sepsis; IE; Cellulitis = Nastycillin Meth Messes w/ Neph
Nafcillin (I.V.) Nasty
Methicillin (I.V.) Methy (messy) Nasty Messy Ox
Oxacillin (Oral; I.V.) Ox Clocks Staph aureus
Dicloxacillin (Oral) Clocks SA Knocks it out!!

AMINO-PCN's Gram(+) - All Inhibits cell wall synthesis Hypersensitivity Rash (Ampicillin)
Gram(-) Rods Colitis (Ampy-crampy; Colicky-amoxy)
Amoxicillin + Clavulanic acid Bronchitis; Sinusitis
Ampicillin + Clavulanic acid UTI's Clavulanic Acid --> Diarrhea

CA competitively inhibits β-lactamase HELPS kill entero's

H Flu; E. Coli; List.; Prot.; Salm.
TICARCILLIN Pseudomonas auruginosa Inhibits cell wall synthesis Hypersensitivity Rash
PIPERACILLIN Gram(-) Rods
CARBINICILLIN Clavulanic Acid --> Diarrhea
Totally pseudo, dude.
"Toke the Pipe and Carb" + hit of Acid!
Add Clavulanic acid

CEPHALOSPORINS Inhibits cell wall synthesis Hypersensitivity Rash

1st Generation Granulocytopenia
1st Generation Proteus I.S. Nephritis
Cephalexin Alex is in E. coli
Cephalothin Alice is in Klebsiella Fn Group
Cefazolin Us all in 2nd Generation ≠A-glycosides + Cephalosporin
2nd Generation H. Flu Proteus
Cefuroxime Fur ox Enterobacter E. coli β-Lactamase Resistance:
Cefotetan Teets [use an] Neisseria Klebsiella Cuts here β-lactamase cleavage of ring
Cefoxitin Ox tin Serratia MRSA
3rd Generation 3rd Generation Enterococci
Ceftriaxone (oral) - AX 'em!! X-BBB - Bacterial Meningitis
Cefotaxime - TAX 'em!! Gram(-) serious infections
Ceftazidime - TAZ 'em!! Gonorrhea (ceftriaxone)
Cefoperazone - Opera will kill too!! 1st = Pro Colie Klub
4th Generation 4th Generation 2nd = Pro Colie Klub+Sarra, Homo, Nice Aunt
Cefepine Pseudomonas & Gram(+) 3rd = Serious bunch
4th = Pseudo

MONOBACTAMS Only Aerobic GNR's Inhibits cell wall synthesis Non-toxic (usually)
Klebsiella GI Sx's (occasional)
Aztreonam P. auruginosa
Serratia Peaceful Tree: Ok w/ Aminoglycosides
β-Lactamase resistant Non-toxic (usually)
Synergistic with Aminoglycosides Aerobic (GNR's)

CARBAPENEMS Everything!!! Inhibits cell wall synthesis Seizures

Skin rash
Imipenem + Cilastatin I'm A Pen = X all bugs out Cilistatin - ≠Dihydropeptidase GI distress
Hydrolized by Dihydropeptidase Dihydropeptidase (renal enzyme)
Cilastatin inhibits above enzyme Most powerful bug drug out there $ Metabolizes and inactivates imipenem
Meropenem
Not hydrolized by Dihydropeptidase

β-Lactamase resistant

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

Cell Wall Inhibitors

 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
AMINOGLYCOSIDES Aerobic GNR's (severe) Bactericidal Nephrotoxic
Aerobes! (amine-O2-glycosides) O2 Required for uptake (aerobic orgs) Ototoxic
"G-TANKS" w/ 30-ott Ammo Aerobic organism produces metabs' Teratogen
Amp-Gent Combo Tx!! $ Alters membrane potential
Gentomycin $ Allows uptake of Rx Grenade goes off
Tobramycin $ Rx binds to 30S Ribosome $ Deaf
Amikacin $ ≠Protein synthesis Hits kidney
Netilmicin Ineffective Blocks initiation
Kanamycin Anaerobes Misreading Resistance:
Streptomycin Streptoccoci Early termination Modification of:
H. Flu Acetylation
Neomycin (topical; not well-absorbed) Syphilis Adenylation
Syngergistic with β-Lactams Phosphorylation
The American Gent, Toby
Strips "Neti" in the Kan

TETRACYCLINES Tet Offensive Dz's Bacteriostatic Deposited in growing bones

STD's - Chlamydia; Ureaplasma Binds 30S Ribosome subunit $ Stains teeth gray-brown to yellow
Minocycline Malaria - P. falciparum (doxy) $ Inhibits protein synthesis Inhibits bone growth in children
Doxycycline (take w/ food; fecal elim Tick-borne - Rickettsia; Lyme $ ≠Aminoacyl-tRNA attachment
Demeclocyline Diarrhea - Vibrio cholera Fanconi syndrome when expired
Tetracyclines Acne Don't Take With
Bio-Rx - B. anthracis Milk Photosensitivity
"Mine Doxy Demands 4 Tetes" (pups) Ellas - Pasteurella, etc. Antacids
$ Takes care of multiple diseases Fe2+ containing substances Think of newborn pups
No Milk! Sharp gray-brown teeth
Shut eyes (photosensitive)

Resistance:
↓Uptake
↑Export

MACROLIDES Gram (+) Cocci Bacteriostatic Eosinophilia

Streptoccoci Binds 50S (23S rRNA)
Azithromycin Px's w/ ≠PCN $ Inhibits protein synthesis GI
Clarithromycin Mycoplasma (#1 for CAP) Nausea; Vomiting; Ab cramps
Erythromycin Legionella (#1) 50c Big Mac Metallic taste (Clarithromycin)
Dirithromycin Chlamydia Cholestatic hepatitis (Erythromycin)
Neisseria Eat a Big Mac
"Big Mac ACED his women" $ GI upset + cholestatic hep
Panting = lung infection CAP Etiology Cardiac
Thrusting = STD's Mycoplasma Arrhythmia (E'mycin + Terf)
Strep pneumonia
Chlamydia Resistance:
Methylation of rRNA

CHLORAMPHENICOL Meningitis Bacteriostatic BM toxicity

H. Flu Binds 50S peptidyl transferase Anemia (reversible)
"Clears a meningitis Call" N. meningitis $ Inhibits peptide bond formation Aplastic anemia (irreversible)
S. pneumonia $ Inhibits protein synthesis Pancytopenia
Only as alternative to: Anaerobes Gray Baby Syndrome
PCN's Bacteroides fragilis ΦGlucuronidation
Cephalosporins (3rd gen) Death
Tetracycline in pregnancy Resistance:
Modification of acetylation

CLINDAMYCIN Anaerobes Bacteriostatic GI

Clostridium Binds 50S ribosomal subunit Causes Pseudomembranous C.
Cleans my sin[ister anaerobes] Bacteroides $ Inhibits peptide bond formation Fever
Gunshot $ Inhibits protein synthesis P. colitis
Clindamycin = ↑Diaphragm ≠O2 bugs Aminoglycosides
Metronidazole = ↓Diaphragm ≠O2 bugs Clindamycin 50c for Linda Resistance
Aspiration pneumonia Methylated rRNA -->no Rx binding

STREPTOGRAMMINS Streptococci Bacteriostatic Myalgias

Staphylococci Binds 50S Ribosome subunit Arthralgias
Dalfopristin (Streptogrammin A) Enterococcus faecium (bact-static) $ Inhibits protein synthesis Phlebitis
Quinupristin (Streptogrammin B) Not E. Faecalis
Bacteriocidal Resistance
Strep A = Near site of Microlides Methylated rRNA -->no Rx binding
Strep B = Overlaps with Microlides
$ Used together = synergistic
$ Bacteriocidal

RNA Inhibitors
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
SULFANOMIDES - SMX TMP-S[MX] Bacteriostatic Displaces protein-bound Rx's (Warfarin
Tree (respiratory) ≠Dihydropteroate Synthase S.E. = Rare (common w/ AIDS Px's)
Rotten eggs (oral) Mouth - GI tract $ ≠Folate synthesis Hypersensitivity
Porto-Potty (urinary excretion) Pee - UTI; Urethritis; Prostatitis $ ≠Purine synthesis (bacterial) Nephrotoxicity; Kernicterus (infants)
Syndrome Dz's - Toxo; PCP; I. Bella $ ≠DNA synthesis (bacterial) Hemolysis (if G6PD deficiency)
$ ≠Growth Blood / WBC abnormalities
All Bacteria
Nocardia Sulfanamide Resistance
Chlamydia Altered target (plasmid-mediated)
Malaria ↓Uptake: Impermeability to Rx
Burns (silver sulfadiazine) ↑PABA synthesis
UTI's
PABA antimetabolite

TRIMETHOPRIM - TMP TMP-S[MX] Bacteriostatic BM Suppression

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

FLUOROQUINOLONES Aerobic GNR's Bactericidal S.E.'s Uncommon - Rare

UTI's ≠DNA gyrase (Topoisomerase II)
Quinolone Pseudomonas - Cipro $ Inhibits DNA synthesis Tendonitis & Tendon ruptures
Nalidixic acid Neisseria Fluoroquinolones hurts
Fluoroquinolones ≈Gram (+) Olfs are Gyrating (dancing) so much they Attachments to your bones
Ciprofloxacin To See Pro Hurt their tendons
Sparfloxacin Sparing Headache; Dizzy GI Upset
Mortifloxacin Mortifies GI Upset Headaches; Dizziness
Enoxacin Enough Superinfections
Ofloxacin Olfs of the Rash
Norfloxacin North
Gatifloxacin Gate
Fluoroquinolone Resistance
Mutation --> DNA gyrase / T.I.

