Brands, Medical Use, Clinical Data
- Anti-Bacterial Agents
- Antifungal Agents
- Antiprotozoal Agents
- Slow intravenous-infusion
Brands / Synonyms
Abelcet; ABLC; AM B Isome; AmB; AmBisome; AMPH-B; Ampho-Moronal; Amphocin; Amphortericin B; Amphotec; Amphotericin; Amphotericin B; Amphotericine B; Amphozone; Fungilin; Fungisone; Fungizone; Fungizone Intravenous; Halizon; HSDB 3008 IAB; IAB; Liposomal Amphotericin B; LNS-AmB; Mysteclin-F; Tegopen
Used to treat potentially life threatening fungal infections.
Amphotericin B shows a high order of in vitro activity against many species of fungi. Histoplasma capsulatum, Coccidioides immitis, Candida species, Blastomyces dermatitidis, Rhodotorula, Cryptococcus neoformans, Sporothrix schenckii, Mucor mucedo, and Aspergillus fumigatus are all inhibited by concentrations of amphotericin B ranging from 0.03 to 1.0 mcg/mL in vitro. While Candida albicans is generally quite susceptible to amphotericin B, non-albicans species may be less susceptible. Pseudallescheria boydii and Fusarium sp. are often resistant to amphotericin B. The antibiotic is without effect on bacteria, rickettsiae, and viruses.
Mechanism of Action
Amphotericin B is fungistatic or fungicidal depending on the concentration obtained in body fluids and the susceptibility of the fungus. The drug acts by binding to sterols in the cell membrane of susceptible fungi with a resultant change in membrane permeability allowing leakage of intracellular components. Ergosterol, the principal sterol in the fungal cytoplasmic membrane, is the target site of action of amphotericin B and the azoles. Amphotericin B, a polyene, binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.
Bioavailability is 100% for intravenous infusion.
Oral, rat: LD50 = >5 gm/kg. Amphotericin B overdoses can result in cardio-respiratory arrest.
Biotrnasformation / Drug Metabolism
This product is contraindicated in those patients who have shown hypersensitivity to amphotericin B or any other
component in the formulation unless, in the opinion of the physician, the condition requiring treatment is
life-threatening and amenable only to amphotericin B therapy.
When administered concurrently, the following drugs may interact with amphotericin B:
Antineoplastic agents: may enhance the potential for renal toxicity, bronchospasm and hypotension.
Antineoplastic agents (e. g., nitrogen mustard, etc.) should be given concomitantly only with great caution.
Corticosteroids and Corticotropin (ACTH): may potentiate amphotericin B- induced hypokalemia which
may predispose the patient to cardiac dysfunction. Avoid concomitant use unless necessary to control side effects of
amphotericin B. If used concomitantly, closely monitor serum electrolytes and cardiac function.
Digitalis glycosides: amphotericin B-induced hypokalemia may potentiate digitalis toxicity.
Serum potassium levels and cardiac function should be closely monitored and any deficit promptly corrected.
Flucytosine: while a synergistic relationship with amphotericin B has been reported, concomitant use
may increase the toxicity of flucytosine by possibly increasing its cellular uptake and/or impairing its renal
Imidazoles (e. g., ketoconazole, miconazole, clotrimazole, fluconazole, etc.): in vitro and
animal studies with the combination of amphotericin B and imidazoles suggest that imidazoles may induce fungal
resistance to amphotericin B. Combination therapy should be administered with caution, especially in
Other nephrotoxic medications: agents such as aminoglycosides, cyclosporine, and pentamidine may
enhance the potential for drug-induced renal toxicity, and should be used concomitantly only with great
caution. Intensive monitoring of renal function is recommended in patients requiring any combination of nephrotoxic
Skeletal muscle relaxants: amphotericin B-induced hypokalemia may enhance the curariform
effect of skeletal muscle relaxants (e.g., tubocurarine). Serum potassium levels should be monitored and deficiencies
Leukocyte transfusions: acute pulmonary toxicity has been reported in patients receiving intravenous
amphotericin B and leukocyte transfusions.