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263 Cards in this Set

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ALPHA-1 AGONISTS
arterial vasoconstriction, ↑ contractility
Phenylephrine (Neosynephrine)
Pure and potent, tx paroxysmal a-tach
Methoxamine
Pure and potent
Norepinephrine
Shock
Epinephrine
↑ BP
Dopamine
Low dose
ALPHA-1 ANTAGONISTS
Phentolamine
IV, Nonselective, competitive, short-acting, Dx pheo, block 5HT
Phenoxybenzamine
Oral, Nonselective, noncompetitive, long-acting, Tx pheo
Prazosin (Minipress)
Selective α1 blocker, prazosin syncope, first dose effect, tachyphylaxis (tolerance)
Terazosin (Hytrin)
Selective α1 blocker, longer τ (less first dose effect), Tx BPH
Doxazosin (Cardura)
Tamsulosin (Flomax)
Urological indications
Alfuzosin (Urotraxal)
ALPHA-2 AGONISTS
Venous vasoconstriction, ↓ NE @ sympathetics
Clonidine (Catapres)
↓BP and CNS, Clonidine rebound, mild ↓ cholesterol, Raynaud’s, ↓ CNS
Methyldopa (Aldomet) à α-methylnorepinephrine
↓BP and CNS, safer mild CO effect, delay in onset (6 hrs), hemolytic anemia (rare)
Tizanidine (Zanaflex)
Shorter τ (2 hrs), rebound, tx muscular spasm
Guanfacine
Long τ (17 hrs), less withdrawl
Guanabenz
ALPHA-2 ANTAGONISTS
↑ sympathetics, ↑ NE release
Yohimbine
Aphrodisiac
Phentolamine
α1 and α2 antagonists
Phenoxybenzamine
BETA AGONISTS
Isoproterenol
Non-selective, ↑HR, CO, contractility
Dobutamine
ß1 selective, no ΔBP
BETA ANTAGONISTS
nonselective tx: portal HT, tremor, vascular headache
Propranolol (Inderal) – the original
Non-selective, cheap, heavy liver metab
Metoprolol (Lopressor)
ß1 selective, no bronchoconstriction (asthma), ß2 hyperresponse?
Atenolol (Tenormin)
ß1 selective, no bronchoconstriction (asthma)
Nadolol (Corgard)
Not lipophilic, Europe, ~ Propranolol
Esmolol
Short τ for IV use, critical care
Labetalol
α1 blocker (S,R), ↑ potency orally; ß1 antag and partial ß2 agonist (R,R: higher clearance) [1:7]
Carvedilol
Potent α1 blocker à ↓PVR à tx CHF, racemic mixture
Pindolol
Some agonist activity
Timolol
Tx glaucoma
DOPAMINE receptor Drugs
D1 – vasodilation, D2 – emesis, ↓prolactin, D4 – risk taking
Bromocriptine
Dopamine Agonists
Fenoldopam (9x D1)
Apomorphine
Metoclopramide
Dopamine Antagonists
Haloperidol
Domperidone
INDIRECT-ACTING Phenylethylamines
Tyramine
Displaces NE into synaptic cleft – cheese, wine, ham
Ephedrine (Ephedra, Ma Huang)
Weight loss, ↑ SKM and CNS
Amphetamine
More potent CNS
Hydroxyamphetamine
Tyramine-like, test for more central Horner’s syndrome
Phenylpropanolamine (Dexatrim)
Sympathomimetic and vasoconstriction
Pseudoephedrine (Sudafed)
Replacement Dexatrim analog
MUSCARINIC AGONISTS
Acetylcholine
Rapid hydrolysis, rarely used
Bethanechol
Gastric emptying, tx urinary retention
Pilocarpine
Miosis and salivation, Tx open-angle glaucoma
Methacholine
Bronchoconstriction, methacholine challenge
Carbachol
Muscarine, Arecholine
Naturally occurring
MUSCARINIC ANTAGONISTS
Atropine – Deadly nightshade (Atropa belladonna)
↑HR, dilate pupils
