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Micafungin
- indication:For use in the treatment of candidemia, acute disseminated candidiasis, and certain other invasive <i>Candida</i> infections, as well as esophageal candidiasis, and prophylaxis of <i>Candida</i> infections in patients undergoing hematopoietic stem cell transplantation. Micafungin is also used as an alternative for the treatment of oropharyngeal candidiases and has been used with some success as primary or salvage therapy, alone or in combination with other antifungals, for the treatment of invasive aspergillosis.
- pharmacologypharmacology:
- mechanism: Micafungin inhibits the synthesis of 1,3-b-D-glucan, an essential component of fungal cell walls, which is not present in mammalian cells.
- toxicity: Intravenous LD<sub>50</sub> in rats is 125mg/kg. In dogs it is >200mg/kg. No cases of overdosage have been reported. Repeated daily doses up to 8 mg/kg (maximum total dose of 896 mg) in adult patients have been administered in clinical trials with no reported dose-limiting toxicity. The minimum lethal dose is 125 mg/kg in rats, equivalent to 8.1 times the recommended human clinical dose for esophageal candidiasis based on body surface area comparisons.
- absorprion: Not absorbed orally
- halflife: 14-17 hours
- roouteelimination: Fecal excretion is the major route of elimination (total radioactivity at 28 days was 71% of the administered dose).
- volumedistribution: * 0.39 ± 0.11 L/kg [adult patients with esophageal candidiasis]
- clearance: * 0.359 +/- 0.179 mL/min/kg [Adult Patients with IC with 100 mg] * 0.321 +/- 0.098 mL/min/kg [HIV- Positive Patients with EC with 50 mg] * 0.327 +/- 0.093 mL/min/kg [HIV- Positive Patients with EC with 100 mg] * 0.340 +/- 0.092 mL/min/kg [HIV- Positive Patients with EC with 150 mg] * 0.214 +/- 0.031 mL/min/kg [hematopoietic stem cell transplant recipients 3 mg/kg] * 0.204 +/- 0.036 mL/min/kg [hematopoietic stem cell transplant recipients 4 mg/kg] * 0.224 +/- 0.064 mL/min/kg [hematopoietic stem cell transplant recipients 6 mg/kg] * 0.223 +/- 0.081 mL/min/kg [hematopoietic stem cell transplant recipients 8 mg/kg]