Drug intelligence / Profile preview

nifedipine + clotrimazole

Development stage
Unknown
Lead developer
Bayer
Modality
Small Molecules
Administration
Topical
01

Overview

Nifedipine + clotrimazole is a combination of two small molecule drugs, each with distinct mechanisms of action. Nifedipine is a dihydropyridine calcium channel blocker that inhibits the influx of calcium ions through L-type calcium channels in vascular smooth muscle and myocardial cells, leading to vasodilation and reduced blood pressure. It is primarily used for hypertension, angina, and as a topical agent for anal fissures due to its smooth muscle relaxant properties[4]. Clotrimazole is an imidazole antifungal agent that disrupts fungal cell membrane synthesis by inhibiting the enzyme lanosterol 14-α-demethylase (a cytochrome P450 enzyme), resulting in increased membrane permeability and inhibition of fungal growth[7]. The combination may be considered for compounded topical preparations where both antifungal activity (from clotrimazole) and local vasodilatory/smooth muscle relaxation (from nifedipine) are desired; however, there are no widely recognized or approved fixed-dose products containing only these two agents together. Notably, co-administration can increase the risk of adverse cardiovascular effects such as ventricular dysfunction or edema due to pharmacokinetic interactions[1].

02

Targets

LTCC (Voltage-gated calcium channel (L-type))CYP51A1 (Sterol 14α-demethylase)

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