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263 Cards in this Set
- Front
- Back
ALPHA-1 AGONISTS
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arterial vasoconstriction, ↑ contractility
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Phenylephrine (Neosynephrine)
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Pure and potent, tx paroxysmal a-tach
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Methoxamine
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Pure and potent
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Norepinephrine
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Shock
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Epinephrine
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↑ BP
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Dopamine
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Low dose
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ALPHA-1 ANTAGONISTS
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Phentolamine
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IV, Nonselective, competitive, short-acting, Dx pheo, block 5HT
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Phenoxybenzamine
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Oral, Nonselective, noncompetitive, long-acting, Tx pheo
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Prazosin (Minipress)
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Selective α1 blocker, prazosin syncope, first dose effect, tachyphylaxis (tolerance)
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Terazosin (Hytrin)
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Selective α1 blocker, longer τ (less first dose effect), Tx BPH
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Doxazosin (Cardura)
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Tamsulosin (Flomax)
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Urological indications
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Alfuzosin (Urotraxal)
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ALPHA-2 AGONISTS
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Venous vasoconstriction, ↓ NE @ sympathetics
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Clonidine (Catapres)
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↓BP and CNS, Clonidine rebound, mild ↓ cholesterol, Raynaud’s, ↓ CNS
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Methyldopa (Aldomet) à α-methylnorepinephrine
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↓BP and CNS, safer mild CO effect, delay in onset (6 hrs), hemolytic anemia (rare)
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Tizanidine (Zanaflex)
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Shorter τ (2 hrs), rebound, tx muscular spasm
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Guanfacine
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Long τ (17 hrs), less withdrawl
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Guanabenz
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ALPHA-2 ANTAGONISTS
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↑ sympathetics, ↑ NE release
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Yohimbine
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Aphrodisiac
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Phentolamine
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α1 and α2 antagonists
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Phenoxybenzamine
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BETA AGONISTS
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Isoproterenol
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Non-selective, ↑HR, CO, contractility
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Dobutamine
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ß1 selective, no ΔBP
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BETA ANTAGONISTS
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nonselective tx: portal HT, tremor, vascular headache
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Propranolol (Inderal) – the original
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Non-selective, cheap, heavy liver metab
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Metoprolol (Lopressor)
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ß1 selective, no bronchoconstriction (asthma), ß2 hyperresponse?
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Atenolol (Tenormin)
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ß1 selective, no bronchoconstriction (asthma)
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Nadolol (Corgard)
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Not lipophilic, Europe, ~ Propranolol
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Esmolol
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Short τ for IV use, critical care
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Labetalol
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α1 blocker (S,R), ↑ potency orally; ß1 antag and partial ß2 agonist (R,R: higher clearance) [1:7]
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Carvedilol
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Potent α1 blocker à ↓PVR à tx CHF, racemic mixture
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Pindolol
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Some agonist activity
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Timolol
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Tx glaucoma
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DOPAMINE receptor Drugs
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D1 – vasodilation, D2 – emesis, ↓prolactin, D4 – risk taking
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Bromocriptine
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Dopamine Agonists
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Fenoldopam (9x D1)
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Apomorphine
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Metoclopramide
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Dopamine Antagonists
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Haloperidol
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Domperidone
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INDIRECT-ACTING Phenylethylamines
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Tyramine
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Displaces NE into synaptic cleft – cheese, wine, ham
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Ephedrine (Ephedra, Ma Huang)
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Weight loss, ↑ SKM and CNS
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Amphetamine
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More potent CNS
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Hydroxyamphetamine
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Tyramine-like, test for more central Horner’s syndrome
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Phenylpropanolamine (Dexatrim)
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Sympathomimetic and vasoconstriction
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Pseudoephedrine (Sudafed)
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Replacement Dexatrim analog
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MUSCARINIC AGONISTS
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Acetylcholine
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Rapid hydrolysis, rarely used
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Bethanechol
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Gastric emptying, tx urinary retention
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Pilocarpine
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Miosis and salivation, Tx open-angle glaucoma
