II. Indications
- Chronic stable Angina
- Hypertension
III. Mechanism
- Blocks calcium influx at 2 types of calcium channels
- L-type (long-acting) channels
- Blocked by standard Calcium Channel Blockers
- T-type (transient) channels
- Blocked uniquely by Mibefradil
- Activated at lower voltages
- Present in:
- Vascular smooth muscle
- Myocardial conduction system
- Absent in
- Ventricular Myocardium
- L-type (long-acting) channels
- Effect of Mibefradil
- Produces coronary and peripheral vasodilatation
- Does not result in reflex Tachycardia
IV. Efficacy
- Antihypertensive
- More effective then Diltiazem
- As effective as Amlodipine and Nifedipine
- Synergistic effect with ACE Inhibitors
- Anti-Anginal
V. Contraindications
- Sick Sinus Syndrome
- AV Block without a Pacemaker
VI. Drug Interactions
- Fatal arrhythmia risk with
- Terfenadine
- Astemizole
- Cisapride
- Increases levels of
VII. Adverse Effects
- Dizziness
- Fatigue
- Light headedness
- Peripheral Edema LESS common than others in class
VIII. Dosing
- 50 mg PO qd (up to 100 mg PO qd)
IX. References
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| 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, МИБЕФР�ДИЛ |
| Japanese | ミベフラジル |
| Polish | Mibefradyl |
| French | Mibéfradil |
| German | Mibefradil |
| Italian | Mibefradile |
| Portuguese | Mibefradil |
