Ciclosporin: An Immunosuppressant (Neoral)
Comprehensive guide to ciclosporin (Neoral): uses in transplants, arthritis, psoriasis, dosage, side effects, and patient advice for safe use.
Ciclosporin, also known as cyclosporine and marketed as Neoral, is a calcineurin inhibitor immunosuppressant medication primarily used to prevent organ transplant rejection and treat various autoimmune and inflammatory conditions. It works by selectively inhibiting T-lymphocytes, reducing the production of inflammatory cytokines like interleukin-2 (IL-2).
About ciclosporin tablets and liquid
Ciclosporin is available in oral formulations such as capsules and oral solution under the brand name Neoral, which forms a microemulsion in aqueous environments for improved absorption compared to older formulations like Sandimmune. The active ingredient is a cyclic polypeptide of 11 amino acids produced by the fungus Beauveria nivea (formerly Tolypocladium inflatum). Neoral provides more consistent blood levels, with AUC 20-50% higher and Cmax 40-106% greater than Sandimmune in transplant patients.
There are two main oral forms: modified (Neoral, Gengraf) and non-modified (Sandimmune). Doses are not interchangeable due to differences in bioavailability; blood levels must be monitored closely when switching.
Key facts about ciclosporin
- Ciclosporin is taken twice daily, typically every 12 hours.
- The oral solution should be diluted with orange or apple juice (not grapefruit juice) and taken with a meal for better absorption.
- Blood levels are monitored regularly to adjust dosage and avoid toxicity, especially in transplant patients.
- Common side effects include high blood pressure, kidney issues, tremor, and increased hair growth.
- Treatment duration varies: short-term (up to 1 year) for psoriasis, lifelong for transplants.
About immunosuppressants
Immunosuppressants like ciclosporin weaken the immune response to prevent rejection of transplanted organs or control overactive immunity in autoimmune diseases. Ciclosporin specifically targets T-cells by binding to cyclophilin, forming a complex that inhibits calcineurin phosphatase. This blocks dephosphorylation of NF-AT, preventing transcription of IL-2 and other cytokines essential for T-cell activation and proliferation.
Unlike broader immunosuppressants like corticosteroids, ciclosporin is steroid-sparing, primarily affecting cell-mediated immunity while sparing humoral immunity to some extent.
What is ciclosporin used for?
Ciclosporin is FDA-approved for preventing rejection in kidney, liver, heart, and bone marrow transplants, often combined with corticosteroids and azathioprine. It treats severe rheumatoid arthritis unresponsive to methotrexate, severe plaque psoriasis not controlled by other therapies (PUVA, retinoids), and nephrotic syndrome. Off-label uses include Crohn’s disease, eczema, and dry eye (as eye drops like Restasis).
| Condition | Typical Use | Evidence Level |
|---|---|---|
| Organ Transplant Rejection (kidney, liver, heart) | Prolongs allograft survival | FDA-approved |
| Rheumatoid Arthritis | Severe cases post-methotrexate failure | FDA-approved |
| Plaque Psoriasis | Severe, refractory to other treatments | FDA-approved |
| Nephrotic Syndrome | Steroid-dependent/resistant | Approved |
| Graft-vs-Host Disease | Bone marrow transplant complication | Standard |
Dosage
Dosage is highly individualized based on blood levels (target trough 100-400 ng/mL depending on transplant type), body weight, and response. For transplants, initial oral dose is 4-12 hours pre-op: kidney/liver 15 mg/kg/day (divided BID), heart 7-14 mg/kg/day. Maintenance reduces gradually.
For rheumatoid arthritis: 2.5 mg/kg/day BID, max 4 mg/kg/day. Psoriasis: 2.5 mg/kg/day, up to 4 mg/kg/day for 12 weeks max, then taper.
- Adults/Children (transplants): Neoral dose adjusted by doctor; often starts high, tapers over months.
- Missed dose: Take as soon as remembered unless near next dose; do not double up.
- Switching formulations: Requires blood level monitoring; Neoral not bioequivalent to Sandimmune.
How and when to take ciclosporin
Take consistently with respect to meals and time of day for stable absorption. Swallow capsules whole; mix oral solution with 30-150 mL of room-temperature orange/apple juice, stir vigorously, drink immediately, then rinse glass with more juice and drink. Avoid grapefruit/grapefruit juice (increases levels).
