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79 Cards in this Set
- Front
- Back
tyrosine hydroxylase
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tyrosine -> DOPA
(-)metyrosine |
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Dopa Decarboxylase
(aromatic L-aminoacid decarboxylase) |
DOPA -> dopamine
(-) carbidopa |
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Dopamine b hydroxylase
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dopamine -> NE
(-) disulfiram (antabase) |
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momoamine oxidase
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breaks down catecholmines to aldehydes
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catechol O methyltransferase
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NE -> normetanephrine
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Unfractioned heparin
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indirect thromnin and Xa inhibitor
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LMW heparin
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Indirect Xa inhibitor
Less variability and monitoring than heparin slower clearance than heparin |
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Protamine
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tx for heparin overdose
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Fondaparinux
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pentasaccharide factor Xa inhibitor
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Lepirudin
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direct thrombin inhibitor
tx HIT renal clearance |
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Argatroban
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Direct thrombin inhibitor (active site only), tx HIT, liver metab
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Bivalrudin
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Direct thrombin inhibitor, tx angioplasty, renal clearance
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Hirudin
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Direct thrombin inhibitor, leech recombinant protein
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Warfarin (Coumadin)
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Vitamin K antagonist -- ↓post-translational carboxylase, ↓factor 2,7,9,10,C,S, INR
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Aspirin
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Irreversibly acylates cyclooxygenase, blocking TxA2 synth
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Dipyridamole (Persantine)
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Inhibits PDE -> ↑cAMP
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ASA w/ Dipyridamole (Aggrenox)
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good stroke preventing combination
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Ticlopidine (Ticlid)
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Inhibit ADP platelet activation, more potent
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Clopidogrel (Plavix)
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Inhibit ADP platelet activation, less potent
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Abciximab (Reopro)
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GP IIb/IIIa antagonist prevents fibrinogen binding
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Ibopamine
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ORAL AGENT FOR ↑ CONTRACTILITY
Dopaminergic agonist |
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Inamrinone (Amrinone)
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ORAL AGENTS FOR ↑ CONTRACTILITY
PDE inhibitor ↑cAMP -> ↑CO and ↓SVR, short-term CHF tx, ↑AV cond, ARR, oral ↑toxic |
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Milrinone (Primacor)
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ORAL AGENTS FOR ↑ CONTRACTILITY
Shorter τ (30 min vs 2.5 h), more selective, fewer side fx (e.g. thrombocytopenia, gi, liver, fever) |
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Pimobendan
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ORAL AGENTS FOR ↑ CONTRACTILITY
PDE inhibitor w/ Ca sensitizing properties |
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Nesiritide
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ORAL AGENTS FOR ↑ CONTRACTILITY
Natriuretic peptide |
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Omapatrilat
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ORAL AGENTS FOR ↑ CONTRACTILITY
Neutral endopeptidase inhibitor—blocks both ACE and natriuretic peptide degradation |
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Digoxin
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INHIBITS NAKATPASE -> ↑ CALCIUM; TREAT CHF, ARRHYTHMIAS;
Preferred, Renal excretion, shorter τ (1.6d), SS@1 wk, metabolized by gut bacteria (10%) |
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Digitoxin
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INHIBITS NAKATPASE ↑ CALCIUM; TREAT CHF, ARRHYTHMIAS;
No 12-OH, Hepatic metab, longer τ (7d), ss@1 mo |
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Streptokinase (SK)
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Plasminogen activator
1° Non-enzymatic protein from streptococci, indirect, antibodies to drugy -> agg |
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Urokinase (UK)
