Vaginal candidiasis ketoconazole

Fluconazole is very effective in the treatment of infections with most Candida spp. Thrush in the end-stage AIDS patient, often refractory to nystatin, clotrimazole, and ketoconazole, can usually be suppressed with oral fluconazole. AIDS patients with esophageal candidiasis also usually respond to fluconazole. A single 150-mg dose has been shown to be effective treatment for vaginal candidiasis. A 3-day course of oral fluconazole is effective treatment for Candida urinary tract infection and is more convenient than amphotericin B bladder irrigation. Preliminary findings suggest that Candida endophthalmitis can be successfully treated with fluconazole. Stable nonneutropenic patients with candidemia can be adequately treated with fluconazole, but unstable, immunosuppressed patients should initially receive... 

Vaginal candidiasis is treated by clotrimazole, econazole, isoconazole, ketoconazole, miconazole or nystatin as pessaries or vaginal tablets or cream inserted once or twice a day with cream or ointment on surrounding skin. Failure may be due to a concurrent intestinal infection causing reinfection and nystatin tablets may be given by mouth... 

B. Azole antifungals include systemic agents such as keto-conazole, fluconazole, itraconazole, and voriconazole. Topical agents used for the treatment of vaginal candidiasis and thrush include miconazole and clotrimazole. The pharmacologic properties of the systemic azoles differ considerably. Ketoconazole, the first oral azole developed, has poor bioavailability and requires an acidic environment for enhanced absorption. Thus, initial studies required ketoconazole to be administered with a cola to increase bioavailability. Fluconazole, unlike itraconazole and ketoconazole, is hydrophillic and has increased penetration across the blood-brain barrier. Fluconazole is also the only azole that is renally eliminated. 

Terconazole and butoconazole Terconazole is a ketal triazole with structural similarities to ketoconazole. The mechanism of action of terconazole is similar to that of the imidazoles. The 80-mg vaginal suppository is inserted at bedtime for 3 days, whereas the 0.4% vaginal cream is used for 7 days, and the 0.8% cream for 3 days. Clinical efficacy and patient acceptance of both preparations are at least as good as for clotrimazole in patients with vaginal candidiasis. Butoconazole is an imidazole that is pharmacologically quite comparable to clotrimazole. 

Terconazole (Fig. 40.6) is a close analogue of ketoconazole and itraconazole. It is approved only for the treatment of vaginal candidiasis and is not used systemically (Table 40.1) (19,20). 

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