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Winter Exam #2 - Antiarrhythmics
n/a
26
Pharmacology
Graduate
01/07/2010

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Term
Class 1A drugs - quinidine, procainamide (Procanbid)
Definition
agents that slow rate of rise of phase 0 of AP (slowing conduction velocity) and increase AP duration & effective refractory period (ERP); have INTERMEDIATE speed of interaction with phase 0 Na channels
Term
Class 1B drugs - lidocaine (Xylocaine)
Definition
agents that have less slowing effect on rate of rise of phase 0 (less slowing of conduction velocity) & decrease AP duration & ERP; they RAPIDLY interact with phase 0 Na channels
Term
Class 1C drugs - flecainide (Tambocor)
Definition
agents that markedly depress rate of rise of phase 0 (marked slowing of conduction velocity); have LITTLE net effect on AP duration or ERP; interacts SLOWLY with phase 0 Na channels
Term
quinidine
Definition
class 1A antiarrhythmic, inhibits Na channels but also K channels with changes in AP; Uses: tx of various supreventricular & ventricular arrhythmias, inhibits ectopic atrial & ventricular arrhythmias, prevents reentry arrhythmias by transforming unidirectional block into bidirectional block, used to maintain NORMAL RHYTHM after CARDIOVERSION of atrial flutter or fibrillation; IV & oral
Term
SEs of quinidine
Definition
causes other arrhythmias (prolonged QT --> torsades de pointes [TdP]); nausea, vomiting, DIARRHEA; CINCHONISM (ringing of ears, headache); decreased BP, increased regular sinuse rate; Increases digoxin levels
Term
procainamide (Procanbid)
Definition
class 1A antiarrhythmic that inhibits Na channels but inhibits K channels due to a metabolite of drug; Pk: oral & IV, metabolite NAPA (N-acetylprocainamide) that prolongs AP duration but also has class 3 properties that inhibit K channels
Term
SEs of procainamide (Procanbid)
Definition
reversible lupus syndrome; CNS side effects; GI intolerance; less decrease in BP & increase in regular sinus rate than other 1A drug; ventricular arrhythmias but less of TdP
Term
lidocaine (Xylocaine)
Definition
Class 1B antiarrhythmic that rapidly interacts with Na channels, shortens phase 3 repolarization, decreasing AP duration & ERP, with only slight decrease in phase 0 slope; Uses: emergency tx of ventricular arrhythmias during myocaridal ischemia (MI), suppresses ventricular arrhythmias caused by automaticity b/c it can decrease slope of phase 4, abolishes ventricular reentry despite decrease in AP duration & decrease in ERP & little decrease in conduction; STOPS TdP; Pk: ONLY IV
Term
SEs of lidocaine (Xylocaine)
Definition
wide toxic-therapeutic ratio; little impairment of left ventricular fcn (no neg. inotropic fcn); CNS: drowsiness, slurred speech, confusion, convulsions; cardiach arrhythmias may occur, aggravated by hyperkalemia
Term
flecainide (Tambocor)
Definition
Class 1C antiarrhythmics interact more slowly but more notably by blocking Na channels, markedly suppresses phase 0 slope --> marked slowing of conduction, also inhibits some K channels in ventricles but blocks some late-opening Na channels but NO NET EFFECT on duraiton of AP & ERP, increase in threshold of phase 0; Uses: refractory (resistant) arrhythmias; Pk: oral
Term
SEs of flecainide (Tambocor)
Definition
neg. inotropic effects that aggravates CHF; dizziness, blurred vision, HA, nausea; aggravates preexisting arrhythmias, induces life-threatening ventricular tachycardia
Term
Class II Antiarrhythmics - propanolol [Inderal-LA], acebutalol [Sectral], esmolol [Brevibloc]
Definition
