FLUCONAZOLE - AN UPDATE OF ITS ANTIMICROBIAL ACTIVITY, PHARMACOKINETIC PROPERTIES, AND THERAPEUTIC USE IN VAGINAL CANDIDIASIS

Fluconazole is a bis-triazole antifungal drug,which has a pharmacokine tic profile characterised by its high water solubility, low affinity f or plasma proteins, and metabolic stability. After a single 150mg oral dose, therapeutic concentrations in vaginal secretions are rapidly ac hieved and are sustained for a duration sufficient to produce high cli nical and mycological responses in nonimmunocompromised patients with vaginal candidiasis (candidosis). At this dosage, clinical and mycolog ical responses have compared favourably with responses achieved after multiple dose regimens of other oral and intravaginal antifungal agent s. Clinical efficacy rates have ranged between 92 and 99% at short ter m evaluation (5 days post-treatment). At 80 to 100 days post-treatment clinical efficacy rates of 91% have been reported. In addition, limit ed data indicate that fluconazole is more effective than placebo as pr ophylactic treatment of frequently recurring vaginal candidiasis. Sing le oral doses of fluconazole 150mg are well tolerated Most frequently observed adverse events are gastrointestinal symptoms, which are gener ally mild and transient in nature. Thus, fluconazole is a valuable alt ernative to established systemic and intravaginal azole antifungal dru gs which are used to treat vaginal candidiasis. Moreover; in view of i ts favourable patient acceptability and compliance profile compared wi th alternative treatments, single-dose oral fluconazole should be cons idered as a first-line therapeutic choice for the treatment of women w ith vaginal candidiasis.