Indications
Terconazole is primarily indicated for the treatment of candidiasis, a yeast-like fungal infection affecting the vulva and vagina. This condition, commonly known as a vaginal yeast infection, is characterized by symptoms such as itching, burning, and discharge, and terconazole serves as an effective remedy in mitigating these symptoms.
Pharmacodynamics
Terconazole functions as a triazole antifungal agent designed for intravaginal application. It is closely related to imidazole-derivative antifungal agents, differentiated by its triazole ring consisting of three nitrogen atoms. The mechanism of action involves the inhibition of the 14-alpha-demethylase enzyme, crucial for ergosterol synthesis in fungal cells. The depletion of ergosterol disrupts the fungal cell membrane's structure and functionality, thereby inhibiting fungal growth.
Absorption
The absorption profile of terconazole following intravaginal administration reveals variability dependent on patient-specific factors. In studies conducted on humans, the absorption rate ranged from 5-8% among hysterectomized subjects, while subjects who had not undergone a hysterectomy but had tubal ligations exhibited a higher absorption rate of 12-16%.
Metabolism
Once systemically absorbed, terconazole undergoes rapid and extensive metabolic processing. The primary metabolic pathways include oxidative N- and O-dealkylation, cleavage of the dioxolane ring, and subsequent conjugation. These processes transform terconazole into various metabolites, facilitating its elimination from the body.
Mechanism of Action
Terconazole functions as an antifungal agent by disrupting the integrity of fungal cell membranes. It operates by inhibiting the cytochrome P450 enzyme 14-alpha-demethylase in susceptible fungi. This inhibition results in increased levels of lanosterol and other methylated sterols, while simultaneously reducing ergosterol concentrations. Ergosterol is a crucial component of fungal cell membranes, and its depletion undermines the membrane's structural and functional integrity, ultimately inhibiting or reducing fungal growth.
