Antifungal Drugs

AMPHOTERICIN B
 Nearly insoluble in water; prepared as a
colloidal suspension

 Newer Preparation follows lipid delivery

system

 Poorly absorbed. (Can only be use for gut

fungus)
 Pharmacokinetics
 More than 90% plasma bound

 The serum t1/2 is approximately 15 days

 Hepatic and renal adjustment is not required

 Cross BBB (Intrathecal injection for fungal

meningitis)
 Mode of action
 The major component of fungal cell wall is
Ergosterol while for human and bacterial cells
its cholesterol.

 Amphotericin B binds to ergosterol and alters

the permeability of the cell by forming
amphotericin B-associated pores in the cell
membrane.
 Mode of action
 The pore allows the leakage of intracellular
ions and macromolecules, eventually leading
to cell death.

 Drug Toxicity

 Resistance if ergosterol is binds less to drug

 Antifungal Activity

 Candida albicans
 Cryptococcus neoformans
 Histoplasma capsulatum
 Blastomyces dermatitidis
 Coccidioides immitis
 Aspergillus fumigatus
 Clinical uses
 Initial regimn but withdrawn latter in therapy

 severe fungal pneumonia (with altered mental

state)

 Sepsis syndrome

 Relapse
 Clinical uses
 Final choice for fungal meningitis

 Mycotic corneal ulcers

 keratitis

 Fungal arthritis
 Adverse Drug Effects
 Fever
 Chills
 muscle spasms
 vomiting, headache
 Hypotension
 Azotemia
 Renal Impairment