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Methacholine
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Bronchoconstriction, methacholine challenge
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Carbachol
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Muscarine, Arecholine
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Naturally occurring
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MUSCARINIC ANTAGONISTS
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Atropine – Deadly nightshade (Atropa belladonna)
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↑HR, dilate pupils
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Jimson Weed (Datura stramonium)
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Hallucinogen
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Hyoscine – Henbane (Hyoscyamus niger)
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Hallucinogen
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Pirenzepine
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M1 selective blocker, gastric acid release
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NICOTINIC AGONISTS
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Nicotine
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↑Symp & PS, Bezold-Jarisch reflex
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NICOTINIC ANTAG/ SKM RELAXANT
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Respirator, histamine release
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Tubocuranine
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Nondepolarizing blocker, long τ, reversible by adding ACh
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Succinylcholine
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Depolarizing blocker, short τ, Pseudocholinesterase deficiency
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ANTICHOLINESTERASES
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SLUDGE
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Physostigmine
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Enters CNS à restless, apprehension, HT, nausea
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Neostigmine
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Does not enter CNS, tx myasthenia gravis & glaucoma
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Edrophonium (Tensilon)
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Treat MG
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Ambenonium
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Pyridostigmine
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Parathion à Paraoxon
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Phosphorothionates à oxidation ↑AChE
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Malathion
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Insecticide
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Tacrine (Cognex)
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ALZ, L toxic
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Donezapil (Aricept)
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ALZ, replaced Tacrine
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Rivastigmine (Exelon)
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Pralidoxime
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Counteracts AChE’s and reactivates ChE
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WAR GASES
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Organophosphates – insecticides -- ↑ ALL cholinergic transmission (N&M)
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Sarin Gas
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Irreversible cholinesterase inhibitors (N & M)
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VX
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Binary agents, death by asphyxiation
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SPASMOLYTICS
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Dantrolene
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↓ Ca release à relax muscles, tx malignant hyperthermia
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Baclofen
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Muscle relaxant, partial GABA agonist
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Diazepam
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Anti-anxiety agents that ↓ nerves in muscles
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Chlordiazepoxide
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Carisoprodol
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Meprobamate
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Strychnine
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Glycine antagonist à ↑ respiration, convulsions
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NO-DEPENDENT VASODILATORS
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A&V vasodilation, SM relaxation, Tolerance
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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 à ↑postural hypotension
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Nitroprusside (Nipride) à NO + CN
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Spontaneous conversion to NO + CN, Thiocyanate toxicity (tx Na thiosulfate), no light, short τ
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DIRECT VASODILATORS
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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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CALCIUM CHANNEL BLOCKERS
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↓ Ca à vasodilation, long acting, inhibit CYP3A4
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Nifedipine (1,4-dihydropyridine)
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L channel, ↑ chronotropy and CO, ↑ symp, variable partition coefficients, oral > sublingual
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Amlodipine
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High partition coefficient à high Vd, slow onset of action, prolonged duration
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Verapamil (phenylalkylamine)
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L channel, ↓ino, chrono, dromotropy, SVT, L isomer more active, PGP inhibitionàDIGItoxic
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Diltiazem (benzothiazepines)
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L channel, ↓ino, chrono, dromotropy, SVT, PGP inhibitionàDIGItoxic
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Mibefradil
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T Channel, FDA removed, vasodilation > cardiac depression
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Angiotensin Converting Enzyme Inhibitors
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↑ bradykinin, renin, ang I, ↓angiotension II
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Captopril
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Sulfhydryl, shorter τ, prostaglandin effect
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Fosinopril
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Phosphinyl, L&K
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Trandolapril
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Carboxyl, L&K
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Enalapril
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Carboxyl
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Lisinopril
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Benazepril
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Quinapril
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Ramipril
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Trandolapril
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Moexipril
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Angiotensin Receptor Blockers
