1. The effects of several CYP3A substrates (alpha-naphthoflavone (alphaNF), terfenadine, midazolam, erythromycin) on nifedipine oxidation and testosterone 6beta-hydroxylation activities were investigated in hepatic and intestinal microsomes from mouse and human. 2. alphaNF (10 microM) and terfenadine (100 microM) inhibited nifedipine oxidation activities (at substrate concentration of 100 micro...

Hot flushes are one of the most frequent symptoms in menopausal women. We investigated effect of soybean isoflavones (Soyaflavone HG) on nifedipine-induced flushing in ovariectomized mice. Ovariectomy markedly aggravated nifedipine-induced increase in tail skin temperature. Soyaflavone HG (10 mg/kg, p.o., once a day for 5 days) inhibited nifedipine-induced flushing in ovariectomized mice. The i...

Ten male asthmatic volunteers each inhaled two puffs (200 micrograms) of salbutamol on two separate days 30 minutes after double blind oral administration of either 20 mg nifedipine or identical placebo. FEV1 was recorded before and at intervals for four hours after inhalation of salbutamol. Overall the FEV1 was significantly greater during the four hour period after premedication with nifedipi...

The effect of 5 days of oral nifedipine treatment (~t mg/kg per day in drinking water) on low density lipoprotein (LDL) and cholesterol accumulation in rabbit arteries was determined. Compared with control aortas, nifedipine treatment (w=5) significantly reduced homologous I-tyramine cellobioseLDL accumulation (control versus nifedipine: 45.93±4.3 versus 20.14±3.1 ng LDL per milligram dry weigh...

Agents to inhibit the renin-angiotensin system have been reported to suppress the progression of abdominal aortic aneurysm (AAA). However, the effects of calcium channel blockers (CCBs) are still unclear in terms of the inhibition of the progression of AAA. Recently, several effects of CCBs beyond those associated with blood pressure lowering have attracted much interest. In this study, we exam...

Background: Preeclampsia is a highly prevalent disease among pregnant women. In the event of hypertensive emergency, nifedipine, labetalol, and hydralazine are assigned as first-line therapies in preeclampsia. Further studies needed to compare effectiveness these drugs find most cost-effective drug with minimal side effects. This study aimed lowering blood pressure d...

In a placebo-controlled, randomized, cross-over, double-blind study of 12 patients with stable exertional angina, we measured at rest and during bicycle exercise the effects of 20 mg of nifedipine administered sublingually on hemodynamics and systemic and regional oxygen extraction and metabolism. Nifedipine decreased systemic vascular resistance by 38% at rest (p < .001) and by 28% during exer...

Nine patients with severe coronary artery disease and disabling angina receiving either regular metoprolol or oxprenolol, together with glyceryl trinitrate tablets as required for chest pain, were studied. Nifedipine 10 mg three times per day was compared to placebo in a double blind randomized control trial, using patient diary cards and exercise tests. The number of recorded episodes of angin...

Aim of Work: To compare the safety & efficacy of oral nifedipine with transdermal nitroglycerin in the inhibition of preterm labour. Methods: This study included 60 women in preterm labour, randomly divided into two groups, the first 30 patients received oral nifedipine and the second 30 patients used transdermal nitroglycerin (NTG). Patients in preterm labour with a single gestation, between t...

Midazolam, triazolam (TRZ), testosterone, and nifedipine have all been widely used as probes for in vitro metabolism of CYP3A. We used these four substrates to assess the contributions of CYP3A4 and CYP3A5 to in vitro biotransformation in human liver microsomes (HLMs) and in recombinant enzymes. Recombinant CYP3A4 and CYP3A5 (rCYP3A4 and rCYP3A5) both produced 1-OH and 4-OH metabolites from mid...