Terconazole

(BAN, USAN, rINN)
Terconazole Chemical formula
Synonyms: R-42470; Terconazol; Terconazolum; Terkonatsoli; Terkonazol; Terkonazolas; Triaconazole. 1-{4-[[2-(2,4-Dichlorophenyl)r-2(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolanc-4-yl]methoxy]phenyl}-4-isopropylpiperazine.
Cyrillic synonym: Терконазол.

💊 Chemical information

Chemical formula: C26H31Cl2N5O3 = 532.5.
CAS — 67915-31-5.
ATC — G01AG02.
ATC Vet — QG0 1AG02.

Pharmacopoeias.

In Eur..

Ph. Eur. 6.2

(Terconazole). A white or almost white powder. It exhibits polymorphism. Practically insoluble in water; sparingly soluble in alcohol; soluble in acetone; freely soluble in dichloromethane. Protect from light.

💊 Adverse Effects

Local reactions including burning and itching have been reported with vaginal use of terconazole. Other adverse effects have included dysmenorrhoea and genital, body, and abdominal pain. A flu-like syndrome with headache, fever, chills, and hypotension has been reported in some patients and may be more prevalent with vaginal pessaries providing doses larger than 80 mg.

Flu-like syndrome.

References.
1. Moebius UM. Influenza-like syndrome after terconazole. Lancet 1988; ii: 966–7.

💊 Precautions

Intravaginal preparations of terconazole may damage latex contraceptives and additional contraceptive measures are therefore necessary during local application. For a discussion of the caution needed when using azole antifungals during pregnancy, see under Pregnancy in Precautions of Fluconazole.

💊 Antimicrobial Action

Terconazole is a triazole derivative that is thought to disrupt normal fungal cell membrane permeability. Terconazole is active in vitro against Candida spp. and other fungi. It has some antibacterial activity in vitro but not against usual vaginal flora such as lactobacilli.

💊 Pharmacokinetics

After intravaginal use, 5 to 16% of terconazole is absorbed. Systemically absorbed drug is metabolised by the liver and excreted in urine and faeces.

💊 Uses and Administration

Terconazole is a triazole antifungal used in the local treatment of vulvovaginal candidiasis. Intravaginal dosage regimens are terconazole 40 mg (as 0.8% vaginal cream) or 80 mg (as a pessary) at bedtime for 3 nights or 20 mg (as 0.4% cream) at bedtime for 7 nights.

💊 Preparations

Proprietary Preparations

Belg.: Gyno-Terazol†; Braz.: Ginconazol†; Gyno-Fungix; Canad.: Te r a z o l; Mex.: Fungistat; S.Afr.: Te r a z o l ; Switz.: Gyno-Terazol; USA: Te r azo l ; Za zole; Venez.: Fungistat.
Published December 20, 2018.