Bepridil hydrochloride
Bepridil hydrochloride (Vascor)
Bepridil hydrochloride
( BEH-prih-dill)
Pregnancy Category: C Vascor (Rx)

Classification: Antianginal, calcium channel blocking drug

See Also: See also Calcium Channel Blocking Agents .

Action/Kinetics: Inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. Increases the effective refractory period of the atria, AV node, His-Purkinje fibers, and ventricles. Dilates peripheral arterioles and reduces total peripheral resistance; reduces HR and arterial pressure at rest and at a given level of exercise. Rapidly and completely absorbed following PO use. Onset: 60 min. Time to peak plasma levels: 2-3 hr. Greater than 99% bound to plasma protein. Food does not affect either the peak plasma levels or the extent of absorption. Therapeutic serum levels: 1-2 ng/mL. t 1/2, distribution: 2 hr; terminal elimination: 24 hr. Steady-state blood levels do not occur for 8 days. Metabolized in the liver and metabolites are excreted through both the kidney (70%) and the feces (22%).

Uses: Chronic stable angina (classic effort-associated angina) in clients who have failed to respond to other antianginal medications or who are intolerant to such medications. May be used alone or with beta blockers or nitrates. An additive effect occurs if used with propranolol.

Contraindications: Clients with a history of serious ventricular arrhythmias, sick sinus syndrome, second- or third-degree heart block (except in the presence of a functioning ventricular pacemaker), hypotension (less than 90 mm Hg systolic), uncompensated cardiac insufficiency, congenital QT interval prolongation, and in those taking other drugs that prolong the QT interval (e.g., quinidine, procainamide, tricyclic antidepressants). Use in clients with MI during the previous 3 months. Lactation.

Special Concerns: Safety and effectiveness have not been determined in children. Use with caution in clients with CHF, left bundle block, sinus bradycardia (less than 50 beats/min), serious hepatic or renal disorders. New arrhythmias can be induced. Geriatric clients may require more frequent monitoring.

Side Effects: CV: Induction of new serious arrhythmias such as torsades de pointes type ventricular tachycardia, prolongation of QTc and QT interval, increased PVC rates, new sustained VT and VT/VF sinus tachycardia, sinus bradycardia, hypertension vasodilation, palpitations. GI: Nausea (common), dyspepsia, GI distress, diarrhea, dry mouth, anorexia, abdominal pain, constipation, flatulence, gastritis, increased appetite. CNS: Nervousness, dizziness, drowsiness, insomnia, depression, vertigo, akathisia, anxiousness, tremor, hand tremor, syncope, paresthesia. Respiratory: Cough, pharyngitis, rhinitis, dyspnea, respiratory infection. Body as a whole: Asthenia, headache, flu syndrome, fever, pain, superinfection. Dermatologic: Rash, skin irritation, sweating. Miscellaneous: Tinnitus, arthritis, blurred vision, taste change, loss of libido, impotence, agranulocytosis.

Laboratory Test Alterations: ALT, transaminase. Abnormal liver function tests.

Drug Interactions: Cardiac glycosides / Exaggeration of the depression of AV nodal conduction Digoxin / Possible serum digoxin levels Potassium-wasting diuretics / Hypokalemia, which causes an risk of serious ventricular arrhythmias Procainamide / Risk of serious side effects due to exaggerated prolongation of the QT interval Quinidine / Risk of serious side effects due to exaggerated prolongation of the QT interval Tricyclic antidepressants / Risk of serious side effects due to exaggerated prolongation of the QT interval

How Supplied: Tablet: 200 mg, 300 mg

Dosage
?Tablets Chronic stable angina.
Adults, initial: 200 mg once daily; after 10 days the dosage may be adjusted upward depending on the response of the client (e.g., ability to perform ADL, QT interval, HR, frequency and severity of angina). Maintenance: 300 mg/day, not to exceed 400 mg/day. The minimum effective dose is 200 mg.