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Plasminogen activator
1° Trypsin-like enzyme, LMW, direct, (-) PAI-1, non-antigenic |
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Aniosylated Plasminogen Streptokinase Complex (APSAC)
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PLASMINOGEN ACTIVATOR
2° SK and human plasminogen complex -> spontaneous deacylation, long τ (60m), IV bolus, Ab |
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t-PA (Alteplase)
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PLASMINOGEN ACTIVATOR
2° Fibrin/clot-specific binding (1000x), glycosylation, short τ (6m), (-) PAI-1 |
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Reteplase
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PLASMINOGEN ACTIVATOR
3° t-PA derivative, kringle #2 and protease domain, non-glycosylated, no EGF -> longer τ (15m) |
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TNK-t-PA (Tenecteplase)
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PLASMINOGEN ACTIVATOR
3° no glycosylation, less PAI-1 effect, ↑ fibrin specificity |
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Amicar (ε-aminocaproic acid)
Tranexamic acid |
PLASMINOGEN ACTIVATOR
Antifibrinolytic – inhibits plasmin to stop bleeding |
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Quinidine
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Intermediate recovery (1-5s), ↑ QRS, QT, APD, blocks Na and K channels;
α receptor block and vagal inhibition; ↑[DIG] |
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Procainamide -> N-acetylprocainamide (NAPA)
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Intermediate recovery (1-5s), ↑ QRS, QT, APD, blocks Na and K channels;
Metabolite blocks K channels only, renal dose adjustment, lupus syndrome |
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Disopyramide
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Intermediate recovery (1-5s), ↑ QRS, QT, APD, blocks Na and K channels;
Aggravates CHF and prostatism, effect ↑ with dose |
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Lidocaine
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Fast recovery (<1s), shorten repolarization
IV, ↓ v-fib, ↑ mortality, CNS toxicity, dose adjustment (CHF and liver) |
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Mexiletine, Tocainide
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Fast recovery (<1s), shorten repolarization
Oral ,CNS toxic |
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Phenytoin
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Fast recovery (<1s), shorten repolarization
Anticonvulsant, effective for digitalis intoxication |
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Flecainide
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Slow recovery, marked ↑PR, ↑QRS, ± QT
Very long τ from block, very effective for isolated PVC, RSVT, ↑DIG |
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Encainide
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Slow recovery, marked ↑PR, ↑QRS, ± QT
↑ mortality post-MI, FDA removed |
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Propafenone
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Slow recovery, marked ↑PR, ↑QRS, ± QT
~ Flecainide, Weak ß blocker (↑ at high conc), |
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Moricizine
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Slow recovery, marked ↑PR, ↑QRS, ± QT
Phenothiazine analog, unique, weaker version, multiple metabolites |
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Esmolol
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Ultra short acting (τ = 9m), nonselective ß blocker, good for testing
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Amiodarone
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K CHANNEL BLOCKERS, ↑ AP DURATION, ↑ QT
Class I,II,III,IV actions, effective most arr, multiple toxic (esp lung), LONG τ (50d), ↑DIG |
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Bretylium
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K CHANNEL BLOCKERS, ↑ AP DURATION, ↑ QT
No longer marketed, still available – biphasic NE effects (↑ then ↓) |
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Dofetilide
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K CHANNEL BLOCKERS, ↑ AP DURATION, ↑ QT
Pure class III, Renal dose adjustment, causes TdP (1-3%) |
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Sotalol
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K CHANNEL BLOCKERS, ↑ AP DURATION, ↑ QT
Non-selective ß blocker, causes TdP |
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Ibutilide
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K CHANNEL BLOCKERS, ↑ AP DURATION, ↑ QT
Acute IV, stop A-flutter (60%) and A-fib (40%), block K, opens Na, Causes TdP (6%) |
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*N-acetylprocainamide
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K CHANNEL BLOCKERS, ↑ AP DURATION, ↑ QT
Might have some class III effects |
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Verapamil (phenylalkylamine)
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CA CHANNEL BLOCKERS, ↓ HR AND ↑ PR
Most potent AV blocking, hypotensive; AVOID: wide-complex tachy,WPW,CHF,AVblock,DIG |
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Diltiazem (benzothiazepines)
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CA CHANNEL BLOCKERS, ↓ HR AND ↑ PR
