cyclosporine(redirected from cyclosporines)
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cyclosporine ophthalmic emulsion
Pharmacologic class: Polypeptide antibiotic
Therapeutic class: Immunosuppressant
Pregnancy risk category C
Respiratory: cough, dyspnea, Pneumocystis jiroveci pneumonia, bronchospasm
FDA Box Warning
• Drug should be prescribed only by physicians experienced in managing systemic immunosuppressive therapy for indicated disease. At doses used for solid-organ transplantation, it should be prescribed only by physicians experienced in immunosuppressive therapy and management of organ transplant recipients. Patient should be managed in facility with adequate laboratory and medical resources. Physician responsible for maintenance therapy should have complete information needed for patient follow-up.
• Neoral may increase susceptibility to infection and neoplasia. In kidney, liver, and heart transplant patients, drug may be given with other immunosuppressants.
• Sandimmune should be given with adrenal corticosteroids but not other immunosuppressants. In transplant patients, increased susceptibility to infection and development of lymphoma and other neoplasms may result from increased immunosuppression.
• Sandimmune and Neoral aren't bioequivalent. Don't use interchangeably without physician supervision.
• In patients receiving Sandimmune soft-gelatin capsules and oral solution, monitor at repeated intervals (due to erratic absorption).
Unclear. Thought to act by specific, reversible inhibition of immunocompetent lymphocytes in G0-G1 phase of cell cycle. Preferentially inhibits T lymphocytes; also inhibits lymphokine production. Ophthalmic action is unknown.
Capsules: 25 mg, 100 mg
Injection: 50 mg/ml
Oral solution: 100 mg/ml
Solution (ophthalmic): 0.05% (0.4 ml in 0.9 ml single-use vial)
Indications and dosages
Adults: Neoral only-1.25 mg/kg P.O. b.i.d. for 4 weeks. Based on patient response, may increase by 0.5 mg/kg/day once q 2 weeks, to a maximum dosage of 4 mg/kg/day.
➣ Severe active rheumatoid arthritis
Adults: Neoral only-1.25 mg/kg P.O. b.i.d. May adjust dosage by 0.5 to 0.75 mg/kg/day after 8 weeks and again after 12 weeks, to a maximum dosage of 4 mg/kg/day. If no response occurs after 16 weeks, discontinue therapy. Gengraf only-2.5 mg/kg P.O. daily given in two divided doses; after 8 weeks, may increase to a maximum dosage of 4 mg/kg/day.
➣ To prevent organ rejection in kidney, liver, or heart transplantation
Adults and children: Sandimmune only-Initially, 15 mg/kg P.O. 4 to 12 hours before transplantation, then daily for 1 to 2 weeks postoperatively. Reduce dosage by 5% weekly to a maintenance level of 5 to 10 mg/kg/day. Or 5 to 6 mg/kg I.V. as a continuous infusion 4 to 12 hours before transplantation.
➣ To increase tear production in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca
Adults: 1 drop in each eye b.i.d. given 12 hours apart
• Aplastic anemia
• Atopic dermatitis
• Hypersensitivity to drug and any ophthalmic components
• Rheumatoid arthritis, psoriasis in patients with abnormal renal function, uncontrolled hypertension, cancer (Gengraf, Neoral)
• Active ocular infections (ophthalmic use)
Use cautiously in:
• hepatic impairment, renal dysfunction, active infection, hypertension
• herpes keratitis (ophthalmic use)
• pregnant or breastfeeding patients
• children younger than age 16 (safety and efficacy not established for ophthalmic use).
• For I.V. infusion, dilute as ordered with dextrose 5% in water or 0.9% normal saline solution. Administer over 2 to 6 hours.
• Mix Neoral solution with orange juice or apple juice to improve its taste.
• Dilute Sandimmune oral solution with milk, chocolate milk, or orange juice. Be aware that grapefruit and grapefruit juice affect drug metabolism.
• In postoperative patients, switch to P.O. dosage as tolerance allows.
• Be aware that Sandimmune and Neoral aren't bioequivalent. Don't use interchangeably.
• Before administering eyedrops, invert unit-dose vial a few times to obtain a uniform, white, opaque emulsion.
• Know that eyedrops can be used concomitantly with artificial tears, allowing a 15-minute interval between products.
