Drug Groups

approved

Description

Terconazole is an anti-fungal medication, primarily used to treat vaginal fungal infections. [Wikipedia]

Indication

For the treatment of candidiasis (a yeast-like fungal infection) of the vulva and vagina.

Pharmacology

Terconazole is a triazole antifungal agent available for intravaginal use. It is structurally related to imidazole-derivative antifungal agents, although terconazole and other triazoles have 3 nitrogens in the azole ring. By inhibiting the 14-alpha-demethylase (lanosterol 14-alpha-demethylase), Terconazole inhibits ergosterol synthesis. Depletion of ergosterol in fungal membrane disrupts the structure and many functions of fungal membrane leading to inhibition of fungal growth.

Toxicity

The oral LD₅₀ values were found to be 1741 and 849 mg/kg for the male and female in rat.

Affected Organisms

Biotransformation

Systemically absorbed drug appears to be rapidly and extensively metabolized. Terconazole primarily undergoes oxidatative N- and O-dealkylation, dioxolane ring cleavage, and conjugation.

Absorption

Following intravaginal administration of terconazole in humans, absorption ranged from 5-8% in three hysterectomized subjects and 12-16% in two non-hysterectomized subjects with tubal ligations

Half Life

6.9 hours (range 4.0-11.3)

Protein Binding

94.9%

Elimination

Following oral (30 mg) administration of 14C-labelled terconazole, excretion of radioactivity was both by renal (32-56%) and fecal (47-52%) routes.

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