Immunosporin (Ciclosporin)

Immunosporin (ciclosporin) acts on the calcineurin pathway to modulate immune responses in several chronic conditions.

• Organ transplant rejection: helps prevent graft rejection by inhibiting T‑cell activation and interleukin‑2 production, supporting long‑term graft survival.
• Rheumatoid arthritis: reduces joint inflammation, pain, and structural damage in patients with moderate to severe disease when other therapies are insufficient.
• Psoriasis: improves extensive plaque lesions by dampening the overactive immune response, leading to reduced scaling and erythema.

• Ciclosporin binds to the intracellular protein cyclophilin, forming a complex that inhibits the phosphatase activity of calcineurin. This blockade prevents dephosphorylation of nuclear factor of activated T‑cells (NF‑AT), thereby reducing transcription of interleukin‑2 and other cytokines essential for T‑lymphocyte activation and proliferation. The inhibition is dose‑dependent and results in a broad suppression of cell‑mediated immunity, affecting both helper and cytotoxic T cells as well as downstream immune pathways.

Ciclosporin may cause a range of adverse reactions, varying from mild to severe.

Common Side Effects

• Headache: mild to moderate intensity.
• Tremor: fine shaking of hands or limbs.
• Hypertension: elevated blood pressure requiring monitoring.
• Gastrointestinal discomfort: nausea, abdominal pain or diarrhea.
• Hyperlipidemia: elevated cholesterol or triglycerides.
• Gingival hyperplasia: overgrowth of gum tissue.

Serious or Rare Side Effects

• Nephrotoxicity: impaired kidney function that may be irreversible.
• Infections: increased susceptibility to bacterial, viral or fungal infections.
• Malignancy risk: heightened incidence of lymphomas and skin cancers with long‑term use.

When prescribing Immunosporin, clinicians should observe several precautionary measures to minimise risk.

• Monitor renal function: assess serum creatinine and glomerular filtration rate regularly.
• Check blood pressure: control hypertension before and during therapy.
• Evaluate lipid profile: manage hyperlipidaemia that may develop.
• Screen for infections: treat active infections prior to initiation.
• Avoid concomitant nephrotoxic drugs: limit use of aminoglycosides and NSAIDs.
• Store at ambient temperature: keep below 25 °C, in original packaging, protected from moisture.

Ciclosporin interacts with several medicines that can alter its concentration or enhance toxicity.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir): markedly increase ciclosporin levels, risking nephrotoxicity.
• Macrolide antibiotics (e.g., erythromycin, clarithromycin): elevate drug exposure and may cause severe adverse effects.
• Certain antifungals (e.g., itraconazole, voriconazole): raise ciclosporin concentrations to dangerous levels.

Moderate Interactions (Monitor Closely)

• Calcium channel blockers (e.g., diltiazem, verapamil): may increase ciclosporin levels; monitor renal function.
• NSAIDs (e.g., ibuprofen, naproxen): can enhance nephrotoxic risk; assess kidney parameters.
• St. John’s wort: may reduce ciclosporin exposure, decreasing efficacy; consider alternative therapy.