IV, AV node blocking w/o hypotension, great for A-fib |
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Adenosine
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Purinergic receptor blocker, ultra-short acting AV blocker (seconds) – acute tx, rapid IV, short Sx
|
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Captopril
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↑ BRADYKININ, RENIN, ANG I, ↓ANGIOTENSION II
Sulfhydryl, shorter τ, prostaglandin effect |
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Fosinopril
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↑ BRADYKININ, RENIN, ANG I, ↓ANGIOTENSION II
Phosphinyl, L&K |
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Trandolapril
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↑ BRADYKININ, RENIN, ANG I, ↓ANGIOTENSION II
Carboxyl, L&K |
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Saralasin
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ANGIOTENSIN RECEPTOR BLOCKERS, ↑ ANGIOTENSIN II, FETOTOXIC
Original, IV, partial agonist |
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Losartan -> EXP-3174
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ANGIOTENSIN RECEPTOR BLOCKERS, FETOTOXIC
Non-peptide, short τ, normal-high renin levels, uricosuric effect |
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Mannitol
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MOST OF TUBULE: IV VOLUME EXPANSION (FILTERED, NOT REABSORBED)
IV |
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Acetazolamide (Diamox)
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Proximal tubule: ↓NAHCO3 REABSORPTION (METABOLIC ACIDOSIS), SULFONAMIDES
Tx glaucoma |
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Furosemide (Lasix)
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Thick acending loop: NAKCL2 SYMPORT INHIBITOR, MOST POTENT, CA AND MG LOSS
Releases vasodilator prostaglandin from kidneys ↑ venous capacitance |
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Ethacrynic Acid (Edecrin)
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Thick acending loop: NAKCL2 SYMPORT INHIBITOR, MOST POTENT, CA AND MG LOSS
Non-sulfamide |
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Hydrochlorothiazide (HCTZ, Esidrex)
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DCT: NACL COTRANSPORT INHIBITOR, ↑ GLU,UREA,CA; ↓ K,H,NA
Sulfonamide, hyperuricemia gout; tx diabetes insipidus |
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Amiloride
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Collecting Tube: NA CHANNEL INHIBITORS, ↓ K EXCRETION; CAREFUL! (ACEI, ↑K, ARF)
Partially absorbed; inhibits NaH antiporter (lumen) and NaK ATPas (basal); tx Liddle’s |
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Triamterene
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Collecting Tube: NA CHANNEL INHIBITORS, ↓ K EXCRETION; CAREFUL! (ACEI, ↑K, ARF)
Well absorbed, renal and metabolism |
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Spironolactone -> Canrenone
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STEROID ANALOGUES COMPETE WITH ALDOSTERONE, BEST FOR CIRRHOSIS
Affects estrogen receptors (gynecomastia), tx Cohn’s |
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Nifedipine (1,4-dihydropyridine)
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↓ CA -> VASODILATION, LONG ACTING, INHIBIT CYP3A4
L channel, ↑ chronotropy and CO, ↑ symp, variable partition coefficients, oral > sublingual |
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Verapamil (phenylalkylamine)
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L channel, ↓ino, chrono, dromotropy, SVT, L isomer more active, PGP inhibition->DIGItoxic
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Diltiazem (benzothiazepines)
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L channel, ↓ino, chrono, dromotropy, SVT, PGP inhibition->DIGItoxic
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Dantrolene
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↓ Ca release -> relax muscles, tx malignant hyperthermia
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Nitroglycerin (TNG)
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Nitrate ester, Sublingual, high clearance (minutes)
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IsoSorbide DiNitrate (Isordil)
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Nitrate ester, Oral, variable τ of metabolites, intermediate clearance
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Isosorbide MonoNitrates (2-IMN > 5-IMN)
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Nitrate ester, 100% bioavailable, less variable, low clearance
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**Sildenafil (Viagra)
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Inhibits cGMP phosphodiesterase V ↑postural hypotension
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Nitroprusside (Nipride) NO + CN
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Spontaneous conversion to NO + CN, Thiocyanate toxicity (tx Na thiosulfate), no light, short τ
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Hydralazine (Apresoline)
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Arterial vasodilator, tx HT & CHF
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Minoxidil (Loniten)
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Arterial vasodilator, tx HT
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