mibefradil

Mibefradil is a small molecule calcium channel blocker that was used for the treatment of hypertension and chronic angina pectoris. It is structurally distinct from traditional calcium antagonists and acts primarily by selectively blocking transient (T-type) voltage-gated calcium channels over long-lasting (L-type) channels in vascular smooth muscle and myocardium. This selectivity confers unique pharmacological properties such as minimal negative inotropic effects at therapeutic concentrations and lack of reflex sympathetic activation. Mibefradil also inhibits cytochrome P450 enzymes CYP3A4 and CYP2D6, leading to significant drug-drug interaction risks. The drug was developed by Roche but was withdrawn from the market less than a year after FDA approval due to potentially fatal interactions with other medications[1][2][9].

Brand names

PosicorBatenacBefralCerateQuotaTaxben

Other names

mibefradil dihydrochloride