Products
Mibefradil (Posicor tablets) was launched in many countries in 1996 and withdrawn from the market in 1998 because of potential interactions. It is no longer commercially available.
Structure and properties
Mibefradil (C29H38FN3O3, Mr = 495.6 g/mol) is a benzimidazole and a tetralol derivative. It is present in drugs as mibefradildihydrochloride.
Effects
Mibefradil (ATC C08CX01) has vasodilatory, antiischemic, and antihypertensive properties. It blocks T-type (transient, low-voltage-activated) calcium channels rather than L-type like most agents in this drug group.
Indications
For the treatment of hypertension (essential hypertension) and angina.
Interactions
Mibefradil is an inhibitor of CYP3A4, CYP2D6, and CYP1A2 and can cause numerous and potentially dangerous drug-drug interactions. Therefore, it was withdrawn from the market in 1998. Another reason was that a study of its use in heart failure showed negative results. However, numerous drugs with which mibefradil can cause interactions are no longer on the market today (e.g., astemizole, terfenadine, cisapride).
