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QuickView for amphotericin b (compound)


PubChem
Name: Amphotericin B
PubChem Compound ID: 10533925
Description: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.
Molecular formula: C47H73NO17
Molecular weight: 964.778 g/mol
DrugBank
Identification
Name: Amphotericin B
Name (isomeric): DB00681
Drug Type: small molecule
Description: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.
Synonyms:
Amphotericine B; AMPH-B; Amphortericin B; Liposomal Amphotericin B
Brand: Abelcet, Amphotec, LNS-AmB, ABLC, SinuNase, Amphotericin, HSDB 3008 IAB, Fungisone, Fungizone Intravenous, Amphocin, IAB, Fungilin, Ampho-Moronal, AmB, Mysteclin-F, Fungizone, Tegopen, Halizon, AmBisome, Amphozone
Category: Anti-Bacterial Agents, Antiprotozoal Agents, Antifungal Agents, Amebicides
CAS number: 1397-89-3
Pharmacology
Indication: Used to treat potentially life threatening fungal infections.
Pharmacology:
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 a...
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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 (ergosterol) in the cell membrane of susceptible fungi. This creates a transmembrane channel, and the resultant change in membrane permeability allowing leakage of intracellular...
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Absorption: Bioavailability is 100% for intravenous infusion.
Protein binding: Highly bound (>90%) to plasma proteins.
Biotransformation: Exclusively renal
Half Life: An elimination half-life of approximately 15 days follows an initial plasma half-life of about 24 hours.
Clearance: 39 +/- 22 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 1 mg/kg/day at Day 1] 17 +/- 6 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 1 mg/kg/day 3-20 days later] 51 +/- 44 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 2.5 mg/kg/day at Day 1] 22 +/- 15 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 2.5 mg/kg/day 3-20 days later] 21 +/- 14 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 5 mg/kg/day at Day 1] 11 +/- 6 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 5 mg/kg/day 3-20 days later]
Toxicity: Oral, rat: LD50 = >5 gm/kg. Amphotericin B overdoses can result in cardio-respiratory arrest.
Affected organisms: Various Fungus Species
Interactions
Drug interaction:
ColistimethateAmphotericin B may enhance the nephrotoxic effect of Colistimethate. Due to the potential for additive or synergistic nephrotoxicity between colistimethate and other nephrotoxic drugs, such as amphotericin B, this combination should be avoided whenever possible. If these agents must be used together, patients' renal function should be monitored closely.
TobramycinIncreased risk of nephrotoxicity
TacrolimusAdditive renal impairment may occur during concomitant therapy with Amphotericin B. Use caution during concomitant therapy.
CyclosporineMonitor for nephrotoxicity

Targets