Ciclosporin (Cyclosporine)
Immunosuppressant — Calcineurin Inhibitor
Quick Facts About Ciclosporin
Key Takeaways About Ciclosporin
- Prevents organ rejection: Ciclosporin is a cornerstone immunosuppressant used after kidney, liver, heart, and bone marrow transplantation to prevent the body from attacking the transplanted tissue
- Treats severe autoimmune diseases: Effective for severe psoriasis, atopic dermatitis, rheumatoid arthritis, uveitis, and nephrotic syndrome when other treatments have failed
- Requires regular monitoring: Blood pressure, kidney function, and ciclosporin blood levels must be checked regularly due to the risk of nephrotoxicity and hypertension
- Many drug interactions: Ciclosporin interacts with a large number of medications; never start or stop any medicine without consulting your doctor. Avoid grapefruit and St. John's wort
- Increased infection and cancer risk: Because it suppresses the immune system, ciclosporin increases susceptibility to infections and certain cancers, especially skin cancer and lymphoma. Sun protection is essential
What Is Ciclosporin and What Is It Used For?
Ciclosporin is an immunosuppressant medication belonging to the calcineurin inhibitor class. It works by selectively suppressing the immune system to prevent organ rejection after transplantation and to treat severe autoimmune conditions where the body's immune system attacks its own tissues.
Ciclosporin (internationally also known as cyclosporine or ciclosporin A) was first isolated from the fungus Tolypocladium inflatum in the 1970s and revolutionised transplant medicine by dramatically improving survival rates for organ transplant recipients. It remains one of the most important immunosuppressive agents in clinical use worldwide and is included on the WHO Model List of Essential Medicines.
The medication works by binding to an intracellular protein called cyclophilin, forming a complex that inhibits calcineurin — a key enzyme in T-lymphocyte activation. By blocking the production of interleukin-2 (IL-2) and other pro-inflammatory cytokines, ciclosporin selectively dampens the adaptive immune response without completely eliminating immune function. This selective mechanism makes it particularly valuable in transplant medicine and autoimmune disease management.
Transplant rejection prevention
If you have received an organ transplant (kidney, liver, heart, lung, or pancreas) or undergone bone marrow or stem cell transplantation, ciclosporin is used to control your immune system and prevent rejection. The body naturally recognises transplanted tissue as foreign and mounts an immune attack against it. Ciclosporin blocks this response by preventing T-cells from developing and attacking the transplanted organ, allowing the graft to survive and function normally.
Autoimmune disease treatment
In autoimmune diseases, the immune system mistakenly attacks the body's own cells and tissues. Ciclosporin can halt this inappropriate immune response and is approved for several severe autoimmune conditions:
- Endogenous uveitis — Severe inflammatory eye disease that threatens vision, including Behçet's uveitis
- Severe atopic dermatitis (eczema) — When conventional therapies have failed to provide adequate relief
- Severe psoriasis — For patients who do not respond to or are intolerant of other systemic treatments
- Severe rheumatoid arthritis — Particularly when conventional disease-modifying drugs are insufficient
- Nephrotic syndrome — A kidney disorder characterised by excessive protein loss in the urine
Ophthalmic uses
Ciclosporin is also available as eye drops (brands include IKERVIS and Verkazia) for treating severe dry eye disease (keratoconjunctivitis sicca) and vernal keratoconjunctivitis. The ophthalmic formulation acts locally on the eye surface to reduce inflammation without the systemic side effects associated with oral ciclosporin.
Ciclosporin should only be prescribed by physicians experienced in transplant medicine or the management of autoimmune diseases. The advice in this article is general — always follow your prescribing physician's specific instructions, as they may differ based on your individual condition.
What Should You Know Before Taking Ciclosporin?
Before taking ciclosporin, your doctor must be informed about all your medical conditions, allergies, and other medications. Ciclosporin must not be combined with St. John's wort, dabigatran, bosentan, or aliskiren. Special caution is needed in patients with kidney problems, high blood pressure, infections, or a history of cancer.
Ciclosporin is a potent medication with significant potential for serious side effects and drug interactions. Your prescribing physician will carefully weigh the benefits against the risks before starting treatment. Thorough medical assessment including blood tests, blood pressure measurement, and kidney function evaluation is required before initiating therapy.
