1st pharm test

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tyrosine hydroxylase: tyrosine -> DOPA
(-)metyrosine
Dopa Decarboxylase (aromatic L-aminoacid decarboxylase): DOPA -> dopamine
(-) carbidopa
Dopamine b hydroxylase: dopamine -> NE
(-) disulfiram (antabase)
momoamine oxidase: breaks down catecholmines to aldehydes
catechol O methyltransferase: NE -> normetanephrine
Unfractioned heparin: indirect thromnin and Xa inhibitor
LMW heparin: Indirect Xa inhibitor
Less variability and monitoring than heparin
slower clearance than heparin
Protamine: tx for heparin overdose
Fondaparinux: pentasaccharide factor Xa inhibitor
Lepirudin: direct thrombin inhibitor
tx HIT
renal clearance
Argatroban: Direct thrombin inhibitor (active site only), tx HIT, liver metab
Bivalrudin: Direct thrombin inhibitor, tx angioplasty, renal clearance
Hirudin: Direct thrombin inhibitor, leech recombinant protein
Warfarin (Coumadin): Vitamin K antagonist -- â†“post-translational carboxylase, â†“factor 2,7,9,10,C,S, INR
Aspirin: Irreversibly acylates cyclooxygenase, blocking TxA2 synth
Dipyridamole (Persantine): Inhibits PDE -> â†‘cAMP
ASA w/ Dipyridamole (Aggrenox): good stroke preventing combination
Ticlopidine (Ticlid): Inhibit ADP platelet activation, more potent
Clopidogrel (Plavix): Inhibit ADP platelet activation, less potent
Abciximab (Reopro): GP IIb/IIIa antagonist prevents fibrinogen binding
Ibopamine: ORAL AGENT FOR â†‘ CONTRACTILITY
Dopaminergic agonist
Inamrinone (Amrinone): ORAL AGENTS FOR â†‘ CONTRACTILITY
PDE inhibitor â†‘cAMP -> â†‘CO and â†“SVR, short-term CHF tx, â†‘AV cond, ARR, oral â†‘toxic
Milrinone (Primacor): ORAL AGENTS FOR â†‘ CONTRACTILITY
Shorter Ï„ (30 min vs 2.5 h), more selective, fewer side fx (e.g. thrombocytopenia, gi, liver, fever)
Pimobendan: ORAL AGENTS FOR â†‘ CONTRACTILITY
PDE inhibitor w/ Ca sensitizing properties
Nesiritide: ORAL AGENTS FOR â†‘ CONTRACTILITY
Natriuretic peptide
Omapatrilat: ORAL AGENTS FOR â†‘ CONTRACTILITY
Neutral endopeptidase inhibitorâ€”blocks both ACE and natriuretic peptide degradation
Streptokinase (SK): Plasminogen activator

1° Non-enzymatic protein from streptococci, indirect, antibodies to drugy -> agg
Urokinase (UK): Plasminogen activator

1° Trypsin-like enzyme, LMW, direct, (-) PAI-1, non-antigenic
Aniosylated Plasminogen Streptokinase Complex (APSAC): PLASMINOGEN ACTIVATOR

2Â° SK and human plasminogen complex -> spontaneous deacylation, long Ï„ (60m), IV bolus, Ab
t-PA (Alteplase): PLASMINOGEN ACTIVATOR

2Â° Fibrin/clot-specific binding (1000x), glycosylation, short Ï„ (6m), (-) PAI-1
Reteplase: PLASMINOGEN ACTIVATOR

3Â° t-PA derivative, kringle #2 and protease domain, non-glycosylated, no EGF -> longer Ï„ (15m)
TNK-t-PA (Tenecteplase): PLASMINOGEN ACTIVATOR

3Â° no glycosylation, less PAI-1 effect, â†‘ fibrin specificity
Amicar (ε-aminocaproic acid) Tranexamic acid: PLASMINOGEN ACTIVATOR

Antifibrinolytic â€“ inhibits plasmin to stop bleeding
Quinidine: Intermediate recovery (1-5s), â†‘ QRS, QT, APD, blocks Na and K channels;

Î± receptor block and vagal inhibition; â†‘[DIG]
Procainamide -> N-acetylprocainamide (NAPA): Intermediate recovery (1-5s), â†‘ QRS, QT, APD, blocks Na and K channels;

Metabolite blocks K channels only, renal dose adjustment, lupus syndrome
Disopyramide: Intermediate recovery (1-5s), â†‘ QRS, QT, APD, blocks Na and K channels;

Aggravates CHF and prostatism, effect â†‘ with dose
Lidocaine: Fast recovery (<1s), shorten repolarization

IV, â†“ v-fib, â†‘ mortality, CNS toxicity, dose adjustment (CHF and liver)
Mexiletine, Tocainide: Fast recovery (<1s), shorten repolarization

Oral ,CNS toxic
Phenytoin: Fast recovery (<1s), shorten repolarization

Anticonvulsant, effective for digitalis intoxication
Flecainide: Slow recovery, marked â†‘PR, â†‘QRS, Â± QT

Very long Ï„ from block, very effective for isolated PVC, RSVT, â†‘DIG
Encainide: Slow recovery, marked â†‘PR, â†‘QRS, Â± QT

â†‘ mortality post-MI, FDA removed
Propafenone: Slow recovery, marked â†‘PR, â†‘QRS, Â± QT

~ Flecainide, Weak ÃŸ blocker (â†‘ at high conc),
Moricizine: Slow recovery, marked â†‘PR, â†‘QRS, Â± QT

