Pharmacologic and pharmacokinetic profile of mibefradil, a T- and L-type calcium channel antagonist.
Mibefradil is a recently introduced calcium antagonist that, as a tetralol derivative, is chemically distinct from previous calcium antagonists. This article will review pertinent results from in vitro, animal, and clinical investigations to report the pharmacologic properties that distinguish mibefradil from all of the calcium channel antagonists in use today, all of which operate on the "L-type" calcium channel. Mibefradil's pharmacokinetic profile indicates it can be used as a once-daily oral treatment for hypertension and chronic stable angina pectoris.
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Department of Medicine and Pharmacology, Georgetown University Medical Center, Washington, DC 20007, USA.
D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001665:Binding Sites; D002121:Calcium Channel Blockers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002318:Cardiovascular Diseases / Q000188:drug therapy; D018849:Controlled Clinical Trials as Topic; D003331:Coronary Vessels / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006207:Half-Life; D006329:Heart Conduction System / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D020748:Mibefradil; D009130:Muscle, Smooth / Q000187:drug effects; D012079:Renal Circulation / Q000187:drug effects; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D014655:Vascular Resistance / Q000187:drug effects
D001562:Benzimidazoles; D002121:Calcium Channel Blockers; D013764:Tetrahydronaphthalenes; D020748:Mibefradil