Contraindications
You must not take ciclosporin in the following situations:
- Allergy to ciclosporin or any of the other ingredients in the formulation
- Concurrent use of St. John's wort (Hypericum perforatum), which dramatically reduces ciclosporin levels
- Concurrent use of dabigatran etexilate (an anticoagulant used to prevent blood clots)
- Concurrent use of bosentan (used to treat pulmonary arterial hypertension)
- Concurrent use of aliskiren (used to treat high blood pressure)
If you are prescribed ciclosporin for an autoimmune condition (not transplant-related), you must additionally not take it if you have:
- Kidney problems (except nephrotic syndrome patients, where careful monitoring is applied)
- An active, uncontrolled infection
- Any type of cancer or a history of malignancy
- Uncontrolled high blood pressure that does not respond to antihypertensive treatment
Warnings and Precautions
Before and during treatment with ciclosporin, inform your doctor immediately if any of the following apply:
- Signs of infection (fever, sore throat, unusual fatigue) — ciclosporin weakens the immune system and impairs the body's ability to fight infections
- Liver problems — dose adjustment may be necessary
- Kidney problems — regular blood tests are required, and dose modification may be needed
- High blood pressure — blood pressure will be monitored regularly and antihypertensive treatment may be added
- Low magnesium levels — supplementation may be required, especially after surgery
- High potassium levels — dietary adjustments may be needed
- Gout — ciclosporin can raise uric acid levels
- Planned vaccinations — live vaccines should be avoided during treatment
Ciclosporin suppresses the immune system and significantly increases the risk of developing cancers, particularly skin cancer and lymphoma. You must limit your exposure to sunlight and UV radiation by wearing protective clothing and frequently applying high-SPF sunscreen. Regular skin examinations are recommended throughout treatment and afterwards.
Pregnancy and Breastfeeding
Ciclosporin should generally not be taken during pregnancy due to limited safety data. However, in transplant recipients where stopping the medication poses a serious risk to the mother's health or graft survival, your doctor will discuss the potential benefits versus risks with you. Animal studies have shown adverse effects on reproduction, although the relevance to humans is uncertain.
Breastfeeding is not recommended during ciclosporin treatment. The active substance passes into breast milk and could affect the nursing infant's immune system. If you are breastfeeding or planning to breastfeed, discuss alternative treatment options with your doctor.
Ciclosporin may cause drowsiness, disorientation, or blurred vision. Exercise caution when driving or operating machinery until you know how this medication affects you. The oral formulation contains a small amount of ethanol (alcohol), though this is unlikely to cause noticeable effects at therapeutic doses.
Monitoring during treatment
Your doctor will regularly check:
- Ciclosporin blood levels — especially important after transplantation and when starting or stopping other medications
- Blood pressure — before starting treatment and at regular intervals
- Kidney function — through blood tests (serum creatinine) to detect nephrotoxicity early
- Liver function — through liver enzyme blood tests
- Blood lipid levels — ciclosporin can elevate cholesterol and triglycerides
- Potassium and magnesium levels — electrolyte imbalances are common
How Does Ciclosporin Interact with Other Drugs?
Ciclosporin has extensive drug interactions. Many common medications can increase or decrease ciclosporin blood levels, potentially leading to toxicity or treatment failure. Some combinations are strictly contraindicated. Always inform your doctor about all medications, supplements, and herbal products you take.
Drug interactions with ciclosporin are clinically very significant because the drug has a narrow therapeutic index — meaning the difference between an effective dose and a toxic dose is small. Changes in ciclosporin blood levels can lead to either organ rejection (if levels drop too low) or serious side effects including kidney damage (if levels rise too high). Ciclosporin is primarily metabolised by the cytochrome P450 3A4 (CYP3A4) enzyme system and is a substrate for P-glycoprotein, which explains many of its interactions.
