Cyclosporine is indicated for use in transplantation and certain non-transplant conditions, including: Transplantation:

• Solid organ transplantation
• Bone marrow transplantation

Non-transplant indications:

• Endogenous uveitis
• Nephrotic syndrome
• Rheumatoid arthritis
• Psoriasis
• Atopic dermatitis

Cyclosporine is a cyclic polypeptide composed of 11 amino acids. It is a powerful immunosuppressive agent that prolongs the survival of allogeneic transplants, including skin, heart, kidney, pancreas, bone marrow, small intestine, and lung. It acts specifically and reversibly on lymphocytes. Unlike cytotoxic drugs, it does not suppress bone marrow function and has no significant effect on phagocytic cell activity. Patients treated with cyclosporine generally have a lower risk of infection compared to those receiving other immunosuppressive therapies.

Solid organ transplantation: Solid organ transplantation: Initially 10 to 15 mg/kg given in 2 divided doses starting 12 hours before surgery and to continue for 1 to 2 weeks post-operatively. Maintenance dose should be gradually reached to 2 to 6 mg/kg given in 2 divided doses.

Bone marrow transplantation: Bone marrow transplantation: Initially 12.5 to 15 mg/kg given in 2 divided doses, starting on the day before transplantation. Maintenance treatment of 12.5 mg/kg in 2 divided doses should be continued for at least 3 months (and preferably for 6 months) before the dose is gradually decreased to zero by 1 year after transplantation.

Endogenous uveitis: Endogenous uveitis: Initially 5 mg/kg per day orally given in 2 divided doses are recommended. For maintenance treatment, the dose should be slowly reduced to the lowest effective level.

Nephrotic syndrome: Nephrotic syndrome: Initially 5 mg/kg for adults and 6 mg/kg for children given in 2 divided doses. In case of renal impairment, the initial dose should not exceed 2.5 mg/kg per day. For maintenance treatment, the dose should be slowly reduced to the lowest effective level.

Rheumatoid arthritis :Rheumatoid arthritis: For the first 6 weeks, the recommended dose is 3 mg/kg per day in 2 divided doses. To achieve full effectiveness, up to 12 weeks of therapy may be required. For maintenance treatment, the dose has to be titrated individually according to tolerability.

Psoriasis & Atopic dermatitis: Psoriasis & Atopic dermatitis: Initially 2.5 mg/kg per day orally given in 2 divided doses and up to 5 mg/kg per day for patients whose condition requires rapid improvement. For maintenance treatment, doses have to be titrated individually to the lowest effective level.

Drugs that may decrease Cyclosporine levels include barbiturates, carbamazepine, oxcarbazepine, phenytoin, nafcillin, intravenous sulfadimidine, rifampicin, octreotide, probucol, orlistat, Hypericum perforatum (St. John’s wort), ticlopidine, sulfinpyrazone, terbinafine, and bosentan.

Drugs that may increase Cyclosporine levels include macrolide antibiotics (e.g., erythromycin, azithromycin, clarithromycin), azole antifungals (ketoconazole, fluconazole, itraconazole, voriconazole), calcium channel blockers (diltiazem, nicardipine, verapamil, lercanidipine), metoclopramide, oral contraceptives, danazol, high-dose methylprednisolone, allopurinol, amiodarone, bile acid derivatives, protease inhibitors, imatinib, and colchicine.

Other important interactions: Cyclosporine may reduce the clearance of drugs such as digoxin, colchicine, prednisolone, and HMG-CoA reductase inhibitors (statins), increasing their toxicity risk.

Cyclosporine is contraindicated in patients with hypersensitivity to ciclosporin or any excipients of the formulation. Additional contraindications in non-transplant use include:

• Kidney failure (except nephrotic syndrome cases with controlled serum creatinine levels).
• Uncontrolled hypertension.
• Uncontrolled infections.
• History of malignancy of any type, except premalignant or malignant skin lesions.

Renal: Kidney dysfunction.
Cardiovascular: Hypertension.
Nervous system: Tremor, headache, paresthesia.
Gastrointestinal: Loss of appetite, nausea, vomiting, abdominal pain, diarrhea, gingival hyperplasia, liver dysfunction.
Metabolic: Increased lipids, uric acid, potassium; decreased magnesium.
Musculoskeletal: Muscle cramps, myalgia, rarely muscle weakness or myopathy.
Hematologic: Anemia and thrombocytopenia (uncommon).
Skin: Excess hair growth (hypertrichosis), allergic rash.

There are no adequate controlled studies in pregnant women. Cyclosporine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. The drug passes into breast milk; therefore, breastfeeding is not recommended during treatment.

Cyclosporine increases the risk of lymphoma and other malignancies, especially skin cancer; therefore, excessive sunlight exposure should be avoided. It may also increase susceptibility to bacterial, fungal, viral, and parasitic infections, requiring long-term monitoring. Early therapy may cause reversible increases in serum creatinine and urea; dose adjustment usually improves this. Kidney function should be closely monitored, especially in elderly patients. Regular blood pressure monitoring is essential, and hypertension should be treated appropriately. Cyclosporine may cause hyperkalemia, particularly in renal impairment, and caution is needed with potassium-sparing drugs. It may also lower magnesium levels, so supplementation may be required. Caution is advised in hyperuricemia. Vaccination response may be reduced; live vaccines should be avoided. Non-transplant patients with kidney failure, uncontrolled hypertension, infections, or malignancy should not receive cyclosporine.

Overdose may cause kidney dysfunction, which is usually reversible after stopping the drug. Since cyclosporine is not effectively removed by dialysis or charcoal hemoperfusion, treatment is mainly supportive, including gastric lavage if necessary.

Immunosuppressants, Vaccines, Anti-sera & Immunoglobulins

Sporium oral solution should be used within 2 months after opening. Store between 15°C and 30°C, preferably not below 20°C for long periods. At low temperatures, the oily components may solidify, forming a jelly-like consistency that reverses at up to 30°C. Slight sediment may occur but does not affect safety or efficacy.