SANDIMMUNE ORAL SOLUTION Dosage & Rx Info

Sandimmune Oral Solution Generic Name & Formulations

Legal Class

General Description

Cyclosporine 100mg/mL; contains alcohol.

Pharmacological Class

Immunosuppressant.

How Supplied

Caps—3x10 blister cards; Soln—50mL; Inj (5mL)—10

Manufacturer

Novartis Pharmaceuticals Corp

Mechanism of Action

The exact mechanism of action of cyclosporine is not known. Experimental evidence suggests that the effectiveness of cyclosporine is due to specific and reversible inhibition of immunocompetent lymphocytes in the G₀- or G₁-phase of the cell cycle. T-lymphocytes are preferentially inhibited. The T-helper cell is the main target, although the T-suppressor cell may also be suppressed. Cyclosporine also inhibits lymphokine production and release, including interleukin-2 or T-cell growth factor (TCGF).

Sandimmune Oral Solution Indications

Indications

Organ rejection prophylaxis in kidney, liver, and heart allogeneic transplants, in combination with corticosteroids. Treatment of chronic rejection in patients previously treated with other immunosuppressants. IV: reserved for patients who are unable to take caps or oral soln.

Sandimmune Oral Solution Dosage and Administration

Adult

Give consistently with regard to meals and time of day. Initially 15mg/kg as a single dose given 4–12hrs prior to transplantation. Continue initial daily dose for 1–2wks post-op then taper by 5% per week to maintenance dose of 5–10mg/kg/day. Adjunct corticosteroid therapy is recommended. Oral soln: dilute with room temp milk, chocolate milk, or orange juice before administration; avoid switching diluents frequently. Conversion from Neoral, blood concentration monitoring: see full labeling.

Children

See full labeling.

Sandimmune Oral Solution Contraindications

Contraindications

IV: hypersensitivity to Cremophor EL.

Sandimmune Oral Solution Boxed Warnings

Boxed Warning

Prescribe only by physicians experienced in immunosuppressive therapy. May increase risk of infections, lymphomas and other malignancies. Decreased bioavailability compared to Neoral; do not use interchangeably.

Sandimmune Oral Solution Warnings/Precautions

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). Monitor BP, renal and hepatic function. Control hypertension if develops. Malabsorption. Elderly. Pregnancy. Nursing mothers.

Sandimmune Oral Solution Pharmacokinetics

Absorption

Absolute bioavailability: ~30%.Time to peak blood concentrations (Tmax): ~3.5 hours.

Distribution

Distributed largely outside the blood volume. Plasma protein bound: ~90% (primarily lipoproteins).

Elimination

Biliary (primarily), renal (6%). Half-life: ~19 hours (range: 10–27 hours).

Sandimmune Oral Solution Interactions

Interactions

Avoid other nephrotoxic drugs (eg, ciprofloxacin, gentamicin, tobramycin, vancomycin, SMX/TMP, melphalan, amphotericin B, ketoconazole, cimetidine, ranitidine, tacrolimus, NSAIDs, colchicine), fibric acid derivatives, methotrexate. 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 (avoid), phenobarbital, phenytoin, octreotide, sulfinpyrazone, terbinafine, ticlopidine, St. John's wort), orlistat. Avoid potassium-sparing diuretics. Caution with concomitant rifabutin. Concomitant repaglinide: monitor blood glucose. Concomitant aliskiren: not recommended. Concomitant sirolimus: separate by 4 hours. May antagonize mycophenolic acid; monitor efficacy. May decrease effectiveness of vaccines; avoid live attenuated vaccines. May increase levels of digoxin (monitor), colchicine, statins (reduce dose), ambrisentan, and anthracycline antibiotics, dabigatran (avoid). Gingival hyperplasia with nifedipine. Convulsions with high-dose methylprednisolone.

Sandimmune Oral Solution Adverse Reactions

Adverse Reactions

Renal dysfunction, tremor, hirsutism, hypertension, gum hyperplasia, cramps, convulsions, headache, diarrhea, nausea, vomiting; increased risk of infections or malignancies, progressive multifocal leukoencephalopathy, polyoma virus-associated nephropathy, hypomagnesemia, hyperkalemia, hyperuricemia, thrombotic microangiopathy, hepatotoxicity, neurotoxicity; IV: anaphylactic reactions.

Sandimmune Oral Solution Clinical Trials

See Literature

Sandimmune Oral Solution Note

Not Applicable

Sandimmune Oral Solution Patient Counseling