Terconazole (R42470)

A triazole antifungal

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50mg

￥975.00

780.00

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100mg

￥1300.00

1040.00

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Background

Terconazole is an orally bioavailable broad-spectrum triazole antifungal agent that completely inhibits growth of T. rubrum, M. audouini, M. canis, and T. verrucosum, as well as some C. albicans and A. fumigatus strains and other fungi when used at a concentration of 100 μg/ml.¹ It also has bacteriostatic activity against E. coli, P. aeruginosa, S. aureus, and S. pyogenes when used at a concentration of 100 μg/ml. Terconazole eliminates vaginal C. albicans candidiasis infection in 97% of rats when administered as a 1% topical ointment and in 50% of rats when orally administered at a dose of 10 mg/kg. It inhibits cytochrome P450 (CYP) isoforms involved in ergosterol biosynthesis, interfering with fungal cell membranes.² It decreases synthesis of 14α-desmethyl sterols and increases synthesis of methylated sterols in C. albicans (IC₅₀ = 3 nM).³ Formulations containing terconazole have been used in the treatment of candidiasis of the vulva and vagina.

1.Van Cutsem, J., Van Gerven, F., Zaman, R., et al.Terconazole - a new broad-spectrum antifungalChemotherapy29(5)322-331(1983) 2.Vanden Bossche, H., and Marichal, P.Mode of action of anti-Candida drugs: Focus on terconazole and other ergosterol biosynthesis inhibitorsAm. J. Obstet. Gynecol.165(4 Pt 2)1193-1199(1991) 3.Isaacson, D.M., Tolman, E.L., Tobia, A.J., et al.Selective inhibition of 14α-desmethyl sterol synthesis in Candida albicans by terconazole, a new triazole antimycoticJ. Antimicrob. Chemother.21(3)333-343(1988)

Protocol

Animal experiment:

Rats: The rats are infected intravaginally with C. albicans. They are treated topically twice daily for 3 days, starting 24 hours after infection with a volume of 0.2 mL of various concentrations of terconazole (0.125%, 0.25%, 0.4%, 0.5%, 1%, 2%), miconazole, clotrimazole, econazole, nystatin, or amphotericin B[2].

参考文献:

[1]. Tolman EL, et al. Anticandidal activities of terconazole, a broad-spectrum antimycotic. Antimicrob Agents Chemother. 1986 Jun;29(6):986-91.
[2]. Van Cutsem J, et al. The in vitro activity of terconazole against yeasts: its topical long-acting therapeutic efficacy in experimental vaginal candidiasis in rats. Am J Obstet Gynecol. 1991 Oct;165(4 Pt 2):1200-6.