Cyclosporin (Ciclosporin) โ NZ Medication Guide
๐ Reviewed by a Registered Pharmacist NZ โ This information is for general educational purposes only and does not replace professional medical advice. Always consult your doctor or pharmacist before starting, stopping, or changing any medication.
What is Cyclosporin (Ciclosporin)?
Ciclosporin is a potent calcineurin inhibitor immunosuppressant used to prevent organ transplant rejection and treat severe autoimmune conditions. This medication is funded by Pharmac for transplantation and severe immune-mediated conditions under Special Authority.
What is Cyclosporin (Ciclosporin) Used For?
Ciclosporin is used for prevention and treatment of organ transplant rejection (kidney, liver, heart, lung), severe refractory rheumatoid arthritis, severe psoriasis, severe atopic dermatitis (eczema), and aplastic anaemia.
How Does Cyclosporin (Ciclosporin) Work?
Ciclosporin inhibits calcineurin โ a phosphatase enzyme activated by the calcium-calmodulin complex in T lymphocytes. Calcineurin normally activates NFAT transcription factors that drive IL-2 gene expression (essential for T cell activation and proliferation). By blocking calcineurin, ciclosporin profoundly suppresses T cell-mediated immune responses โ preventing graft rejection and autoimmune tissue damage.
How to Take Cyclosporin (Ciclosporin)
Doses are highly individualised and weight-based (typically 3โ5 mg/kg/day in 2 divided doses for transplant). Administered consistently at the same time each day, with or without food โ but always the same way. Blood level monitoring (trough levels) is mandatory. Dose adjustments based on levels, renal function, and clinical response.
Common Side Effects of Cyclosporin (Ciclosporin)
- Nephrotoxicity (dose-related โ most significant long-term concern)
- Hypertension
- Hirsutism (increased body and facial hair)
- Gingival hyperplasia (gum overgrowth)
- Tremor
- Nausea and vomiting
- Hyperlipidaemia
Serious Side Effects โ Seek Medical Attention
Contact your doctor or call 111 immediately if you experience any of the following:
- Chronic nephrotoxicity (irreversible reduction in renal function with long-term use)
- Serious infections (due to immunosuppression โ bacterial, viral, fungal, and opportunistic)
- Hypertension (requires treatment)
- Lymphoma and skin malignancy (long-term immunosuppression)
- Neurotoxicity (encephalopathy, seizures โ with high levels)
- Drug interactions causing toxicity (many)
Drug Interactions
Cyclosporin (Ciclosporin) may interact with other medicines. Always inform your doctor and pharmacist of all medications you are taking. Key interactions include:
- MANY significant interactions โ comprehensive review essential before prescribing anything new
- Nephrotoxic medicines (NSAIDs, gentamicin, vancomycin โ increased nephrotoxicity)
- CYP3A4 inhibitors (ketoconazole, clarithromycin, verapamil โ increase levels)
- CYP3A4 inducers (rifampicin, carbamazepine โ reduce levels)
- Statins (increased myopathy/rhabdomyolysis risk โ avoid simvastatin; use rosuvastatin or pravastatin at low doses)
- Potassium-sparing agents (additive hyperkalaemia)
- Grapefruit juice (markedly increases levels โ avoid completely)
New Zealand Prescribing Information
Ciclosporin (Neoralยฎ 25 mg, 50 mg, 100 mg soft gelatin capsules; 100 mg/mL oral solution; Sandimmunยฎ IV) is funded by Pharmac. Therapeutic drug monitoring (trough or 2-hour post-dose levels) is mandatory. Grapefruit and grapefruit juice must be completely avoided โ grapefruit inhibits CYP3A4 in the gut and increases ciclosporin levels unpredictably by up to 3-fold.
Frequently Asked Questions
Why do I need blood level monitoring for ciclosporin?
Ciclosporin has a very narrow therapeutic index โ levels too low cause rejection, levels too high cause nephrotoxicity and other serious side effects. Regular blood level measurements allow precise dose adjustments to maintain levels in the safe therapeutic range.
Why must I completely avoid grapefruit on ciclosporin?
Grapefruit contains furanocoumarins that irreversibly inhibit CYP3A4 enzymes in the gut wall, dramatically increasing ciclosporin absorption and blood levels by up to 200โ300%. Even one glass of grapefruit juice can cause toxic ciclosporin levels. Grapefruit and grapefruit juice must be completely avoided.
โ ๏ธ Disclaimer: This page is for educational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your doctor or a qualified health provider. In New Zealand, medication availability and funding may vary โ check with Pharmac or your pharmacist for current information.
Reviewed by a Registered Pharmacist NZ
References & Further Information
The following New Zealand and international resources were used to inform this page: