Itraconazole: a single-day oral treatment for acute vulvovaginal candidosis.

Itraconazole is an oral broad-spectrum antifungal agent with a propensity to leave the plasma and achieve high and persistent levels in tissues where fungi reside. Indeed, the highly lipophilic character of itraconazole results in a favourable tissue:blood ratio: most tissue concentrations exceed by far concentrations in the blood. Itraconazole has a depot effect in the skin and mucous membranes without leaking back into the plasma. In addition, the high lipophilicity and the specific molecular shape result in the ability to easily penetrate Candida cell membranes and in a high selectivity for Candida cytochrome P450. At therapeutic doses there is no known interference with human enzyme systems. This promising pharmacological profile has been challenged in extensive clinical trials. The feasibility of one-day therapy was assessed in a clinical study in which three different dosage regimens were compared in a total of 552 patients with acute vulvovaginal candidosis: 200 mg twice daily for one day; 200 mg once daily for two days; and 200 mg once daily for three days. A total dose of 400 mg of itraconazole given in one single day cured 80% of patients (defined as mycologically negative) one month after the end of treatment. The results indicate that the difference in the length of therapy (one, two or three days) plays no statistically significant role in determining the final cure rate of itraconazole in acute vulvovaginal candidosis. Subsequent pharmacokinetic analysis indicated that therapeutic concentrations of itraconazole persist in the vaginal wall for at least three days after discontinuation of therapy, suggesting that one-day therapy would be appropriate.