Caspofungin

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: 9-11 hours; Volume of distribution: 9.67L; Clearance (total): 12ml/min; Protein binding: 97%; Table 3

Adverse Effects

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

Body as a whole: Fever

Respiratory: Wheezing, Bronchoconstriction

Dermatologic: Edema, flushing, wheals, rash

Metabolic: Hypercalcemia (Postmarketing experience)

Dosage

Intravenous only available as 50mg and 70mg powder for reconstitution vials.

70mg loading dose IV x 1, followed by 50mg IV q24h

Disease state based dosing:

Hepatic failure: In mild hepatic impairment, daily maintenance doses should be 35mg  IV q24h

Renal failure: No dosing adjustment recommended

Drug Interactions

Cyclopsorin: Increases the AUC of Caspofungin by 35%, with associated elevations in ALT and AST elevations

Tacrolimus: Concomitant administration decreases AUC of tacrolimus by 20%. Montoring of tacrolimus blood concentrations recommended

Other: Reductions in caspofungin concentrations may occur when coadministered with inducers of drug clearance such as efavirenz, nevirapine, phenytoin, dexamethasone, or carbamazepine. Caspofungin dose escalation may be considered in this setting

Pregnancy

Category C: Risk unknown. Human studies inadequate.

Monitoring Requirements

Routine monitoring of hepatic enzymes is recommended

Brand names/Manufacturer

Cancidas/Merck pharmaceuticals

Marketed as Cancidas in the following countries

U.S.A., United Kingdom, Australia, Chile, Sweden, Denmark, France, Israel, Finland, Belgium, Norway, Italy, Germany, Switzerland, Czech Republic, Thailand, Spain, Canada, Ireland, Hong Kong, Singapore, New Zealand