Drugs that increase ciclosporin levels
The following medications can raise ciclosporin blood levels, increasing the risk of side effects:
| Drug Category | Examples | Clinical Significance |
|---|---|---|
| Macrolide antibiotics | Erythromycin, azithromycin | Major — monitor levels closely |
| Antifungals | Voriconazole, itraconazole | Major — significant level increase |
| Calcium channel blockers | Diltiazem, verapamil, nicardipine | Major — dose adjustment likely needed |
| HIV protease inhibitors | Ritonavir, saquinavir | Major — substantial level increase |
| Other | Oral contraceptives, danazol, metoclopramide, amiodarone, allopurinol, cannabidiol, colchicine | Moderate to major — monitoring required |
Drugs that decrease ciclosporin levels
The following medications can lower ciclosporin blood levels, potentially leading to treatment failure or organ rejection:
| Drug Category | Examples | Clinical Significance |
|---|---|---|
| Anticonvulsants | Carbamazepine, phenytoin, barbiturates | Major — significant level reduction |
| Anti-TB drugs | Rifampicin, isoniazid | Major — can reduce levels by 50-80% |
| Herbal products | St. John's wort (Hypericum perforatum) | Contraindicated — must not be combined |
| Other | Octreotide, orlistat, ticlopidine, terbinafin, bosentan | Moderate to major — monitoring required |
Nephrotoxic drug combinations
Special caution is required when ciclosporin is used with other medications that can affect the kidneys, as the combination may increase the risk of kidney damage:
- Aminoglycoside antibiotics (gentamicin, tobramycin)
- Amphotericin B (antifungal)
- NSAIDs (diclofenac, ibuprofen) — non-steroidal anti-inflammatory drugs
- Ciprofloxacin and trimethoprim
- Tacrolimus — combined use significantly increases nephrotoxicity risk
- Melphalan (cancer chemotherapy agent)
- Fibrates (used to lower blood lipids)
Do not take ciclosporin with grapefruit or grapefruit juice. Grapefruit inhibits CYP3A4 enzymes in the intestinal wall, which can significantly increase ciclosporin absorption and blood levels, raising the risk of kidney damage and other side effects.
Other important interactions
Ciclosporin can also affect the levels and effects of other drugs you take. Medications whose levels may be increased by ciclosporin include:
- Digoxin (heart medication)
- Statins (cholesterol-lowering drugs) — increased risk of muscle damage (rhabdomyolysis)
- Prednisolone (corticosteroid)
- Repaglinide (diabetes medication)
- Mycophenolate (immunosuppressant)
- Methotrexate — increased levels and toxicity risk
Nifedipine, when taken concurrently with ciclosporin, may cause gingival overgrowth (swollen gums growing over the teeth). This is a well-documented interaction and good oral hygiene is particularly important if you take both medications.
What Is the Correct Dosage of Ciclosporin?
Ciclosporin dosage is carefully individualised by your doctor based on your body weight, the condition being treated, and your blood levels. Doses are always divided into two daily doses taken 12 hours apart. Never change your dose without medical supervision.
The dose of ciclosporin varies considerably depending on whether it is used for transplant rejection prevention or autoimmune disease treatment. Your doctor will use blood level monitoring (therapeutic drug monitoring) to fine-tune the dose, aiming for the lowest effective level that prevents rejection or controls disease activity while minimising side effects. It is critically important to take the medication at the same times each day, as consistent timing ensures stable blood levels.
Adults — Transplant Indications
Organ, Bone Marrow, or Stem Cell Transplant
The total daily dose usually ranges from 2 mg to 15 mg per kilogram of body weight, divided into two equal doses. Higher doses are typically used before and immediately after transplantation, with gradual dose reduction once the transplanted organ or marrow has stabilised. Your doctor will adjust the dose based on blood level monitoring.
Adults — Autoimmune Conditions
| Condition | Total Daily Dose | Administration | Notes |
|---|---|---|---|
| Endogenous uveitis | 5–7 mg/kg/day | Divided into 2 doses | Until inflammation is controlled |
| Nephrotic syndrome | 5 mg/kg/day | Divided into 2 doses | Max 2.5 mg/kg/day if kidney impaired |
| Rheumatoid arthritis | 3–5 mg/kg/day | Divided into 2 doses | Start at 3 mg/kg/day, increase gradually |
| Psoriasis | 2.5–5 mg/kg/day | Divided into 2 doses | Typical treatment course: 8 weeks |
| Atopic dermatitis | 2.5–5 mg/kg/day | Divided into 2 doses | Typical treatment course: 8 weeks |
Children
In children, ciclosporin is primarily used for nephrotic syndrome and organ transplantation. For nephrotic syndrome, the recommended total daily dose for children is 6 mg per kilogram of body weight, divided into two doses. If the child has kidney impairment, the starting dose should not exceed 2.5 mg/kg/day. Ciclosporin should generally not be given to children for non-transplant indications other than nephrotic syndrome.
Elderly Patients (65 years and older)
Experience with ciclosporin in elderly patients is limited. Kidney function must be monitored particularly closely, as age-related decline in renal function increases the risk of nephrotoxicity. In patients over 65 with psoriasis or atopic dermatitis, ciclosporin should only be used for very severe disease that has not responded to other treatments.