METRONIDAZOLE Anaerobes Bactericidal ≠Alcohol!

Bacteroides fragilis Forms toxic metabolites in cell wall $ Disulfiram-like reaction with alcohol
Clindamycin = ↑Diaphragm ≠O2 bugs Clostridium difficile $ Alters cell membrane e-potential Headache
Metronidazole = ↓Diaphragm ≠O2 bugs Protozoa
Giardia (flagellate) Kills bugs in GI tract lumen On the metro:
Entamoeba No drinking alcohol!
Gardnerella vaginalis Metallic taste (of train water)
Trichomonas (flagellate) GI Upset (from motion)

Gee your aunt's guard tricked me

to get on the metro
3X Tx (H, pylori)
Metro + Amoxicillin + Bismuth
Tetracycline + PPI + Bismuth

POLYMIXINS / POLYPEPTIDES Resistant Gram (-) Cationic, basic proteins Neurotoxicity

$ Act like detergents Acute renal tubular necrosis
Polymixin B $ Bind to cell membrane
Colistin
Polymixin E $ Disrupt osmotic integrity Polymixin Resistance
Proteus
Serratia
Impermeable cell walls
$ Rx cannot reach target

MISC. ANTIBIOTICS
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
ISONIAZID - INH TB ↓Mycolic acid synthesis Neurotoxicity (Tx = Pyridoxine [B6])
Solo prophylaxis Hepatotoxicity
SLE-like syndrome
Hemolysis (if G6PD)

INH = Injures Neurons and Hepatocytes

RIFAMPIN M. TB; M. avian ≠DNA-dependent RNA polymerase Hepatotoxic (P450)

Leprosy
4 R's
RNA polymerase inhibitor Always used in combo with other Rx's
Revs up microsomal P450
Red/orange body fluids Meningococcal prophylaxis
Resistance (rapid) if used alone H. Flu B prophylaxis

TB DRUGS
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
BACTERIAL PROPHYLAXIS

Rifampin (1st line); Minocycline Meningococcal

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

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 MRSA; Staph; Enteros

Ampicillin Enteros
Imipenem Enteros

Tough Bug Drugs

 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
AMPHOTERICIN B Systemic Mycoses Binds to membrane ergosterols >> Chol. "Ampho-terrible"
Cryptococcus $ Forms pore in fungal cell membrane Fever; Chills = Shake & Bake (44%)
I.V. Blastomyces $ ↑Permeability & leakage of e'lytes Nausea; Vomiting; Ab. pain; Anorexia
Not absorbed IM or orally Coccidioides $ ≠Homeostasis Phlebitis (common)
≠Cross BBB Aspergillus $ Cell death Heparin controls this S.E.
t1/2 = 1 day Histoplasma Anemia (common)
Intrathecal Candida albicans "AmphoTears holes in membranes" Nephrotoxicity (common)
Fungal meningites (rare) Mucor mycoses Monitor K+, Mg++, BUN, CRE, A-B
↓K+emia

NYSTATIN Oral Candidiasis Binds to membrane ergosterols >> Chol.

$ Forms pore in fungal cell membrane
Swish and swallow $ ↑Permeability
$ ≠Homeostasis
$ Cell death

IMIDAZOLE DERIVATIVES #1 Itraconazole > Ketocanazole C14 demethylase inhibitors (via P450) Hormone synthesis inhibition
Blastomycoses $ ≠ Ergosterol & FA synthesis in wall $ Gynecomastia (Keto)
Itraconazole Cociidioides $ ↑Permeability & leakage of e'lytes Liver dysfunction (via ≠P450)
Ketocanazole (No Amp B!) Histoplasma $ ≠Homeostasis Fever; Chills
Fluconazole (X-BBB) Candidiasis (mucocutaneous) $ Cell death Nausea; Anorexia
Clotrimazole Hypercortisolism
Voriconazole Fluconazole Combo Tx - Anti-HA
Miconazole (topical) Cryptococcal meningitis (L. term) $ Q-T interval prolongation
Crypto prophylaxis (AIDS) $ Torsade de Pointes
Candida albicans Voriconazole
H2 acids or antacids ↓absorption Voriconazole / Itraconazole Visual disturbances (30min after Tx)
Liver metabolism Aspergillosis!! $ Warn Px's if driving,etc.
Clotrimazole / Miconazole
Dermatophytosis Resistance
Related to efflux pump

GRISEOFULVIN Superficial infections ≠Microtubule function Deposits in kertin-containing tissues

Dermatophytes $ ≠Mitosis Teratogenic / Carcinogenic
Oral Tx Tinea CNS: Headaches; Confusion
Ringworm ↑Warfarin metabolism
Grizzlies are full of ringworm & tinea Grizzlies interfere with might! (mitosis)

CASPOFUNGIN Aspergillosis Inhibits Beta(1-3) glucan synthesis Well-tolerated

In amphotericin intolerant Px's $ Fungal cell wall disruption HA release possible
IV only Candidiasis
↓Renal excretion Disseminated
↓Liver metabolism
No P450
Highly protein bound
5-FLUORO-CYTOSINE - 5-FC Chromomycosis RX entry into yeast cell (cytosine permease) BM suppression (#1 problem)
Candida $ 5-FC --> 5-FU (via cytosine deaminase) Diarrhea (10%)
Combo Tx (mostly) Aspergillosis $ 5-FU inhibits transcription of RNA Watch renal failure Px's
5-FC + Ampho B Cryptococcal $ Blocks tymidylate synthetase
$ Stops DNA synthesis Resistance
Loss of permease or deaminase
Crypto

Anti-Fungal Rx's
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
IVERMECTIN Onchocerciasis (River blindness) Kills microfilariae
Black flies ≠Microfilariae from leaving uteri of worms
"rIVER blindness" $ Fibrous nodules
"rIVER es muy ancho" $ Lizard skin

MEBENDAZOLE Nematode / Roundworm Paralyzes worm

THIOBENDAZOLE Whipworm $ Passes out stool
Pinworm
"Bendy, like worms"

PYRANTEL PAMOATE 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 Broad spectrum antiparasitic
Schistosomiasis (flukes)
Praze tha Lord: Paragonimus
"Christ's Sister Schisto Clonorchis
is a Paragon Clone" All tapeworms

NICLOSAMIDE Cestode (tapeworm) ≠Mitochondrial Ox-Phos

D. latum ≠GLU uptake by parasite
"Nickle = ¢es-toad / Tapeworm" Hymenolepsis nana
Toad with nickle tape Taenia solium (#2 Rx)
$ Making a "teeny lata"

PENTAVALENT ANTIMONY Leishmania

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

CHLOROQUINE Malaria (chloroquine) P. falciparum = Aggressive

QUININE vivax Human resistance to Vivax & Falciparim $ 30% of RBC's
MEFLOQUINE ovale Vivax = ΦDuffy a + b Mefloquine resistant
malariae Falcip: SSD-->rupture-->Φinfxn Chloroquine resistant
Quinine (if chloro-resistant) Quinine resistant
Tx = Artemethol for severe P. falc.
PRIMAQUINE Malara (latent hypnozoite--liver) Exo-RBC cycle: vivax; ovale Chloroquine resistant
Plasmodium vivax $ Liver Hemolysis in G6PD
Prima Viva Ova!! Plasmodium ovale GI upset

METRONIDAZOLE Giardia Metallic taste

Entameba histolytica
Sitting on the METRO gives you Gardnerella vaginalis
Diarrhea Trichomonas (nasty vadge discharge)
Vadge infections
"Gee-ur Aunt's Guard Tricked me to get on the metro"

PENTAMIDINE Prophylaxis:
Pneumocystis carinii pneumonio
I'm all Pent up I might die [AIDS PCP]

NIFURTIMOX Chagas Dz (Trypanosoma cruzi)

SURAMIN Sleeping sickness (African tryp)

Tripanosomiasis (tsetse fly)
" I Sure Am Sleepy; I might trip"

Antiparasitics
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
AMANTADINE Influenza A (prophylaxis) ≠Viral penetration / uncoating CNS
Parkinson's Dz Ataxia
Don't ask "a man to dine" with you if: Rubella Dizziness
He has A Flu (sneeze on your dish) Slurred speech
He's got Parkinson's (throw food)
He's dizzy, ataxic, slurring

Rimantidine = derivative w/ few S.E.'s

ZANAMIVIR Influenza Virus A ≠Influenza Neuraminidase Bronchoconstriction (asthma)

Zanamivir (inhaled) Influenza Virus B $ Use Oseltamivir, not Zanamivir
Oseltamivir (oral) ≠Asthmatics (use Oseltamivir)

RIBAVIRIN RSV ≠IMP dehydrogenase Hemolytic anemia

$ ≠Synthesis of guanine nucleotides Teratogen (severe)!!
Ribavirin is rabid
RSV (RibaVirin)
Eats the IMP
Rabid and bloody (hemolytic)

ACYCLOVIR HSV Phosphorylated by viral thymidine kinase Delerium

VZV $ Diphosphate --> Triphosphate (active) Tremor
A cycle of Di-p --> Tri-p --> ≠DNA EBV $ Competes w/ Deoxyguanose TRFP Nephrotoxicity
Zovirax Prophylaxis (compromised Px's) $ ≠Viral HSV DNA polymerase
ACV $ ≠DNA synthesis Resistance: CMV
Valacyclovir (pro-drug)

