Cylosporine is an immunosuppressant drug 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 cyclosporin and ciclosporin, 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.
Cyclosporine is best known as a drug used to prevent the rejection of organ transplants and bone grafts.
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 useful 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 severe rheumatoid arthritis, and is being used investigationally as a drug that may help to temper multidrug 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.
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.
Cyclosporine can 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
More than 10% of patients taking this drug experience the following:
- high blood pressure
- unusual hair growth
- kidney toxicity
- 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.
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 include: carbamazepine, phenobarbital, phenytoin, and others. Drugs that may increase cyclopsporine's toxicity include: acyclovir, amphotericin B, corticosteroids, erythromycin, certain antibiotics, and some antifungals including fluconazole, itraconazole, and ketaconazole. Cyclosporine should not be taken with grapefruit or related juices because the combination can make it more toxic. Vaccinations should not be given while a person is taking cyclosporine.
Diane M. Calabrese
—A tube that is inserted directly into a vein to carry medicine directly to the bloodstream, bypassing the stomach and other digestive organs that might alter the medicine.
—The system that collects and returns fluid in tissues to the blood vessels and produces defensive agents for fighting infection and invasion by foreign bodies.
—Metric measure that equals 2.2 pounds.
—One-thousandth of a gram. A gram is the metric measure that equals about 0.035 ounces.