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Calcineurin inhibitor Pregnancy: No adequate well-controlled studies in pregnancy; embryofoetal toxicity seen in animals below the maximum recommended human dose. Should not be used during pregnancy unless potential benefit to the mother outweighs the risk to the foetus. Not recommended during breast-feeding.

Ciclosporin

Brand names: Neoral, Sandimmun, Capimune, Deximune, Vanquoral

Ciclosporin is a calcineurin-inhibitor immunosuppressant used in rheumatology as a disease-modifying agent for severe rheumatoid arthritis and other autoimmune conditions unresponsive to first-line therapy.

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 initially (started within 12 hours before surgery), maintained for 1-2 weeks post-operatively then gradually reduced per blood levels to a maintenance dose of about 2 to 6 mg/kg/day
Route: Oral
Frequency: In two divided doses daily
Max: Non-transplant indications: total daily dose must never exceed 5 mg/kg (except sight-threatening endogenous uveitis and children with nephrotic syndrome)
Dose ranges are guidelines only; give on a consistent schedule relative to meals. Only to be prescribed by/with a physician experienced in immunosuppressive therapy and/or transplantation, with ciclosporin blood-level monitoring. When combined with other immunosuppressants (e.g. corticosteroids, triple/quadruple therapy), lower initial doses (e.g. 3-6 mg/kg/day in two divided doses) may be used. Bone marrow transplantation: IV concentrate 3 to 5 mg/kg/day is usually preferred initially for up to 2 weeks, then oral maintenance ~12.5 mg/kg/day in 2 divided doses (continue at least 3 months, preferably 6, then taper to zero by 1 year); if oral used to initiate, 12.5 to 15 mg/kg/day in 2 divided doses from the day before transplantation. GVHD after discontinuation: oral loading dose 10 to 12.5 mg/kg then previous maintenance dose. Non-transplantation indications: establish baseline renal function (>=2 measurements) before starting; except in sight-threatening endogenous uveitis and children with nephrotic syndrome, the total daily dose must never exceed 5 mg/kg. Endogenous uveitis: initially 5 mg/kg/day orally in 2 divided doses (up to 7 mg/kg/day in refractory cases for a limited period). Nephrotic syndrome (normal renal function): adults 5 mg/kg/day, children 6 mg/kg/day in 2 divided oral doses; if renal impairment, initial dose not to exceed 2.5 mg/kg/day. If eGFR falls >25% below baseline on more than one measurement, reduce dose by 25-50%; discontinue if dose reduction does not improve eGFR within one month.

Dose adjustments

Renal

Non-transplant indications: if eGFR decreases >25% below baseline on more than one measurement, reduce dose by 25-50%; if decrease exceeds 35%, consider further reduction; discontinue if dose reduction does not improve eGFR within one month. In nephrotic syndrome with impaired renal function, initial dose should not exceed 2.5 mg/kg/day.

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 ciclosporin 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) where elevated plasma concentrations cause serious/life-threatening events, e.g. bosentan, dabigatran etexilate, aliskiren

Side effects

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

Interactions

  • St John's Wort (contraindicated)
  • P-glycoprotein / OATP substrates such as bosentan, dabigatran etexilate, aliskiren (contraindicated)
  • Substances that interfere with ciclosporin pharmacokinetics may warrant ciclosporin blood-level monitoring in non-transplant indications

Clinical monograph

How it works

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

Prescribing in practice

  • Nephrotoxic and hypertensive — renal function and blood pressure must be measured before and regularly during treatment, with dose reduction or withdrawal if creatinine rises persistently.
  • Numerous interactions occur via CYP3A4 and P-glycoprotein; avoid concurrent live vaccines and minimise other nephrotoxins.
  • Prescribe and dispense by brand name because formulations are not interchangeable, and check the SPC for the relevant indication.

Monitoring

Monitor serum creatinine, blood pressure, potassium, liver function, lipids and (where indicated) blood ciclosporin concentrations during therapy.

Counselling the patient

  • Report swelling, reduced urine output or persistent headache.
  • Avoid grapefruit juice and tell clinicians about all other medicines.
  • Use sun protection and attend monitoring appointments.

Evidence & guidelines

Long-standing use is supported by controlled trials and UK guidance for severe refractory inflammatory arthritis.

Reference: NICE TA180; 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).

Related

Curated clinical cross-links plus same-class fallbacks.