FAMCYCLOVIR HSV-1 (labialis) Potent inhibitor of HBV DNA P-ase Rarely side effects
Denavir cream (oral) $ Nucleoside Analogue Headache; Nausea
Zovirax HSV-2 $ Deacylated + oxidized in liver
ACV Acute (3x/day) $ Converted to Pencyclovir
Valacyclovir (pro-drug) Recurrent; Suppression (2x/day) $ Taken up by infected cells
VZV (3x/day) $ Phosphorylated by viral TK
HBV $ ↑Affinity for P-ase

GANCICLOVIR CMV Phosphorylated by viral thymidine kinase Leukopenia; Thrombocytopenia

$ ≠Viral CMV DNA polymerase Nephrotoxicity
"C MoVe the GAN GAN (kankan)"
Toxicity: Ganciclovir > Acyclovir
DHPG (dihydroxy-2-propoxymethyl guanine)
GCV GCSF: G'cyle stim. Factor
Ctyovene
Valgancyclovir (pro-drug)

FOSCARNET Use when Ganciclovir fails Binds to pyrophosphate binding site ≠E'lytes
CMV $ ≠Viral CMV DNA polymerase Thrombophlebitis
IV only CMV retinitis in immunocomrpomised
Pyrophosphate analog (Foscarnet) No need for phosphorylation
Foscavir

INTERFERONS HBV (chronic) ≠Viral RNA and DNA synthesis Neutropenia

HBC (cronic)
Glycoproteins from Leukocytes Kaposi's Sarcoma

Antivirals
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
BARBITURATES (BARBITALS) Sedative ↑Cl- channel open duration Dependence
Anxiety $ ↓Neuronal firing CNS depression w/ alcohol --> Death
Phenobarbital Seizures $ GABAa facilitator Cyt. P450 - Rx interactions
Pentobarbital Insomnia
Thiopental Anesthesia induction (thiopental) Barbiturates ↑DURATion of Cl- ch.
Secobarbital
≠Porphyria
BENZODIAZEPINES (EPAMS) Anxiety ↑Cl- channel open duration Sedation
Spasticity $ ↓Neuronal firing Dependence
Diazepam Status epilepticus (diazepam) $ GABAa facilitator CNS depression w/ alcohol --> Death
Lorazepam Detoxification (delerium tremens) Benzo's < Barb's in CNS depression
Temazepam ie respiratory depression
Chlordiazepoxide Insomnia Flumazenil (overdose Tx)
≠GABA-r (competitive antagonist) Overdose Tx = Flumazenil
Short-Acting
Triazolam like "TOM's thumb"
Oxazepam Tri = three
Midazolam
↑Frequency
Frenzodiazepines (FREquent)

ANTIPSYCHOTICS Schizophrenia (excess DA) ≠D2-r Sedation; Extrapyramidal S.E.'s

Psychosis Endocrine S.E.'s
"Clears thy halo fluff, Psycho!" Neuroleptic Malignant Syndrome ≠Muscarinic-r's; ≠HA-r's; ≠α-r's
Rigidity; Autonomic instability; Hyperreflex
Chlorpromazine Tardive dyskiniesia Dystopnia (4 hrs)
Thioridazine Stereotyped oral-facial mvnts (chr. use) $ Akinesia (4 days)
Haloperidol $ Akathisia (3 wks)
Fluphenazine $ Tardive dyskinesia (4 mos)

ATYPICAL ANTIPSYCHOTICS Schizophrenia - (+) & (-) Sx's ≠5HT2-r's + ≠DA-r's Fewer extrapyramidal S.E.'s

Olanzapine O lands! OCD (olanzapine) Clozapine = agranulocytosis (monitor)

Clozapine A Close! Anxiety (olanzapine)
Risperidone A respite! Depression (olanzapine)

LITHIUM Bipolar affective disorder ??PIP Cascade?? Tremor

Acute manic events (≠relapse) Hypothyroidism
Mood stabilizer Polyuria (ADH antagonist)
Teratogen / Toxic!

TRICYCLIC ANTIDEPRESSANT Depression ≠NE & SE reuptake Sedation

(IPRAMINE; TRIPTYLINE) Bed wetting (imipramine) α-Blocking S.E.'s
OCD (clomipramine) Anticholinergic S.E.'s
Nortriptyline (2') Holy trinity / TRI-C TRI - C's
Doxepin Nor tripping Convulsions
Clomipramine Doxology Clomping Coma
Amitriptyline (3') Am I Cardiotoxicity (arrhythmias)
Imipramine Desciple 3' > 2' (Amitriptyline > Nortriptyline)
Desipramine Desipramine is least sedating

SSRI's Depression ≠SE reuptake (serotonin-specific) SSRI's < TCA's

2-3 wks for effect CNS - Anxiety; Insomnia; Tremor
Fluoxetine Nausea; Vomiting
Sertraline Serotonin Syndrome w/ MAOI's
Paroxetine Hyperthermia; Rigidity; CV collapse
Citalopram

HETEROCYCLICS Major depressive disorders

Mirtazapine Heterosexuals Depression; α2 Antagonist --> ↑NE & SE release; 5HT2-r Sedation; ↑Cholesterol; ↑Appetite
Buproprion "Mirt & Bupee Depression; Smoking cessation ??? Tachycardia; Dry mouth; Psychosis
Venlafaxine Vem la pra Tranzar" Depression; Anxiety disorder ≠DA & SE reuptake; 5HT2-r antagonist Anxiety; Agitation; Headache; Insomnia
Trazodone Depression; ≠SE reuptake Sedation; Nausea; Priapism; HypoTN

CNS Rx's
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
MOA INHIBITORS (GENERAL) Atypical depressions ≠Monoamine Oxidase Inhibition MAO I + Tyramine + Meperidine
Depression + Psychosis $ ↓Degredation of monamines $ HTN crisis
Phenylzine Depression + Phobias CNS stimulation
Tranylcypromine Anxiety ≠SSRI's; ≠β-Agonists
Hypochondriasis
MAO-B INHIBITOR Parkinson's adjuvant Rx ≠MAO-B selective inhibition Enhances L-DOPA S.E.'s
L-DOPA + Selegiline $ ↑DA availability
Selegiline (Deprenyl)

L-DOPA + CARBIDOPA Parkinson's L-DOPA Arrhythmias (from periferal conversion)

L-DOPA crosses BBB Dyskinesias
$ Dopa decarboxylase conversion
$ DA (in brain)

Carbidopa
≠Dopa decarboxylase in periphery
$ ↓S.E.'s; ↑Bioavailability of DA in brain

OPIOID ANALGESICS Pain Opioid-r Agonists Addiction

Cough (dextromethorphan) mu = morphine CNS depression
"MMM, Dexter Fenan's Code is Heroin" Diarrhea (loperamide; diphenoxylate) delta = enkephalin Respiratory distress
Acute pulmonary edema kappa = dynorphin Pinpoint pupils
Morphine Withdrawal (methadone) Modulate synaptic transmission Constipation
Meperidine
Methadone Toxicity Antidote
Dextromethorphan Naloxone
Fentanyl Naltrexone
Codeine
Heroin

SUMATRIPTAN Acute migraine 5-HT1d Agonist Chest discomfort

Cluster headache attacks 1/2 life < 2 hrs Mild tingling
I assume a trip and you 5HiT your head
$ Headaches; Migraines ≠Prinzmetal's Angina; ≠CAD

ONDANSETRON Vomiting (control) 5-HT3 Antagonist Headache

Post-op vomit control $ Central-acting anti-emetic Diarrhea
"On Dan it runs (vomit)" Cancer Tx vomit control

CNS Rx's
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
PHENYTOIN Grand mal seizures ≠Na+ Channels (use-dependent) Nystagmus; Diploplia
Ataxia; Peripheral neuropathy
"Fee Na+ To In" Lethargy; Megaloblastic Anemia (↓B12)
Na+ has a fee to enter so it can't Gingival hyperplasia
Hirsutism
Teratogenic - Fetal hydantoin syndrome

CNS Rx's
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
ACETAZOLAMIDE Glaucoma ≠Carbonic anhydrase in PCT Acidosis (hyperchloremic metabolic)
Alkalosis (metabolic; urinary) $ NaHCO3 diureses Neuropathy
"Aceta acidifies" Altitude sickness $ HCO3 excretion NH3 toxicity
Sulfa allergy

"Aceta acidifies"

FEROSEMIDE Edema (CHF; Cirrhosis; Pulm) ≠Na+ / K+ / 2Cl- Cotransporter in TAL ↓K+-emia
HTN $ ↓Hypertonicity of medulla ↓Ca2+-emia
Sulfonamide loop diuretic ↑Ca2+-emia $ ≠Concentration of urine Ototoxicity
$ Diuresis / Dilute urine I.S. Nephritis
$ ↑Na+ to DT --> K+ swapping Allergy (sulfa)
$ ↓K+-emia Gout
$ ↑Ca2+ excretion --> ↓Ca2+-emia Dehydration

ETHACRYNIC ACID Edema ≠Na+ / K+ / 2Cl- Cotransporter in TAL ↓K+-emia

HTN $ ↓Hypertonicity of medulla ↓Ca2+-emia
Phenoxyacetic acid derivative ↑Ca2+-emia $ ≠Concentration of urine Ototoxicity
Not sulfonamide $ Diuresis / Dilute urine I.S. Nephritis
NOTE: $ ↑Na+ to DT --> K+ swapping Dehydration
"Ferocious Etha cryin" cuz Diuresis in Px's w/ sulfa allergies $ ↓K+-emia No uricemia (no gout)
she got sulfa allergies $ ↑Ca2+ excretion --> ↓Ca2+-emia No sulfa allergies

