What is Cyclosporine?

Generic name: Cyclosporine A

Brand name: Neoral, Gengraf, Sandimmune

Cyclosporine or Ciclosporin (as it is sometimes spelled) is an immunosuppressant drug (suppresses the immunity of the body), similar in effectiveness to methotrexate.

Besides its other uses, it is used in the treatment of severe forms of psoriasis that is widespread and difficult to treat.

The Food and Drug Administration (FDA) approved it as late as 1997 for the treatment of severe psoriasis in adults with a normal immune system.

It was first used to prevent organ rejection after an organ transplant in 1978. Being an immunosuppressant, it works by weakening the immune system so that it does not reject the new-transplanted organ such as the kidney, liver, and heart. Your body then accepts the new organ as if it were your own.

Cyclosporine is available as an oral capsule, an oral solution, eye drops, and an injectable form.

How to use Cyclosporine?

Cyclosporine is available in microemulsion capsule and liquid form and is usually advised to be taken orally twice daily with or without food. Once started, continue to take it in the same fashion – either with food or without it.

It is necessary that the levels of cyclosporine stay consistent for maximum effects and you are, therefore, advised to stick to the same dosage and the same time to take the drug. Dosage varies depending on the medical condition of the patient, kidney function, and response to the drug.

You should take the liquid form diluted either with milk or with orange or apple juice and preferably at room temperature Do not take grapefruit or its juice when on cyclosporine as it causes increased levels of this drug in the blood, which can increase the risk of its side effects.

When taking the liquid form 100 mg/ml, you should carefully measure the dose using the syringe provided.

In psoriasis, it may take 2 to 4 weeks to notice any improvement in the symptoms and up to 4 months to see the full benefit.

Long-term use of cyclosporine in psoriasis is limited and unless advised by your dermatologist, this drug usage is advised for one year only.

Uses

  • Organ transplant
  • Psoriasis
  • Rheumatoid arthritis
  • Atopic dermatitis
  • Chronic urticaria
  • As cyclosporine ophthalmic drops in dry eyes
  • Ulcerative colitis

Cyclosporine eye drops uses

Ophthalmic cyclosporine A drops are used to increase the production of tears in people who suffer from dry eye disease. It works by decreasing swelling in the eye. This facilitates more tear production.

According to Bennie H. Jeng, MD, an associate professor of ophthalmology at the University of California, San Francisco, “Cyclosporine is a steroid-sparing agent, which is safer to use topically for prolonged periods of time,”

Mechanism of action

Cyclosporine is a calcineurin inhibitor. It inhibits the activation of  T cells as well as the activation of the nuclear factor of activated T cells. These are the factors, which normally cause inflammatory reactions.

The nuclear factor of activated T cells promotes the production of cytokines such as IL-2, IL-4, interferon-gamma, and TNF-alpha. These are the cytokines, which are involved in the inflammatory process.

Specifically, it is the inhibition of IL-2, which is necessary for T cell activation that is accountable for cyclosporine’s immunosuppressive actions

Side effects of cyclosporine

Many people do not develop side effects and though side effects exist, you will be advised this medication only when its benefits far outweigh its side effects. The risk of side effects increases with higher dosage and long-term therapy.

Being an immunosuppressant, the risk of infections and cancer is high when taking this drug. Risk of skin cancer with cyclosporine increases if you have been previously treated with UVB, coal tar, radiation therapy, methotrexate, or some other immunosuppressant drug.

Other possible side effects are:

  • Headache
  • Nausea and vomiting
  • Blurring of vision
  • Stomach upsets
  • Increased hair growth on face and body
  • Acne outbreaks
  • Tremors
  • Muscle, bone, and joint pains
  • Renal toxicity. The risk of this side effect increases when cyclosporine is taken with non-steroidal anti-inflammatory drugs. The dose of cyclosporine is reduced if the creatinine levels rise more than 30%.
  • High blood pressure (hypertension), which is treated with antihypertensive drugs
  • Increased cholesterol levels
  • A feeling of tiredness

Of all the oral drugs prescribed for severe psoriasis, cyclosporine is the safest drug that can be used in pregnancy. However, the FDA lists cyclosporine in the Category B list of drugs for pregnancy.

What is pregnancy category B? Quoting from Wikipedia below.

“Pregnancy category B: Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women OR Animal studies have shown an adverse effect, but adequate and well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester.”

Precautions when taking Cyclosporine

  • Inform your doctor if you develop any allergy to it.
  • Limit the use of alcohol and avoid the use of any illicit drug.
  • Inform your doctor if you are suffering from any kidney or liver disease, cancer, skin lesions such as psoriasis, electrolyte imbalance, hyperlipidemia.
  • Taking this drug can increase your risk of infections. Inform your doctor if you are suffering from any infection.
  • Stick to the same time and format when taking your dose to maintain same blood levels of this drug for better results.
  • You should check your blood pressure before starting this drug and also periodically when on this therapy.
  • Similarly, you should keep a watch on your serum creatinine levels.
  • Cyclosporine is an immunosuppressant. It weakens your immune system. You should, therefore, be alert and stay safe by avoiding going near any persons who suffer from any contagious disease.
  • Drug interactions

Cyclosporine can interact with several other drugs if taken together. These interactions can either interfere with its efficacy or can increase its side effects.

Below is a list of some of these drugs:

  • Antibiotics such as ciprofloxacin, gentamicin, azithromycin
  • Nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen and diclofenac
  • Antifungals such as ketoconazole, fluconazole
  • Acid reflux drugs such as ranitidine, cimetidine
  • Birth control pills
  • Drugs for high cholesterol such as fenofibrate, gemfibrozil, atorvastatin
  • Other drugs include medicines taken for hypertension, steroids, anticonvulsants, drugs for gout

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