ciclosporin: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
ciclosporin: clinical details
Prescribing considerations
- Systemic treatment requires an experienced specialist and reliable follow-up; review infection, malignancy, renal, hepatic, cardiovascular and interaction risks.
- Prescribe and dispense systemic ciclosporin by brand. Supervise switching and reassess ciclosporin exposure, renal function, blood pressure and clinical control.
- Minimise excessive ultraviolet exposure; do not combine systemic ciclosporin with ultraviolet-B irradiation or PUVA photochemotherapy.
- Reserve intravenous concentrate for appropriate transplant settings when oral administration or absorption is unsuitable; observe closely for anaphylactoid reactions.
- Topical ocular treatment should be initiated and supervised by an ophthalmologist, with periodic eye examinations.
Contraindications and cautions
- Hypersensitivity to ciclosporin or relevant excipients.
- Systemic co-administration with St John’s wort, bosentan, dabigatran etexilate or aliskiren.
- For non-transplant systemic indications: impaired renal function other than the permitted nephrotic-syndrome context, uncontrolled hypertension, uncontrolled infection or malignancy.
- For selected eye drops: active or suspected ocular or periocular infection, or ocular or periocular malignant or premalignant disease.
Monitoring
- Before systemic treatment, assess blood pressure, renal and liver function, blood count, lipids, potassium, magnesium, infection risk and vaccination status as clinically appropriate.
- During treatment, monitor renal function and blood pressure closely; follow liver function, blood count, glucose, lipids and electrolytes according to indication and risk.
- Use ciclosporin blood concentrations routinely in transplantation and when clinically indicated by switching, interactions, toxicity or loss of efficacy.
- Monitor for infections, neurological toxicity, malignancy and skin changes; maintain appropriate cancer screening and sun protection.
- For eye drops, monitor the ocular surface and consider closer review with glaucoma, ocular hypertension or suspected infection.
Clinical pharmacology
Ciclosporin is a calcineurin inhibitor metabolised mainly through CYP3A4 and transported by P-glycoprotein. It also inhibits CYP3A4, P-glycoprotein and OATP transporters. Oral Neoral provides more consistent absorption than older Sandimmun oral formulations; systemic exposure after selected eye drops is negligible.
Formulation and product differences
- Neoral capsules and oral solution are bioequivalent, but oral products and brands should not be interchanged without supervision.
- The oral solution is a microemulsion preconcentrate requiring measurement and dilution immediately before administration; it contains ethanol and propylene glycol.
- Sandimmun intravenous concentrate contains polyoxyl castor oil and ethanol and carries a specific risk of anaphylactoid reactions.
- Vevizye is a topical ocular formulation for adult dry eye disease; its licensing, contraindications, adverse effects and systemic exposure differ substantially from oral or intravenous ciclosporin.
ciclosporin preparations and strengths
Solution for infusion
Route: Intravenous
Strengths: 50 mg/mL
Eye drops
Route: Ophthalmic
Strengths: 0.9 mg/mL, 1 mg/mL
Capsule
Route: Oral
Strengths: 25 mg, 50 mg, 100 mg
ciclosporin interactions
Ciclosporin has many important interactions. Check prescribed, pharmacy-bought and herbal products before starting or stopping them.
St John’s wort
Contraindicated with systemic ciclosporin because it can lower ciclosporin exposure and reduce immunosuppression.
Macrolide antibiotics and azole antifungals
Erythromycin, clarithromycin, fluconazole and itraconazole can substantially increase ciclosporin exposure and toxicity risk.
Rifampicin and enzyme-inducing antiseizure medicines
They can lower ciclosporin concentrations and jeopardise disease or transplant control.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.