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Indications and Dosage
Oral
Angina pectoris Adult: Initially, 200 mg/day. If necessary, increase to 300 mg/day after 10 days. Max dose: 400 mg once daily.
Elderly: Dose reduction may be necessary. |
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Renal Impairment
Dose reduction may be necessary.
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Hepatic Impairment
Dose reduction may be necessary.
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Administration
Should be taken with food.
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Contraindications
Hypersensitivity, history of serious ventricular or atrial arrhythmias, uncompensated cardiac insufficiency, congenital QT interval prolongation.
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Special Precautions
Lactation; pregnancy; history of idiopathic hypertrophic subaortic stenosis, 2nd or 3rd ° AV block, cardiogenic shock; CHF; significant hypotension; severe left ventricular dysfunction; hypertrophic cardiomyopathy (especially obstructive); concomitant therapy with β-blockers or digoxin; oedema; increased intracranial pressure with cranial tumours; elderly; children <18 yr; impaired renal or hepatic function. Abrupt withdrawal may cause chest pain. Avoid use in patients in the immediate period postinfarction.
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Adverse Reactions
Dizziness, nausea, dyspnea, bradycardia, oedema, palpitations, QT prolongation, CHF, nervousness, headache, drowsiness, psychiatric disturbances, insomnia, rash, sexual dysfunction, GI disturbances, weakness, tremor, paraesthesia, blurred vision, tinnitus, rhinitis, dyspnoea, cough, flu syndrome, diaphoresis, akathisia, arrhythmia, leukopenia, neutropenia, ventricular torsade de pointes.
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Drug Interactions
Inhibits CYP206. 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. |
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Food Interaction
Garlic may increase antihypertensive effects. Dong Quai has oestrogenic activity. Ephedra, yohimbe and ginseng may worsen hypertension. St John's wort.
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Action
Description:
Mechanism of Action: Bepridil 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: 1 hr. |
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MIMS Class
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