235114-32-6 Micafungin 208538-73-2
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Micafungin is an echinocandin antifungal drug. Micafungin is indicated for the treatment of candidemia, acute disseminated candidiasis, Candida peritonitis, abscesses and esophageal candidiasis. Since January 23, 2008.It inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls. Micafungin is administered intravenously. It received final approval from the U.S. Food and Drug Administration on March 16, 2005, and gained approval in the European Union on April 25, 2008.
Indications Micafungin is indicated for the treatment of candidemia, acute disseminated candidiasis, Candida peritonitis, abscesses and esophageal candidiasis. Since January 23, 2008, micafungin has been approved for the prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplantation (HSCT).Micafungin works by way of concentration-dependent inhibition of 1,3-beta-D-glucan synthase resulting in reduced formation of 1,3-beta-D-glucan, which is an essential polysaccharide comprising one-third of the majority of Candida spp. cell walls. This decreased glucan production leads to osmotic instability and thus cellular lysis. Contraindications Known hypersensitivity to micafungin or any other ingredient contained in the formulation is a contraindication for its use. Dosage For the treatment of candidemia, acute disseminated candidiasis, Candida peritonitis, and abscesses, the dosage of micafungin is 100 mg once daily. For the treatment of esophageal candidiasis, the dosage is 150 mg once daily. For prophylaxis of Candida infections in HSCT recipients, the dosage is 50 mg once daily. The metabolism of micafungin occurs hepatically as the drug molecule is a substrate of CYP3A4, a liver enzyme. Precautions should be taken with regards to dosing, as micafungin also inhibits its own clearance via weak CYP3A4 inhibition Dosage forms Micafungin is a natural antifungal product derived from other fungi as a defense mechanism for competition of nutrients, etc. To be specific, micafungin is derived from FR901379, and is produced by Coleophoma empetri Mycamine 100mg for IV infusion (manufacturer Astellas) Brand names in countries other than the US may vary. Mycamine is a sterile, lyophilized product for intravenous (IV) infusion that contains micafungin sodium. Micafungin sodium is a semisynthetic lipopeptide (echinocandin) synthesized by a chemical modification of a fermentation product of Coleophoma empetri F-11899. Micafungin inhibits the synthesis of 1, 3-beta-D-glucan, an integral component of the fungal cell wall. Each single-use vial contains 50 mg or 100 mg micafungin sodium, 200 mg lactose, with citric acid and/or sodium hydroxide (used for pH adjustment). Mycamine must be diluted with 0.9% Sodium Chloride Injection, USP, or 5% Dextrose Injection, USP [see DOSAGE AND ADMINISTRATION]. Following reconstitution with 0.9% Sodium Chloride Injection, USP, the resulting pH of the solution is between 5-7. Micafungin sodium is chemically designated as: Pneumocandin A0,1-[(4R,5R)-4,5-dihydroxy-N2-[4-[5-[4-(pentyloxy)phenyl]-3isoxazolyl]benzoyl]-L-ornithine]-4-[(4S)-4-hydroxy-4-[4-hydroxy-3-(sulfooxy)phenyl]-Lthreonine]-, monosodium salt. The empirical/molecular formula is C56H70N9NaO23S and the formula weight is 1292.26. Micafungin sodium is a light-sensitive, hygroscopic white powder that is freely soluble in water, isotonic sodium chloride solution, N,N-dimethylformamide and dimethylsulfoxide, slightly soluble in methyl alcohol, and practically insoluble in acetonitrile, ethyl alcohol (95%), acetone, diethyl ether and n-hexane. |
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