Micafungin Sodium

(USAN, rINNM)
Micafungin Sodium Chemical formula
Synonyms: FK-463; Micafungina sódica; Micafungine Sodique; Natrii Micafunginum. 5-((1S,2S)-2-{(2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)20-[(1R)-3-Amino-1-hydroxy-3-oxopropyl]-2,11,12,15-tetrahydroxy-6-[(1R)-1-hydroxyethyl]-16-methyl-5,8,14,19,22,25-hexaoxo-9-[(4-{5-[4-(pentyloxy)phenyl]isoxazol-3-yl}benzoyl)amino]tetracosahydro-1H-dipyrrolo[2,1c:2′,1′l][1,4,7,10,13,16]hexaazacyclohenicosin-23-yl}-1,2-dihydroxyethyl)-2-hydroxyphenyl sodium sulfate.
Cyrillic synonym: Натрий Микафунгин.

💊 Chemical information

Chemical formula: C56H70N9NaO23S = 1292.3.
CAS — 235114-32-6 (micafungin); 208538-73-2 (micafungin sodium).
ATC — J02AX05.
ATC Vet — QJ02AX05.

💊 Adverse Effects

As for Caspofungin. Isolated cases of renal dysfunction or acute renal failure have also occurred in patients taking micafungin.

💊 Precautions

Patients who develop abnormal liver or renal function tests while taking micafungin should be monitored for deterioration in hepatic or renal function respectively.

💊 Interactions

Micafungin may increase the area under the concentration-time curve for nifedipine and sirolimus.

💊 Antimicrobial Action

As for Caspofungin.

💊 Pharmacokinetics

Micafungin is absorbed from the gastrointestinal tract after oral doses. It is more than 99% bound to plasma proteins, mainly albumin. Micafungin is metabolised by arylsulfatase to its catechol form and further metabolised to the methoxy form by catechol-Omethyltransferase. Some hydroxylation to micafungin via cytochrome P450 isoenzymes also occurs. After 28 days about 71% of a dose is recovered in the faeces and 12% in the urine. Mean half-lives of 14.0 to 17.2 hours have been reported.

💊 Uses and Administration

Micafungin is an echinocandin antifungal with general properties similar to those of caspofungin. It is used for the treatment and prophylaxis of candidiasis and also in the treatment of aspergillosis. It is given as the sodium salt by intravenous infusion in doses of 50 mg once daily for candidiasis. For the treatment of oesophageal candidiasis the recommended dose is 150 mg daily. For aspergillosis 50 to 150 mg is given once daily. Doses up to 300 mg daily have been used in severe or refractory disease. A dose of 50 mg daily is used for prophylaxis of candidiasis in patients undergoing haematopoietic stem cell transplantation.
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2. Jarvis B, et al. Micafungin. Drugs 2004; 64: 969–84
3. Carver PL. Micafungin. Ann Pharmacother 2004; 38: 1707–21
4. van Burik JA, et al. Micafungin versus fluconazole for prophylaxis against invasive fungal infections during neutropenia in patients undergoing hematopoietic stem cell transplantation. Clin Infect Dis 2004; 39: 1407–16
5. Chandrasekar PH, Sobel JD. Micafungin: a new echinocandin. Clin Infect Dis 2006; 42: 1171–8
6. Fritz JM, et al. Micafungin for the prophylaxis and treatment of Candida infections. Expert Rev Anti Infect Ther 2008; 6: 153–62.

💊 Preparations

Proprietary Preparations

Jpn: Funguard; UK: Mycamine; USA: Mycamine.
Published November 30, 2018.