Menelri (Ciclosporin)

Ciclosporin is a calcineurin inhibitor used to modulate immune‑mediated conditions.

• Organ transplant rejection: prevents graft rejection by suppressing T‑cell activation.
• Severe psoriasis: reduces skin inflammation and plaque formation.
• Rheumatoid arthritis: diminishes joint inflammation and disease progression.

• 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), reducing transcription of interleukin‑2 and other cytokines essential for T‑cell activation and proliferation, thereby producing immunosuppression. The inhibition also lowers production of IL‑3, IL‑4 and interferon‑γ, further dampening immune responses and contributes to the therapeutic effect in transplant and autoimmune diseases.

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

Common Side Effects

• Headache: mild to moderate headache.
• Hypertension: elevated blood pressure.
• Nausea: gastrointestinal upset.
• Tremor: fine hand tremors.

Serious or Rare Side Effects

• Nephrotoxicity: impaired kidney function.
• Infections: increased susceptibility to bacterial, viral or fungal infections.
• Malignancy: higher risk of lymphomas or skin cancers.

When prescribing Ciclosporin, clinicians should consider several safety precautions to minimise risk.

• Monitor renal function: check serum creatinine and glomerular filtration rate regularly.
• Assess liver enzymes: perform periodic hepatic function tests.
• Check blood pressure: manage hypertension that may develop during therapy.
• Review drug interactions: avoid concomitant nephrotoxic or CYP3A4‑inhibiting agents when possible.
• Pregnancy and lactation: use only if benefits outweigh potential risks, as safety data are limited.
• Store at ambient temperature: keep below 25 °C, in original packaging, protected from moisture.

Ciclosporin interacts with several medicines through metabolic pathways and additive pharmacologic effects.

Major Interactions (Avoid)

• Ketoconazole: strong CYP3A4 inhibition markedly increases ciclosporin levels.
• Rifampicin: potent CYP3A4 induction reduces ciclosporin exposure, risking graft rejection.
• Nephrotoxic drugs (e.g., aminoglycosides): combined use can cause severe kidney injury.

Moderate Interactions (Monitor Closely)

• Calcium channel blockers (e.g., diltiazem): may raise ciclosporin concentrations modestly.
• Statins (especially simvastatin): increased risk of myopathy; dose adjustment may be needed.
• NSAIDs: can enhance renal toxicity when used together.