HYDROCHLOROTHIAZIDE HTN ≠NaCl reabsorption in early DT ↓K+ metabolic alkalosis

CHF $ ↓Diluting capacity of nephron ↓Na+emia
Thiazide diuretic ↑Ca2+uria $ ↓Ca2+ excretion ↑Ca2+emia
Nephrogenic Diabetes Insipidus ↑GLU HyperGLUC
↑Lipids
↑Uricemia
Sulfa allergy

K+ SPARING DIURETICS ↑ALD Competitively binds ALD-r in CCT (Spiro) ↑K+emia

K+ Depletion ≠Na+ channel in CCT (Triam; Amilo) Endocrine effects - gynecomastia
"Try and Sprint A mile" - Km sparing CHF Blocks ALD --> backflow

Triamterene
Spironolactone
Amiloride

MANNITOL Shock Osmotic Diuretic Pulmonary edema

Drug overdose Dehydration
Intraocular pressure (decreases it)

≠Anuria
≠CHF

DIURETIC E'LYTE CHANGES URINE BLOOD

Carbonic Anhydrase Inhibitors ↑NaCl (All) ↓pH (acidosis) - Carb-A Inhib.; K+ sparing
K+ Sparing ↑K+ (except K+ sparing) ↑pH (alkalosis) - Loops; Thiazides
Loops ↑Ca2+ (loops)
Thiazides ↓Ca2+ (thiazides)

Diuretics
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
β-BLOCKERS Impotence
Ca2+ Ca2+ Bronchospasm
β1 Selectivity (heart only) HTN ↓CO; ↓Renin Ca2+ Bradycardia; AV block
Atenolol Angina ↓HR; ↓Contractility Ca2+ Ca2+ Sedation; Sleep alterations
Betaxolol MI ↓Mortality Ca2+ Ca2+ ↑TG's and ↓HDL
Esmolol SVT ↓AV conduction velocity
Acebutolol CHF ↓Progression P
Metoprolol Glaucoma ↓Secretion cAMP
β1 = β2
Propranolol ≠Asthma β1
ATP
Pindolol !Diabetics!
Nadolol
Labetalol
↓cAMP
$ ↓Ca2+ influx
$ ↓HR, Contractility
$ ↑Refractory period

HYDRALAZINE HTN (severe) ↑cGMP Nausea; Headache

CHF $ Smooth muscle relaxation Hypotension; Reflex tachycardia
"Hydra-relaxing" $ Arterioles > Veins Relaxation Fluid retention
$ ↓Afterload SLE-like syndrome

Hydra (H2O-retention)

ACE INHIBITORS HTN ≠Antiotensin-converting enzyme Cough

CHF Angio-edema
Captopril Diabetic Renal Dz Angiotensin I Proteinuria
Enalapril Taste changes
Lisinopril ACE HypO-TN
Pregnancy problems (fetal renal injury)
Angiotensin II-R Antagonist ↓AT II Rash
Losartan (no cough S.E.) $ ≠Vasoconstriction Increased Renin
≠↑Na+/H2O Lower A-II
≠↓Bradykinin Hyperkalemia
≠↓Sympathetics
$ ↑Renin release (compensatory) CAPTOPRIL

NITRATES Angina NO release from smooth muscle Tachycardia

Edema (pulmonary) $ ↑cGMP Hypotension
Nitroglycerin Aphrodesiac; Erection enhancer $ Smooth muscle relaxation "Monday Dz"
Isosorbide Dinitrate $ Vasodilation (veins > arteries) Tolerance during work week
Intolerance on weekends
$ Tachycardia
Dizziness; Headache

GLYCOSIDES CHF ≠Na+/K+ ATPase Nausea; Vomiting; Diarrhea

Atrial Fib $ ↑Na+ I.C. Na Blurry yellow vision (Van Gogh)
Digoxin $ Na+ / Ca2+ swap Arrhythmia
75% bioavailability
Na+
25% protein-bound Renal Failure
Na+
t1/2 = 3 days Na+ Na+K+ $ ↓Excretion
Peed out $ ↑Risk for toxicity
Ca2+ Ca2+ ↑K+
Ca2+ $ Potentiates glycosides --> Toxic!!
Ca2+ Ca2+
Quinidine
Na+ Ca2+
$ ↓Clearance of digoxin
Ca2 Na+
Na+
Antidote = K+; Lidocaine; Pacer;
Na+ Na+
↑Na+ (IC) Anti-dig Fab fragments
$ ↑Ca2+ (IC)

PHOSPHODIESTERASE INHIB

AMP
P-DiesterasecAMP
β1
ATP

Cardiovascular
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
CLASS IA Atrial arrythmias Local anasthetics Quinidine:
Ventricular arrhythmias ↓ / ≠ Conduction Headache; Tinnitus
Quinidine Queen $ ↓Slope of phase 4 depolarization Thrombocytopenia
Amiodarone Amy $ ↑Threshold in abnormal pacemaker cells Torsade de pointes (↑QT)
Procainamide Proclaims Slectively depress frequent depolarizers Procainamide:
Disopyramide Dis Ol' pyramid SLE-like syndrome (reversible)
≠K+ Channel
$ ↑K+ (IC)
$ ↑↑Repol.
$ ↑PR
↑QRS K+ K+ K+
↑↑QT K+ K+ K+
K+
K+

CLASS IB Acute ventricular arrhythmias ↓AP duration Local anesthetic

Post-MI $ Affects ischemic or depolarized CNS stimulation/depression
Lidocaine Digitalis-induced arrhythmias Ventricula tissue Cardiovascular depression
Mexiletine Purkinje tissue
Tocainide

CLASS IC Last resort b/c of toxicities Proarrhythmic

Ventricular Tach / Fib
Flecainide SVT (intractable)
Encainide No effect on AP duration
Propafenone

CLASS II - β-BLOCKERS Suppress abnormal pacemakers ↓caMP; ↓Ca2+ currents

$ ↓Phase 4 slope
Esmolol (short acting) Esmo $ ↓Abnormal pacemakers
Metoprolol Met $ ↑PR interval
Timolol Tim AV Node sensitive
Atenolol A 10
Propranolol Pro

CLASS III - K+ CH. BLOCKERS Use when other antiarrythmics fail ↑AP duration Sotalol - Torsade de pointes
↑ERP Ibutilide - Arrhythmias; HypoTN
Sotalol ↑QT interval Bretylium
Ibutilide Amiodarone - Pulmonary fibrosis
Bretylium Hepatotoxicity
Amiodarone Hypo/Hyper-Thyroidism
Neuro; Skin; Photoderm

CLASS IV Ca2+ CH. BLOCKERS Nodal arrhythmias (ie SVT) Affect AV nodal cells Constipation
Prevention $ ↓Conduction velocity Flushing
Verapamil ↑ERP Edema
Diltiazem ↑PR interval CHF; AV block; SN dep.
Torsades de pointes (bepridil)

Ca2+ CHANNEL BLOCKERS HTN ≠L-type Ca2+ channels (cardiac; smooth m) Cardiac depression
Angina $ ↓Contractility Peripheral edema
"Knife Dealt [you] A Vera!!" Arrhythmias Flushing; Dizziness
Constipation
Nifedipine > Diltiazem > Verapamil Smooth muscle: Knife dealt you a vera

Verapamil > Diltiazem > Nifedipine Heart: Vera dealt a knife

MISCELLANEOUS

Adenosine #1 Rx for AV nodal arrhythmias

K+ Ectopic pacemakers; Digoxin toxicity
Mg+ Torsades de pointes; Digoxin toxicity

Antiarrhythmics
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
SILDENAFIL Erectile dysfunction ≠cGMP phosphodiesterase Headache
$ ↑cGMP Flushing
"Sildenafil FILLS the penis" $ Relaxation of smooth muscle Dyspepsia
$ Corpus Venosum fills with blood Blue-green vision
$ Erection
!!Hypotension!! (Heart Px's; Nitrates)

H2 BLOCKERS PUD ≠H2-r (reversible blockage) Anti-androgenic effect (cimetidine)

Gastritis $ ↓H+ production ↑CRE (cimetidine)
Cimetidine GERD
Ranitidine Z-E Syndrome ≠P450 (potent inhibitor)
Famotidine
Nizatidine

OMEPRAZOLE PUD ≠H+/K+ ATPase in parietal cells (irreversible)

LANSOPRAZOLE Gastritis $ ↓H+ Production in stomach
GERD
Z-E Syndrome

SUCRALFATE PUD Polymerizes in ↓pH (stomach env.)