Phenothiazine analog, unique, weaker version, multiple metabolites
Esmolol: Ultra short acting (Ï„ = 9m), nonselective ÃŸ blocker, good for testing
Amiodarone: K CHANNEL BLOCKERS, â†‘ AP DURATION, â†‘ QT

Class I,II,III,IV actions, effective most arr, multiple toxic (esp lung), LONG Ï„ (50d), â†‘DIG
Bretylium: K CHANNEL BLOCKERS, â†‘ AP DURATION, â†‘ QT

No longer marketed, still available â€“ biphasic NE effects (â†‘ then â†“)
Dofetilide: K CHANNEL BLOCKERS, â†‘ AP DURATION, â†‘ QT

Pure class III, Renal dose adjustment, causes TdP (1-3%)
Sotalol: K CHANNEL BLOCKERS, â†‘ AP DURATION, â†‘ QT

Non-selective ÃŸ blocker, causes TdP
Ibutilide: K CHANNEL BLOCKERS, â†‘ AP DURATION, â†‘ QT

Acute IV, stop A-flutter (60%) and A-fib (40%), block K, opens Na, Causes TdP (6%)
*N-acetylprocainamide: K CHANNEL BLOCKERS, â†‘ AP DURATION, â†‘ QT

Might have some class III effects
Verapamil (phenylalkylamine): L channel, â†“ino, chrono, dromotropy, SVT, L isomer more active, PGP inhibition->DIGItoxic
Diltiazem (benzothiazepines): L channel, â†“ino, chrono, dromotropy, SVT, PGP inhibition->DIGItoxic
Adenosine: Purinergic receptor blocker, ultra-short acting AV blocker (seconds) â€“ acute tx, rapid IV, short Sx
Captopril: â†‘ BRADYKININ, RENIN, ANG I, â†“ANGIOTENSION II

Sulfhydryl, shorter Ï„, prostaglandin effect
Fosinopril: â†‘ BRADYKININ, RENIN, ANG I, â†“ANGIOTENSION II

Phosphinyl, L&K
Trandolapril: â†‘ BRADYKININ, RENIN, ANG I, â†“ANGIOTENSION II

Carboxyl, L&K
Saralasin: ANGIOTENSIN RECEPTOR BLOCKERS, â†‘ ANGIOTENSIN II, FETOTOXIC

Original, IV, partial agonist
Losartan -> EXP-3174: ANGIOTENSIN RECEPTOR BLOCKERS, FETOTOXIC

Non-peptide, short Ï„, normal-high renin levels, uricosuric effect
Mannitol: MOST OF TUBULE: IV VOLUME EXPANSION (FILTERED, NOT REABSORBED)

IV
Acetazolamide (Diamox): Proximal tubule: â†“NAHCO3 REABSORPTION (METABOLIC ACIDOSIS), SULFONAMIDES

Tx glaucoma
Furosemide (Lasix): Thick acending loop: NAKCL2 SYMPORT INHIBITOR, MOST POTENT, CA AND MG LOSS

Releases vasodilator prostaglandin from kidneys ïƒ â†‘ venous capacitance
Ethacrynic Acid (Edecrin): Thick acending loop: NAKCL2 SYMPORT INHIBITOR, MOST POTENT, CA AND MG LOSS

Non-sulfamide
Hydrochlorothiazide (HCTZ, Esidrex): DCT: NACL COTRANSPORT INHIBITOR, â†‘ GLU,UREA,CA; â†“ K,H,NA

Sulfonamide, hyperuricemia ïƒ gout; tx diabetes insipidus
Amiloride: Collecting Tube: NA CHANNEL INHIBITORS, â†“ K EXCRETION; CAREFUL! (ACEI, â†‘K, ARF)

Partially absorbed; inhibits NaH antiporter (lumen) and NaK ATPas (basal); tx Liddleâ€™s
Triamterene: Collecting Tube: NA CHANNEL INHIBITORS, â†“ K EXCRETION; CAREFUL! (ACEI, â†‘K, ARF)

Well absorbed, renal and metabolism
Spironolactone -> Canrenone: STEROID ANALOGUES COMPETE WITH ALDOSTERONE, BEST FOR CIRRHOSIS

Affects estrogen receptors (gynecomastia), tx Cohnâ€™s
Nifedipine (1,4-dihydropyridine): â†“ CA -> VASODILATION, LONG ACTING, INHIBIT CYP3A4

L channel, â†‘ chronotropy and CO, â†‘ symp, variable partition coefficients, oral > sublingual
Dantrolene: â†“ Ca release -> relax muscles, tx malignant hyperthermia
Nitroglycerin (TNG): Nitrate ester, Sublingual, high clearance (minutes)
IsoSorbide DiNitrate (Isordil): Nitrate ester, Oral, variable Ï„ of metabolites, intermediate clearance
Isosorbide MonoNitrates (2-IMN > 5-IMN): Nitrate ester, 100% bioavailable, less variable, low clearance
**Sildenafil (Viagra): Inhibits cGMP phosphodiesterase V ïƒ â†‘postural hypotension
Nitroprusside (Nipride)  NO + CN: Spontaneous conversion to NO + CN, Thiocyanate toxicity (tx Na thiosulfate), no light, short Ï„
Hydralazine (Apresoline): Arterial vasodilator, tx HT & CHF
Minoxidil (Loniten): Arterial vasodilator, tx HT

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Deck Info

Number of cards 75