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?
- Pimecrolimus cream
- Tacrolimus ointment
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.