Jimson Weed (Datura stramonium)
Hallucinogen
Hyoscine – Henbane (Hyoscyamus niger)
Hallucinogen
Pirenzepine
M1 selective blocker, gastric acid release
NICOTINIC AGONISTS
Nicotine
↑Symp & PS, Bezold-Jarisch reflex
NICOTINIC ANTAG/ SKM RELAXANT
Respirator, histamine release
Tubocuranine
Nondepolarizing blocker, long τ, reversible by adding ACh
Succinylcholine
Depolarizing blocker, short τ, Pseudocholinesterase deficiency
ANTICHOLINESTERASES
SLUDGE
Physostigmine
Enters CNS à restless, apprehension, HT, nausea
Neostigmine
Does not enter CNS, tx myasthenia gravis & glaucoma
Edrophonium (Tensilon)
Treat MG
Ambenonium
Pyridostigmine
Parathion à Paraoxon
Phosphorothionates à oxidation ↑AChE
Malathion
Insecticide
Tacrine (Cognex)
ALZ, L toxic
Donezapil (Aricept)
ALZ, replaced Tacrine
Rivastigmine (Exelon)
Pralidoxime
Counteracts AChE’s and reactivates ChE
WAR GASES
Organophosphates – insecticides -- ↑ ALL cholinergic transmission (N&M)
Sarin Gas
Irreversible cholinesterase inhibitors (N & M)
VX
Binary agents, death by asphyxiation
SPASMOLYTICS
Dantrolene
↓ Ca release à relax muscles, tx malignant hyperthermia
Baclofen
Muscle relaxant, partial GABA agonist
Diazepam
Anti-anxiety agents that ↓ nerves in muscles
Chlordiazepoxide
Carisoprodol
Meprobamate
Strychnine
Glycine antagonist à ↑ respiration, convulsions
NO-DEPENDENT VASODILATORS
A&V vasodilation, SM relaxation, Tolerance
Nitroglycerin (TNG)
Nitrate ester, Sublingual, high clearance (minutes)
IsoSorbide DiNitrate (Isordil)
Nitrate ester, Oral, variable τ of metabolites, intermediate clearance
Isosorbide MonoNitrates (2-IMN > 5-IMN)
Nitrate ester, 100% bioavailable, less variable, low clearance
**Sildenafil (Viagra)
Inhibits cGMP phosphodiesterase V à ↑postural hypotension
Nitroprusside (Nipride) à NO + CN
Spontaneous conversion to NO + CN, Thiocyanate toxicity (tx Na thiosulfate), no light, short τ
DIRECT VASODILATORS
Hydralazine (Apresoline)
Arterial vasodilator, tx HT & CHF
Minoxidil (Loniten)
Arterial vasodilator, tx HT
CALCIUM CHANNEL BLOCKERS
↓ Ca à vasodilation, long acting, inhibit CYP3A4
Nifedipine (1,4-dihydropyridine)
L channel, ↑ chronotropy and CO, ↑ symp, variable partition coefficients, oral > sublingual
Amlodipine
High partition coefficient à high Vd, slow onset of action, prolonged duration
Verapamil (phenylalkylamine)
L channel, ↓ino, chrono, dromotropy, SVT, L isomer more active, PGP inhibitionàDIGItoxic
Diltiazem (benzothiazepines)
L channel, ↓ino, chrono, dromotropy, SVT, PGP inhibitionàDIGItoxic
Mibefradil
T Channel, FDA removed, vasodilation > cardiac depression
Angiotensin Converting Enzyme Inhibitors
↑ bradykinin, renin, ang I, ↓angiotension II
Captopril
Sulfhydryl, shorter τ, prostaglandin effect
Fosinopril
Phosphinyl, L&K
Trandolapril
Carboxyl, L&K
Enalapril
Carboxyl
Lisinopril
Benazepril
Quinapril
Ramipril
Trandolapril
Moexipril
Angiotensin Receptor Blockers
↑ bradykinin, renin, ang I, ↑ angiotensin II, fetotoxic
Saralasin
Original, IV, partial agonist
Losartan à EXP-3174
