It covers the chemical nature, mechanism of action, uses, side effects, and recent developments related to ketoconazole in pharmaceutical applications.

1. Use of Ketoconazole
• Pharmaceutical Applications and Mechanism
of Action
• Presented by: [Your Name]
• [Institution Name]

2. Introduction
• Ketoconazole is a broad-spectrum antifungal
agent belonging to the imidazole class, used to
treat fungal infections in humans and animals.

3. Objectives
• • Understand the chemical nature and
mechanism of ketoconazole
• • Explore its therapeutic applications
• • Identify adverse effects and limitations

4. Chemical Nature
• • Chemical Formula: C26H28Cl2N4O4
• • Belongs to imidazole derivatives
• • Acts by inhibiting ergosterol synthesis in
fungal cell membranes

5. Mechanism of Action
• • Inhibits fungal cytochrome P450 enzyme
(lanosterol 14α-demethylase)
• • Prevents conversion of lanosterol to
ergosterol
• • Disrupts cell membrane integrity, leading to
fungal death

6. Pharmaceutical Uses
• • Treatment of systemic and superficial fungal
infections
• • Effective against dermatophytes, yeasts, and
dimorphic fungi
• • Available in topical, oral, and shampoo
formulations

7. Common Indications
• • Tinea infections (ringworm, athlete’s foot)
• • Seborrheic dermatitis and dandruff
• • Candidiasis (oral, cutaneous, systemic)
• • Fungal prostatitis and chronic
mucocutaneous candidiasis

8. Topical Applications
• • Ketoconazole creams and shampoos used
for local fungal infections
• • Reduces inflammation and itching
• • Typical concentration: 1–2% formulations

9. Systemic Administration
• • Oral ketoconazole used for systemic fungal
infections
• • Absorbed well in acidic environment
• • Must monitor liver function due to potential
hepatotoxicity

10. Adverse Effects
• • Hepatotoxicity (rare but serious)
• • Gastrointestinal disturbances
• • Endocrine effects: decreases testosterone
and cortisol synthesis
• • Allergic reactions or skin irritation (topical)

11. Drug Interactions
• • Inhibits CYP3A4 enzyme – can increase
plasma levels of other drugs
• • Avoid co-administration with certain
antihistamines, anticoagulants, and statins

12. Recent Developments
• • Decline in oral use due to safety concerns
• • Preference for safer azoles like fluconazole
and itraconazole
• • Continued use in dermatology as topical
formulation

13. Advantages
• • Broad antifungal spectrum
• • Dual anti-inflammatory and antifungal
properties
• • Effective topical control for scalp and skin
infections

14. Limitations
• • Systemic toxicity limits oral use
• • Resistance development in long-term use
• • Requires acidic medium for absorption

15. Conclusion
• Ketoconazole remains an important antifungal
agent, especially in topical therapy, despite
reduced systemic use due to safety concerns.

16. References
• • Goodman & Gilman’s Pharmacological Basis
of Therapeutics
• • WHO Model List of Essential Medicines
• • FDA Drug Safety Communications
• • Research Articles in Antimicrobial Agents
and Chemotherapy Journal