Cyclosporine is a calcineurin inhibitor immunosuppressant used to prevent organ transplant rejection and to treat immune‑mediated conditions such as psoriasis, rheumatoid arthritis, nephrotic syndrome, and chronic dry eye (ophthalmic drops). By blocking T‑cell activation and interleukin‑2 transcription, it lowers harmful immune activity. Available as oral capsules/solution (modified and non‑modified) and ophthalmic emulsions, cyclosporine requires careful dosing and monitoring of trough levels, kidney function, blood pressure, electrolytes, and lipids. Important risks include nephrotoxicity, hypertension, infection, and lymphoma/skin cancer with long‑term use. Patients should review interactions, avoid grapefruit, and follow a consistent brand/formulation under clinician supervision. Sun protection is strongly recommended too.
Cyclosporine (also spelled cyclosporin) is a calcineurin inhibitor that suppresses T‑lymphocyte activation, reducing interleukin‑2 and other cytokines. Systemically, it is used to prevent and treat rejection in kidney, liver, and heart transplantation, often in combination with corticosteroids and other immunosuppressants. In non‑transplant settings, oral cyclosporine treats moderate‑to‑severe plaque psoriasis and active rheumatoid arthritis when patients have not responded adequately to other therapies. It is also used for certain cases of nephrotic syndrome to reduce proteinuria and preserve kidney function under specialist care.
Ophthalmic cyclosporine emulsions (for example, 0.05% and 0.09% formulations) are prescribed for chronic dry eye disease (keratoconjunctivitis sicca) to increase tear production when inflammation contributes to reduced tear quantity and quality. Unlike systemic use, topical ocular therapy acts locally on ocular surface inflammation with minimal systemic absorption.
Cyclosporine is available as non‑modified (Sandimmune) and modified microemulsion formulations (Neoral, Gengraf, and generics). These are not interchangeable on a milligram‑for‑milligram basis due to differences in absorption. If switching formulations or brands, a clinician should adjust dosing and monitor blood levels. In transplant recipients, initial oral doses commonly range from 5–10 mg/kg/day in two divided doses, then are titrated to target trough concentrations and the patient’s clinical status. For rheumatoid arthritis and psoriasis, lower doses are used (for example, 2.5–4 mg/kg/day in divided doses), balancing efficacy with safety and renal monitoring.
Administer oral cyclosporine consistently with regard to meals to reduce variability in absorption. Swallow capsules whole. For oral solution, mix in glass (not polystyrene) with room‑temperature orange or apple juice per product instructions and drink immediately; rinse the glass to ensure the full dose is consumed. Avoid grapefruit or grapefruit juice, which can markedly increase cyclosporine levels.
Ophthalmic cyclosporine is typically instilled as one drop in each affected eye twice daily, about 12 hours apart. Remove contact lenses before use and wait at least 15 minutes before reinserting lenses or using other eye drops. Benefits in dry eye often appear after several weeks; continue as directed unless a clinician advises otherwise.
Cyclosporine carries boxed warnings for serious infections and malignancies due to immunosuppression, as well as for hypertension and nephrotoxicity. Use the lowest effective dose and monitor regularly. Key labs include cyclosporine trough levels (for systemic therapy), serum creatinine and eGFR, liver enzymes, electrolytes (potassium and magnesium), fasting lipids, and uric acid. Blood pressure should be checked frequently, particularly after dose changes. Report reduced urine output, swelling, shortness of breath, severe fatigue, or persistent fever promptly.
Sun protection is essential. Cyclosporine increases the risk of skin cancers, especially with prior phototherapy. Use broad‑spectrum sunscreen, wear protective clothing, and avoid tanning beds. Vaccination response may be blunted; live vaccines are generally avoided during systemic immunosuppression. Discuss immunization plans before starting therapy. People with a history of malignancy, uncontrolled hypertension, or significant renal impairment require extra caution and specialist oversight.
Pregnancy and lactation require individualized risk‑benefit assessment. Cyclosporine has been used during pregnancy in transplant patients under careful monitoring, but potential risks exist; effective contraception is advised if pregnancy is not planned. Small amounts pass into breast milk—discuss feeding plans with your clinician. Older adults and those with hepatic impairment may be more susceptible to adverse effects and often need closer monitoring.
Do not use cyclosporine in anyone with a known hypersensitivity to cyclosporine or any component of the formulation. For psoriasis, systemic cyclosporine is contraindicated in uncontrolled hypertension, abnormal renal function, or a history of malignancy, and it should not be combined with PUVA, UVB, methotrexate, or other immunosuppressive antimetabolites due to additive toxicity. Active serious infections are a reason to defer systemic therapy until adequately treated.
For ophthalmic cyclosporine, avoid use in active ocular infections, and discontinue if severe eye pain, marked vision changes, or intense inflammation occurs; seek prompt ophthalmic evaluation. Always verify suitability if you have had prior ocular surgery or wear contact lenses.
Common systemic side effects include tremor, headache, hypertension, hirsutism, and gingival hyperplasia. Gastrointestinal effects such as nausea, abdominal discomfort, and diarrhea can occur, especially early in therapy. Metabolic changes are frequent: hyperlipidemia, hyperuricemia (with gout flares), hyperkalemia, and hypomagnesemia. Many effects are dose‑related and may improve with dose adjustments.
