cyclosporine

also cy·clo·spor·in (-ĭn)
n.
An immunosuppressive drug obtained from certain soil fungi, used mainly to prevent the rejection of transplanted organs.

Key Terms: Intravenous line, Lymphatic system, Kilogram.

Definition

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.

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 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 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 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 patient without consulting the patient's doctor. Patients should inform 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 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

n

trade name: Sandimmune; drug class: immunosuppressant; action: produces immunosuppression by inhibiting lymphocytes; uses: to prevent rejection of tissues and/or organ transplants.

Brand names: Gengraf®Neoral®Pulminiq™Restasis™Sandimmune®SangCya™

Chemical formula:

Drug Forms:
• Cyclosporine Ophthalmic drops, suspension (below)
• Cyclosporine Oral capsule
• Cyclosporine oral solution
• Cyclosporine Solution for injection
• Cyclosporine Oral solution
• Cyclosporine ophthalmic emulsion
• Cyclosporine, Modified Oral capsule
• Cyclosporine, Modified Oral solution
• Cyclosporine Ophthalmic drops, emulsion

Español:
• Ciclosporina, Suspensión para gotas oftalmicas
• Ciclosporina, Cápsula oral
• Solución oral de ciclosporina
• Ciclosporina, Solución para inyección
• Ciclosporina, Solución oral
• Emulsión oftálmica de ciclosporina
• Ciclosporina, Cápsula oral de liberación modificada
• Ciclosporina, Solución oral modificada
• Ciclosporina, Gotas oftálmicas, emulsión

Cyclosporine Ophthalmic drops, suspension

What is this medicine?

CYCLOSPORINE eye drops are used to increase tear production in patients who have dry eyes due to eye inflammation.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• an active eye infection
• a history of herpes keratitis
• using punctal plugs
• wear contact lenses
• an unusual or allergic reaction to cyclosporine, medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

This medicine is only for use in the eye. Do not take by mouth. Follow the directions on the prescription label. Turn the vial upside down once or twice to shake the contents before use. Wash hands before and after use. Use the product immediately after opening the vial and throw the vial away right after use. Tilt your head back slightly and pull your lower eyelid down with your index finger to form a pouch. Try not to touch the tip of the dropper to your eye, fingertips, or any other surface. Squeeze the prescribed number of drops into the pouch. Close the eye for a few moments to spread the drops and apply gentle finger pressure to the inner corner of the eye for 1 to 2 minutes. Use your doses at regular intervals. Do not use your medicine more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

• other eye products, especially those that contain antiinflammatory agents

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular eye exams. Ask your doctor or health care professional if you should continue to use this medicine if you injure your eyes or need eye surgery. If you develop an eye infection, contact your doctor or health care professional immediately.

If you wear contact lenses, you should not put this medicine in your eyes while wearing the lenses. After using the eye drops, wait about 15 minutes before putting lenses in your eyes.

You can use artificial tear products while using this medicine; however you should wait at least 15 minutes before using the this medicine.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
• eye discharge
• swelling around the eye

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• blurred vision
• excessive tearing
• eye burning or stinging
• eye itching
• feeling as if something is in your eye

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 25 degrees C (59 and 77 degrees F). Once a vial is open, use it right away and throw away any remaining medicine in the vial. Throw away any unused vials after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A neutral cyclic peptide, the major metabolic product of the fungus Tolypocladium inflatum; a specific suppressor of the T lymphocyte response, important in tissue transplantation.