Paper II
2025 March (Supplementary (SAY)) (2019 Scheme) · 100 marks · 180 min

Question

Classify antifungal drugs. Explain the mechanism of action, uses, and adverse effects of Amphotericin B. Add a note on the various liposomal formulations of Amphotericin B (2+6+2)

Q210 marksEssays

Answer

Classification of antifungal drugs

ClassExamples
PolyenesAmphotericin B, Nystatin
AzolesFluconazole, Itraconazole, Ketoconazole
EchinocandinsCaspofungin, Micafungin
OthersFlucytosine, Terbinafine, Griseofulvin

Amphotericin B — mechanism, uses, adverse effects Mechanism: binds ergosterol directly in the fungal cell membrane, forming pores that disrupt membrane integrity and cause leakage of intracellular contents — fungicidal. Selectivity depends on ergosterol-versus-cholesterol binding preference, real but imperfect (residual cholesterol affinity, particularly renal tubular cells).

Uses: severe systemic/invasive fungal infections (invasive candidiasis, aspergillosis, cryptococcal meningitis), visceral leishmaniasis.

Adverse effects: nephrotoxicity (dose-limiting), infusion-related reactions (fever, chills, rigors), hypokalemia, hypomagnesemia, anemia.

Note on liposomal formulations Lipid-based formulations (liposomal amphotericin B, amphotericin B lipid complex, amphotericin B colloidal dispersion) encapsulate the drug in a lipid carrier, substantially reducing off-target renal tubular binding while preserving — and in visceral leishmaniasis, actually improving via preferential reticuloendothelial uptake — antifungal efficacy. This favorable safety profile allows higher doses and shorter treatment courses, at significantly higher cost than conventional amphotericin B.

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