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Ketoconazol

e
– First orally effective broad spectrum antifungal
– Effective against
• Dermatophytosis, Deep mycosis , Candidiasis
Pharmacokinetics
• Effective orally
• acidic environment
favours
absorption
• High protein
binding
• Readily distributed, not to
BBB
• Metabolized in liver,
excreted in bile
• t1/2 = 8- 10 hrs
Adverse events
• Nausea , vomiting , anorexia
• Headache , paresthesia, alopecia
• ↓ steroid, testosterone & estrogen
synthesis
– Gynaecomastia, oligospermia , loss of
libido &
impotence in males
– Menstrual irregularities & amenorrhoea
in females
• Elevation of liver enzymes
• Hypersensitivity reaction - skin rashes,
Drug Interactions
Uses
• Dermatophytosis: conc in stratum corneum
• Monilial vaginitis : 5-7 days
• Systemic mycosis: blastomycosis,
histoplasmosis, coccidiodomycosis
– Less efficacy than AMB & slower
response
– ↓Efficacy in immunocompromized
and meningitis
– Lower toxicity than AMB higher than
triazoles
• High dose used in cushings

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