Comparative Pharmacology
Head-to-head clinical analysis: CARDIZEM versus CARDIZEM CD.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CARDIZEM versus CARDIZEM CD.
CARDIZEM vs CARDIZEM CD
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Diltiazem inhibits calcium influx into cardiac and vascular smooth muscle cells during depolarization by binding to L-type calcium channels. This results in coronary vasodilation, decreased myocardial oxygen demand, and negative chronotropic and inotropic effects.
Diltiazem is a calcium channel blocker that inhibits calcium ion influx across cardiac and vascular smooth muscle cell membranes, resulting in dilation of coronary arteries and peripheral arterioles, and decreased myocardial contractility and conduction velocity.
Oral: 30-120 mg three to four times daily; extended-release: 120-360 mg once daily. IV: Initial 0.25 mg/kg (max 25 mg) bolus over 2 minutes, may repeat in 15 minutes (0.35 mg/kg); maintenance: 5-15 mg/hour continuous infusion.
Hypertension: 180-360 mg once daily orally. Angina: 120-360 mg once daily orally. Maximum dose: 480 mg/day.
None Documented
None Documented
Terminal elimination half-life is 3.0-4.5 hours in healthy adults; may be prolonged to 7-9 hours in elderly, hepatic impairment, or renal impairment; clinically relevant for dosing frequency.
Terminal elimination half-life: 6-8 hours (single dose), prolonged to 10-15 hours with multiple dosing or in elderly/hepatic impairment. Clinical context: Therapeutic steady-state achieved in 2-4 days.
Primarily hepatic metabolism with extensive first-pass effect; approximately 2-4% excreted unchanged in urine; fecal excretion accounts for about 65% of dose as metabolites; renal excretion accounts for about 35% of dose as metabolites.
Renal: ~2-4% (unchanged), Hepatic metabolism to multiple metabolites; ~65% renal (metabolites), ~35% fecal/biliary. Total clearance: 5-7 mL/kg/min.
Category C
Category C
Calcium Channel Blocker
Calcium Channel Blocker