$ Binds necrotic peptic ulcer tissue
Aluminum sucrose sulfate Cannot work w/ $ Barrier to acid, pepsin, and bile
Antacids
PPI's; H2 blockers

MISOPROSTOL NSAID-Peptic-Ulcer prevention PGE1 Analog Diarrhea

Induce labor $ ↑Mucous secretion of GI mucosa
≠Childbearing potential (abortative)

ANTACIDS GERD pH buffers

PUD ↓K+ (all)
Al2+ hydroxide Al2+ hydroxide = Constipation; ↓PO4-
Mg2+ hydroxide Mg2+ hydroxide = Diarrhea
Ca2+ carbonate Ca2+ carbonate = ↑Ca2+; ↑Acid

Can affect absorption of other Rx's

GI Rx's
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
HEPARIN IMMEDIATE anticoagulation Catalyzes activation of antithrombin III Bleeding
Pulmonary embolism $ AT II Activation Thrombocytopenia
LMWH Storke Rx-Rx Interactions
Better bioavailability Angina
Longer hal-life MI Antidote = Protamine sulfate Antidote = Protamine sulfate
Subcutaneous w/o lab monitoring DVT (+) charged molecule
$ Binds HA(-) Follow PTT
Short 1/2 life Pregnancy = OK Check aPTT

WARFARIN Chronic coagulation ≠ γ carboxylation of Vit K-dependent Factors Bleeding

Hypercoagulable state (prolonged) ≠Protein C & S (via vit. K antagonism) Teratogenic
Coumadin Follow PT values Rx-Rx interactions
II, VII, IX, X
Long 1/2 life ≠Pregnancy (X-placenta)
O2 NADP
Vit K
CO2
NADPH

IIa, VIIa, IXa, Xa

≠NADPH oxidation
$ ↓Reduced Vit. K
$ ↓Activation of II, VII, IX, and X

"War-far-in hits 2, 7, 9 and 10"

ANTICOAGULANTS

THROMBOLYTICS Early MI ↑Plasminogen --> Plasmin (direct/indirect) Bleeding

$ Plasmin cleaves thrombin & fibrin
Streptokinase
Urokinase
t-PA (ALTEPLASE)
APSAC (anistreplase)
THROMBOLYTICS

CLOPIDOGREL Acute Coronary Syndrome ≠ADP pathway Neutropenia (ticlopine)

TICLOPIDINE Coronary stenting $ ≠Binding of fibrinogen
Prevention of thrombotic stroke $ ≠Platelet aggregation Use only for Aspirin intolerant Px's
Use only for Aspirin intolerant Px's
ANTIPLATELETS

Anticoagulants
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
BILE ACID RESINS ≠Reuptake of bile acids in lumen Px's HATE it!!
$ ↓↓LDL Tastes bad
Cholestyramine =HDL GI discomfort
Colestipol ~↑TG

HMG-CoA REDUCTASE INHIB. ≠HMG CoA Reductase $$$

$ ≠CE synthesis in liver Myositis; Muscle stiffness
Simvastatin Sim the $ ↓↓↓LDL ↑LFT's (reversible)
Atorvastatin Actor ↑HDL
Pravastatin Prays for ↓TG
Lovastatin Love

HMG Studios on
Statin Island

NIACIN ≠Hepatic release of VLDL Flushing; Red face; Tx w/ aspirin

$ ↓↓LDL
↑↑HDL
↓TG

LIPOPROTEIN LIPASE STIM ↑↑LPL activity Myositis; Muscle stiffness

$ ↑Breakdown of VLDL --> IDL --> LDL ↑LFT's
Gemfibrozil $ ↓LDL
Clofibrate ↑HDL
↓↓↓TG

Lipid-Lowering
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
METHOTREXATE Leukemias Folic acid analog Myelosuppresion
Lymphomas $ ≠Dihydrofolate reductase Reverse w/ Leucovorin or
S Phase antimetabolite Choriocarcinoma $ ↓dTMP Folinic acid
Sarcomas $ ↓DNA + Protein synthesis Liver macrovesicular fatty change
Abortion
Ectopic pregnancy
Rheumatoid Arthritis
Psoriasis

5-FU (5-FLUOROURACIL) Colon CA Pyrimidine analog activated --> 5F-dUMP Myelosuppresion (not reversible)
Solid tumors $ Complexes to folic acid Photosensitivity
S Phase antimetabolite Basal Cell CA (topical) $ ≠Thymidylate synthase
≈Effects as Methotrexate $ ↓dTMP
Synergy w/ methotrexate

6-MP (6-MERCAPTOPURINE) Leukemias ≠Purine synthesis ≠BM

Lymphomas (ΦCLL or HD) ≠Liver
Metabolized by xanthine oxidase ≠GI
$ ↑Toxicity w/ Allopurinol
↑Toxicity w/ Allopurinol

BUSULFAN CML Alkylating agent Pulmonary fibrosis

$ X-links DNA ↑Pigmentation

CYCLOPHOSPHAMIDE Non-Hodgkin's Lymphoma Alkylating agent Myelosuppression

Breast CA $ Liver bioactivation Hemorrhagic cystitis
Ovarian CA $ X-links DNA at guanine N-7
Immunosuppressant
NITROSOUREAS Brain tumors Alkylating agent CNS toxicity
Glioblastoma multiforme $ Liver bioactivation Dizziness
Carmustine $ X-links DNA Ataxia
Lomustine
Semustine X-BBB
Streptozocin

CISPLATIN Testicular CA ≈Alkylating agent (acts like one) Nephrotoxicity

Bladder CA $ Hydrolysis of Cl- groups ≠CN VIII
Ovary CA $ X-links DNA
Lung CA
DOXORUBICIN HD (ABVD) Intercalates DNA strands (non-covalent) ≠Heart
Myelomas $ ↓Replication and transcription Myelosuppression
Adriamycin Sarcomas $ Free radical generation Alopecia
Solid Tumors (Breast; Lung; Ovary) $ Breakage Toxic extravasation
BLEOMYCIN Testicular CA Intercalates DNA strands Pulmonary fibrosis
Lymphomas $ Free radical generation ≠Skin
$ Strand breaks

ETOPOSIDE Lung CA (Oat cell) ≠Topoisomerase II (G2-phase) Myelosuppression

Prostate CA $ ≠Break repair in DNA ≠GI
Testicular CA $ Degradation of DNA Alopecia

PREDNISONE #1 Corticoid in CA Tx ???; Triggers apoptosis Cushing Syndrome; Immunosuppresion

CLL Osteoporosis; HTN; Peptic ulcers
Hodgkin's (MOPP) Cataracts; Acne;
Autoimmune Dz's ↑GLU; Psychosis
TAMOXIFEN / RALOXIFENE Breast CA Estrogen mixed Agonist / Antagonist ↑Risk of endometrial cancer
$ ≠Binding of estrogen to ER+ cells Hot flashes

VINCRISTINE / VINBLASTINE Lymphomas (MOPP) M-phase alkaloid Neurotoxicity

Wilm's tumor $ Binds to tubulin Areflexia
Oncovin / Vincristine Choriocarcinoma $ ≠Polymerization of microtubules Peripheral neuritis
$ ≠Mitotic spindle formation Paralytic ileus
≠BM (Vinblastine BLASTS BM)

PACLITAXEL Ovarian CA M-phase alkaloid Myelosuppression

Breast CA $ Binds to tubulin Hypersensitivity
$ Hyperstabilizes polymerized microtubles
$ ≠Mitotic spindle breakdown
$ ≠Anaphase

Cancer Drugs
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
INSULIN Diabetes Mellitus Binds Insulin-R (liver; muscle; adipose) ↓GLU
↑K+ (life-threatening) $ Tyrosine Kinase activity Allergy (rare)
↑GLU $ GLU --> Glycogen (Liver)
$ Synthesis of glycogen + protein (Muscle)
$ Tryglyceride storage (Fat)

SULFONYLUREAS DM II (NIDDM) Close K+ channels in β-cell membrane ↓GLU

$ Cell depolarization Disulfiram-like effects
So fun you'll race a Car (hyperglycemic) $ Ca2+ influx Glyburide; Glipizide
$ Insulin release stimulated
Chlorpropamide Chlar pool
Glyburide Glide your ride Ca2+ / Car release
Glipizide Glip the side [of the]
Tolbutamide Toll booth

METFORMIN ↑GLU ??Unknown?? Lactic acidosis

≠Gluconeogenesis (liver)
Oral Biguanide $ ↓GLU levels

"Metformin = Stops GLU Formin' "

GLITAZONES DM II MonoTx ↑Targe cell response to insulin Hepatotoxic (troglitazone)

Combo + Above agents Weight gain
Pioglitazone
Rosiglitazone Glitazone = Lit a zone up (↑sensitivity) Glitazone = Glutton zone --> Wt. Gain!
Troglitazone

α-GLUCOSIDASE INHIBITORS DM II MonoTx ≠Inestinal brush border α-glucosidase GI Disturbances

Combo + Above agents $ ↓Sugar hydrolysis and absorption
Acarbose $ ↓GLU serum levels (post-prandial)
Miglitol
DIABETIC Rx's

LEUPROLIDE Infertility (pulsatile) Continuous Anti-androgen

Prostate cancer (continuous) $ LH and FSH Burst (transient) Nausea; Vomiting
GnRH Analog / Agonist Leuprolide + Flutamide
Uterine fibroids
Leuprolide = Leutonizing H / Follicle SH

PROPYLTHIOURACIL Hyperthryoidism ≠TH synthesis coupling Skin rash

≠T4 --> T3 conversion in periphery Aplastic anemia
Thio = Thyro Agranulocytosis

FINASTERIDE Benign Prostastic Hypertrophy ≠5α-reductase

$ ≠Testosterone --> Dihydrotestosterone
Anti-androgen Finasteride = Fine ass rubber ball
Big prostate = rubber ball in ass Finasteride = Final steroid (no conversion)

FLUTAMIDE Prostate Carcinoma Competitive inhibitor of Testosterone-r

$ ≠Androgens
Non-steroidal Anti-androgen

KETOCONAZOLE Polycystic ovarian syndrome ≠Steroid synthesis

SPIRONOLACTONE (Prevents hirsutism)

Anti-androgen

Endocrine
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
CLOMIPHENE Infertility Pituitary ER(+) Estrogen agonist (partial) Hot flashes
$ Prevents (-)feedback Ovarian enlargement
$ ↑LH & FSH release Multiple spontaneous pregnancies
$ Ovulation stimulation ≠Visual

MIFEPRISTONE (RU-486) Abortifacient ≠Progestin (competitive inhibitor) Heavy vaginal bleeding

