Calcineurin Inhibitor (CNI) Pregnancy: Should not be used during pregnancy unless the potential benefit to the mother outweighs the potential risk to the foetus; animal studies show embryofoetal toxicity below the maximum recommended human dose, and transplant recipients are at risk of premature delivery. Not recommended during breast-feeding (enters breast milk; potential for adverse reactions in the infant). Ethanol content of the formulation should also be considered.

Ciclosporin

Brand names: Neoral, Sandimmun

Ciclosporin is a calcineurin-inhibitor immunosuppressant used to prevent transplant rejection and to treat certain glomerular diseases such as steroid-dependent or relapsing nephrotic syndrome.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Solid organ transplantation: 10 to 15 mg/kg/day given in two divided doses, initiated within 12 hours before surgery; maintained for 1-2 weeks post-operatively then gradually reduced to a maintenance dose of about 2 to 6 mg/kg/day in 2 divided doses

Route: Oral (soft capsules; two divided doses daily)

Frequency: Twice daily (daily dose split into 2 divided doses)

Max: Initial peri-operative dose up to 15 mg/kg/day; non-transplant indications must never exceed 5 mg/kg/day (except sight-threatening endogenous uveitis and children with nephrotic syndrome)

Capimune 100 mg soft capsules (SPC). Give on a consistent schedule with regard to time of day and meals; only prescribe by/with a physician experienced in immunosuppressive therapy and/or organ transplantation. When combined with other immunosuppressants (e.g. corticosteroids, or triple/quadruple therapy), lower initial doses (e.g. 3-6 mg/kg/day in two divided doses) may be used. Bone marrow transplantation: recommended IV dose 3-5 mg/kg/day (usually start with the concentrate for infusion the day before transplantation) for up to 2 weeks, then change to oral maintenance ~12.5 mg/kg/day in 2 divided doses; if initiating with oral Capimune, 12.5-15 mg/kg/day in 2 divided doses from the day before transplantation; continue maintenance at least 3 (preferably 6) months then taper to zero by 1 year. GVHD after discontinuation: oral loading 10-12.5 mg/kg then the previously satisfactory maintenance dose. Nephrotic syndrome (adults): 5 mg/kg/day in 2 divided oral doses if renal function (except proteinuria) is normal; if renal function impaired, initial dose must not exceed 2.5 mg/kg/day. Establish baseline renal function from at least two measurements before starting non-transplant therapy.

Dose adjustments

Renal

Nephrotic syndrome with impaired renal function: initial dose must not exceed 2.5 mg/kg/day. General non-transplant rule: reduce dose by 25-50% if eGFR falls >25% below baseline at more than one measurement; consider further reduction if the fall exceeds 35%; discontinue if reduction does not improve eGFR within one month. Renal transplant patients require differentiation of ciclosporin nephrotoxicity from chronic rejection.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or any excipient
Combination with products containing Hypericum perforatum (St John's Wort)
Combination with medicines that are substrates for P-glycoprotein (Pgp) or organic anion transporter proteins (OATP) for which elevated plasma concentrations are associated with serious/life-threatening events, e.g. bosentan, dabigatran etexilate, aliskiren

Side effects

Renal dysfunction (dose-dependent rise in serum creatinine and urea)
Tremor and headache (very common)
Hirsutism
Hypertension
Gastrointestinal: anorexia, nausea, vomiting, diarrhoea
Hyperlipidaemia (very common); hyperuricaemia, hyperkalaemia, hypomagnesaemia

Interactions

St John's Wort (Hypericum perforatum) — contraindicated
Pgp/OATP substrates with serious risk at raised levels: bosentan, dabigatran etexilate, aliskiren — contraindicated
Substances that interfere with ciclosporin pharmacokinetics — monitor ciclosporin blood levels when co-administered
Nephrotoxic drugs / factors — additive renal impairment risk (dose-dependent nephrotoxicity)

Clinical monograph

How it works

It binds cyclophilin and inhibits calcineurin, blocking transcription of interleukin-2 and other cytokines, thereby suppressing T-lymphocyte activation.

Prescribing in practice

Ciclosporin is itself nephrotoxic and causes dose-dependent renal impairment and hypertension, so renal function and blood pressure must be monitored closely and dosing guided by blood levels.
It has a narrow therapeutic index with numerous interactions via CYP3A4 and P-glycoprotein (e.g. azole antifungals, macrolides, grapefruit juice raise levels); prescribe by brand as formulations are not interchangeable.
Watch for hyperkalaemia, hypomagnesaemia, gum hyperplasia, hypertrichosis and an increased long-term risk of infection and malignancy.

Monitoring

Monitor whole-blood ciclosporin trough levels, serum creatinine, potassium, magnesium, lipids and blood pressure throughout treatment.

Counselling the patient

Always use the same brand and take doses at consistent times relative to food.
Avoid grapefruit juice and check before starting any new medicine, including over-the-counter products.
Attend for regular blood tests, which guide your dose and protect your kidneys.

Evidence & guidelines

Ciclosporin is an established calcineurin inhibitor in transplantation and steroid-sparing therapy of nephrotic syndrome, with therapeutic drug monitoring central to balancing efficacy against nephrotoxicity.

Reference: KDIGO Transplant Guidelines; UK Renal Association; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Drugs

Tacrolimus · Calcineurin Inhibitor (CNI)

Pathways