VASCOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VASCOR (VASCOR).
VASCOR (bepridil) is a calcium channel blocker that inhibits calcium ion influx across cardiac and smooth muscle cells, reducing contractility and oxygen demand. It also has class I and IV antiarrhythmic properties.
| Metabolism | Primarily metabolized by CYP3A4 to active metabolites; also undergoes N-dealkylation and oxidation. |
| Excretion | Primarily hepatic metabolism; ~70% excreted in feces as metabolites, ~30% in urine (largely as metabolites). <2% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life: 6-8 hours (normal renal/hepatic function). May be prolonged in hepatic impairment; unchanged in renal impairment. |
| Protein binding | 99% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Vd: 0.04 L/kg. Does not cross the blood-brain barrier. Low Vd consistent with high protein binding and limited tissue distribution. |
| Bioavailability | Oral bioavailability: 30%. Reduced by food. |
| Onset of Action | Oral: 30-60 minutes for a 10% reduction in mean arterial pressure. |
| Duration of Action | Oral: 12-24 hours, consistent with once-daily dosing. Antihypertensive effect persists for 24 hours after a single dose. |
Bepridil hydrochloride (Vascor) is typically dosed as 200 mg to 400 mg orally once daily.
| Dosage form | TABLET |
| Renal impairment | No specific GFR-based dose adjustments are established; use with caution in renal impairment. |
| Liver impairment | Contraindicated in patients with clinically significant hepatic impairment. For Child-Pugh class A, use with caution; no specific dose reduction defined. Contraindicated in class B or C. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; no recommended dosing. |
| Geriatric use | Elderly patients may have increased sensitivity; start at the lower end of dosing range (200 mg daily) with careful monitoring for QT prolongation and bradycardia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VASCOR (VASCOR).
| Breastfeeding | Excreted into human milk; M/P ratio unknown. Potential for infant bradycardia and hypotension. Discontinue breastfeeding or drug, considering importance of drug to mother. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: potential risk of fetal skeletal abnormalities and cardiovascular defects based on animal studies. Second and third trimesters: risk of fetal bradycardia, hypoglycemia, and impaired placental perfusion. Avoid use unless benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
Bepridil can cause serious ventricular arrhythmias, including torsade de pointes and QT prolongation. Use is contraindicated in patients with hypokalemia, hypomagnesemia, or concurrent use of other QT-prolonging drugs. Electrolyte monitoring and ECG evaluation are required.
| Serious Effects |
History of serious ventricular arrhythmias; QT interval >440 msec; hypokalemia; hypomagnesemia; concurrent use of drugs that prolong QT interval; sick sinus syndrome; second- or third-degree AV block without pacemaker; hypotension; cardiogenic shock; decompensated heart failure; hypersensitivity.
| Precautions | Risk of ventricular arrhythmias (torsade de pointes); QT prolongation; hypokalemia and hypomagnesemia; hepatic impairment; renal impairment; use with other QT-prolonging drugs; avoid grapefruit juice. |
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| Monitor maternal heart rate, blood pressure, and ECG. Fetal monitoring for bradycardia and growth restriction. Assess placental function and amniotic fluid volume. |
| Fertility Effects | No evidence of impaired fertility in animal studies. Limited human data, but potential for reduced libido and erectile dysfunction in males. |