What it does
Cyclosporine is a medication that helps to suppress the immune system.
Commonly used for: prevention of organ transplant rejection, treatment of autoimmune diseases like rheumatoid arthritis and psoriasis
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
Ask about this medicine
Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.
Hard to find? We help patients in Kenya source rare medicines. We don't sell or dispense medicines - licensed pharmacies do.
Source this medicineRegistration & product details
Source: Pharmacy and Poisons Board · fetched 2026-01-28 21:10:12 · updated 2026-07-20 08:53:20
About this medicine
Cyclosporine is a medication that helps to suppress the immune system.
What it treats
- prevention of organ transplant rejection
- treatment of autoimmune diseases like rheumatoid arthritis and psoriasis
How it works
It works by reducing the activity of the immune system to prevent it from attacking its own body or a transplanted organ.
Who it's for
It is for people who have had an organ transplant or those with certain autoimmune conditions.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: cyclospoirne
Cyclosporine is an immunosuppressant medication primarily used to prevent organ transplant rejection and to treat various autoimmune disorders. It is a peptide derived from the fungus Tolypocladium inflatum and acts by inhibiting T-lymphocyte activation. Cyclosporine has been a cornerstone in transplant medicine since its introduction, significantly improving graft survival rates.
Indications
- Prevention of organ transplant rejection
- Rheumatoid arthritis
- Psoriasis
- Nephrotic syndrome
- Autoimmune hepatitis
- Uveitis
Dosage
Children: Refer to the BNF for Children for appropriate dosing information based on age, weight, and specific condition.
Adults: Refer to the specific guidelines for dosing based on the condition being treated, as doses can vary significantly depending on the indication and individual patient factors.
Mechanism of action
Cyclosporine works by binding to cyclophilin, a cytosolic protein. This complex then inhibits calcineurin, a serine/threonine phosphatase that activates T-cell transcription factors, particularly nuclear factor of activated T-cells (NFAT). The inhibition of NFAT prevents the transcription of interleukin-2 (IL-2) and other cytokines essential for T-cell proliferation and activation, thus suppressing the immune response.
Pharmacodynamics
Cyclosporine is effective in reducing immune responses and preventing graft rejection. Its immunosuppressive effects are dose-dependent, with higher doses leading to more significant suppression of T-cell function. The drug also has a variable pharmacological response among individuals, influenced by genetic factors and concurrent medications.
Pharmacokinetics
Cyclosporine is administered orally or intravenously and is highly lipophilic. It is approximately 90% absorbed after oral administration, but its bioavailability can be significantly affected by food and gastrointestinal motility. The drug is extensively metabolized by the liver via cytochrome P450 enzymes, particularly CYP3A4, with a half-life ranging from 8 to 12 hours. Renal excretion is the primary route of elimination for cyclosporine, with 0.1% excreted unchanged in urine.
Contra-indications
- Hypersensitivity to cyclosporine or any of its components
- Uncontrolled hypertension
- Malignancies or active infections
- Concurrent use with certain hepatotoxic drugs
Adverse effects
- Nephrotoxicity
- Hypertension
- Gingival hyperplasia
- Hirsutism
- Neurotoxicity including tremors and seizures
- Increased risk of infections
- Nausea and vomiting
- Diarrhea
Interactions
- Increased risk of nephrotoxicity with NSAIDs
- Grapefruit juice can increase cyclosporine levels
- CYP3A4 inhibitors may increase cyclosporine levels
- CYP3A4 inducers may decrease cyclosporine levels
- Additive immunosuppressive effects with other immunosuppressants
Precautions
- Monitor renal function regularly during treatment
- Assess blood pressure periodically
- Use with caution in patients with liver impairment
- Avoid live vaccines during therapy
Pregnancy
Cyclosporine is categorized as FDA pregnancy category C. It should only be used if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
Cyclosporine is excreted in breast milk. Caution should be exercised when administering to nursing mothers.
Storage
Store in a cool, dry place away from light. Keep out of reach of children.
Formulations
- Capsules
- Oral solution
- Injection
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.