$ ↓Hospitality of uterus for enpregnation ≠GI (nausea; vomiting; anorexia)
Abdominal pain

ORAL CONTRACEPTIVES Contraception ↑TG'S

Regulation of menses Depression
Estrogen ↓Endometrial & Ovarian CA risk ↑Weight
Progestins ↓Ectopic pregnancy incidence Nausea
↓Pelvic infections HTN
< 1% Failure ↑Coagulable state

PROGESTERONE Converts endometrium to decidualized state ≠Non-REM sleep

Withdrawal --> Endometrial shedding Fatigue; Sedation
Produced by corpus luteum Maintains pregnancy ↓Sleep onset
↓Myometrial excitability; Uterine relaxation Night wakenings
↑Thick mucus production (inhibits sperm)
↑Temp Immunosuppressant
(-) Feeback (LH; FSH)
Competitively Inhibits aldosterone
$ ↑Ald secretion (compensatory)

ESTROGEN Menopause (replacement Tx) Growth of follicle Excessive / Unopposed Estrogen Tx

$ ↓Hot flashes Endometrium proliferation $ ↑Risk of endometrial cancer
Estradiol (ovary) ↓Bone loss Genitalia development Tx = Progesterone to balance
Estriol (placenta) Breast stroma development; Lactation prep
Aromatizaztion (in blood) Fat distribution (women) ≠REM sleep
Estrogen (Testes) Protein synthesis and transport (liver) ≠Sleep wake cycle
(-) Feedback (FSH)
Estradiol > Estione > Estriol (potency) (+) Feedback (LH)
↑Myometrial excitability
Ovarian & Extraovarian
$ Estrone (E1) = Estradiol (E2) Estriol Test = tests fetoplacental function

Cholesterol (mother) Placental Sulfatase deficieny

$ Pregnenolone (mother; placenta) X-linked metabolic Dz in males
$ DHA sulfate (fetus) Post-date pregnancies
$ DHA --> E1; E2 (placenta) ≠Labor inducement
$ 16αOH DHA sulfate (fetus --> placenta) ↓Estriol in mother
$ Estriol (E3); (placenta; mother) ↑DHEA-S in amniotic fluid

ANDROGENS Finasteride inhibits Test --> DHT Wolffian duct differentiation --> Gonads
2' Sex characteristics
Testosterone (testes; adrenal) Growth spurt (puberty)
DHT (prostate; peripheral conversion) Spermatogenesis
Androstenedione (adrenal) Anabolic function
$ ↑Muscle
DHT > Testosterone > Andro ↑RBC's
↑Libido
Targets
$ Skin; Prostate Testosterone + 5α-reductase
Epididymis; Seminal vesicles $ DHT
Liver; Muscle; Brain Testosterone / Androstenedione + Aromatase
$ Estrogen (convertsion in adipose tissue)

hCG ↑hCG in Choriocarcinoma Maintains corpus luteum (1st tri.)

↑Hydatidiform Mole Stimulates CL secretion
Human Chorionic Gonadotropin $ Progesteron
Produced by syncytiotrophoblasts Estrogen
$ Placenta (2nd & 3rd Tri) Relaxin
≈LH
Pregnancy Test hCG(+) < 8 days

hPL Anti-insulin effects on mom

$ Facilitates GLU delivery to fetus
Human Placental Lactogen

Hormones
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
OCP's Endometriosis Pseudopreganncy state
↓Menstrual flow
Ethinyl Estradiol ↓PG's in Luteal phase
Progestine

GnRH AGONISTS Endometriosis (-) Feeback on Hypothalamus Hypoestrogenic state (profound)

$ Inhibition of GnRH Hot flushes
Leuprolide Acetate ↓Bone density
Nafarelin Costly drug
Goserelin

GnRH ANTAGONISTS Endometriosis (-) Feeback on Hypothalamus

$ Inhibition of GnRH
Antagonists > Agonists (efficacy)

Ganirelix
Cetrorelix

PROGESTINS Endometriosis (-) Feeback on Hypothalamus

$ Inhibition of GnRH
Norethindrone acetate
Medroxyprogesterone Acetate

≈GnRH Analogs

ANDROGENS Endometriosis Antigonadotropic action Virilization

Estrogen deficiency
Danazol

AROMATASE INHIBITORS Endometriosis ↓Androgen --> Estrogen conversion

MIFEPRISTONE Anti-progestin

Contraceptives
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
PREDNISONE #1 Corticoid in CA Tx ≠Phospholipase A2 & ≠COX-2 Expression Cushing Syndrome; Immunosuppresion
CLL $ ↓LKT's & PG's Osteoporosis; HTN; Peptic ulcers
Hodgkin's (MOPP) Cataracts; Acne;
Autoimmune Dz's ↑GLU; Psychosis
CYCLOSPORINE Transplant immunosuppression Binds to peptidyl proline cis-trans isomerase Prone to viral infections
Autoimmune disorders $ ≠IL-2 synthesis & ≠IL-2-r Prone to lympomas
$ ≠Diff. & Activation of T Cells Nephrotoxic (Tx = mannitol diuresis)

AZOTHIOPRINE Kidney transplant I-suppression Anti-metabolite derivative of 6-MP

Autoimmune disorders $ ≠Metabolism & Synthesis of nucleic acid
GN $ ≠L'cyte proliferation
Hemolytic Anemia Antigenic stimulation
$ Toxic to L'cytes

METHOTREXATE Leukemias Folic acid analog Myelosuppresion

Lymphomas $ ≠Dihydrofolate reductase Reverse w/ Leucovorin or
S Phase antimetabolite Choriocarcinoma $ ↓dTMP Folinic acid
Sarcomas $ ↓DNA + Protein synthesis Liver macrovesicular fatty change

DACTINOMYCIN

CYCLOPHOSPHAMIDE Non-Hodgkin's Lymphoma Alkylating agent Myelosuppression

Breast CA $ Liver bioactivation Hemorrhagic cystitis
Ovarian CA $ X-links DNA at guanine N-7
Immunosuppressant
ANTI-L'CYTIC GLOBULIN

Monoclonal anti-T L'cyte Ab's

Rh3(D) Ig

TACROLIMUS (FK506) Transplant immunosuppression Binds FK-binding protein Nephrotoxicity

$ ≠Secretion of cytokines (IL-2; others) Peripheral neuropathy
≈Cyclosporine $ ≠Diff. & Activation of T Cells HTN
Pleural effusion
↑GLU
IMMUNOSUPPRESSANTS
GLUCOCORTICOIDS Addison's Dz ≠Phospholipase A2 & ≠COX-2 Expression Cushing's Syndrome
Hydrocortisone Inflammation $ ↓LKT's & PG's Dorsal fat pads; Turnkal obesity
Prednisone Immune suppression Moon facies
Triamcinolone Asthma Muscle waisting; Osteoporosis
Dexamethasone Bruising
Beclomethasone Adrenocortical atrophy

Immunosuppressants
 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
ASPIRIN Anti-pyretic Acetylation action GI ulceration
Analgesic $ ≠COX-1 & COX-2 (IRREVersible inhibitionBleeding
NSAID Anti-inflammatory $ ≠Arachidonic acid --> PGE's Hyperventilation
Antiplatelet Reye's syndrome
Tinnitus (CN VIII)

OTHER NSAIDS Anti-pyretic Acetylation action GI ulceration

Analgesic $ ≠COX-1 & COX-2 (REVersible inhibition) Bleeding
Ibuprofen Anti-inflammatory $ ≠Arachidonic acid --> PGE's Hyperventilation
Naproxen Antiplatelet Reye's syndrome
Indomethacin Tinnitus (CN VIII)
Patent ductus arteriosus (Indomethacin)
NSAIDS
COX-2 INHIBITORS Rheumatoid arthritis ≠COX-2 (cyclo-oxygenase isoform 2) NO GI ulceration
Osteoarthritis $ ≠Inflammation Bleeding
Celecoxib ≠Pain Hyperventilation
Rofecoxib $ Spares COX-1 Reye's syndrome
$ OK = GI Mucosa maintenance Tinnitus (CN VIII)

COX INHIBITORS

ACETAMINOPHEN Anti-pyretic ≠COX (CNS mostly) - Reversible Hepatic necrosis (overdose)

Analgesic Glutathione depletion
!!ΦAnti-inflammatory!! Inactivated peripherally $ Toxic adducts in liver

NSAIDS & ≠COX

 INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
INHALED ANESTHETICS Inhaled Heart depression
↑Lipid solubility = ↑Potency = 1 / MAC Respiratory depression
Halothane (hepatotoxic) ↓Blood solubility = Rapid induction Nausea; Vomiting
Enflurane (convulsant) ↑CNS blood flow
Isoflurane
Sevoflurane Hepatotoxicity (halothane)
Methoxyflurance (nephrotoxic) Nephrotoxicity (methoxyflurane)
Nitrous oxide Convulsant (enflurane)

I.V. ANESTHETICS

BARBITURATES Anesthesia induction (thiopental) ↑Cl- channel open duration Dependence

Short surgical procedures $ ↓Neuronal firing CNS depression w/ alcohol --> Death
Thiopental $ GABAa facilitator Cyt. P450 - Rx interactions
Sedative
Anxiety Barbiturates ↑DURATion of Cl- ch.
Seizures
Insomnia ↑Lipid solubility --> X-BBB
≠Porphyria
BENZODIAZEPINES (EPAMS) Anesthesia induction ↑Cl- channel open duration Post-operative respiratory distress
Endoscopy (#1 Rx) $ ↓Neuronal firing Amnesia
Short-Acting $ GABAa facilitator
Triazolam Anxiety Sedation
Oxazepam Spasticity Dependence
Midazolam Status epilepticus (diazepam) Flumazenil (overdose Tx) CNS depression w/ alcohol --> Death
Detoxification (delerium tremens) ≠GABA-r (competitive antagonist) Benzo's < Barb's in CNS depression
Insomnia ie respiratory depression

