Pharmacology of calcineurin antagonists

M. H. Kapturczak, H. U. Meier-Kriesche, B. Kaplan

Research output: Contribution to journalArticle

105 Scopus citations


Cyclosporine and tacrolimus share the same pharmacodynamic property of activated T-cell suppression via inhibition of calcineurin. The introduction of these drugs to the immunosuppressive repertoire of transplant management has greatly improved the outcomes in organ transplantation and constitutes arguably one of the major breakthroughs in modern medicine. To this date, calcineurin inhibitors are the mainstay of prevention of allograft rejection. The experience gained from the laboratory and clinical use of cyclosporine and tacrolimus has greatly advanced our knowledge about the nature of many aspects of immune response. However, the clinical practice still struggles with the shortcomings of these drugs: the significant inter- and intraindividual variability of their pharmacokinetics, the unpredictability of their pharmacodynamic effects, as well as complexity of interactions with other agents in transplant recipients. This article briefly reviews the pharmacological aspects of calcineurin antagonists as they relate to the mode of action and pharmacokinetics as well as drug interactions and monitoring.

Original languageEnglish (US)
Pages (from-to)S25-S32
JournalTransplantation proceedings
Issue number2 SUPPL.
StatePublished - Mar 2004

ASJC Scopus subject areas

  • Surgery
  • Transplantation

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    Kapturczak, M. H., Meier-Kriesche, H. U., & Kaplan, B. (2004). Pharmacology of calcineurin antagonists. Transplantation proceedings, 36(2 SUPPL.), S25-S32.