Generic Name and Formulations:
Cyclosporine (modified) 25mg, 100mg; caps; contains alcohol.

Company:
Novartis Pharmaceuticals Corp
Indications for NEORAL:
Severe, active rheumatoid arthritis unresponsive to methotrexate alone.

Adult:
Give consistently with regard to meals and time of day. ≥18yrs: 1.25mg/kg twice daily; may increase by 0.5–0.75mg/kg per day after 8 weeks and again after 12 weeks; max 4mg/kg per day (many patients on concomitant methotrexate can be treated with doses of 3mg/kg per day or less). Dilute soln in a glass of room temp orange or apple juice. Reduce dose by 25–50% if adverse events (eg, hypertension or serum creatinine increases ≥30% above baseline) occur. Renal or severe hepatic impairment: consider reducing dose. Discontinue if adverse events are severe or persistent, or if no benefit by week 16.

Children:
<18yrs: not established.

Contraindications:
Renal impairment. Uncontrolled hypertension. Malignancies.

Warnings/Precautions:
Be fully familiar with immunosuppressive therapy before prescribing. Not bioequivalent to all other forms of cyclosporine; do not interchange without physician supervision. Increased risk of infections, lymphomas and other malignancies (eg, skin). Avoid sun or UV light exposure. Monitor renal and hepatic function, BP, CBC, serum magnesium, potassium, uric acid, lipids (see full labeling for monitoring frequency). Reduce dose if hypertension occurs; do not attempt to manage medically. Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interactions:
Avoid other nephrotoxic drugs (eg, ciprofloxacin, gentamicin, tobramycin, vancomycin, SMX/TMP, melphalan, amphotericin B, ketoconazole, cimetidine, ranitidine, tacrolimus, NSAIDs, colchicine), fibric acid derivatives. Cyclosporine levels increased by CYP3A inhibitors (eg, calcium channel blockers, amiodarone, azithromycin, azole antifungals, erythromycin, clarithromycin, quinupristin/dalfopristin, boceprevir, telaprevir, methylprednisolone, allopurinol, colchicine, bromocriptine, danazol, metoclopramide; probably indinavir, saquinavir, nelfinavir, ritonavir, imatinib, nefazodone, oral contraceptives). Avoid alcohol, grapefruit juice. Cyclosporine levels decreased by CYP3A inducers (eg, nafcillin, rifampin, carbamazepine, oxcarbazepine, bosentan, phenobarbital, phenytoin, octreotide, ticlopidine, St. John's wort), orlistat. Avoid potassium-sparing diuretics. Concomitant repaglinide: monitor blood glucose. Concomitant aliskiren: not recommended. Concomitant sirolimus: separate by 4 hours. May decrease effectiveness of vaccines; avoid live attenuated vaccines. May increase levels of digoxin (monitor), colchicine, prednisolone, statins (reduce dose), ambrisentan, and anthracycline antibiotics. Gingival hyperplasia with nifedipine (avoid). Convulsions with high-dose methylprednisolone.

See Also:
NEORAL ORAL SOLUTION

Pharmacological Class:
DMARD (immunosuppressant).

Adverse Reactions:
Renal dysfunction, hypertension, headache, GI disturbances, hirsutism, hypertrichosis, leg cramps, pain, tremor, paresthesia, edema, dizziness, gum hyperplasia, liver dysfunction; increased risk of infections or malignancies, progressive multifocal leukoencephalopathy, hyperkalemia, thrombotic microangiopathy, possible encephalopathy.

Metabolism:
Hepatic (CYP3A).

Elimination:
Biliary (primarily), renal.

Generic Availability:
YES

How Supplied:
Caps—30; Soln—50mL