CV: hypertension, chest pain, myocardial infarction
EENT: visual disturbances, hearing loss, tinnitus, rhinitis; (with ophthalmic use) ocular burning, conjunctival hyperemia, discharge, epiphora, eye pain, foreign body sensation, itching, stinging, blurring
GI: nausea, vomiting, diarrhea, constipation, abdominal discomfort, gastritis, peptic ulcer, mouth sores, difficulty swallowing, anorexia, upper GI bleeding, pancreatitis
GU: gynecomastia, hematuria, nephrotoxicity, renal dysfunction, glomerular capillary thrombosis Hematologic: anemia, leukopenia, thrombocytopenia
Metabolic: hyperglycemia, hypomagnesemia, hyperuricemia, hyperkalemia, metabolic acidosis
Musculoskeletal: muscle and joint pain
Respiratory: cough, dyspnea, Pneumocystis jiroveci pneumonia, bronchospasm
Skin: acne, hirsutism, brittle fingernails, hair breakage, night sweats
Other: gum hyperplasia, flulike symptoms, edema, fever, weight loss, hiccups, anaphylaxis
The following interactions pertain to oral and I.V. routes only.
Drug-drug. Acyclovir, aminoglycosides, amphotericin B, cimetidine, diclofenac, gentamicin, ketoconazole, melphalan, naproxen, ranitidine, sulindac, sulfamethoxazole, tacrolimus, tobramycin, trimethoprim, vancomycin: increased risk of nephrotoxicity
Allopurinol, amiodarone, bromocriptine, clarithromycin, colchicine, danazol, diltiazem, erythromycin, fluconazole, imipenem and cilastatin, itraconazole, ketoconazole, methylprednisolone, nicardipine, prednisolone, quinupristin/dalfopristin, verapamil: increased cyclosporine blood level
Azathioprine, corticosteroids, cyclophosphamide: increased immunosuppression Carbamazepine, isoniazid, nafcillin, octreotide, orlistat, phenobarbital, phenytoin, rifabutin, rifampin, ticlopidine: decreased cyclosporine blood level
Digoxin: decreased digoxin clearance
Live-virus vaccines: decreased antibody response to vaccine
Lovastatin: decreased lovastatin clearance, increased risk of myopathy and rhabdomyolysis
Potassium-sparing diuretics: increased risk of hyperkalemia
Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, bilirubin, blood urea nitrogen, creatinine, glucose, low-density lipoproteins: increased levels
Hemoglobin, platelets, white blood cells: decreased values
Drug-food. Grapefruit, grapefruit juice: decreased cyclosporine metabolism, increased cyclosporine blood level
High-fat diet: decreased drug absorption (Neoral)
Drug-herbs. Alfalfa sprouts, astragalus, echinacea, licorice: interference with immunosuppressant action St. John's wort: reduced cyclosporine blood level, possibly leading to organ rejection
• Observe patient for first 30 to 60 minutes of infusion. Monitor frequently thereafter.
• Monitor cyclosporine blood level, electrolyte levels, and liver and kidney function test results.
• Assess for signs and symptoms of hyperkalemia in patients receiving concurrent potassium-sparing diuretic.
• Advise patient to dilute Neoral oral solution with orange or apple juice (preferably at room temperature) to improve its flavor.
• Instruct patient to use glass container when taking oral solution. Tell him not to let solution stand before drinking, to stir solution well and then drink all at once, and to rinse glass with same liquid and then drink again to ensure that he takes entire dose.
• Tell patient taking Neoral to avoid high-fat meals, grapefruit, and grapefruit juice.
• Advise patient to dilute Sandimmune oral solution with milk, chocolate milk, or orange juice to improve its flavor.
• Instruct patient to invert vial a few times to obtain a uniform, white, opaque emulsion before using eyedrops and to discard vial immediately after use.
• Inform patient that eyedrops can be used with artificial tears but to allow 15-minute interval between products.
• Caution patient not to wear contact lenses because of decreased tear production; however, if contact lenses are used, advise patient to remove them before administering eyedrops and to reinsert 15 minutes after administration.
• Inform patient that he's at increased risk for infection. Caution him to avoid crowds and exposure to illness.
• Instruct patient not to take potassium supplements, herbal products, or dietary supplements without consulting prescriber.
• Tell patient he'll need to undergo repeated laboratory testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.