Micafungin

Antibiotic Class:

Echinocandin

Antifungal Activity:

Candida sp. including azole-resistant strains. Activity against molds difficult to quantify but includes Aspergillus sp Table 1, Table 2

Mechanism of Action:

Non-competitive inhibition of the enzyme b-(1,3)-glucan synthase.

Pharmacodynamics:

Echinocandins have more fungicidal effects against Candida species compared to filamentous organisms. In-vitro studies have demonstrated concentration-dependent fungicidal activity against Candida sp.

Pharmacokinetics:

Half-life: 11.6-15.2 hours; Volume of distribution: 14L; Clearance (total): 13ml/min; Protein binding: 99%; Table 3

Adverse Effects:

Hepatic: mild elevation in liver transaminases dose related and reversible upon discontinuation of drug, and bilirubinemia

Dermatologic: rash, pruritis,

Dosage:

Intravenous only available as 50mg single use vials

Esophageal Candidiasis: 150mg I.V. q24h

Candida prophylaxis in hematopoetic stem cell recipients: 50mg I.V. q24h

Disease state based dosing:

Hepatic failure: In mild to moderate hepatic impairment, dosage adjustment is not necessary. Pharmacokinetic data are lacking in patients with severe hepatic failure.

Renal failure: No dosing adjustment necessary

Geriatric: No dosing adjustment necessary

Drug Interactions:

Sirolimus: Concomitant administration with caspofungin leads to a 21% AUC increase in sirolimus. Sirolimus levels should be monitored and adjusted.

Nifedipine: Concomitant administration with caspofungin leads to an 18% AUC increase in nifedipine. Monitoring for toxicity is recommended

Pregnancy:

Category C: Risk unknown. Human studies inadequate.

Monitoring Requirements:

Routine monitoring of hepatic enzymes is recommended

Brand names/Manufacturer:

Mycamine/Astellas pharmaceuticals

Marketed as Mycamine in the United States

Marketed as Funguard in Japan