治療心絞痛 高血壓 (CCB) Atrial fibrillation; Hypertension; Paroxysmal supraventricular tachycardia (Treatment and prevention); Stable angina, chronic; Unstable or Variant angina
藥理
Verapamil hydrochloride is an L-type calcium channel inhibitor (slow-channel blocker) that selectively blocks the transmembrane influx of calcium ions into arterial smooth muscles including conductile and contractile myocardial cells, without affecting the concentration of serum calcium. Its hypertensive effect is attributed to the reduction of systemic vascular resistance and selective vasodilation of peripheral arteries. Its antianginal effect is related to inhibition of coronary spasm, and relaxation of main coronary artery and coronary arterioles.
藥動學
Absorption:
1. Time to peak concentration: 11 hr
2. Bioavailability: 13% to 65%; increased in hepatic insufficiency patients
3. Effect of food: lowers Cmax, delays Tmax, and decreases AUC Distribution:
1. Vd: 3.8 L/kg
2. Protein binding, Albumin: 86% to 94% Metabolism:
Hepatic: 65% to 80% P450 CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18; O-demethylation, N-dealkylation and first-pass metabolism, extensively metabolized Excretion:
1. Fecal: 9% to 16% or more as metabolites; Renal: approximately 70% as metabolites (about 3% to 4% unchanged)
2. Renal clearance: 7.3 to 8.7 mL/hour/kg
3. Dialyzable: no (hemodialysis) Elimination Half Life:
1. Extended release: 4 hr to 12 hr
2. Extended release: (age 19 yr to 43 yr): 13 hr
3. Extended release: (age 65 yr to 80 yr): approximately 20 hr
4. Liver disease: 14 to 16 hours
禁忌症
atrial fibrillation/flutter associated with accessory bypass tract (eg, Wolff-Parkinson-White, Lown-Ganong-Levine).
cardiogenic shock.
hypersensitivity to verapamil hydrochloride (Calan(R))
hypotension (less than 90 mmHg systolic pressure)
left ventricular dysfunction, severe (ejection fraction less than 30%)
second- or third-degree atrioventricular block (without functioning artificial pacemaker)
sick sinus syndrome (without functioning artificial pacemaker).
懷孕分類
Fetal risk cannot be ruled out.
哺乳分類
Infant risk cannot be ruled out.
副作用
Headache , Gingival hyperplasia, Constipation
劑量和給藥方法
Atrial fibrillation and flutter:
Initial, 240 to 320 mg QD in 3 to 4 divided doses in digitalized patients; MAX dose 480 mg/day Hypertension:
Initial, 180 mg QD in the morning; may titrate dose up to 240 mg Q12H at weekly based on response 24 hours after dosing Migraine; Prophylaxis:
80 mg ORALLY 3-4 times daily
小兒調整劑量
Atrial fibrillation and flutter:
4 to 10 mg/kg/day divided 3 times daily Hypertension:
1. Initial: 3 mg/kg in 3 divided doses
2. Usual dosage: 3 to 4 mg/kg in 3 divided doses
3. MAX 8 mg/kg up to 480 mg daily in 3 divided doses Supraventricular tachycardia:
1 to 3 mg/kg orally every 8 hours
腎功能調整劑量
1. Initial dose of 100 mg/day may be warranted in some patients.
2. Dialysis: No dosage adjustments are needed
肝功能調整劑量
Severe: Use 30% of dose given to patients with normal hepatic function.
安定性
Room temperature, 25 °C, with excursions permitted from 15 to 30°C . Protect from light and moisture.