Non-peptide, short τ, normal-high renin levels, uricosuric effect
Valsartan
Irbesartan
Candesartan
Osmotic Diuretics
Most of tubule: IV volume expansion (filtered, not reabsorbed)
Mannitol
IV
Urea
IV
Glycerin
Oral
Carbonic Anhydrase Inhibitors
PT: ↓NaHCO3 reabsorption (metabolic acidosis), sulfonamides
Acetazolamide (Diamox)
Tx glaucoma
Dichlorphenamide
Loop Diuretics (high ceiling)
TALH: NaKCl2 symport inhibitor, MOST potent, Ca and Mg loss
Furosemide (Lasix)
Releases vasodilator prostaglandin from kidneys à ↑ venous capacitance
Bumetanide (Bumex)
Ethacrynic Acid (Edecrin)
Non-sulfamide
Torsemide (Demadex)
Thiazides
DCT: NaCl cotransport inhibitor, ↑ Glu,Urea,Ca; ↓ K,H,Na
Chlorothiazide (Diuril)
Hydrochlorothiazide (HCTZ, Esidrex)
Sulfonamide, hyperuricemia à gout; tx diabetes insipidus
Chlorthalidone (Hygroton)
Metolazone (Zaroxolyn)
K Sparing Diuretics
CT: Na channel inhibitors, ↓ K excretion; careful! (ACEI, ↑K, ARF)
Amiloride
Partially absorbed; inhibits NaH antiporter (lumen) and NaK ATPas (basal); tx Liddle’s
Triamterene
Well absorbed, renal and metabolism
Aldosterone Antagonists
steroid analogues compete with aldosterone, best for cirrhosis
Spironolactone à Canrenone
Affects estrogen receptors (gynecomastia), tx Cohn’s
Eplerenone
Newer version
ADH Antagonists
CT: ↓ADH effects and ↓water reabsorption
Demeclocycline (Declomycin)
Tetracycline derivative; tx SIADH
ANTIARRYTHMIC DRUGS
Class I
Na Channel Blockers, “local anesthetics”
Class Ia
Intermediate recovery (1-5s), ↑ QRS, QT, APD, blocks Na and K channels;
Quinidine
α receptor block and vagal inhibition; ↑DIG
Procainamide à N-acetylprocainamide (NAPA)
Metabolite blocks K channels only, renal dose adjustment, lupus syndrome
Disopyramide
Aggravates CHF and prostatism, effect ↑ with dose
Class Ib
Fast recovery (<1s), shorten repolarization
Lidocaine
IV, ↓ v-fib, ↑ mortality, CNS toxicity, dose adjustment (CHF and liver)
Mexiletine
Oral, CNS toxic
Tocainide
Oral ,CNS toxic, agranulocytosis
Phenytoin
Anticonvulsant, effective for digitalis intoxication
Class Ic
Slow recovery, marked ↑PR, ↑QRS, ± QT
Flecainide
Very long τ from block, very effective for isolated PVC, RSVT, ↑DIG
Encainide
↑ mortality post-MI, FDA removed
Propafenone
~ Flecainide, Weak ß blocker (↑ at high conc),
Moricizine
Phenothiazine analog, unique, weaker version, multiple metabolites
Class II
Beta Blockers, ↓ HR and ↑ PR (slow down)
Esmolol
Ultra short acting (τ = 9m), nonselective ß blocker, good for testing
Propranolol
Sotalol
Esmolol
Timolol
Acebutolol
Class III
K channel blockers, ↑ AP duration, ↑ QT
Amiodarone
Class I,II,III,IV actions, effective most arr, multiple toxic (esp lung), LONG τ (50d), ↑DIG
Bretylium
No longer marketed, still available – biphasic NE effects (↑ then ↓)
Dofetilide
Pure class III, Renal dose adjustment, causes TdP (1-3%)
Sotalol
Non-selective ß blocker, causes TdP
Ibutilide
Acute IV, stop A-flutter (60%) and A-fib (40%), block K, opens Na, Causes TdP (6%)
*N-acetylprocainamide
Might have some class III effects
Class IV