beta-adrenergic antagonists that block cardiac beta receptor actions on Ca channel, decreasing inward Ca currents; diminish phase 4 depolarization, depressing automaticity, decrease phase 0 slope which slows conduction, increases AP duration & ERP; uses: treat arrhythmias caused by increases SNA or excess catecholamine release, atrial flutter, fibrillation, AV nodal reentrant tachycardia, prevents supraventricular arrhythmias, suppresses DADs
Term
propanolol (Inderal-LA)
Definition
Class II antiarrhythmic; reduces incidence of sudden adrenergically-driven arrhythmic deaths after MIs; has membrane stabilizing properties
Term
acebutalol (Sectral)
Definition
class II antiarrhythmic; its beta-1-specificity reduces risk of bronchospasm; partial agonist activity may decrease risk of too much suppression of normal cardiac function
Term
esmolol (Brevibloc)
Definition
class II antiarrhythmic; very short acting beta blocker used IV in acute arrhythmias that occur during surgeries or emergencies
Term
SEs of Beta-blockers - propanolol, acebutalol, esmolol
Definition
sinus bradycardia, AV blockade, Rebound angina, asthmatic attacks,masks severe hypoglycemic rxns, CNS: sedation, fatigue, sleep alterations; AVOID combining with Ca Channel blockers
Term
Class III Antiarrhythmics - amiodarone (Cordarone), dofetilide (Tikosyn)
Definition
agents that inhibit K channels during AP --> diminish outward K current --> prolongs repolarization (Phase 3), prolonging AP duration & ERT
Term
amiodarone (Cordarone), dronadarone (newly FDA approved)
Definition
Class III antiarrhythmic; decreases conduction velocity by decreasing cell-to-cell coupling --> prolongs AP duration & ERP; Uses: severe, refractory (resistant) supraventricular & ventricular tachyarrhythmias, pts that wear ICDs (implantable cardioverter defibrillators) --> reduces how often ICD must deliver shocks; Limited by toxicity; PK: oral, concentrates in tissues w/ prolonged half-life of several wks; contains iodine
Term
SEs of amiodarone (Cordarone)
Definition
interstitial pulmonary fibrosis, dizziness, hyper- or hypothyroidism, blue skin discoloration (iodine accumulation in skin), TdP can occur due to increase AP duration in ventricular tissues (rare)
Term
dofetilide (Tikosyn)
Definition
PURE class III agent; inhibits only K channels, prolonging APD & ERP; Uses: supraventricular arrhythmias, atrial fibrillation, suppression of "Reentry" phenomena; Pk: oral & IV; SEs: ventricular TdP (high dosed IV)
Term
Class IV Antiarrhythmics - verapamil (Calan), diltiazem (Cardizem)
Definition
agents that block voltage-sensitive L-type Ca channels --> decrease inward current carried by Ca in phase 0, 2 & 4 --> suppresses phase 0 & 4 slopes, slightly prolonging APD & ERP late in phase 3
Term
verapamil (Calan), diltiazem (Cardizem)
Definition
class IV drugs that bind mostly to Ca channels --> decrease inward Ca current --> decrease slopes of phase 0 & phase 4 --> slowing conudction, suppressing automaticity --> increases APD & ERP, Uses: arrhythmias that traverse highly Ca-dependent cardiac tissues, supraventricular arrhythmias, stops DADs, reentrant supraventricular tachycarida, protects normal ventricular rate during atrial flutter & fibrillation; MAKES WPW WORSE when accompanied by atrial fibrillation
Term
SEs of diltiazem (Cardizem), verapamil (Calan)
Definition
decreases normal sinus rate & normal AV conduction; negative inotropic action; avoid combo with Beta-blockers
Term
adenosine
Definition
miscellaneous antiarrhythmic; decreases conduction velocity & decreasese abnormal impulse formation in AV node by inhibiting Ca influx & by activating ACh-sensitive phase 4 K current (hyperpolarization of resting membrane potential); IV is drug of choice for abolishing acute paroxysmal supraventricular tachycardia;
Term
SEs of Adenosine
Definition
low toxicity; flushing, shortness of breath, chest pain due to bronchospasm
Term
magnesium sulfate
Definition
used to treat TdP
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