Diltiazem (malate)

Diltiazem malate is a potent and orally active L-type calcium channel inhibitor. Diltiazem malate shows antihypertensive and antiarrhythmic effects. Diltiazem malate can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris^[1][2][3]. In Vitro:Diltiazem malate (200 μM) elicits a use-dependent blockade that proceeded within a relatively small number of pulses^[1]. Diltiazem malate reduces Ca²⁺ influx by accelerating inactivation during action potentials, and that the use-dependent blockade is due to increases in the number of channels in a sustained closed state^[1]. In Vivo:Diltiazem malate (100 mg/kg; p.o.; daily for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner^[3]. Diltiazem malate (100 mg/kg; p.o.; daily for 6 days) with ATII (1.44 mg/kg; p.o.; daily for 6 days) reduces the ATII-induced vascular inflammation and macrophage accumulation in ApoE?/? mice^[3]. Diltiazem malate (2 mg/kg; i.v.) exhibits T_1/2 of 61.2 min, CL_el of 3.2 mL/min in rats^[4].