For best absorption: Take with food, but consistently. Use same juice type daily. Do not store diluted solution.
Using ciclosporin eye drops
Ophthalmic formulations (Restasis, Cequa, Verkazia) treat dry eyes (keratoconjunctivitis sicca) from Sjögren’s or post-surgery. Instill 1 drop BID in each eye, 12 hours apart. Remove contact lenses before use; wait 15 min to reinsert. May cause temporary burning.
Side-effects of ciclosporin
Common side effects (>10%): tremor, hirsutism, hypertension, gum hyperplasia, nausea. Serious: nephrotoxicity (monitor creatinine), hepatotoxicity, lymphoma risk, infections due to immunosuppression.
| Very Common (>10%) | Common (1-10%) | Serious (Report Immediately) |
|---|---|---|
| High BP, kidney dysfunction, tremor, excess hair | Headache, acne, abdominal pain, diarrhea | Seizures, vision changes, severe infection, cancer signs |
Manage hypertension with diet/exercise; gingival hyperplasia with dental hygiene.
Pregnancy and breastfeeding with ciclosporin
Limited data; category C. Use only if benefits outweigh risks. Monitor infant if breastfeeding (low levels in milk). Contraception advised.
Other medicines, food and drink with ciclosporin – interactions
Food: Grapefruit increases levels (avoid); potassium-rich foods if on K-sparing diuretics.
Drugs: Interacts with CYP3A4 inhibitors (keto/azoles, erythromycin ↑ levels), inducers (rifampin ↓ levels), statins (rhabdo risk), NSAIDs (nephrotoxicity).
- Do not take with tacrolimus/sirolimus without monitoring.
- Live vaccines contraindicated.
Common questions about ciclosporin
Why do I need blood tests?
To monitor levels (trough 12 hours post-dose), kidney/liver function, BP, lipids, due to narrow therapeutic index and toxicity risk.
How long until it works?
Transplants: immediate effect. Arthritis/psoriasis: 4-8 weeks.
Can I drink alcohol?
Limit; may worsen liver/kidney effects.
Does it cause cancer?
Increased risk (skin/lymphoma); use sunscreen, avoid sun.
Can I stop suddenly?
No; taper under doctor supervision to avoid rejection.
Frequently Asked Questions (FAQs)
Q: What is the main use of ciclosporin?
A: Primarily to prevent organ transplant rejection by suppressing T-cell activity.
Q: Is Neoral the same as Sandimmune?
A: No, Neoral has better bioavailability; doses not interchangeable without monitoring.
Q: What are the most serious side effects?
A: Kidney damage, high blood pressure, infections, and malignancies require regular monitoring.
Q: Can children take ciclosporin?
A: Yes, for transplants; dose by weight, monitored closely.
Q: How does ciclosporin work?
A: Inhibits calcineurin, blocking IL-2 production in T-cells.
References
- Ciclosporin – Wikipedia — Wikipedia. 2023-10-01. https://en.wikipedia.org/wiki/Ciclosporin
- Neoral FDA Label — U.S. Food and Drug Administration. 2009-05-14. https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/050715s028,050716s029lbl.pdf
- Cyclosporine (oral route) – Mayo Clinic — Mayo Clinic. 2023. https://www.mayoclinic.org/drugs-supplements/cyclosporine-oral-route/description/drg-20075815
- Cyclosporine: Uses, Interactions | DrugBank — DrugBank. 2023. https://go.drugbank.com/drugs/DB00091
- Cyclosporine (Sandimmune, Neoral) – CHP — Children’s Hospital of Pittsburgh. 2023. https://www.chp.edu/our-services/transplant/liver/education/medications/cyclosporine-sandimmune-neoral
- Cyclosporine Capsules – Cleveland Clinic — Cleveland Clinic. 2023. https://my.clevelandclinic.org/health/drugs/19532-neoral-or-gengraf-cyclosporine-oral-capsule
- Cyclosporine – MedlinePlus — MedlinePlus (NIH). 2023-06-15. https://medlineplus.gov/druginfo/meds/a601207.html
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