Showing posts with label Calcium-Entry Blocking Agent (Antidysrhythmic Agent Class IV). Show all posts
Showing posts with label Calcium-Entry Blocking Agent (Antidysrhythmic Agent Class IV). Show all posts

Bepridil (Vascor)

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Name: Bepridil (Vascor)

Class: Calcium-Entry Blocking Agent (Antidysrhythmic Agent Class IV)

Mechanism: Binds to L-type Ca2+ channels ® ¯ Ca2+ in arterial smooth muscle cells ® vasodilation ® ¯ TPR, ­ coronary blood flow, ¯ cardiac afterload. Little/no effect on venous vessels. ¯ inotropy, chronotropy, & dromotropy. Blocks cardiac Na+/K+ channel. May inhib. platelet. aggreg.

Absorption: Oral ® nearly complete absorption. 1st pass Metabolism®¯ bioavail. IV.

Dist.: Significant protein binding.

Metabolism.: Hepatic.

Excretion, : Long (24-50 hr.). Repeated oral dose ® ­ t½ due to hepatic saturation. Longer t½ in elderly or pts w/hepatic cirrhosis or renal insuff.

Toxicity/S.E.s: 2° to vasodilation—dizziness, hypotension, headache, flushing, edema. Aggravation of myocardial ischemia. Drug-induced long QT syndrome (DILQT, “torsades de pointes”). C/i w/CHF, b-blockers.

Utility: Rx angina (stable, variant, unstable), supraventricular tachycardia, reentry arrhythmias, hypertension.

Special Features:

 

Diltiazem (Cardizem)

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Name: Diltiazem (Cardizem)

Class: Calcium-Entry Blocking Agent (Antidysrhythmic Agent Class IV)

Mechanism: Binds L-type Ca2+ channels® ¯ Ca2+ in arterial smooth muscle cells ® vasodilation ® ¯ TPR, ­ coronary blood flow, ¯ cardiac afterload. Little/no effect on venous vessels. ¯ inotropy, chronotropy, & dromotropy. Net = ¯ HR, ¯ contractility, ¯ BP. May inhib. platelet aggreg.

Absorption: Oral ® nearly complete absorption. 1st pass Metabolism®¯ bioavail. IV.

Dist.: Significant protein binding.

Metabolism.: Hepatic. Inducible Metabolism. Inhib. hepatic enzymes. Active Metabolismolites.

Excretion, : 1.5-6 hr. Repeated oral dose ® ­ t½ due to hepatic saturation. Longer t½ in elderly or pts w/hepatic cirrhosis or renal insuff.

Toxicity/S.E.s: Dizziness, hypotension, headache, flushing, edema, constipation (less than verapamil), bradycardia, gingival hyperplasia. Aggravation of myocardial ischemia (less than w/DHPs). ­ digoxin levels. C/i for pts. w/systolic BP<90 style=""> C/i w/CHF, b-blockers, quinidine.

Utility: Rx angina (stable, variant, unstable). Supraventricular tachycardia, reentry arrhyth..

Special Features: Blocking action is frequency and voltage dependent. \ more effective in rapidly depolarizing cells. Hemodynamic effects between those of dihydropyridines and verapamil.