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What drugs are calcineurin inhibitors?

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Sophia Bowman

Updated on February 24, 2026

What drugs are calcineurin inhibitors?

Calcineurin inhibitors (CNI) are composed of three drugs (cyclosporine, tacrolimus, and pimecrolimus). They are primarily used as immunosuppressive drugs, and inhibit the key signaling phosphatase calcineurin, thus called calcineurin inhibitors.

Consequently, what are calcineurin inhibitors?

Calcineurin inhibitors are medicines which inhibit the action of calcineurin. Calcineurin is an enzyme that activates T-cells of the immune system. T-cells (also called T-lymphocytes) are a type of white blood cell that play a key role in cell-mediated immunity.

Similarly, what are the side effects of calcineurin inhibitors? Oral calcineurin inhibitors can cause the following side effects:

  • Nephrotoxicity (the most common adverse effect)
  • Hypertension.
  • Neurotoxicity (tremors, severe headache, visual abnormalities, seizures, encephalopathy, and coma)

Also to know, what are some topical calcineurin inhibitors?

There are two types of topical calcineurin inhibitors called tacrolimus ointment (Protopic 0.03% and 0.1%) and pimecrolimus cream (Elidel). They are classified as immunomodulating agents. This means that they act on the immune system to reduce skin inflammation.

Is cyclosporine A calcineurin inhibitor?

Cyclosporine and tacrolimus selectively inhibit calcineurin, thereby impairing the transcription of interleukin (IL)-2 and several other cytokines in T lymphocytes. Calcineurin inhibitors have been mainstays of immunosuppression in solid organ transplantation for over three decades.

How do calcineurin inhibitors work?

Mechanism of action of calcineurin inhibitors is suppressing synthesis of pro-inflammatory cytokines. In the cytoplasm of the target cells, pimecrolimus and tacrolimus bind to the intracellular protein macrophilin-12, also called FKBP (FK506-binding protein). Similarly, cyclosporine A binds to cyclophilin.

Is Protopic safe to use around eyes?

A safer, effective treatment is the topical immunomodulators, such as tacrolimus (Protopic) or pimecrolimus (Elidel). These can be used twice daily to the affected area until the rash clears. They are safe to use around the eyes and do not have the side effects associated with topical corticosteroid use.

What is the best ointment for atopic dermatitis?

A nonprescription hydrocortisone cream, containing at least 1 percent hydrocortisone, can temporarily relieve the itch. Apply it no more than twice a day to the affected area, after moisturizing. Using the moisturizer first helps the medicated cream penetrate the skin better.

What is the best over the counter cream for dermatitis?

  • Aveeno Eczema Therapy Moisturizing Cream for Sensitive Skin.
  • Gladskin Eczema Cream.
  • Cetaphil Body and Face Moisturizing Lotion.
  • Neosporin Eczema Essentials Daily Moisturizing Cream.
  • Skinfix Eczema Hand Repair Cream.
  • Eucerin Eczema Relief Body Creme.
  • FineVine Super Balm.
  • Aveeno Baby Eczema Therapy Moisturizing Cream.

Can I use tacrolimus on my face?

Unlike topical corticosteroids, topical tacrolimus has not been shown to cause skin thinning, hence it is suitable for application to areas of skin that are thin such as the face, neck and flexures.

Is tacrolimus ointment safe?

In summary, tacrolimus ointment seems to be safe and effective for moderate to severe atopic dermatitis in children and adults. It should be used with caution, though, in those having diseases with a severely damaged skin barrier. We found no risk of skin thinning with its use, even for longer periods.

What is CNI toxicity?

Renal calcineurin inhibitor (CNI) toxicity is a frequent side effect of immunosuppression with CNIs in solid organ transplantation, leading to acute and chronic renal failure.

What are antiproliferative agents?

Antiproliferative agents, also known as antimetabolites, inhibit cell-cycle pathways to limit T- and B-cell proliferation and thereby reducing the cytotoxic response directed toward the cardiac allograft.

Is Vaseline good for eczema?

The good news is that the National Eczema Association has affirmed that Vaseline® Jelly Original is suitable for eczema sufferers and people with sensitive skin conditions. You can use petroleum jelly on eczema-prone areas, to help combat the dry skin symptoms.

How long can I use steroid cream?

The treatment can last anywhere between a few days and six weeks. This will depend on the strength of the corticosteroid and the affected areas of skin. Steroid medication generally shouldn't be applied to sensitive areas of the body for longer than a few days.

What is a topical immunomodulator?

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Topical immunomodulators are nonsteroidal agents that target the immune system for therapeutic effect in the skin. The macrolactams, pimecrolimus and tacrolimus, act as anti-inflammatory agents by binding immunophilin and inhibiting cytokine production.

What creams have steroids in them?

Topical Steroid Class III
  • Amcinonide 0.1% (Cyclocort cream, lotion)
  • Mometasone furoate 0.1% (Elocon ointment)
  • Fluticasone propionate 0.005% (Cutivate ointment)
  • Betamethasone dipropionate 0.05% (Betanate cream)
  • Triamcinolone acetonide 0.5% (Kenalog cream, ointment)

Can you drink alcohol while using tacrolimus ointment?

