Cherie: Learn a Drug a Day

Today's drug is bepridil. Its trade name is Vascor.
What is bepridil indicated for?
INDICATIONS :

It is indicated for the treatment of angina pectoris. (chest pain due to poor blood flow through the coronary arteries.)
It may be used alone or in combination with beta blockers and/or nitrates.

How does bepridil work?
MECHANISMS OF ACTION :

Bepridil acts as calcium antagonist.
It inhibits calcium ion from entering the "slow channels" of vascular smooth muscle and myocardium during depolarization, thus causing relaxation of coronary vascular smooth muscle and coronary vasodilatation.
It may also inhibit fast sodium channels (inward), which may account for some of its side effects; a direct bradycardia effect has been postulated via direct action on the SA node.
Onset of action : 1 hr.

How is bepridil being used?
ROUTE OF ADMINISTRATION :

Is there any contraindication?

CONTRAINDICATIONS :

It is contraindicated in

patients with a history of serious ventricular arrhythmias
patients with sick sinus syndrome or patients with second- or third-degree AV block, except in the presence of a functioning ventricular pacemaker
patients with hypotension (less than 90 mm Hg systolic)
patients with uncompensated cardiac insufficiency
patients with congenital QT interval prolongation
patients taking other drugs that prolong QT interval.

Are there any possible side effects?
SIDE EFFECTS :

What precautions are necessary?
PRECAUTIONS :

(i) General

Caution should be exercised when using bepridil in patients with left bundle branch block or sinus bradycardia (less than 50 b.p.m.). Care should also be exercised in patients with serious hepatic or renal disorders because such patients have not been studied and bepridil is highly metabolized, with metabolites excreted primarily in the urine.

(ii) Recent Myocardial Infarction

In US clinical trials with bepridil, patients with myocardial infarctions within three months prior to initiation of drug treatment were excluded. The initiation of bepridil therapy in such patients, therefore, cannot be recommended.

(iii) Pulmonary Infiltration

There have been cases of noninfective, noncardiogenic pulmonary interstitial infiltrates (with or without the presence of eosinophilia), including cases of pulmonary fibrosis in patients taking bepridil. These cases may present as dyspnea or cough within a few weeks of commencing bepridil; infiltrates may be seen on chest x-ray.
Although the relationship of pulmonary infiltration to bepridil is unclear, any patient who develops dyspnea or cough of unspecified etiology should be adequately evaluated. If other causes cannot be identified, discontinuation of bepridil therapy should be considered.

DRUG INTERACTIONS :

Bioavailability increased by H2-blocker.
Use with β-blockers may increase cardiac depressant effects on AV conduction.
May increase serum levels/effects of carbamazepine, ciclosporin, digitalis, quinidine and theophylline.
Concurrent use with fentanyl may increase hypotension.
Potentially Fatal: Increased risk of toxicity with amprenavir, ritonavir, sparfloxacin, gatifloxacin and moxifloxacin. Concurrent admin with ritonavir, amprenavir, sparfloxacin, cisapride, other drugs that prolong QT interval.
More drug interactions ---> click here!

Pregnancy and breastfeeding:

There are no well-controlled studies in pregnant women. Use bepridil in pregnant or nursing women only if the potential benefit justifies the potential risk.
Bepridil is excreted in human milk. Bepridil concentration in human milk is estimated to reach about one third the concentration in serum. Because of the potential for serious adverse reactions in nursing infants from bepridil a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

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