Overdose Tx = Flumazenil

OPIOID ANALGESICS Anesthesia induction Opioid-r Agonists Addiction

mu = morphine CNS depression
Morphine delta = enkephalin Respiratory distress
Fentanyl Pain kappa = dynorphin Pinpoint pupils
Cough (dextromethorphan) Modulate synaptic transmission Constipation
Diarrhea (loperamide; diphenoxylate)
Acute pulmonary edema Toxicity Antidote
Withdrawal (methadone) Naloxone
Naltrexone

KETAMINE Dissociative anesthetic Disorientation

Cardiovascular stimulant Hallucinations
PCP analog ↑CNS blood flow Bad dreams
PROPOFOL Anesthesia induction (RAPID) Less post-op S.E. than thiopental
Short procedures

LOCAL ANESTHETICS Local pain numbing ≠Na+ channels (via inner channel receptors) Allergies to Esters
Minor surgical procedures $ ≠Action potential conduction $ Give Amides
Esters Anesthetic + Epinephrine (v. const.) $ ≠Pain signal
Progaine Spinal anesthesia $ Small fibers > Large fibers CNS excitation
Cocaine $ Myelanted > Unmyelinated Cardiovascular toxicity (bupivacaine)
Tetracaine ≠Infected (acidic) tissue $ Pain > Temp. > Touch > Pressure HTN
Amides Charged anesthetics cannot X Arrhythmias (cocaine)
Lidocaine $ More anesthetic needed 3' Amines penetrate membrane
Bupivacaine $ Bind to channel-r's on inner side

Anesthetics
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
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

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

COMA

Airway (protect) Rule Out

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

CNS Rx
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
EYE EXAM (PUPIL DILATION)

Atropine Anti-Muscarinic
Homatropine Anti-Muscarinic
Tropicamide Anti-Muscarinic

GLAUCOMA

"ABCD P"

α-Agonists ↑Outflow of aqueous humor Mydriasis + Stinging (epi)

Epinephrine ≠Closed-angle glaucoma (epi)
Brimonidine No pupillary or vision changes (brimo)
β-Blockers ↓Secretion of aqueous humor No pupillary or vision changes
Timolol
Betaxolol
Carteolol
Cholinomimetics Ciliary muscle contraction Miosis
Pilocarpine $ Opening of trabecular meshwork Cyclospasm
Carbachol $ ↑Outflow of aqueous humor
Physostigmine
Echothiophate
Diuretics ↓HCO3- (via ≠carbonic anhydrase) No pupillary or vision changes
Acetazolamide $ ↓Secretion of aqueous humor
Dorzalamide
Brinzolamide
Prostaglandins ↑Outflow of aqueous humor Iris darkening (browning)
Latanoprost

Eye Rx
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
CHF

β-Blockers ↓Progression to CHF

ANGINA

β-Blockers ↓HR; ↓Contractility --> ↓O2 demand

MI

β-Blockers ↓HR; ↓Contractility --> ↓O2 demand

HTN

β-Blockers ↓CO; ↓Renin secretion

SVT

β-Blockers ↓AV conduction velocity

Heart Rx
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
ASTHMA

Isoproterenol β Agonist (non-specific) ↑HR

$ Relaxes bronchial smooth muscle
Albuterol Acute attack β2 Agonist (acute attack)
$ Relaxes bronchial smooth muscle
Salmeterol Long-acting β2 Agonist (acute attack) Arrhythmia
$ Relaxes bronchial smooth muscle Tremor
Theophylline ≠Phosphodiesterase Narrow TI
$ ↓Hydrolysis of cAMP Cardiotoxicity
$ Bronchodilation Neurotoxicity
Ipratropium ≠Muscarinic (competitive antagonist)
$ ≠Bronchoconstriction
Cromolyn Prophylaxis only ≠Release of Mast cell mediators Rare S.E.

Corticosteroids Inactivates NF-κB

Beclomethasone $ ≠Synthesis of Cytokines (TNF-α & other cytokines)
Prednisone
Zileuton ≠5-Lipoxygenase
$ ≠Arachidonic acid --> LKT's
Zafirlukast ≠LKT-r's

Lung Rx
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
CHRONIC HBV
Immunolo-Tx BindS membrane-R's
IFN-α (high dose) $ ≠Viral replication; ↓Prolif; ↑Phago.
Nucleoside Analogs Incorporates into viral DNA Adefovir = Renal tubular injury
Lamivudine ≠Priming; ≠R-transcriptase; ≠RNAse
Adefovir ≠DNA polymerase; ≠Chaperone
Tenofovir
Deoxyguanosine analog
Entecavir

Interfere before it's too LATE

CHRONIC HCV
Immunolo-Tx BindS membrane-R's
IFN-α (high dose) $ ≠Viral replication; ↓Prolif; ↑Phago.
Nucleoside Analogs Enhances IFN; ??Mechanism
Ribavirin
PRIMARY BILIARY CIRRHOSIS
Immunomodulator Folic Acid antagonist Nausea; BM Suppression
Methotrexate $ ≠DNA synthesis --> Apoptosis Hepatotoxic; Tx = Glucovorin to reverse
Biliary Product (Brown Bear)
Ursodeoxycholic acid

Cholchicine
Antibiotics

ASCITES
Diuretics
Furosemide
Spironolactone
Spontaneous Bacterial Peritonitis
Cephalosporins
Quinolones

VARICEAL BLEED
Non-Selective β-Blockers Non-Selective β-Blockers ≠Indications
Propanolol Splanchnic vasoconstriction Hypersensitivity; HypoTN
Naldolol ↓Heart rate and CO Cardio shock, block, bradycardia
Nitrates Vasodilator ≠Indications: Hypotension
Somatostatin Analogs Inhibits Serotonin, Gastrin, VIP release
Octreotide (#1 Emergency bleed Rx) $ ≠Vasodilation
Vasopressin $ Splanchnic Constriction
Angiotensin II Inhibitors $ ↓Portal HTN

GI Rx
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
ENDOMETRIOSIS

Estrogen antagonists
NSAIDS
Danazol (Androgens)
Oral contraceptives
Mifepristone (anti-progestins)
Aromatase Inhibitors
E.C. Matrix Modulators
Immunotherapy

WILSON'S DISEASE Trientine D-PCN

Weaker chelator of copper? Hypersensitivity; Rash
Copper Chelators Zinc Acetate Proteinuria
D-PCN ↑E'cytes metallothionein production Blood dyscrasias
Trientine Binds Copper > Zinc Anorexia; Nausea; Vomiting
Copper Absorption Reducers $ Traps copper inside enterocytes Trientine
Zinc Acetate Enterocyte sloughing Less SE's than D-PCN
Tetrathiomolybdate $ Copper eliminated in stools Zinc Acetate
Does not chelate copper from tissues Well-tolerated
Non-specific epigastric irritation
Pancreatitis

MENOPAUSE Φestrogen production Hot flashes

α w/ ↓Ovarian follicles with age Atrophy of Vagina
↓Estrogen Age of onset = 51 yrs old Osteroporosis
↑GnRH Early onset in smokers CAD
↑↑FSH; ↑LH
HAVOC

DIABETES
INSULIN Binds Insulin-R (liver; muscle; adipose) ↓GLU
To Tx DM $ Tyrosine Kinase activity Allergy (rare)
$ GLU --> Glycogen (Liver)
↑K+ (life-threatening) $ Synthesis of glycogen + protein (Muscle)
↑GLU $ Tryglyceride storage (Fat)

SULFONYLUREAS Close K+ channels in β-cell membrane ↓GLU

To Tx DM II (NIDDM) $ Cell depolarization Disulfiram-like effects
$ Ca2+ influx Glyburide; Glipizide
So fun you'll race a Car (hyperglycemic) $ Insulin release stimulated
Chlorpropamide Chlar pool
Glyburide Glide your ride Ca2+ / Car release
Glipizide Glip the side [of the]
Tolbutamide Toll booth

METFORMIN ??Unknown?? Lactic acidosis

To Tx ↑GLU ≠Gluconeogenesis (liver)
$ ↓GLU levels
Oral Biguanide

"Metformin = Stops GLU Formin' "

GLITAZONES ↑Targe cell response to insulin Hepatotoxic (troglitazone)

DM II MonoTx Weight gain
Combo+Above Rx's

Pioglitazone
Rosiglitazone Glitazone = Lit a zone up (↑sensitivity) Glitazone = Glutton zone --> Wt. Gain!
Troglitazone

α-GLUCOSIDASE INHIBITORS DM II MonoTx ≠Inestinal brush border α-glucosidase GI Disturbances

Combo+Above Rx's $ ↓Sugar hydrolysis and absorption
Acarbose $ ↓GLU serum levels (post-prandial)
Miglitol
DIABETIC Rx's

Endocrine Rx
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
GOUT

Colchicine Acute Gout Depolymerizes microtubules ≠GI

Indomethacin (more common) Acute Gout $ ≠Lk'cyte chemotaxis & degranulation Indomethacin < toxic
Probenecid Chronic Gout ≠Absorption of uric acid
≠PCN secretion
Allopurinol Chronic Gout ≠Xanthing oxidase
$ ↓Xanthine --> uric acid

