Pharmacology · Antifungal and Antiviral Drugs (Antiretrovirals)

Amphotericin B causes nephrotoxicity via a direct tubular mechanism. The strategy of using liposomal amphotericin B (L-AmB) reduces nephrotoxicity because:

  • A Liposomal encapsulation reduces renal tubular delivery of free amphotericin B while maintaining bioavailability to fungal cell membranes
  • B Liposomes decrease gastrointestinal absorption, reducing systemic exposure
  • C Liposomal formulation enhances hepatic first-pass metabolism, lowering plasma drug levels
  • D Liposomes chelate amphotericin B in the kidney tubule, preventing direct toxicity
Correct answer: A. Liposomal encapsulation reduces renal tubular delivery of free amphotericin B while maintaining bioavailability to fungal cell membranes

Explanation

Liposomal amphotericin B preferentially accumulates in organs rich in reticuloendothelial (mononuclear phagocyte) cells (liver, spleen, lungs — sites of fungal infection) while delivering less free drug to renal tubular epithelium. The lipid vehicle shields the drug from renal tubule exposure; drug is released preferentially at sites of fungal infection where phospholipase activity and altered membrane composition trigger release. This selective tissue distribution markedly reduces nephrotoxicity without compromising antifungal efficacy.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.

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