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Selected pharmacokinetic characteristics of the echinocandins in adults

Selected pharmacokinetic characteristics of the echinocandins in adults
Variable Caspofungin Micafungin Anidulafungin
Elimination half-life adult* (hours) 27 to 50 14 to 17.2 40 to 50
Metabolism Hepatic: slow peptide hydrolysis and N-acetylation, with some spontaneous degradation to peptide product Hepatic: catechol-O-methyltransferase (COMT) and to a lesser extent, CYP1A2, 2B6, 2C, and 3A4 Not metabolized: undergoes slow spontaneous degradation to inactive metabolites
Dose adjustment for hepatic insufficiency Although manufacturer's labeling recommends a maintenance dose reduction of 50% for moderate hepatic insufficiency, pharmacokinetic data support use of full doses (ie, no adjustment) in all degrees of hepatic impairment to avoid subtherapeutic concentrations.[1]
  • Mild and Moderate (Child-Pugh 5 to 9): none
  • Severe (Child-Pugh >9): no data
 Not necessary
Dose adjustment for renal insufficiency Not necessary Not necessary Not necessary
Drug interactions
  • Cyclosporine can increase caspofungin AUC; elevated hepatic transaminases also observed with this combination.
  • Inducers of drug metabolism (eg, rifampin, efavirenz, nevirapine, phenytoin, dexamethasone, carbamazepine) can reduce caspofungin AUC and may cause subtherapeutic serum concentrations. Adjustment of therapy may be warranted.
 N/A N/A
CSF penetration (% of plasma) <0.1 <0.1 <0.1
Urinary excretion of unchanged drug (%) Approximately 1 0.7 <1
Protein binding (%) 96 to 97 99.8 99
Vd (L/kg) 0.14 0.39 +/– 0.11 0.50

AUC: area under time versus concentration curve; CYP: cytochrome P; N/A: not applicable; CSF: cerebrospinal fluid; Vd: volume of distribution.

* Half-life of caspofungin and micafungin may be reduced in young children and infants compared with adults due to more rapid clearance.

¶ This is not a complete list. For additional interactions, refer to the appropriate UpToDate clinical topics and Lexicomp drug interactions program included with UpToDate.
Data from:
  1. US Food and Drug Administration-approved product information.
  2. Stone JA, Holland SD, Wickersham PJ, et al. Single- and multiple-dose pharmacokinetics of caspofungin in healthy men. Antimicrob Agents Chemother 2002; 46:739.
  3. Stone JA, Xu X, Winchell GA, et al. Disposition of caspofungin: role of distribution in determining pharmacokinetics in plasma. Antimicrob Agents Chemother 2004; 48:815.
  4. Dodds Ashley E, Lewis R, Lewis J, et al. Pharmacology of systemic antifungal agents. Clin Infect Dis 2006; 43 Suppl 1:S28.
  5. Sucher AJ, Chahine EB, Balcer HE. Echinocandins: the newest class of antifungals. Ann Pharmacotherapy 2009; 43:1647.
  6. Lexicomp Online. Copyright ©1978-2023 Lexicomp, Inc. All Rights Reserved.

Reference:

  1. Gustot T, Ter Heine R, Brauns E, et al. Caspofungin dosage adjustments are not required for patients with Child-Pugh B or C cirrhosis. J Antimicrob Chemother 2018; 73:2493.
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