| Item |
Information |
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Drug Groups
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approved |
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Description
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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 |
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| 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. |
| External Links |
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