Missed Dose
If you forget a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and continue with your regular schedule. Do not take a double dose to make up for a forgotten one. Consistent dosing is critical for maintaining therapeutic blood levels, especially after transplantation.
Overdose
If you take too much ciclosporin, or if a child accidentally ingests the medication, contact your doctor, hospital emergency department, or poison control centre immediately. Overdose can cause significant kidney damage and other serious effects. There is no specific antidote for ciclosporin overdose; treatment is supportive.
Your daily dose should always be divided into two doses, taken approximately 12 hours apart at the same times each day. Remove capsules from the blister pack only when you are ready to take them. Swallow capsules whole with water — do not crush or chew them. A characteristic odour when opening the blister is normal and does not indicate any problem with the capsules.
Continue taking ciclosporin even if you feel well. Stopping the medication without your doctor's guidance — especially after organ transplantation — can significantly increase the risk of organ rejection. Your doctor will advise you on how long treatment should continue and will manage any dose changes or discontinuation.
What Are the Side Effects of Ciclosporin?
Like all immunosuppressive medications, ciclosporin can cause side effects. The most common include kidney problems, high blood pressure, headache, tremor, and excessive hair growth. Serious side effects include increased susceptibility to infections and cancers (especially skin cancer and lymphoma). Regular monitoring helps detect and manage side effects early.
Not everyone who takes ciclosporin will experience side effects, and many side effects are dose-dependent — meaning they are more likely at higher doses. Your doctor will aim to use the lowest effective dose to minimise risks. It is important to report any new or worsening symptoms to your healthcare provider promptly, as early intervention can often prevent complications.
- Signs of severe infection (high fever, severe sore throat, persistent cough)
- Vision changes, confusion, seizures, or muscle weakness (possible brain infection or encephalopathy)
- Yellowing of skin or eyes, dark urine, or loss of appetite (possible liver damage)
- Significant reduction in urine output (possible severe kidney problems)
- Unusual bruising or bleeding, pale skin, extreme fatigue (possible blood disorders)
Side effects by frequency
Very Common
May affect more than 1 in 10 people
- Kidney problems (nephrotoxicity)
- High blood pressure (hypertension)
- Headache
- Uncontrollable tremor (shaking)
- Excessive body and facial hair growth (hirsutism)
- Elevated blood lipid levels (hyperlipidaemia)
Common
May affect up to 1 in 10 people
- Seizures
- Liver problems
- High blood sugar (hyperglycaemia)
- Fatigue
- Loss of appetite, nausea, vomiting, abdominal pain, diarrhoea
- Abnormal hair growth, acne, flushing
- Fever
- Low white blood cell count
- Numbness or tingling (paraesthesia)
- Muscle pain, muscle cramps
- Stomach ulcer
- Gum overgrowth (gingival hyperplasia)
- High uric acid or potassium, low magnesium in blood
Uncommon
May affect up to 1 in 100 people
- Encephalopathy symptoms (confusion, disorientation, seizures, vision disturbance)
- Skin rash
- Generalised swelling (oedema)
- Weight gain
- Low red blood cell or platelet count (anaemia, thrombocytopenia)
Rare to Very Rare
May affect up to 1 in 1,000 people or fewer
- Peripheral neuropathy (numbness, tingling in fingers and toes)
- Pancreatitis (severe upper abdominal pain)
- Muscle weakness, loss of muscle strength (myopathy)
- Haemolytic uraemic syndrome (breakdown of red blood cells with kidney problems)
- Menstrual cycle changes, breast enlargement in men
- Swelling in the back of the eye (papilloedema)
- Migraine or severe headache
- Hearing loss
- Pain in legs and feet
Infection and cancer risk
As with all immunosuppressive medications, ciclosporin can impair the body's ability to fight infections and may increase the risk of developing tumours or other cancers, particularly lymphoma and skin cancer. This is an inherent consequence of immune suppression and underlines the importance of using the lowest effective dose, practising sun protection, and attending regular medical check-ups. Progressive multifocal leukoencephalopathy (PML), a rare but serious brain infection, has been reported in patients taking immunosuppressants including ciclosporin.
Children and adolescents
No additional side effects are expected in children and adolescents compared with adults. However, children may be more susceptible to certain effects, and careful monitoring is equally important in the paediatric population.
How Should You Store Ciclosporin?
Store ciclosporin capsules below 25°C (77°F) in the original blister packaging. Keep out of reach and sight of children. Do not remove capsules from the blister until ready to take them. A characteristic smell when opening the blister is normal.
