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
Fungi
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.
