FDA Section 12 \u2022 mechanism \u2022 pharmacokinetics

Butoconazole - How It Works

Clinical pharmacology details from the US FDA-approved label: how Butoconazole works in your body, how it's absorbed, how long it stays active, and how it's eliminated.

CLINICAL PHARMACOLOGY Following vaginal administration of butoconazole nitrate vaginal cream, 2% to 3 women, 1.7% (range 1.3-2.2%) of the dose was absorbed on average.

Peak plasma levels (13.6-18.6 ng radioequivalents/mL of plasma) of the drug and its metabolites are attained between 12 and 24 hours after vaginal administration.

Microbiology - The exact mechanism of the antifungal action of butoconazole nitrate is unknown; however, it is presumed to function as other imidazole derivatives via inhibition of steroid synthesis.

Imidazoles generally inhibit the conversion of lanosterol to ergosterol, resulting in a change in fungal cell membrane lipid composition.

This structural change alters cell permeability and, ultimately, results in the osmotic disruption or growth inhibition of the fungal cell.

Butoconazole nitrate is an imidazole derivative that has fungicidal activity in vitro against Candida spp. and has been demonstrated to be clinically effective against vaginal infections due to Candida albicans .

Candida albicans has been identified as the predominant species responsible for vulvovaginal candidiasis.

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