Serious adverse reactions require urgent attention: nephrotoxicity (rising creatinine, decreased urine output), severe hypertension, opportunistic infections (fever, cough, chills), neurotoxicity (confusion, seizures, visual disturbances, posterior reversible encephalopathy syndrome), hepatotoxicity (jaundice, dark urine), and thrombotic microangiopathy. Long‑term use increases malignancy risk, particularly lymphomas and skin cancers; routine skin checks and avoidance of excessive UV exposure are vital.
Ophthalmic cyclosporine may cause temporary eye burning or stinging upon instillation, conjunctival redness, itching, or blurred vision. These are usually mild and transient. Discontinue and seek care if you develop intense ocular pain, purulent discharge, marked swelling, or signs of infection.
Cyclosporine is a substrate of CYP3A4 and P‑glycoprotein. Strong inhibitors can raise cyclosporine levels and toxicity risk: macrolide antibiotics (erythromycin, clarithromycin), azole antifungals (ketoconazole, itraconazole, voriconazole, fluconazole), certain calcium channel blockers (diltiazem, verapamil), protease inhibitors, and grapefruit products. Potent inducers can lower levels and efficacy: rifampin, rifabutin, carbamazepine, phenytoin, phenobarbital, and the herbal supplement St. John’s wort. Always inform your clinician about all medicines and supplements, including over‑the‑counter products.
Additive nephrotoxicity is a major concern. Combining cyclosporine with aminoglycosides, amphotericin B, high‑dose NSAIDs, tacrolimus, or iodinated contrast increases the risk of kidney injury. Concomitant use with potassium‑sparing diuretics, ACE inhibitors, or ARBs can raise potassium levels; monitor electrolytes closely. Cyclosporine can elevate exposure to certain statins (especially simvastatin, lovastatin, and atorvastatin), increasing myopathy/rhabdomyolysis risk—lower statin doses or alternative agents may be required.
Other notable interactions include colchicine (risk of neuromyopathy), digoxin (toxicity), and oral contraceptives (possible increased levels). Vaccines may be less effective during systemic immunosuppression; live vaccines are generally avoided. For ophthalmic cyclosporine, wait at least 15 minutes between different eye drops to prevent washout and interactions with tear film dynamics.
If you miss an oral cyclosporine dose, take it as soon as you remember unless it is close to the next scheduled dose. Do not double up to make up for a missed dose. Resume your regular schedule. For ophthalmic drops, instill the missed dose when remembered, then continue with the next dose at the usual time. If you miss multiple doses, contact your healthcare professional for guidance.
Signs of cyclosporine overdose may include severe tremor, confusion, vomiting, dizziness, marked hypertension, electrolyte disturbances, and worsening kidney function (reduced urine output). There is no specific antidote. Management is supportive, with close monitoring of vitals, renal function, electrolytes, and cyclosporine concentrations. Due to high protein binding, hemodialysis has limited benefit. If an overdose is suspected, contact your local poison control center or seek emergency care immediately. Do not attempt to induce vomiting unless instructed by a medical professional.
Store oral cyclosporine at room temperature, away from excessive heat and moisture, and keep the bottle tightly closed. Follow the package insert for specific instructions for capsules versus solution; do not refrigerate the microemulsion unnecessarily, and avoid storing the solution in polystyrene containers. Keep ophthalmic emulsions at recommended room temperature; do not freeze. For single‑use vials, discard any remaining contents immediately after one use. Keep all medications out of reach of children and pets.
In the United States, cyclosporine (oral and ophthalmic) is a prescription medication. Federal and state regulations require that dispensing occurs pursuant to a valid prescription issued after an appropriate medical evaluation, with ongoing monitoring for safety. Purchasing cyclosporine from unverified sources or without clinical oversight risks counterfeit products, unsafe dosing, dangerous interactions, and legal consequences.
HealthSouth Rehabilitation Hospital of Las Vegas offers a legal and structured solution for acquiring cyclosporine without a formal pre‑existing prescription by connecting you with licensed clinicians through a compliant, telehealth‑style review. Your medical history, current medications, and necessary monitoring are assessed, a prescription is issued when appropriate, and the pharmacy dispenses accordingly. This integrated pathway features identity verification, pharmacist support, transparent pricing, and shipping only where permitted—providing convenience without compromising U.S. safety and regulatory standards.
Cyclosporine is a calcineurin inhibitor that suppresses T‑cell activation by blocking calcineurin‑NFAT signaling and reducing interleukin‑2 production, thereby lowering immune responses that drive transplant rejection and certain autoimmune diseases.
It is used to prevent organ transplant rejection and to treat severe psoriasis and rheumatoid arthritis when other therapies fail; ophthalmic cyclosporine treats chronic dry eye disease, and systemic cyclosporine is sometimes used off‑label for severe atopic dermatitis and refractory nephrotic syndrome.
