First discovered in soil fungus in 1970, cyclosporine is marketed under the brand names Sandimmune and Neoral. Insoluble in water, the compound is soluble only in organic solvents or lipids, and blocks certain signals to lymphocytes. An immune system suppressant, it is most commonly given to patients following organ transplant surgery to help prevent rejection of the new organ. Cyclosporine is also sometimes used for treatment of rheumatoid arthritis and psoriasis, and infrequently for alopecia areata, aplastic anemia, Crohn's disease, nephropathy, and dermatomyositis as well as other severe skin disorders. Some doctors are beginning to use cyclosporine as an experimental treatment for chronic urticaria.

There are a number of side effects associated with cyclosporine. The primary side effects are high blood pressure, hirsutism, kidney damage, tremor, and excessive growth of the gums. Other common side effects include abdominal discomfort, acne, breathing difficulty, convulsions (especially when combined with methylprednisone), coughing, cramps, diarrhea, flu-like symptoms, flushing, headache, liver damage, lymph system tumors, muscle, bone, or joint pain, nasal or sinus inflammation, nausea, numbness, vomiting, and wheezing. Less common side effects include abdominal distention, anemia, appetite changes, bleeding gums, brittle fingernails, confusion, conjunctivitis, dizziness, fever, fluid retention, frequent urination, hearing loss, hiccups, high blood sugar, indigestion, infection, insomnia, nervousness, rash, tinnitus, ulcers, and vertigo. Rare side effects may include anxiety, blood in the urine, chest pain, constipation, depression, difficulty swallowing, gynecomastia, heart attack, mouth sores, night sweats, stomach and upper intestinal bleeding, tingling, visual disturbances, weakness, and weight loss.

Because cyclosporine is a powerful immune suppressant, there are a number of special warnings given to individuals who must take the drug.

  • Patients taking cyclosporine are at an increased risk of infection and certain malignancies, including cancer. Patients should also avoid any immunizations, as the possibility exists that they will contract the virus from the live vaccine.
  • At high doses, the drug is toxic to the liver and kidneys. Patients must go for urinalysis regularly while on cyclosporine.
  • Cyclosporine generally should not be used by pregnant women, though a physician may determine the benefit outweighs the potential risk to the unborn child. The drug does appear in breast milk and should not be used by breastfeeding mothers. In addition, oral contraceptives should not be used without a doctor's approval - barrier methods such as condoms and diaphrams must be used instead.
  • Blood pressure may increase while a patient is taking cyclosporine, especially if the individual is elderly.
  • A number of other drugs react with cyclosporine. A doctor should be consulted before combining it with other drugs, including common ones such as Tegretol, Tagamet, Diflucan, Nizoral, Zantac, and Dilantin. In addition, patients on cyclosporine should not eat grapefruit or drink grapefruit juice.

Sandimmune and Neoral are available in capsules and liquid form. When opened, the capsule container may smell bad - this typically dissipates right away. For the liquid, the outside of the dosage syringe should be washed and dried. To make Sandimmune more palatable, it may be mixed with warm milk, chocolate milk, or orange juice; Neoral should be mixed with room-temperature orange or apple juice but not with milk because this will make it taste bad. Liquid cyclosporine should be mixed in a container made of glass and not plastic, and should be swallowed right away without being left standing. To ensure the full dosage is obtained, patients should also fill the cup with more of the primary liquid and drink that until the cup is cleaner. The usual dosage of cyclosporine is about 10mg per 2.2 pounds of body weight.

Sources: The PDR Pocket Guide to Prescription Drugs, page 1111. Also

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