País: Canadá
Idioma: inglés
Fuente: Health Canada
TERCONAZOLE
TARO PHARMACEUTICALS INC
G01AG02
TERCONAZOLE
0.4%
CREAM
TERCONAZOLE 0.4%
VAGINAL
45G
Prescription
AZOLES
Active ingredient group (AIG) number: 0122582001; AHFS:
APPROVED
2003-06-11
PRODUCT MONOGRAPH PR TARO-TERCONAZOLE TERCONAZOLE VAGINAL CREAM 0.4% ANTIFUNGAL AGENT Taro Pharmaceuticals Inc. Date of Revision: 130 East Drive December 23, 2021 Brampton, Ontario L6T 1C1 Control No.: 253982 _TARO-TERCONAZOLE Vaginal Cream 0.4% Product Monograph_ Page 2 of 21 PRODUCT MONOGRAPH PR TARO-TERCONAZOLE Terconazole Vaginal Cream 0.4% Antifungal Agent CLINICAL PHARMACOLOGY Terconazole is a synthetic triazole antifungal agent. Terconazole is active in vitro against various strains of Candida albicans. At fungistatic concentrations terconazole inhibits the transformation of yeast cells into their mycelial form. Terconazole inhibits the cytochrome P450-dependent synthesis of ergosterol, which is a vital component of the fungal cell membranes. ABSORPTION Most of an intravaginally-applied dose of terconazole (mean > 60%) remains in the vaginal area. Absorption into the systemic circulation is slow and limited (<20%). Maximum plasma concentrations of terconazole occur 5 to 10 hours after application of the cream. Systemic exposure to the drug is approximately proportional to the applied dose. The rate and extent of absorption of terconazole are similar in patients with vulvovaginal candidiasis (pregnant or non-pregnant) and healthy subjects. DISTRIBUTION Terconazole is highly protein bound (94.9%) and the degree of binding is independent of drug concentration. METABOLISM Systemically absorbed terconazole is extensively metabolized (>95%). ELIMINATION Across several studies, the mean elimination half-life from plasma for unchanged terconazole ranged from 6.4 to 8.5 hours. Excretion from the systemic circulation after application of a radiolabeled intravaginal dose occurs by both the renal (3 to 10%) and fecal (2 to 6%) routes. MULTIPLE DOSING There is no significant increase in maximum plasma concentration or overall exposure (AUC) after multiple daily applications of the cream. INDICATIONS AND CLINICAL USE TARO-TERCONAZOLE (terconazole) Vaginal Cream 0.4% is indicated for the local treatment of vulvovaginal c Leer el documento completo