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Amphotericin B

Amphotericin B is an antifungal medication used for serious fungal infections and leishmaniasis. The fungal infections it is used to treat include aspergillosis, blastomycosis, candida, coccidioidomycosis, and cryptococcosis. More

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Description

Amphotericin B is an antifungal medication used for serious fungal infections and leishmaniasis. The fungal infections it is used to treat include aspergillosis, blastomycosis, candida, coccidioidomycosis, and cryptococcosis.

Generic Name

Amphotericin B

Chemical names

Amphotericin b, Amphocin, Abelcet, Amphotericine B, Ambisome, Amfotericina B

Brand names

Ambilip, Ambisome, Amfitas, Amfocan, Amfocare, Amfotex, Amfy, Ampholip, Amphotin, Amphotin-LIP, Amphotret, Envocin, Fungicin, Fungisome, Fungitericin, Fungizone I.V, Lambin, Mycol, Phoricin, Phosome.

IUPAC name

(1R,3S,5R,6R,9R,11R,15S,16R,17R,18S,19E,21E,23E,25E,27E,29E,31E,33R,5S,36R,37S)-33-{[(2R,3S,4S,5S,6R)-4-amino-3,5-dihydroxy-6-methyloxan-2-yl]oxy} 1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo 14,39dioxabicyclo[

Pharmacokinetics

  • Absorption: Bioavailability is 100% for intravenous infusion.
  • Distribution: >90% bound to protein
  • Metabolism: Renal
  • Excretion: Urine

Actions

It shows a high order of in vitro activity against many species of fungi. Coccidioides immitisHistoplasma capsulatumCandida speciesBlastomyces dermatitidisRhodotorulaCryptococcus neoformansMucor mucedo, Sporothrix schenckii, and Aspergillus fumigatus are all inhibited by concentrations of amphotericin B ranging from 0.03 to 1.0 mcg/mL in vitro. Pseudallescheria boydii and Fusarium sp. are often resistant to amphotericin B. While Candida albicans is generally quite susceptible to amphotericin B, non-albicans species may be less susceptible. The antibiotic is without effect on bacteria, rickettsiae, and viruses.

Dosage/Dosage form

Usual dose 0.7 mg/kg injected slowly through IV route.

Therapeutic uses

Used to treat potentially life threatening fungal infections.

Adverse effects/Side effects

Fever, chills, convulsions, malaise, nausea, vomiting, diarrhoea, anorexia, tinnitus, vertigo, hearing loss, hypotension, cardiac arrhythmias, hypertension, phloebitis, peripheral neuropathy, pain at injection site, disturbance in renal function and renal toxicity. Anaphylactic reaction, leucoencephalopathy. Overdosage can result in cardio-respiratory arrest.

Interaction

  • Corticosteroids : Increased risk of hypokalemia
  • Foscarnet, Ganciclovir, Tenofovir, and Adefovir: Risk of hematological and renal side-effects of Amphotericin B increased.
  • Cytostatic drugs: Increased risk of kidney damage, hypotension and bronchospasms.
  • Carcinogenesis, mutagenesis and impairment of fertility
  • Other nephrotoxic drugs: Increased risk of serious renal damage.

Contraindications

  • Do not give to patients receiving anti cancer drugs
  • Hypersensitivity
  • Lactation 

Storage

Protected against exposure to light, 36?to 46?F (2? to 8?C).

Information

Molecular weight

924.079

Molecular formula

C47H73NO17

CAS number

1397-89-3

Precautions

  • Should be used with care in patients with reduced renal function.
  • Amphotericin B should be administered intravenously under close clinical observation by medically trained personnel.
  • Rapid intravenous infusion has been associated with hypokalemia, hypotension, arrhythmias, and shock and should, therefore, be avoided.