mibefradil


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mibefradil

A calcium-channel blocker that vasodilates without reflex tachycardia, which was used to manage hypertension or chronic stable angina. It was pulled from the market due to its inhibition of the liver metabolism of certain drugs (e.g., antihistamines) and statins, and increased mortality in patients with congestive heart failure.

mibefradil

Posicor® Cardiology A CCB that vasodilates without reflex tachycardia, used to manage HTN and angina pectoris; it was pulled from the market as it inhibits liver metabolism of certain drugs–eg, antihistamine, Histamal, and statin cholesterol-lowering agents. See Calcium channel blocker.
References in periodicals archive ?
T-type calcium channel antagonists, mibefradil and NNC-55-0396 inhibit cell proliferation and induce cell apoptosis in leukemia cell lines.
* LATUDA should not be used concomitantly with strongCYP3A4 inhibitors (eg, ketoconazole, clarithromycin, ritonavir, voriconazole, mibefradil) (1)
In addition, we measured the [Ca.sup.2+] current in [Na.sup.+]-free solution plus 20 [micro]M TTX, which is sensitive to mibefradil, a T-type calcium channel blocker.
(fenfluramine), Posicor (mibefradil), and Duract (bromfenac) in 1997,
Exclusion criteria were the following: (1) coronary heart disease; (2) allergy to simvastatin; (3) active hepatitis and/or severe renal impairment (serum creatinine > 200 [micro]mol/L); (4) pregnancy or lactation; (5) taking medication(s) that may increase the effective concentration of simvastatin (e.g., a tetralol-derived calcium-channel blocker such as mibefradil); and (6) hyperlipidemia.
Several medicines were withdrawn from the market due to their interaction with other substances (mainly related to the CYPs) for example: Seldane[R] (Terfenadine, Aventis Pharmaceuticals, USA), Posicor[R] (Mibefradil, Roche, Switzerland), Propulsid[R] (Cisapride, Janssen-Ortho, Canada), Lotronex[R] (Alosetron, Prometheus Laboratories Inc., USA), Baycol[R] (Cerivastatin, Bayer A.G., Germany) and Serzone[R] (Nefazodone, Bristol-Myers Squibb, USA) (25).
Sodium hydrosulfide hydrate (NaHS), EGTA, thapsigargin (TG), nifedipine, nimodipine, and mibefradil were obtained from Sigma-Aldrich.
* Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir, voriconazole, mibefradil, etc.) [see Drug Interactions (7.1)].
Anti-adhering and anti-migratory compounds ilomastat (a matrix metalloproteinase inhibitor), naphtyl urea suramin, [44] salmosin (a disintegrin), [45] mibefradil (Ca- channel inhibitor), [46] RGD peptide, EDTA, [47] and coating an acrylic IOL surface with MPC polymer; [48]
Nam et al., "Facilitation of [Ca.sup.2+]-activated [K.sup.+] channels (IKCa1) by mibefradil in B lymphocytes," Pflugers Archiv European Journal of Physiology, vol.
All drugs were prepared as stock solutions: capsaicin (10 mM) in DMSO, [Ni.sup.2+] (100 mM), and mibefradil (5 mM) in [H.sub.2]O.
However, selective blockade of [Ca.sub.v]3 (T-type) calcium channels located predominantly in ICCs with mibefradil (3 [micro]M) significantly (P < 0.05) depressed the outflow of adenine nucleosides from both control and TNBS-treated preparations (Figure 4).