CT Dz Rx's
 MECHANISM OF ACTION SIDE EFFECTS / TOXICITY
TUBERCULOSIS
Rifampin Combo Tx: RESPIre Hepatotoxicity (all Rx's)
Isoniazid
Pyrazinamide Prophylaxis
Ethambutol Isoniazid - INH used alone
Streptomycin

Cyclosporine (2nd line Tx)

Tx TB before it's RIPE

RESPIre

BACTERIAL PROPHYLAXIS
Meningococcal Rifampin (1st line); Minocycline
Gonorrhea Ceftriaxone
Syphilis Benzathine PCN G
Recurrent UTI's TMP/SMX
PCP 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 $ ≠Viral assembly Nausea; Diarrhea
Amprenavir "When it RAINS it pro's" Hyperglycemia
Indinavir Lipid abnormalities
Nelfinavir Thrombocytopenia (Indinavir)
Saquinavir
Reverse Transcriptase Inhibitors ≠Reverser transcriptase BM Suppression: Neutropenia; Anemia
Nevirapine $ ≠HIV incorporation into host DNA Peripheral neuropathy
Zidovudine (AZT) "Nevir Efa Delete!" Lactic acidosis (nucleosides)
Zalcitabine (ddC) $ Non-nucleoside Rash (non-nucleosides)
Stavudine (d4T) Megablastic anemia (AZT)
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) Key to Abbreviations
Varicella Zoster Virus (VZV) TK = Thimadine Kinase
Common in immunocompromised P-ase = Polymerase
Cytomegalovirus (CMV) RT = Reverse Transcriptase

RETROVIRUSES NRTI's
Nucleoside analogue Lactic acidosis
Nucleoside Analogues Target = Viral RT Severe hepatomegaly with steatosis
Cornerstone of 3X Tx for HIV Nucelotide RT inhibitor $ May be fatal
Target = Viral RT
Guidelines Non-Nucleoside RT Inhibitor (NNRTI)
Use > 3 drugs against virus Target = Viral RT
Start and stop all drugs at same time Protease Inhibitor
Evaluate risk/benefit Target = Viral Protease
Simpler regimen = better adherence Entry Inhibitor Resistance
Target = Viral Entry Base-pair mutations in RT

Infectious Dz Rx
 MECHANISM OF ACTION DOSAGE SIDE EFFECTS / TOXICITY
TETANUS - DTP Vaccine = toxoid treated w/ formaldehyde Infancy Rare
$ Altered virulence 3 Doses
Clostridium tetani Unaltered immunogenicity W/ Diphtheria and Pertussis Pre-exposed adults
$ ≈100% effective $ Allergic reaction
Booster every 10 yrs

Wound / Trauma
Passive Ab's
Active Vaccine

DIPHTHERIA - DTP Toxoid vaccine Infancy Toxicity minimal for infants

Given with Tetatnus and Pertussis Reactions at injection site (older kids)
Corynebacterium diphtheriae DT = Kids
dT = Adults (less toxins) Booster every 10 yrs

PERTUSSIS - DTP DTP > 6 mo's Febrile & local reactions (mild)
> 1 killed bacteria 1% mortality < 6mo's of age High fever
Bordetella pertussis Impure Given with Tetatnus and Pertussis Convulsions
Highly contagious Recommended > 6 yrs Encephalopathy
DTaP Serious reactions (DTP)
> 1 purified Ag's of B pertussis Milder reactions (DTaP)
P toxoid
Filamentous hemagglutinin, etc.
Better

H. FLU VACCINE Ab of Hib cap. polysacch. (> 2 yrs old) Purified PRP = > 2 yrs old
$ Purified PRP
Type B (Hib) $ T-L'cyte activation (age limited) Conjugate = 2 mo's old
$ Bacterial meningitis > 18-24 months of age
$ Ab production

Conjugate Vaccine (Infants)

$ PRP conugated to protein carrier
$ Creates T-L'cyte dependent Ag's
that infant can make Ab's to

STREP PNEUMONIA CPS's (multivalent) (> 2yrs old) CPS's (multivalent) (> 2yrs old)
$ Purified CPS's of 23 types (~95%)
#1 cause of bacterial infections T-independent Ag's ineffective <2yrs old
Bacteremia Elderly > 65yrs old; Immunocomp.
URTI Underlying Dz
Meningitis
Pneumonia Protein-CPS Conjugate (Infants) Protein-CPS Conjugate (Infants)
$ 7 valent with 80% serotype coverage
Bronchitis $ Immunogenic in infants
Otitis media
Sinusitis

POLIOMYELITIS OPV (oral live-attenuated) OPV (oral live-attenuated)

3 serotypes 4 dose schedule
Poliovirus 4 dose schedule Herd immunity

IPV (parenteral, killed) IPV (parenteral, killed)

3 serotypes 4 dose schedule
4 dose schedule

Vaccines
 ACTION DISEASE S.E. / CONTRA-INDIC.
Anterior Pituitary
Releasing Hormones
GnRH ↑LH, FSH --> Est, Prog, Test ≠Hypothalamus; Replacement Tx Suppression Test
GHRH ↑GH (G; cAMP) GH Deficiency
LHRH ↑LH --> Prog, Test
TRH ↑TSH; ↑Prl
CRH ↑ACTH
Stimulating Hormones
ACTH (cosyntropin)
ACTH (corticotropin)
FSH
TSH
hCG Insulin Resistance
HMG
Target Hormones
GH GH Deficiency; RF; Turner; PW ≠Neoplasia; DM; Carpel T
Somatostatin ↑Pituitary Dz - Acromegaly
Somatotropin
Prolactin Insulin Resistance
Posterior Pituitary
Vasopressin Agonists
Vasopressin (ADH) V1 Agonist Hypo-TN; Septic shock; GI Bleed Cardio; CVA; Short t1/2
Desmopresssin (DDAVP) V2 Agonist DI; Bed wetting; Hemophliacs
Vasopressin Antagonists
Oxytocin ↑Uterine cont.; Milk eject
Dopamine Agonists
Bromocriptine Binds D2-r --> Blocks Prl Prolactinoma
Cabergoline Binds D2-r --> Blocks Prl Prolactinoma

Anterior Pituitary
Thyroid
Thyroxine (T4)
Triiodothyronine (T3)
Iodide
PTU (Propylthiouracil) ≠Thyroid peroxidase --> ≠T4-->THyperthyroidism
Parathryroid
Hypo-Ca2+
Ca2+ Gluc/Lac/Citrate Ca2+ Supplement
Thiazied Diuretic Ca2+ Sparing diuretic
Mg2+ Mg2+ Supplement
Drisdol Vit D2 Supplement
Dihydrotachysterol (DHT) Vitamin D analog
Calciferol Vitamin D analog: 1,25-OHD
Calcitriol Vitamin D analog
Hydroxyapatite
PTH (teriparatide)

Osteoporosis
Calcitonin (salmon)
Alendronate Aminobisphosphonate
Risedronate Aminobisphosphonate
Raloxifene Selective Estrogen-R Mod.
Estradiol
Paget's Dz
Alendronate Bisphosphonate; ↓Resorption Upper GI Sx's
Risedronate Bisphosphonate; ↓Resorption
Pamidronate Bisphosphonate; ↓Resorption Acute phase reaction
Mithramycin (Caution!) Bisphosphonate; ↓Resorption Caution!
Tiludronate Bisphosphonate; ↓Resorption
Osteomalacia
Vit D (1,25 OHD or DHT)
Ca2+ Supplements
Phosphate Supplements Soft tissue Ca2+

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

Pancreas
Adrenal Cortex
Corticosteroids
Hydrocortisone Adrenal I; Surgery; Inflammation Adrenal Insuff; O-Porosis; ↓GH
Cortisone Short
Cortisol Short
Prednisone Intermediate
Prednisolone Intermediate
Dexamethasone Long TEST: CAH; Adrenal Dz
Mineral Corticoid
Fludrocortisone 10X Cortisol!!
Aldosterone
≠Steroid Genesis Cushings
Mitotane Adrenotoxic --> ≠Enzymes GI; Neuro; Severe!!
Ketoconazole ≠Multiple enzymes GI; Hepatic dysfunction
Aminoglutethimide ≠Multiple enzymes Neuro; Fever; Rash
Metyrapone ≠11-β-hydroxylase GI; HTN; Acne; Hirsutism
Trilostane ≠3-β-Hydroxysteroid dehyd. GI; Parasthesias
Kidney

Dexomethazone Suppresses ACTH 1' ↑ALD 2' Adrenal insufficiency

Octreotide
K+ Sparing Diuretic
Amiloride ≠Na+ reabsorption in DT / CD 1' ↑ALD ↑K+
Spironolactone ≠p450; ≠ALD-r; ≠Androgen-r 1' ↑ALD; ↑Androgenism Gynecomastia; ↑K+

Adrenal Cortex / Kidney

Gonads
Testolactone
Testosterone
Estradiol
Ethinyl Estradiol
Norgestrel
Progesterone Insulin Resistance
Fluoxymesterone
Medroxyprogesterone
Mestranol
Male Dev't Hormones
MIS Anti-mullerian hormone
Testosterone Testicular descent; Wolff duct d
Dihydrotestosterone

Gonads
ANTIBIOTICS - SITES OF ACTION

Antibacterial Tree
ANTIBIOTICS - SITES OF ACTION

Antibiotics
ANTIVIRALS - SITES OF ACTION

Antivirals
INDICATIONS MECHANISM OF ACTION SIDE EFFECTS / TOXICITY

TEMPLATE