Brands, Medical Use, Clinical Data
Drug Category
- Vasodilator Agents
- Antihypertensive Agents
- Antiarrhythmic Agents
- Calcium Channel Blockers
Dosage Forms
Brands / Synonyms
Bepadin; Vascor
Indications
For the treatment of chronic stable angina (classic effort-associated angina).
Pharmacology
Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride.
Mechanism of Action
Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works.
Absorption
Rapidly and completely absorbed after oral administration.
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Hepatic.
Contraindications
VASCOR (bepridil hydrochloride) is contraindicated in patients with a known sensitivity to bepridil
hydrochloride.
VASCOR is contraindicated in (1) patients with a history of serious ventricular arrhythmias, (2) patients with
sick sinus syndrome or patients with second- or third-degree AV block, except in the presence of a functioning
ventricular pacemaker, (3) patients with hypotension (less than 90 mm Hg systolic), (4) patients with uncompensated
cardiac insufficiency, (5) patients with congenital QT interval prolongation , and (6) patients taking other drugs
that prolong QT interval.
Drug Interactions
Nitrates: The concomitant use of Bepridil with long- and short-acting nitrates has been safely tolerated in patients with stable angina pectoris. Sublingual nitroglycerin may be taken if necessary for the control of acute angina attacks during Bepridil therapy.
Beta-blocking Agents: The concomitant use of Bepridil and beta-blocking agents has been well tolerated in patients with stable angina. Available data are not sufficient, however, to predict the effects of concomitant medication on patients with impaired ventricular function or cardiac conduction abnormalities.
Digoxin: In controlled studies in healthy volunteers, bepridil hydrochloride either had no effect (one study) or was associated with modest increases, about 30% (two studies) in steady-state serum digoxin concentrations. Limited clinical data in angina patients receiving concomitant bepridil hydrochloride and digoxin therapy indicate no discernible changes in serum digoxin levels. Available data are neither sufficient to rule out possible increases in serum digoxin with concomitant treatment in some patients, nor other possible interactions, particularly in patients with cardiac conduction abnormalities (Also see WARNINGS Congestive Heart Failure).
Oral Hypoglycemics: Bepridil has been safely used in diabetic patients without significantly lowering their blood glucose levels or altering their need for insulin or oral hypoglycemic agents.
General Interactions: Certain drugs could increase the likelihood of potentially serious adverse effects with bepridil hydrochloride. In general, these are drugs that have one or more pharmacologic activities similar to bepridil hydrochloride, including anti-arrhythmic agents such as quinidine and procainamide, cardiac glycosides and tricyclic anti-depressants. Anti-arrhythmics and tricyclic anti-depressants could exaggerate the prolongation of the QT interval observed with bepridil hydrochloride. Cardiac glycosides could exaggerate the depression of AV nodal conduction observed with bepridil hydrochloride.
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