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Antianginal, Anti-CHF & Antidysrhythmic Agents
PHAR450
23
Pharmacology
Undergraduate 4
04/01/2014

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Term
Nitroglycerin
Definition
Short acting organic nitrate, anti-anginal
Ester of nitric acid
Industrial potential for use in dynamite & explosives
Increases guanylyl cyclase activity and [cGMP], which activates cGMP-dependent kinase to mediate relaxation
Veno- and arteriolar-dilation, increased perfusion of ischemic myocardium
Term
Isosorbide dinitrate (ISDN)
Definition
Long acting organic nitrate, anti-anginal
Ester of nitric acid
Increases guanylyl cyclase activity and [cGMP], which activates cGMP-dependent kinase to mediate relaxation
Veno- and arteriolar-dilation, increased perfusion of ischemic myocardium
Chronic prophylaxis
Oral admin but high first pass effect
Term
Glyceryl trinitrate (GTN)
Definition
Short acting organic nitrate, anti-anginal
Ester of nitric acid
Increases guanylyl cyclase activity and [cGMP], which activates cGMP-dependent kinase to mediate relaxation
Veno- and arteriolar-dilation, increased perfusion of ischemic myocardium
Termination/prevention of anginal attack (sublingual) and chronic prophylaxis (transdermal patches)
Term
Verapamil
Diltiazem
(Anti-anginal)
Definition
Calcium entry blocker, anti-anginal
Negative inotropic effect (decreased SA and AV conduction)
Arteriolar dilation
Prevent/inhibit variant angina
Term
Nifedipine
Definition
Calcium entry blocker, anti-anginal
Potent vasodilator (for arterioles)
Prevent/inhibit variant angina
Term
Propranolol
(Anti-anginal)
Definition
Beta-blocker, anti-anginal
Decreased oxygen consumption via decreased heart rate and contractility
Not useful for variant angina
Term
Metoprolol
Carvedilol
Definition
Beta-blocker, anti-anginal
Improves mortality in CHF patients
Term
Ivabradine
Definition
Newer anti-anginal drug
Blocks channels that mediate Phase 4 depolarization (If channel)
Decreased heart rate due to inhibition of SA node, but no effect on contractility
Approved for patients with stable CAD
Term
Fasudil
Definition
Newer anti-anginal drug
Inhibits rho kinase (normally inhibits MLC phosphatase) and promotes relaxation
Decreased vasospasm and improved exercise tolerance in CAD
Term
Digitalis
Definition
Anti-CHF drug
Inhibits Na/K ATPase in cardiac tissue leading to increased [Ca]
Increases CO to reduce compensatory mechanisms of heart with little increase in heart rate
Decreases heart size, sympathetic activity and edema
Ca overload can cause delayed afterdepolarizations and dysrhythmias (automaticity)
Cardiovascular toxicity due to electrical effects
Narrow margin of safety - GI, neurological and vision related adverse effects
Excretion by renal system
Term
Oral/I.V. K+
Definition
Used to treat adverse effects of digitalis
Occupies the same binding site as digitalis
Oral: prevents extra heart beats
I.v.: treats more serious dysrhythmias
Term
Lidocaine
(Anti-CHF)
Definition
Used to treat adverse effects of digitalis
Antidysrhythmic drug
Term
Quinidine
Verapamil
Definition
Drug interaction with digitalis
Displaces digoxin from tissues thus increasing digoxin blood levels
Decreases renal clearance of digoxin
Term
Erythromycin
Tetracycline
Definition
Drug interaction with digitalis
Antibiotics inhibit gut flora that inactivate digoxin thus increasing digoxin blood levels
Term
Quinidine
Procainamide
Definition
Class IA antidysrhythmic drugs: Na channel blockers
Intermediate onset/offset
Also K+ channel blockade
Term
Lidocaine
Mexilitine
Definition
Class IB antidysrhythmic drugs: Na channel blockers
Fast onset/offset
I state block > A state block
Term
Flecainide
Encainide
Definition
Class IC antidysrhythmic drugs: Na channel blockers
Slow onset/offset
Increased mortality in post-infarct patients (CAST Trial)
Limited efficacy and proarryhthmic effects, depressed conduction in normal cells
Term
Propranolol
(Antidysrhythmic)
Definition
Class II antidysrhythmic drug: beta-blocker
Opposes symapthetic activity
Blocks fast upstroke and increased amplitude and conduction velocity in AV nodal cells
Increases ERP and controls ventricular rate
Term
Amiodarone
Definition
Class III antidysrhythmic drug: prolongs action potential duration
Blocks K+ and Na+ channels
Most effective drug for AF with little proarrythmic actions
Maintains normal sinus rhythm
Term
Sotalol
Dofetilide
Definition
Class III antidysrhythmic drug: prolongs action potential duration
Primarily K+ channel blockers
Maintain normal sinus rhythm
Term
Verapamil
Diltiazem
(Antidysrhythmics)
Definition
Class IV antidysrhythmic drugs: calcium entry blockers
Block L-type Ca channels
Decrease slope of phase 0 thus decrease AV conduction
Increase early refractory period (recovery of channel to R state)
Term
Adenosine
Definition
Class V antidysrhythmic drug: Other
Binding to adenosine receptors hyperpolarizes membrane by increased K+ conductance
Decreases cAMP levels thus slowing AV conduction
Used for paroxysmal supraventricular tachycardia
Term
Digoxin
(Antidysrhythmic)
Definition
Class V antidysrhythmic drug: Other
Slows AV conduction via decreased NE sensitivity in AV node
Decreases resting membrane potential via block of NA pump
Increases vagal outflow
Good choice to treat atrial fibrillation and heart failure
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