Cylosporine is an immunosuppressant medicine used to prevent rejection of kidney, liver, and heart transplants, to prevent graft-versus-host disease in patients receiving allogeneic bone marrow transplants, and for severe autoimmune diseases that are resistant to corticosteroids and other therapy. Cyclosporine, also spelled as ciclosporin and cyclosporin, takes several brand names in the United States, including Neoral, Sandimmun, Sandimmune, and Sang Cya. It is also known in slight variant forms, such as cyclosporin A, CsA, and CyA. The Neoral and Sang Cya brand name products are interchangeable, but the Sandimmune brand name product can not be used interchangeably for those other two products.

Purpose

Cyclosporine is best known as a drug used to prevent the rejection of organ transplants and bone grafts.

Description

Discovered in 1972, cyclosporine was first isolated from a fungus. It suppresses (prevents the activity of) the cells in the lymphatic system, known as T cells, that would otherwise mount an immune response. This suppression makes cyclosporine helpful in conjunction with organ transplants. (In a transplant, the patient receiving a donated organ can react to the organ as though it were a foreign substance, rejecting it.) Cyclosporine is also used to treat harsh rheumatoid arthritis, and is being used investigationally as a drug that may help to temper multi-drug resistance in cancer patients.

The drug is available in several forms, including an intravenous (I.V.) solution, an oral solution, and an oral capsule. Cyclosporine is broken down in the liver.

Recommended Dosage

The dosage varies, depending on the reason for use and the patient, and the dosage is also often adjusted by the physician. The dosage is based on the patient’s ideal body weight, and the oral dose is approximately three times higher than the intravenous dose. I.V. use is only reserved for patients who cannot take the oral dose, and it is recommended that patients who can be switched to the oral form be switched as soon as possible.

The usual initial oral dose is 14–18 mg/kg per day, beginning four–twelve hours before organ transplantation. After the transplantation, the dose is decreased, and then usually tapered to 3–10 mg/kg per day.

Precautions

Cyclosporine be able to cause infection and possibly lymphoma, and is toxic to the kidneys. The use of this drug along with other drugs that are toxic to the kidneys must be closely monitored. It should be ingested and swallowed in its capsule without breaking the capsule. The liquid solution should only be mixed in a glass container. Pregnant or nursing women should not take this drug, and patients taking this drug will be more susceptible to infection. Therefore, crowds of people should be avoided, and no live vaccines should be adminstered to the patient without consulting the patient’s doctor. Patients should tell their doctor of any hypersensitivities or drug allergies they have before taking this drug. (Cyclosporine in both liquid and capsule form has some castor oil components in it, which could cause an allergic reaction for some.) Some allergic reactions to the I. V. solution may be severe. This drug has not been specifically studied for use with the elderly.

Side Effects

More than 10% of patients taking this drug experience the following:

• high blood pressure
• unusual hair growth
• kidney toxicity
• tremors
• thickening of the gums Other,

Less common side effects include: seizures, headache, acne, abdominal pain, nausea and vomiting, leg cramps, and some endocrine/metabolic conditions known as hypomagnesia, hypokalemia, hyperkalemia, and hyperlipidemia.

Interactions

Cyclosporine interacts with a long list of other drugs. A physician should be informed about each and every drug a person eligible for treatment with cyclosporine is taking. Drugs that may make cyclosporine less effective consist of: carbamazepine, phenobarbital, phenytoin, and others. Drugs that may boost cyclopsporine’s toxicity include: acyclovir, amphotericin B, corticosteroids, erythromycin, certain antibiotics, and some antifungals including fluconazole, itraconazole, and ketaconazole. Cyclosporine should not be in use with grapefruit or connected juices because the combination can make it more toxic. Vaccinations should not be given while a person is taking cyclosporine.

Related Links