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Pharm 14 Antiarrhythmic agents
pharmacology of antiarrhythmic drugs
51
Pharmacology
Professional
09/01/2011

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Term
What is Class 1 action? What are the effects of Class Ia agents on conduction velocity, action potential duration (APD) and what speed are the kinetics?
Definition
Class 1 - Na+ channel blockers. Ia - slow conduction, prolong RP, prolong APD, intermediate kinetics
Term
What is Class 1 action? What are the effects of Class Ib agents on conduction velocity, refractory period, action potential duration (APD) and what speed are the kinetics?
Definition
Class 1 - Na+ channel blockers. Ib - shorten APD in some tissues, rapid kinetics
Term
What is Class 1 action? What are the effects of Class Ic agents on conduction velocity, action potential duration (APD) and what speed are the kinetics?
Definition
Class 1 - Na+ channel blockers, Ic - minimal effects on APD, slow kinetics
Term
What is Class II action?
Definition
sympatholytic, antagonize adrenergic recepts
Term
What is Class III action?
Definition
III - prolong repolarization, prolong APD, most block Krapid
Term
What is Class IV action?
Definition
IV - block Ca2+, slows conduction in regions where AP upstroke depends on Ca - nodes
Term
Pro-Dis-Quin is which class?
Definition
Class Ia
Term
name the drug: blocks Na and Kr (secondary). Which class?
Definition
procainamide, Ia
Term
name the drug: slows conduction velocity and pacemaker rate, prolongs APD and dissociates with intermediate kinetics, direct depressant effects on SA and AV nodes
Definition
procainamide, Ia
Term
What are the clinical applications of procainamide?
Definition
most atrial and ventricular arrhythmias, drug of second choice for most sustained V-arrhythmias associated with acute MI
Term
name the drug: oral, IV, IM, eliminated by hepatic metabolism to NAPA and renal elimination, NAPA implicated in torsad de pointes in pts with renal failure, tox: hypotension, long term --> lupus-like reversible symptoms
Definition
procainamide
Term
how does disopyramide compare to procainamide?
Definition
similar but significant antimuscarinic effects, may precipitate heart failure
Term
how does quinidine compare to procainamide?
Definition
similar but more toxic - cinchronism, TdP, rarely used
Term
Which class is lidocaine? What's the MOA?
Definition
Ib, sodium channel blockade
Term
Name the drug: blocks activated and inactivated Na channels with rapid kinetics, does not prolong and may shorten AP
Definition
lidocaine
Term
What are the clinical applications for lidocaine?
Definition
terminate V-tachycardias and prevent V-fib after cardioversion
Term
Name the drug: IV, first pass hepatic metabolism, reduce dose in pts with heart failure or liver disease, Tox: Neuro symptoms
Definition
lidocaine
Term
how does mexiletine compare to lidocaine?
Definition
orally active congener, used in V-arrhythmias, chronic pain syndromes
Term
What class is flecainide? What is the MOA?
Definition
Na channel blockade
Term
What class is lido-mex?
Definition
class Ib
Term
What class is flec-prop-mor?
Definition
Ic
Term
Name the drug: dissociates from Na channel with slow kinetics, no change in APD
Definition
flecainide
Term
What are the clinical applications of flecainide?
Definition
supraventricular arrhythmias in pts with normal heart, do not use in ischemic conditions (post-MI)
Term
Name the drug: Oral, hepatic and kidney metabolism, half life ~20hrs, Tox: proarrhythmic
Definition
flecainide
Term
how does propafenone compare to flecainide?
Definition
orally active, weak B blocking, supraventric arrhythmias, hepatic metabolism
Term
Describe moricizine
Definition
Class 1c, phenothiazine derivative, orally active, ventricular arrhythmias, proarrhythmic, withdrawn in US
Term
Propanolol - which class? MOA?
Definition
Class 2, b-blocker
Term
Name the drug: direct membrane effects (Na channel block), and prolongation of APD, slows SA node automaticity and AV nodal conduction velocity
Definition
propranolol
Term
What are the applications for propranolol?
Definition
atrial arrhythmias and prevention of recurrent infarction and sudden death
Term
How does esmolol compare to propranolol?
Definition
short acting, IV only, used for intra-op and other acute arrhythmias
Term
Amiodarone: which class? MOA?
Definition
class 3, blocks Kr, Na, Ca-L channels, B adrenoreceptors
Term
name the drug: prolongs APD and QT interval, slows HR and AV conduction, low incidence of TdP
Definition
amiodarone
Term
what are the applications for amiodarone?
Definition
serious ventricular arrhythmias and supraventricular arrhythmias
Term
name the drug: oral, IV, variable absorption and tissue accumulation, hepatic metabolism, elimination complex and slow, tox: bradycardia and heart block in diseased heart, peripheral vasodilation, pulm and hepatic tox, hyper or hypothyroidism, interactions are many- based on CYP
Definition
amiodarone
Term
name the drug: oral, parenteral, duration 4-6h, tox: asthma, AV blockade, acute heart failure, interactions with other cardiac depressants and hypotensive drugs
Definition
propranolol
Term
Dofetilide - class? MOA?
Definition
class 3, Kr block
Term
Effects of dofetilide?
Definition
prolongs AP, effective refractory period
Term
what are the clinical applications for dofetilide?
Definition
maintenance or restoration of sinus rhythm in A-fib
Term
name the drug: oral, renal excretion, tox: TdP, additive with other QT-prolonging drugs
Definition
dofetilide
Term
describe Sotalol
Definition
class 3, b-blocker, direct AP prolongation, use for ventric arrhythmias and a-fib
Term
decribe ibutilide
Definition
class 3, K channel blocker, may activate inward current, IV, use for conversion in a-flutter and a-fib
Term
describe dronedarone
Definition
class 3, investigational, multichannel actions, reduces mortality in pts with a-fib
Term
describe vernakalant
Definition
investigational, multichannel actions in atria, prolongs atrial refractoriness, effective in a-fib
Term
Verapamil - class? MOA?
Definition
class 4, L type Ca channel blocker
Term
name the drug: slows SA node automaticity and AV nodal conduction velocity, decreases cardiac contractility, reduces BP
Definition
verapamil
Term
what are the applications for verapamil?
Definition
supraventricular tachycardias
Term
verapamil - oral or IV? metabolism? caution in which pts?
Definition
oral and IV, hepatic, hepatic dysfunction
Term
diltiazem is equivalent to...
Definition
verapamil
Term
Name the drug: activates K, blocks Ca, very brief effects, usually complete AV blockade, used for paroxysmal supraventricular tachycardias, IV only, tox: flushing, dizziness, chest tightness
Definition
adenosine
Term
name the drug: poorly understood MOA, interacts with Na/K/ATPase and K and Ca channels, used for TdP, digitalis-induced arrhythmias, IV, duration depends on dose, tox: muscle weakness in overdose
Definition
Mg
Term
name the drug: increases K permeability, K currents, slows ectopic pacemakers, slows conduction velocity, used for digitalis-induced arrhythmias, arrhythmias assoc with hypokalemia, oral, IV, tox: reentrant arrhythmias, fibrillation or arrest in overdose
Definition
potassium
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