Neoral (Ciclosporin)

• Neoral (ciclosporin) is a calcineurin inhibitor used in several immune‑mediated conditions to control abnormal T‑cell activity and reduce inflammation.
• Organ transplant rejection: reduces the risk of acute and chronic graft rejection by inhibiting T‑cell activation and cytokine production.
• Severe psoriasis: decreases keratinocyte proliferation and inflammatory cytokine release, leading to clearance of plaques and improvement of skin lesions.
• Rheumatoid arthritis: provides disease control in patients who have not responded adequately to conventional disease‑modifying antirheumatic drugs, improving joint pain and function.

• Ciclosporin binds to the intracellular protein cyclophilin, forming a complex that inhibits the phosphatase activity of calcineurin. This blockade prevents dephosphorylation of the nuclear factor of activated T‑cells (NF‑AT), thereby suppressing transcription of interleukin‑2 and other cytokines essential for T‑cell activation and proliferation. The resulting immunosuppressive effect reduces the immune system's ability to mount a response against transplanted tissue and diminishes inflammatory processes in autoimmune diseases.

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

Common Side Effects

• Headache: mild to moderate intensity, often transient.
• Tremor: fine shaking of hands or limbs, may worsen with dose.
• Gastrointestinal discomfort: nausea, vomiting, abdominal pain or diarrhea.
• Hypertension: elevated blood pressure, may need antihypertensive therapy.
• Hypertrichosis: excessive hair growth on face or body.
• Hyperlipidemia: increased cholesterol or triglycerides, monitored by lipid profile.

Serious or Rare Side Effects

• Nephrotoxicity: impaired kidney function that can progress to renal failure; monitor creatinine.
• Infections: higher risk of bacterial, viral or fungal infections; may need prophylaxis.
• Malignancies: increased risk of lymphomas and skin cancers with long‑term use.
• Hepatotoxicity: liver enzyme elevations or hepatitis; regular liver function tests advised.

When prescribing ciclosporin, clinicians should observe several precautionary measures to minimize risks.

• Renal function: assess baseline creatinine and monitor regularly.
• Blood pressure: control hypertension before and during therapy.
• Liver function: perform baseline liver enzymes and repeat as needed.
• Infection risk: screen for latent infections and vaccinate appropriately.
• Drug monitoring: adjust dose based on trough blood levels when available.
• Store at ambient temperature: keep below 25°C, protect from moisture and light.

Ciclosporin interacts with several medicines, affecting its concentration or the effect of co‑administered drugs.

Major Interactions (Avoid)

• Ketoconazole and other strong CYP3A4 inhibitors: can markedly increase ciclosporin levels, risking toxicity.
• Rifampicin and other potent CYP3A4 inducers: can substantially lower ciclosporin concentrations, reducing efficacy.
• Nephrotoxic agents (e.g., aminoglycosides): combined use may exacerbate kidney damage.

Moderate Interactions (Monitor Closely)

• Calcium channel blockers (e.g., diltiazem): may increase ciclosporin levels modestly.
• Macrolide antibiotics (e.g., erythromycin): can raise ciclosporin concentrations.
• Diuretics (e.g., furosemide): may enhance hypertension risk when used together.