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↑ bradykinin, renin, ang I, ↑ angiotensin II, fetotoxic
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Saralasin
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Original, IV, partial agonist
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Losartan à EXP-3174
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Non-peptide, short τ, normal-high renin levels, uricosuric effect
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Valsartan
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Irbesartan
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Candesartan
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Osmotic Diuretics
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Most of tubule: IV volume expansion (filtered, not reabsorbed)
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Mannitol
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IV
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Urea
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IV
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Glycerin
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Oral
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Carbonic Anhydrase Inhibitors
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PT: ↓NaHCO3 reabsorption (metabolic acidosis), sulfonamides
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Acetazolamide (Diamox)
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Tx glaucoma
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Dichlorphenamide
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Loop Diuretics (high ceiling)
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TALH: NaKCl2 symport inhibitor, MOST potent, Ca and Mg loss
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Furosemide (Lasix)
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Releases vasodilator prostaglandin from kidneys à ↑ venous capacitance
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Bumetanide (Bumex)
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Ethacrynic Acid (Edecrin)
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Non-sulfamide
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Torsemide (Demadex)
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Thiazides
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DCT: NaCl cotransport inhibitor, ↑ Glu,Urea,Ca; ↓ K,H,Na
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Chlorothiazide (Diuril)
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Hydrochlorothiazide (HCTZ, Esidrex)
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Sulfonamide, hyperuricemia à gout; tx diabetes insipidus
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Chlorthalidone (Hygroton)
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Metolazone (Zaroxolyn)
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K Sparing Diuretics
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CT: Na channel inhibitors, ↓ K excretion; careful! (ACEI, ↑K, ARF)
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Amiloride
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Partially absorbed; inhibits NaH antiporter (lumen) and NaK ATPas (basal); tx Liddle’s
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Triamterene
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Well absorbed, renal and metabolism
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Aldosterone Antagonists
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steroid analogues compete with aldosterone, best for cirrhosis
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Spironolactone à Canrenone
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Affects estrogen receptors (gynecomastia), tx Cohn’s
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Eplerenone
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Newer version
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ADH Antagonists
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CT: ↓ADH effects and ↓water reabsorption
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Demeclocycline (Declomycin)
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Tetracycline derivative; tx SIADH
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ANTIARRYTHMIC DRUGS
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Class I
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Na Channel Blockers, “local anesthetics”
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Class Ia
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Intermediate recovery (1-5s), ↑ QRS, QT, APD, blocks Na and K channels;
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Quinidine
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α receptor block and vagal inhibition; ↑DIG
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Procainamide à N-acetylprocainamide (NAPA)
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Metabolite blocks K channels only, renal dose adjustment, lupus syndrome
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Disopyramide
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Aggravates CHF and prostatism, effect ↑ with dose
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Class Ib
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Fast recovery (<1s), shorten repolarization
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Lidocaine
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IV, ↓ v-fib, ↑ mortality, CNS toxicity, dose adjustment (CHF and liver)
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Mexiletine
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Oral, CNS toxic
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Tocainide
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Oral ,CNS toxic, agranulocytosis
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Phenytoin
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Anticonvulsant, effective for digitalis intoxication
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Class Ic
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Slow recovery, marked ↑PR, ↑QRS, ± QT
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Flecainide
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Very long τ from block, very effective for isolated PVC, RSVT, ↑DIG
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Encainide
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↑ mortality post-MI, FDA removed
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Propafenone
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~ Flecainide, Weak ß blocker (↑ at high conc),
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Moricizine
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Phenothiazine analog, unique, weaker version, multiple metabolites
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Class II
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Beta Blockers, ↓ HR and ↑ PR (slow down)
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Esmolol
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Ultra short acting (τ = 9m), nonselective ß blocker, good for testing
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Propranolol
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Sotalol
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Esmolol
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Timolol
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Acebutolol
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Class III
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K channel blockers, ↑ AP duration, ↑ QT
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Amiodarone
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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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No longer marketed, still available – biphasic NE effects (↑ then ↓)
