BEPRIDIL

Absorption

Rapidly and completely absorbed after oral administration.

Toxicity

There has been one experience with overdosage in which a patient inadvertently took a single dose of 1600 mg of bepridil. The patient was observed for 72 hours in intensive care, but no significant adverse experiences were noted.

The Uses of BEPRIDIL

Bepridil is protective against Ebola virus. Bepridil is used in biological study of shortening of electromechnical window in ketamine/xylazine-anesthetized guinea pig model improved QTc interval prolongation and assessed pro-arrhythmic risk during early drug development. Bepridil is also used in therapeutic use in novel high/low solubility classification methods for new molecular entities.

Indications

For the treatment of hypertension, and chronic stable angina (classic effort-associated angina).

Background

A long-acting, non selective, calcium channel blocker with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. It is no longer marketed in the United States, as it has been implicated in causing ventricular arrhythmias (ie. Torsade de pointes).

Definition

ChEBI: A tertiary amine in which the substituents on nitrogen are benzyl, phenyl and 3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl.

Pharmacokinetics

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.

Enzyme inhibitor

This substituted pyrrolidine (FWfree-base = 366.55 g/mol) is a calcium channel blocker that inhibits the Na+ /Ca2+ exchange, exhibiting antiarrhythmic, antianginal, and vasodilatory properties. Bepridil inhibits the growth of certain brain tumors in vitro. Bepridil also binds to troponin C. Target(s): Ca2+ channels; ATP-sensitive K+ channels; Na+ -activated K+ channels.

Metabolism

Hepatic.