Sandimmun/Sandimmun Neoral

Ciclosporin

Transplantation: Solid organ transplantation (kidney, liver, heart, combined heart-lung, lung, pancreas); bone marrow transplantation. Non-transplantation: Endogenous uveitis; nephrotic syndrome; severe active RA; severe psoriasis.

Solid organ transplantation Initially 10-15 mg/kg in 2 divided doses w/in 12 hr pre-op & continued daily for 1-2 wk post-op. Maintenance: Gradually reduce to 2-6 mg/kg daily in 2 divided doses. Conjunction w/ other immunosuppressants: 3-6 mg/kg in 2 divided doses. Bone marrow transplantation Initially 3-5 mg/kg daily IV infusion initiated 1 day pre-op & continued during post-op for up to 2 wk before shifting to oral therapy w/ Sandimmun Neoral 12.5 mg/kg daily in 2 divided doses for 3-6 mth before gradual w/drawal 1 yr after transplantation. If Sandimmun Neoral is used to initiate therapy, 12.5-15 mg/kg daily in 2 divided doses is given. Endogenous uveitis Inducing remission: Initially 5 mg/kg daily orally in 2 divided doses, may be increased to 7 mg/kg daily for limited period in refractory cases. Systemic corticosteroid treatment w/ prednisone 0.2-0.6 mg/kg daily or equiv may be added if Sandimmun Neoral alone is insufficient to achieve initial remission or to counteract inflammatory ocular attacks. Maintenance: Slowly reduce dose to 5 mg/kg daily. RA 3 mg/kg daily in 2 divided doses for 1st 6 wk, may be increased gradually to max: 5 mg/kg. Up to 12 wk of Sandimmun Neoral treatment may be required to achieve full effectiveness. Psoriasis Inducing remission: Initially 2.5 mg/kg daily orally in 2 divided doses, may be gradually increased up to max: 5 mg/kg daily if no improvement after 1 mth. Maintenance: Titrate individually to 5 mg/kg daily. Nephrotic syndrome Inducing remission: Adult 5 mg/kg daily in 2 divided doses. Childn 6 mg/kg daily in 2 divided doses Renal impairment Not to exceed 2.5 mg/kg daily.

May be taken with or without food: Tab: Swallow whole. Oral soln: Dilute preferably in orange/apple juice, but other drinks (eg, soft drinks) may also be used. Stir well & drink immediately. Avoid grapefruit juice.

Hypersensitivity to ciclosporin, polyoxyl castor oil. Sandimmun Hypersensitivity to cremophor EL.

Closely monitor renal & hepatic function, serum creatinine, K & Mg levels, BP, ciclosporin & lipid blood levels during therapy. Activation of latent polyomavirus infections. Hyperuricaemia; epilepsy; alcoholic patients or on K-rich diet. Avoid excessive unprotected sun & UV light exposure. Long-term immunosuppressive therapy. Avoid use w/ live attenuated vaccines; dabigatran, bosentan. Not recommended in concomitant use w/ aliskiren. Concomitant use w/ K-sparing & -containing drugs; lercanidipine. Acute & chronic nephrotoxicity; hepatotoxicity, liver injury. Not to be used during pregnancy & lactation. Not recommended in childn. Elderly ≥65 yr. Sandimmun Anaphylactoid reactions. Non-transplant indications: Uncontrolled HTN & infection. Endogenous uveitis: Monitor patients w/ neurological Behcet's syndrome. Nephrotic syndrome: Occurrence of malignancies eg, Hodgkin's lymphoma. RA & psoriasis: Discontinue Sandimmun Neoral if HTN develops & cannot be controlled by anti-hypertensives. Increased lymphoproliferative disorders. RA: Concomitant use w/ MTX. Psoriasis: Not to be used concomitantly w/ UVB irradiation or PUVA photochemotherapy.

Anorexia, hyperglycemia; tremor, headache; HTN, nausea, vomiting, abdominal discomfort, diarrhea, gingival hyperplasia; hirsutism; renal dysfunction. Leucopenia; convulsions, paraesthesia; flushing; peptic ulcer; hepatotoxicity; acne, rash; pyrexia, edema.

Avoid use w/ live attenuated vaccines. Increased serum K w/ K-sparing & -containing drugs. Increased AUC w/ lercanidipine. Decreased levels by barbiturates, carbamazepine, oxcarbazepine, phenytoin, nafcillin, sulfadimidine IV, rifampicin, octreotide, probucol, orlistat, Hypericum perforatum (St. John's wort), ticlopidine, sulfinpyrazone, terbinafine, bosentan. Increased levels by macrolides, ketoconazole, fluconazole, itraconazole, voriconazole, diltiazem, nicardipine, verapamil, metoclopramide, OCs, danazol, methylprednisolone (high dose), allopurinol, amiodarone, cholic acid & derivatives, PIs, imatinib, nefazodone. Increased bioavailability w/ grapefruit juice. Potential increased nephrotoxicity w/ aminogylcosides, amphotericin B, ciprofloxacin, vancomycin, trimethoprim + sulfamethoxazole, NSAIDs (including diclofenac, naproxen, sulindac), melphalan, H₂-receptor antagonists, MTX, tacrolimus. Increased bioavailability of diclofenac. Reversible kidney impairment w/ fibric acid derivatives (eg, bezafibrate, fenofibrate). Increased rate of gingival hyperplasia w/ nifedipine. Increased plasma levels of CYP3A4 enzymes & P-gp transporters. Reduced clearance of digoxin, colchicine, prednisolone, HMG-CoA reductase inhibitors (statins), etoposide, aliskiren, bosentan, dabigatran. Increased blood levels of everolimus, sirolimus. Increased repaglinide plasma conc. Increased exposure of ambrisentan, anthracycline antibiotics eg, doxorubicine, mitoxanthrone, daunorubicine.

Immunosuppressants

L04AD01 - ciclosporin ; Belongs to the class of calcineurin inhibitors. Used as immunosuppressants.

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