Calcineurin inhibitor — extra information
Introduction - calcineurin Introduction - calcineurin inhibitor Uses Topical calcineurin inhibitors Oral calcineurin inhibitors Risks
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?
- Ciclosporin
- Tacrolimus
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.
Approved datasheets are the official source of information for medicines, including approved uses, doses, and safety information. Check the individual datasheet in your country for information about medicines.
We suggest you refer to your national drug approval agency such as the Australian Therapeutic Goods Administration (TGA), US Food and Drug Administration (FDA), UK Medicines and Healthcare products regulatory agency (MHRA) / emc, and NZ Medsafe, or a national or state-approved formulary eg, the New Zealand Formulary (NZF) and New Zealand Formulary for Children (NZFC) and the British National Formulary (BNF) and British National Formulary for Children (BNFC).
References
- Immunosuppressants - mechanisms of action and monitoring — Australian Prescriber Independent Review
On DermNet
Other websites
- Effects of Genetic Polymorphisms on the Pharmacokinetics of Calcineurin Inhibitors. Am J Health Syst Pharm. 2006;63(23):2340–8. – Medscape News
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