Do not drink alcohol because it can cause your skin and face to become flushed or red, and feel hot. Your doctor will discuss with you the possibility of a slightly increased risk of cancer (particularly skin cancer) associated with medicines like tacrolimus.

How long can you use pimecrolimus cream?

Pimecrolimus comes as a cream to apply to the skin. It is usually applied twice a day for up to 6 weeks at a time. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.

Does tacrolimus have a black box warning?

In 2005, the Pediatric Advisory Committee of the US FDA implemented a 'black box' warning for tacrolimus ointment and pimecrolimus cream due to the lack of long-term safety data and the potential risk of the development of malignancies.

What is corticosteroid ointment?

What are topical corticosteroids? Corticosteroid hormones are naturally occurring hormones produced by the adrenal glands within the body. Topical corticosteroids are synthetic (man-made) corticosteroid medications used for treating skin conditions such as rash, dermatitis, itching, eczema, and psoriasis.

What is topical tacrolimus used for?

Tacrolimus ointment is used to treat the symptoms of eczema (atopic dermatitis; a skin disease that causes the skin to be dry and itchy and to sometimes develop red, scaly rashes) in patients who cannot use other medications for their condition or whose eczema has not responded to another medication.

How does tacrolimus affect the kidneys?

Tacrolimus is a medicine that lowers the body's natural immunity. The immune system is thought to be involved in a disorder which causes the kidneys to leak protein into the urine (Nephrotic Syndrome). It is widely used to prevent rejection of transplanted organs, such as the kidney, heart, and liver.

What is the difference between cyclosporine and tacrolimus?

We concluded that tacrolimus may be less nephrotoxic than cyclosporine. Tacrolimus patients showed better graft function and easier blood pressure control, but a high incidence of posttransplantation diabetes mellitus.

How was tacrolimus discovered?

Chemically, it is a macrolide lactone that was first discovered in 1987, from the fermentation broth of a Japanese soil sample that contained the bacterium Streptomyces tsukubaensis.

Is Eucrisa a topical calcineurin inhibitor?

Eucrisa (crisaborole) ointment and Elidel (pimecrolimus) cream are indicated for topical treatment of mild to moderate atopic dermatitis (eczema) in patients 2 years of age and older. Eucrisa and Elidel belong to different drug classes. Eucrisa is a phosphodiesterase 4 inhibitor and Elidel is a calcineurin inhibitor.

What are side effects of cyclosporine?

Common side effects of cyclosporine include:
  • High blood pressure.
  • Increased hair growth.
  • Swollen or inflamed gums.
  • Numbness or tingling of the hands or feet.
  • Other common side effects are tremors, restlessness, stomach upset, nausea, cramps, diarrhea, headache, and changes in blood sugar.

Is sirolimus a calcineurin inhibitor?

Unlike the similarly named tacrolimus, sirolimus is not a calcineurin inhibitor, but it has a similar suppressive effect on the immune system. Sirolimus inhibits IL-2 and other cytokine receptor-dependent signal transduction mechanisms, via action on mTOR, and thereby blocks activation of T and B cells.

How does cyclosporine cause hypertension?

The exact mechanism of cyclosporine-induced hypertension is uncertain, but several hypotheses have been proposed, including increased prostaglandin synthesis and decreased water, sodium, and potassium excretion.[46,47] Up to 50% of renal transplant patients receiving cyclosporine treatment have reported elevated blood

When should cyclosporine levels be taken?

For cyclosporine or tacrolimus trough-level monitoring, blood should be drawn 12 h after the last dose (i.e., immediately before the next dose).

What is the mechanism of action of cyclosporine?

Cyclosporine is a potent immunomodulatory agent with an increasing number of clinical applications. Its major mode of action is inhibition of the production of cytokines involved in the regulation of T-cell activation. In particular, cyclosporine inhibits the transcription of interleukin 2.

Is cyclosporine an immunosuppressant?

Cyclosporine and cyclosporine (modified) are in a class of medications called immunosuppressants. They work by decreasing the activity of the immune system.

How do you monitor cyclosporine levels?

Typically a trough level is monitored. A trough level is the lowest concentration reached by a drug before the next dose is administered. For example, if cyclosporine is given twice a day, a blood sample is usually drawn 12 hours after the last dose, before a new dose is given.

What is the role of calcineurin?

Calcineurin (CaN) is a calcium and calmodulin dependent serine/threonine protein phosphatase (also known as protein phosphatase 3, and calcium-dependent serine-threonine phosphatase). It activates the T cells of the immune system and can be blocked by drugs.

Is tacrolimus an immunosuppressant?

Tacrolimus (Prograf ®) is an immunosuppressant drug used to prevent and treat organ rejection in children who have had liver transplants. It is used for long-term immunosuppression.

Is tacrolimus an antibiotic?

Tacrolimus is a macrolide antibiotic produced by the soil fungus Streptomyces tsukubaensis.

Is calcineurin an enzyme?

Calcineurin is a serine-threonine specific Ca(2+)-calmodulin-activated protein phosphatase that is conserved from yeast to humans. Remarkably, this enzyme is the common target for two novel and structurally unrelated immunosuppressive antifungal drugs, cyclosporin A and FK506.

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