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Dofetilide
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Pure class III, Renal dose adjustment, causes TdP (1-3%)
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Sotalol
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Non-selective ß blocker, causes TdP
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Ibutilide
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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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Might have some class III effects
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Class IV
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Ca channel blockers, ↓ HR and ↑ PR
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Verapamil (phenylalkylamine)
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Most potent AV blocking, hypotensive; AVOID: wide-complex tachy,WPW,CHF,AVblock,DIG
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Diltiazem (benzothiazepines)
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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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THROMBOLYTIC
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plasminogen activators
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Streptokinase (SK)
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1° Non-enzymatic protein from streptococci, indirect, antibodies to SK à agg
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Urokinase (UK)
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1° Trypsin-like enzyme, LMW, direct, (-) PAI-1, non-antigenic
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Aniosylated Plasminogen Streptokinase Complex (APSAC)
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2° SK and human plasminogen complex à spontaneous deacylation, long τ (60m), IV bolus, Ab
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t-PA (Alteplase)
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2° Fibrin/clot-specific binding (1000x), glycosylation, short τ (6m), (-) PAI-1
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Reteplase
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3° t-PA derivative, kringle #2 and protease domain, non-glycosylated, no EGF à longer τ (15m)
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TNK-t-PA (Tenecteplase)
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3° no glycosylation, less PAI-1 effect, ↑ fibrin specificity
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Amicar (ε-aminocaproic acid)
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Antifibrinolytic – inhibits plasmin to stop bleeding
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Tranexamic acid
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DIGITALIS
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inhibits NaKATPase à ↑ Calcium; treat CHF, Arrhythmias; DigiToxicity
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Digoxin
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Preferred, Renal excretion, shorter τ (1.6d), SS@1 wk, metabolized by gut bacteria (10%)
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Digitoxin
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No 12-OH, Hepatic metab, longer τ (7d), ss@1 mo
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INOTROPICS
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oral agents for ↑ contractility
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Ibopamine
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Dopaminergic agonist
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Inamrinone (Amrinone)
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PDE inhibitor ↑cAMP à ↑CO and ↓SVR, short-term CHF tx, ↑AV cond, ARR, oral ↑toxic
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Milrinone (Primacor)
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Shorter τ (30 min vs 2.5 h), more selective, fewer side fx (e.g. thrombocytopenia, gi, liver, fever)
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Vesnarinone
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PDE inhibitor
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Pimobendan
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PDE inhibitor w/ Ca sensitizing properties
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Nesiritide
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Natriuretic peptide
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Omapatrilat
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Neutral endopeptidase inhibitor—blocks both ACE and natriuretic peptide degradation
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ANTI-platelets
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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 à ↑cAMP
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ASA w/ Dipyridamole (Aggrenox)
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Work together well
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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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AntiCoagulants
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Unfractioned Heparin
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Indirect thrombin and Xa inhibitor
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Enoxaparin (LMW Heparin)
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Indirect Xa inhibitor
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Dalteparin
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Less variability and monitoring, slower clearance
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Tinzaparin
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Protamine
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Treat 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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Various Enzymes
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And Stuff
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Tyrsosine hydroxylase ***
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Tyrosine à DOPA
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(-) metyrosine
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Dopa Decarboxylase (aromatic-L-aminoacid decarboxylase)
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DOPA à Dopamine
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(-) carbidopa
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Dopamine-ß-hydroxylase
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Dopamine à NE
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(-) Disulfiram (Antabase)
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Dihydroxyphenylserine (DOPS)
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Treat deficiency: DOPS à NE
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Phenylethanolamine-N-methyltransferase
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NE à E
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Adrenal medulla, brain, Zuckerkandl
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(+) glucocorticoids
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(-) feedback inhibition
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Monoamine oxidase
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Breaks down catecholamines à aldehydes
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(-) pargyline, tranylcypromine, selegiline (Deprenyl)
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Cathechol-O-methyltransferase (COMT)
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NE à normetanephrine; L&K
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(-) tricyclic AD, amphetamine, cocaine
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