Which of the following is a broad spectrum systemic antifungal agent?
High-Yield Explanation
Ketoconazole (KTZ) It is the first orally effective broad-spectrum antifungal drug, useful in both dermatophytosis and deep myc osis. The oral absorption of KTZ is facilitated by gastric acidity because it is more soluble at lower pH. Hepatic metabolism is extensive; metabolites are excreted in urine and faeces. Elimination of KTZ is dose dependent: tlh varies from llh to 6 hours. Penetration in CSF is poor: not effective in fungal men ingitis. However, therapeutic concentrations are attained in the skin and vaginal fluid. In spite of relatively sho tlh, a single daily dose is satisfactory in less severe cases. The usual dose is 200 mg OD or BD; higher doses are sometimes required. Clotrimazole It is effective in the topical treatment of tinea infections like ringworm: Econazole It is similar to clotrimazole; penetrates superficial layers of the skin and is highly effective in dermatophytosis, otomycosis, oral thrush, but is somewhat inferior to clotrimazole in vaginitis Miconazole It is a highly efficacious (>90% cure rate) drug for tinea, pityriasis versicolor, otomycosis, cutaneous and vulvovaginal candidiasis. Because of its good penetrating power, it has been found effective, though paially, even in onychomycosis; single application on skin acts for a few days. ESSENTIALS OF MEDICAL PHARMACOLOGY K.D.TRIPATHI SIXTH EDITION PAGE NO:762