Pharmacology Of Caspofungin

Indication For the treatment of esophageal candidiasis and invasive aspergillosis in patients who are refractory to or intolerant of other therapies.
Pharmacodynamics Caspofungin is an antifungal drug, and belongs to a new class termed the echinocandins. It is used to treat Aspergillus and Candida infection, and works by inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase. There is a potential for resistance development to occur, however in vitro resistance development to Caspofungin by Aspergillus species has not been studied.
Mechanism of action Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of Aspergillus species and Candida species. beta-(1,3)-D-glucan is not present in mammalian cells. The primary target is beta-(1,3)-glucan synthase.
Absorption 92% tissue distribution within 36-48 hours after intravenous infusion
Volume of distribution Not Available
Protein binding 97%
Metabolism Metabolized slowly by hydrolysis and N-acetylation
Route of elimination After single intravenous administration of [3H] caspofungin acetate, excretion of caspofungin and its metabolites in humans was 35% of dose in feces and 41% of dose in urine.
Half life 9-11 hours
Clearance
  • 12 mL/min [After single IV administration]
Toxicity Side effects include rash, swelling, and nausea (rare)