II. Indications

  1. Chronic stable Angina
  2. Hypertension

III. Mechanism

  1. Blocks calcium influx at 2 types of calcium channels
    1. L-type (long-acting) channels
      1. Blocked by standard Calcium Channel Blockers
    2. T-type (transient) channels
      1. Blocked uniquely by Mibefradil
      2. Activated at lower voltages
      3. Present in:
        1. Vascular smooth muscle
        2. Myocardial conduction system
      4. Absent in
        1. Ventricular Myocardium
  2. Effect of Mibefradil
    1. Produces coronary and peripheral vasodilatation
    2. Does not result in reflex Tachycardia

IV. Efficacy

  1. Antihypertensive
    1. More effective then Diltiazem
    2. As effective as Amlodipine and Nifedipine
    3. Synergistic effect with ACE Inhibitors
  2. Anti-Anginal
    1. Delays onset of ischemia during Exercise
    2. Increases Exercise tolerance

V. Contraindications

VI. Drug Interactions

  1. Fatal arrhythmia risk with
    1. Terfenadine
    2. Astemizole
    3. Cisapride
  2. Increases levels of
    1. Tricyclic Antidepressant
    2. Cyclosporine

VII. Adverse Effects

  1. Dizziness
  2. Fatigue
  3. Light headedness
  4. Peripheral Edema LESS common than others in class

VIII. Dosing

  1. 50 mg PO qd (up to 100 mg PO qd)

Images: Related links to external sites (from Bing)

Related Studies (from Trip Database) Open in New Window

Ontology: Mibefradil (C0286185)

Definition (MSH) A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D020748
SnomedCT 421651006, 319318006
English mibefradil, Mibefradil (substance), MIBEFRADIL, Mibefradil, Mibefradil [Chemical/Ingredient], (1S,2S)-(2-((3-(2-Benzimidazolyl)Propyl)Methylamino)Ethyl)-6-Fluoro-1,2,3,4-Tetrahydro-1-Isopropyl-2-Naphthyl Methoxyacetate, Acetic acid, methoxy-, 2-(2-((3-(1H-benzimidazol-2-yl)propyl)methylamino)ethyl)-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl ester, (1S-cis)-, Mibefradil (product)
Spanish mibefradil (sustancia), mibefradil (producto), mibefradil, Mibefradil
Swedish Mibefradil
Czech mibefradil
Finnish Mibefradiili
Russian MIBEFRADIL, МИБЕФРАДИЛ
Japanese ミベフラジル
Polish Mibefradyl
French Mibéfradil
German Mibefradil
Italian Mibefradile
Portuguese Mibefradil