Calcineurin inhibitor

Author: A/Prof Amanda Oakley, Dermatologist, Hamilton, New Zealand, January 2016.


What is calcineurin?

Calcineurin is a cellular enzyme that catalyses some processes in activated T-lymphocytes.

What is a calcineurin inhibitor?

A calcineurin inhibitor stops calcineurin working, by binding to proteins in the cells called immunophilins. The results are:

  • Reduced release of the cytokine interleukin-2 from the T cells
  • Reduced T-cell proliferation.

What are calcineurin inhibitors used for in dermatology?

Calcineurin inhibitors are used topically and systemically to treat various inflammatory skin diseases, especially:

What are the topical calcineurin inhibitors?

Ciclosporin can be used topically, but must be compounded extemporaneously in New Zealand.

What are the oral calcineurin inhibitors?

What are the risks of a calcineurin inhibitor?

Side effects and risks of the specific calcineurin inhibitor are described in the individual topics.

As a class of drug, the main concern is the effect of calcineurin on kidney function. Suspected reasons for nephrotoxicity include:

  • Increased endothelin-1, a vascoconstrictor
  • Decreased nitric acid, a vasodilator
  • Increased transforming growth factor beta 1, a cause of interstitial fibrosis.

The risk of nephrotoxicity is reduced by:

  • Keeping the dose of calcineurin inhibitor as low as possible
  • Adding or replacing it with another immune suppressive medication with different side effects and risks.
New Zealand approved datasheets are the official source of information for these prescription medicines, including approved uses and risk information. Check the individual New Zealand datasheet on the Medsafe website.

 

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