Ca channel blockers, ↓ HR and ↑ PR
Verapamil (phenylalkylamine)
Most potent AV blocking, hypotensive; AVOID: wide-complex tachy,WPW,CHF,AVblock,DIG
Diltiazem (benzothiazepines)
IV, AV node blocking w/o hypotension, great for A-fib
Adenosine
Purinergic receptor blocker, ultra-short acting AV blocker (seconds) – acute tx, rapid IV, short Sx
THROMBOLYTIC
plasminogen activators
Streptokinase (SK)
1° Non-enzymatic protein from streptococci, indirect, antibodies to SK à agg
Urokinase (UK)
1° Trypsin-like enzyme, LMW, direct, (-) PAI-1, non-antigenic
Aniosylated Plasminogen Streptokinase Complex (APSAC)
2° SK and human plasminogen complex à spontaneous deacylation, long τ (60m), IV bolus, Ab
t-PA (Alteplase)
2° Fibrin/clot-specific binding (1000x), glycosylation, short τ (6m), (-) PAI-1
Reteplase
3° t-PA derivative, kringle #2 and protease domain, non-glycosylated, no EGF à longer τ (15m)
TNK-t-PA (Tenecteplase)
3° no glycosylation, less PAI-1 effect, ↑ fibrin specificity
Amicar (ε-aminocaproic acid)
Antifibrinolytic – inhibits plasmin to stop bleeding
Tranexamic acid
DIGITALIS
inhibits NaKATPase à ↑ Calcium; treat CHF, Arrhythmias; DigiToxicity
Digoxin
Preferred, Renal excretion, shorter τ (1.6d), SS@1 wk, metabolized by gut bacteria (10%)
Digitoxin
No 12-OH, Hepatic metab, longer τ (7d), ss@1 mo
INOTROPICS
oral agents for ↑ contractility
Ibopamine
Dopaminergic agonist
Inamrinone (Amrinone)
PDE inhibitor ↑cAMP à ↑CO and ↓SVR, short-term CHF tx, ↑AV cond, ARR, oral ↑toxic
Milrinone (Primacor)
Shorter τ (30 min vs 2.5 h), more selective, fewer side fx (e.g. thrombocytopenia, gi, liver, fever)
Vesnarinone
PDE inhibitor
Pimobendan
PDE inhibitor w/ Ca sensitizing properties
Nesiritide
Natriuretic peptide
Omapatrilat
Neutral endopeptidase inhibitor—blocks both ACE and natriuretic peptide degradation
ANTI-platelets
Aspirin
Irreversibly acylates cyclooxygenase, blocking TxA2 synth
Dipyridamole (Persantine)
Inhibits PDE à ↑cAMP
ASA w/ Dipyridamole (Aggrenox)
Work together well
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
AntiCoagulants
Unfractioned Heparin
Indirect thrombin and Xa inhibitor
Enoxaparin (LMW Heparin)
Indirect Xa inhibitor
Dalteparin
Less variability and monitoring, slower clearance
Tinzaparin
Protamine
Treat 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 -- ↓post-translational carboxylase, ↓factor 2,7,9,10,C,S, INR
Various Enzymes
And Stuff
Tyrsosine hydroxylase ***
Tyrosine à DOPA
(-) metyrosine
Dopa Decarboxylase (aromatic-L-aminoacid decarboxylase)
DOPA à Dopamine
(-) carbidopa
Dopamine-ß-hydroxylase
Dopamine à NE
(-) Disulfiram (Antabase)
Dihydroxyphenylserine (DOPS)
Treat deficiency: DOPS à NE
Phenylethanolamine-N-methyltransferase
NE à E
Adrenal medulla, brain, Zuckerkandl
(+) glucocorticoids
(-) feedback inhibition
Monoamine oxidase
Breaks down catecholamines à aldehydes
(-) pargyline, tranylcypromine, selegiline (Deprenyl)
Cathechol-O-methyltransferase (COMT)
NE à normetanephrine; L&K
(-) tricyclic AD, amphetamine, cocaine