Proper storage of ciclosporin is important to ensure the medication remains effective throughout its shelf life. The capsules are moisture-sensitive, which is why they should be kept in the original blister packaging until use.
- Temperature: Store at or below 25°C (77°F). Do not store in warm places or near heat sources
- Packaging: Keep capsules in the original blister pack to protect from moisture
- Timing: Only remove capsules from the blister when it is time to take your medication
- Odour: A characteristic smell when opening the blister is normal and does not indicate any problem
- Expiry: Do not use after the expiry date printed on the packaging
- Disposal: Do not dispose of medicines via wastewater or household waste. Return unused medicines to your pharmacy for safe disposal
What Does Ciclosporin Contain?
Each ciclosporin capsule contains the active substance ciclosporin in doses of 10 mg, 25 mg, 50 mg, or 100 mg. The capsules also contain excipients including ethanol (alcohol), propylene glycol, and macrogolglycerol hydroxystearate.
Understanding the full composition of your medication is important, particularly if you have allergies to specific excipients or need to be aware of alcohol content.
Active substance
The active ingredient is ciclosporin. Each soft capsule contains 10 mg, 25 mg, 50 mg, or 100 mg of ciclosporin, depending on the formulation.
Excipients (inactive ingredients)
- Capsule contents: Alpha-tocopherol, anhydrous ethanol, propylene glycol, corn oil (mono-di-triglycerides), macrogolglycerol hydroxystearate (polyoxyl hydrogenated castor oil)
- Capsule shell: Titanium dioxide (E171), glycerol 85%, propylene glycol, gelatin. The 25 mg and 100 mg capsules also contain black iron oxide (E172)
- Capsule printing: Carmine (E120), aluminium chloride hexahydrate, sodium hydroxide, propylene glycol, hypromellose, isopropanol
Ciclosporin capsules contain a small amount of ethanol (alcohol), corresponding to approximately 11.8% by volume. A 500 mg dose contains approximately 500 mg of ethanol. This small amount is unlikely to produce noticeable effects in most patients. However, inform your doctor if you have alcohol-related health issues, epilepsy, or liver disease, or if this medication is being given to a child.
Macrogolglycerol hydroxystearate may cause stomach upset and diarrhoea. Propylene glycol is present in varying amounts per capsule. If your child is younger than 4 weeks old, consult your doctor or pharmacist before use, especially if the child takes other medications containing propylene glycol or alcohol. The capsules contain less than 1 mmol (23 mg) sodium per capsule, meaning they are essentially sodium-free.
Frequently Asked Questions About Ciclosporin
Medical References and Sources
This article is based on current medical research, international guidelines, and approved prescribing information. All claims are supported by scientific evidence from peer-reviewed sources.
- European Medicines Agency (EMA). "Ciclosporin — Summary of Product Characteristics." EMA Medicines Database European regulatory prescribing information for ciclosporin.
- World Health Organization (WHO). "WHO Model List of Essential Medicines, 23rd List (2023)." WHO Essential Medicines Ciclosporin is listed as an essential immunosuppressive medicine.
- British National Formulary (BNF). "Ciclosporin — Drug Monograph." BNF Drug Information Comprehensive UK prescribing guidance including indications, dosing, and interactions.
- U.S. Food and Drug Administration (FDA). "Cyclosporine — FDA Prescribing Information." FDA Drug Label U.S. regulatory prescribing information for cyclosporine.
- KDIGO (Kidney Disease: Improving Global Outcomes) (2024). "Clinical Practice Guideline for the Care of Kidney Transplant Recipients." International guidelines on immunosuppressive therapy in kidney transplantation.
- Griffiths CEM, et al. (2021). "Systemic therapies for psoriasis: A systematic review and network meta-analysis." British Journal of Dermatology. 185(2):280-291. Evidence for ciclosporin efficacy in severe psoriasis compared to other systemic treatments.
- Wollenberg A, et al. (2022). "European guideline for atopic eczema (EDF/EADV/EAA/ETFAD/EDF)." Journal of the European Academy of Dermatology and Venereology. European guidelines on the use of ciclosporin in severe atopic dermatitis.
Evidence grading: This article uses the GRADE framework (Grading of Recommendations Assessment, Development and Evaluation) for evidence-based medicine. Evidence level 1A represents the highest quality of evidence, based on systematic reviews of randomised controlled trials.
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