How Do Calcineurin Inhibitors Work?

Reviewed on 7/27/2021

HOW DO CALCINEURIN INHIBITORS WORK?

Calcineurin inhibitors are a class of drugs used in the chronic management of patients with allografts (transplant of an organ or tissue from one individual to another of the same species with a different genotype) and inflammatory conditions such as atopic dermatitis, rheumatoid arthritis, and postoperative immunosuppression. Calcineurin inhibitors are “immunosuppressants” as they work by inhibiting calcineurin, an enzyme that activates T-cells of the immune system. T-cell, also called T lymphocyte, is a type of leukocyte (white blood cell) essential for cell-mediated immunity

Calcineurin inhibitors are prescription-only medicines and are administered via oral, intravenous, topical, and ophthalmic routes.

Calcineurin inhibitors work in the following ways:

  • They inhibit the action of calcineurin, an enzyme that plays a key role in cell-mediated immunity.
  • They bind to the proteins in the cells called "immunophilins."
  • This reduces the release of the cytokine interleukin-2 from T-cells and T-cell proliferation.
  • This leads to inhibition of a key signaling phosphatase “calcineurin”; thus, they are known as “calcineurin inhibitors.”
  • In addition, they suppress the immune system so that the body can accept the new organ, thus preventing the rejection reaction.
  • They work by weakening the skin’s defense system, thereby decreasing the allergic reaction and relieving the skin irritation and inflammation.
  • They increase eyes’ natural ability to produce tears, which reduces swelling of the eyes.

SLIDESHOW

What Is Rheumatoid Arthritis (RA)? Symptoms, Treatment, Diagnosis See Slideshow

HOW ARE CALCINEURIN INHIBITORS USED?

Calcineurin inhibitors are used for the prevention and treatment of conditions such as:

WHAT ARE SIDE EFFECTS OF CALCINEURIN INHIBITORS?

Common side effects include:

Tremors (an involuntary, rhythmic shaking movement in one or more parts of body)

Other rare side effects include:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

QUESTION

The term arthritis refers to stiffness in the joints. See Answer

WHAT ARE NAMES OF CALCINEURIN INHIBITORS?

Generic and brand names of calcineurin inhibitors include:

References
https://reference.medscape.com/drugs/calcineurin-inhibitors

https://www.ncbi.nlm.nih.gov/books/NBK558995/

https://www.webmd.com/drugs/2/drug-20330/tacrolimus-topical/details

https://www.webmd.com/drugs/2/drug-10097-6108/tacrolimus-oral/tacrolimus-oral/details

https://medlineplus.gov/druginfo/meds/a602020.html

https://medlineplus.gov/druginfo/meds/a604009.html

https://www.medicinenet.com/cyclosporine-ophthalmic/article.htm#what_is_cyclosporine- ophthalmic_and_how_does_it_work_mechanism_of_action

https://www.webmd.com/drugs/2/drug-22364/pimecrolimus-topical/details https://medlineplus.gov/druginfo/meds/a603027.html https://dermnetnz.org/topics/calcineurin-inhibitors/

Health Solutions From Our Sponsors