Drug
|
Approved Indications
|
Form, Strength, and Dose
|
Time to Peak Effect
|
Elimination Half‐Life
|
Comments
|
Amlodipine (Norvasc®) |
Hypertension; chronic stable and vasospastic angina |
Tablet: 2.5, 5.0, 10 mg once daily |
6–12 h |
30–50 h |
No effect of grapefruit juice on pharmacokinetics; available as a fixed‐dose combination with benazepril |
Bepridil (Vascor®) |
Refractory angina |
Tablet: 200, 300, 400 mg once daily |
2–3 h |
26–64 h |
Can cause torsade de pointes‐type ventricular tachycardia |
Diltiazem (Tiazac®) (Cardizem®) |
Hypertension; chronic stable and vasospastic angina; atrial fibrillation or flutter; paroxysmal SVT |
Immediate‐ and sustained‐release: 80–480 mg once daily |
0.5–1.5 h immediate) 6–11 h (sustained) |
2–5 h
2.5 h |
Contraindicated in patients with sick‐sinus syndrome and 2nd‐ or 3rd‐degree atrioventricular block |
Felodipine (Plendil®) |
Hypertension |
Sustained‐release: 2.5, 5.0, 10.0 mg once daily |
2.5–5.0 h |
11–16h |
Grapefruit juice causes a two‐fold or more ↑ in felodipine bioavailability; metabolized by CYP3A4; available as a fixed‐dose combination with enalapril |
Isradipine (Dynacirc®) |
Hypertension |
Tablet: 2.5, 5.0 mg twice daily |
1.5 h |
8–12 h |
Sustained‐release form in development |
Nicardipine (Cardene®) |
Hypertension; angina |
Immediate‐release tablet: 20–40 mg three times daily sustained‐release tablet: 60–120 mg once daily |
0.5–2.0 h |
8h 8h |
Available in intravenous form for hypertension treatment |
Nifedipine (Adalat®) (Procardia®) (Procardia‐XL) |
Hypertension; angina ® |
Immediate‐release capsule: 10, 20 mg (dose varies by indication); sustained‐release capsule: 30, 60, 90 mg once daily |
0.5 h |
2h |
Immediate‐release capsule should not be used for control of essential hypertension or acute reduction of blood pressure |
Nimodipine (Nimotop®) |
Subarachnoid hemorrhage |
Capsule: 60 mg every 4 h for 21 days |
1h |
1–2 h |
Crosses the blood‐brain barrier readily; oral therapy should commence within 96 h of hemorrhage |
Nisoldipine (Sular®) |
Hypertension |
Sustained‐release tablet: 10, 20, 30, 40 mg once daily |
6–12 h |
7–12 h |
Grapefruit juice significantly ↑ nisoldipine bioavailability |
Verapamil
(Calan®)
(Calan‐SR®)
(Covera‐HS®) |
Hypertension;
angina; atrial
fibrillation or
flutter; |
Immediate‐release
tablet: dose varies
by indication;
sustained release |
0.5–1.0 h |
4.5–12 h |
Nocturnally indicated forms of verapamil available |
(Verelan PM®) |
paroxysmal SVT |
tablet: 120–480 mg/day |
4–6 h |
4.5–12 h |
|
CYP3A4=cytochrome P3A4; SVT=supraventricular tachycardia; AV=atrioventricular
Adapted with permission from N Engl J Med. 1999;341:1447–1457.
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