Systemic formulations include Sandimmune (non‑modified) and Neoral/Gengraf (modified microemulsion); ophthalmic drops include Restasis and Cequa, which are topical cyclosporine for dry eye.
It is taken at the same times each day with consistent relation to food; clinicians monitor trough blood levels, kidney function (serum creatinine), blood pressure, electrolytes (potassium, magnesium), and lipids to balance efficacy and safety.
Common risks include nephrotoxicity, hypertension, tremor, headache, hyperkalemia, hypomagnesemia, hyperlipidemia, hirsutism, and gingival hyperplasia; serious risks include infections and malignancies (especially skin cancer and lymphoma), and rarely neurotoxicity.
For psoriasis and atopic dermatitis, improvement often appears within 2–4 weeks; for rheumatoid arthritis, 4–8 weeks; for dry eye with ophthalmic drops, benefits may take 1–3 months, with full effect by 3–6 months.
No, non‑modified Sandimmune and modified microemulsion products (Neoral/Gengraf) are not bioequivalent; switching requires prescriber oversight and re‑titration with therapeutic drug monitoring.
Cyclosporine is a CYP3A4 and P‑glycoprotein substrate; levels rise with azole antifungals, macrolides, diltiazem/verapamil, and grapefruit, and fall with rifampin, carbamazepine, phenytoin, and St John’s wort; avoid nephrotoxins (NSAIDs, aminoglycosides), limit certain statins, avoid colchicine, and be cautious with potassium‑sparing agents.
It is contraindicated in uncontrolled hypertension, malignancy, active serious infection, and abnormal renal function for psoriasis or RA indications; use only under experienced clinicians in transplant recipients due to boxed warnings for infection, malignancy, and nephrotoxicity.
Routine checks include serum creatinine/BUN, blood pressure, cyclosporine trough levels, potassium, magnesium, fasting lipids, liver enzymes, and sometimes uric acid; skin exams are recommended due to increased skin cancer risk.
Avoid live vaccines; inactivated vaccines are generally safe but may be less effective, so timing relative to drug initiation and boosters may be adjusted.
Cyclosporine is used in pregnancy when benefits outweigh risks (e.g., transplant), but may be associated with prematurity and low birth weight; it passes into breast milk, so breastfeeding requires individualized risk‑benefit discussion with specialists.
Take it as soon as you remember unless it is near the next dose; do not double up, and contact your clinician if multiple doses are missed or if you vomit soon after a dose.
Use the lowest effective dose, attend regular monitoring, control blood pressure and lipids, avoid interacting drugs and grapefruit, practice sun protection, and report new neurologic symptoms or signs of infection promptly.
Temporary burning or stinging, eye redness, and blurred vision can occur; remove contact lenses before use and wait at least 15 minutes before reinsertion.
Both are calcineurin inhibitors; many centers prefer tacrolimus for slightly lower acute rejection rates, while cyclosporine remains a valid option in selected patients based on side‑effect profiles and comorbidities.
Both can cause dose‑related nephrotoxicity; careful therapeutic drug monitoring is essential, with dose adjustments based on creatinine trends and trough levels.
Tacrolimus is more diabetogenic, increasing the risk of new‑onset diabetes after transplant; cyclosporine more commonly raises lipids and blood pressure.
Cyclosporine is associated with hirsutism and gingival hyperplasia, while tacrolimus is more often linked to alopecia; both can cause tremor.
Both are CYP3A substrates affected by azoles, macrolides, rifampin, and grapefruit; cyclosporine more strongly inhibits P‑glycoprotein and can raise levels of drugs like certain statins and colchicine, requiring extra caution.
Both use trough level monitoring, renal function, and blood pressure; some centers also use cyclosporine C2 (two‑hour post‑dose) levels to guide dosing, whereas tacrolimus typically relies on troughs alone.
Voclosporin is a cyclosporine analog approved with mycophenolate for lupus nephritis; it has more predictable pharmacokinetics without routine therapeutic drug monitoring, but carries similar risks of nephrotoxicity, hypertension, and CYP3A‑mediated interactions.
Both can reduce GFR; voclosporin may cause an early, reversible decline in eGFR, necessitating close monitoring, while classic cyclosporine nephrotoxicity is dose‑related and cumulative—choice depends on indication and individual risk.
Pimecrolimus cream is a topical calcineurin inhibitor for mild‑to‑moderate atopic dermatitis with a favorable safety profile; systemic cyclosporine is reserved for severe, refractory cases and requires intensive monitoring for systemic toxicity.
Both inhibit calcineurin; ophthalmic cyclosporine is approved for dry eye, while topical tacrolimus (often used off‑label) may help severe allergic keratoconjunctivitis when cyclosporine is inadequate; tolerability and access often guide choice.
Modified microemulsions (Neoral/Gengraf) have more consistent absorption than non‑modified Sandimmune, reducing variability; they are not directly interchangeable without careful supervision.
Hypertension is more common and often more pronounced with cyclosporine; both require blood pressure control and lifestyle measures.
Both can cause tremor, headache, and paresthesias; tacrolimus is more often linked to severe neurotoxicity such as confusion or seizures at high levels, underscoring the need for level monitoring and dose adjustments.