Sertaconazole

Chemical formula: C₂₀H₁₅Cl₃N₂OS  Molecular mass: 437.77 g/mol  PubChem compound: 65863

Mechanism of action

Sertaconazole, an azole antifungal agent, inhibits fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylase enzyme. This enzyme functions to convert lanosterol to ergosterol. Ergosterol is a key component of fungal cell membranes and lack of this component leads to fungal cell injury by leakage of key constituents in the cytoplasm from the cell.

Pharmacodynamic properties

Activity In Vitro and in Clinical Infections

Sertaconazole nitrate has been shown to be active against isolates of the following microorganisms in clinical infections:

Trichophyton rubrum
Trichophyton mentagrophytes
Epidermophyton floccosum

Pharmacokinetic properties

In a multiple dose pharmacokinetic trial that included 5 male subjects with interdigital tinea pedis (range of diseased area, 42-140 cm²; mean, 93 cm²), sertaconazole cream, 2%, was topically applied every 12 hours for a total of 13 doses to the diseased skin (0.5 grams sertaconazole nitrate per 100 cm²). Sertaconazole concentrations in plasma measured by serial blood sampling for 72 hours after the thirteenth dose were below the limit of quantitation (2.5 ng/mL) of the analytical method used.

© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.