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Name: Mibefradil
PubChem Compound ID: 10393179
Description: A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.
Molecular formula: C29H40Cl2FN3O3
Molecular weight: 568.55 g/mol
Name: Mibefradil
Name (isomeric): DB01388
Drug Type: small molecule
Description: A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.
Brand: Posicor
Category: Vasodilator Agents, Calcium Channel Blockers, Antihypertensive Agents
CAS number: 116644-53-2
Indication: For the treatment of angina and high blood pressure.
Mibefradil belongs to a group of medicines called calcium channel blocking agents, or, more commonly, calcium channel blockers. Calcium channel blocking agents affect the movement of calcium into the cells of the heart and blood vessels. As a result, they relax blood vessels and increase the supply of blood and oxygen to the heart while reducing it...
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Mechanism of Action:
Mibefradil is a tetralol calcium channel blocking agent that inhibits the influx of calcium ions across both the T (low-voltage) and L (high-voltage) calcium channels of cardiac and vascular smooth muscle, with a greater selectivity for T channels. Vasodilation occurs in vascular smooth muscle, causing a decrease in peripheral vascular resistance a...
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Absorption: Bioavailability after a single dose is 70%. After multiple dosing, the proportion of mibefradil undergoing first-pass metabolism is reduced, resulting in a steady state bioavailability of approximately 90%. Food does not affect the rate or extent of absorption of mibefradil.
Protein binding: ≥ 99%, primarily to alpha 1-acid glycoprotein.
Biotransformation: The two metabolic pathways that mibefradil undergoes are esterase-catalyzed hydrolysis of the ester side chain (producing an alcohol metabolite) and cytochrome P450 3A4-catalyzed oxidation (that becomes less important during chronic dosing). The pharmacologic effect of the metabolite is approximately 10% of that of the parent mibefradil.
Half Life: 17 to 25 hours at steady state.
Affected organisms: Humans and other mammals
Drug interaction:
TacrolimusThe calcium channel blocker, Mibefradil, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Mibefradil therapy is initiated, discontinued or altered.
AtomoxetineThe CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
TerfenadineIncreased risk of cardiotoxicity and arrhythmias
AstemizoleIncreased risk of cardiotoxicity and arrhythmias
CisaprideMibefradil increases levels of cisapride