Cyclosporine
Also known as: CsA, Cyclosporin A, Gengraf, Neoral, Restasis, Sandimmun, Sandimmune
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Summary
Cyclosporine A is a cyclic undecapeptide immunosuppressant used to prevent organ transplant rejection and treat autoimmune conditions; it acts via calcineurin inhibition.
Mechanism of Action
Binds cyclophilin, forming a complex that inhibits calcineurin phosphatase activity, suppressing IL‑2 transcription and T‑cell activation
Routes of Administration
Goals & Uses
- Dry eye diseaseOphthalmologyHigh
- Plaque psoriasisDermatologyHigh
- Dry eye disease (topical)OphthalmologyHigh
- Nephrotic syndromeNephrologyModerate
- Rheumatoid arthritisAutoimmune DiseaseModerate
- Severe plaque psoriasisDermatologyModerate
- Organ transplant prophylaxisImmunosuppressionHigh
- Prevention of solid organ transplant rejectionImmunosuppressionHigh
- Atopic dermatitisDermatologyModerate
Contraindications
- Concurrent use of potassium-sparing diureticsDrug InteractionModerate
- Hypersensitivity to cyclosporineAllergyHigh
- Live vaccinesVaccinationModerate
- Active malignancy or history of malignancy (for non-transplant use)OncologyHigh
- Renal impairment (for non-transplant indications)RenalHigh
- Severe renal impairment (CrCl <30 mL/min)RenalHigh
- Hypersensitivity to cyclosporine or polyoxyethylated castor oil (IV formulation)AllergyHigh
- Uncontrolled hypertensionCardiovascularModerate
Adverse Effects
- HypertensionCardiovascularCommonHigh blood pressure
- HirsutismDermatologicCommon
- TremorNeurologicCommonInvoluntary shaking
- Increased infection riskImmunologicCommon
- Gingival hyperplasiaOralCommon
- Neurotoxicity (tremor, headache, paresthesia)NeurologicalCommon
- Increased risk of infection and malignancyImmunologicCommon
- NephrotoxicityRenalCommon
- HyperlipidemiaMetabolicCommon
Drug Interactions
- RifampinModerate
- CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's Wort)High
- CYP3A4 inhibitors (e.g., ketoconazole, diltiazem, erythromycin)High
- KetoconazoleHigh
- Potassium-sparing diuretics / ACE inhibitors / ARBsModerate
- Statins (HMG-CoA reductase inhibitors)High
- AzithromycinModerate
- NSAIDsModerateMay increase renal risk in susceptible patients
- MethotrexateModerate
- TacrolimusHigh
Population Constraints
- PregnancyReproductive SafetyRelative
- Pediatric patientsAgeRelative
- ElderlyAgeRelative
- Patients with hepatic impairmentOrgan FunctionRelative
- Elderly patientsAgeRelative
- BreastfeedingReproductiveRelative
Regulatory Status
- European UnionApprovedApproved: organ transplantation prophylaxis, psoriasis, rheumatoid arthritis, dry eye diseaseApproved under EMA with similar indications
- United StatesApprovedApproved: organ transplantation prophylaxis, psoriasis, rheumatoid arthritis, dry eye diseaseMultiple formulations (oral, IV, ophthalmic)
- United KingdomApprovedApproved: organ transplantation prophylaxis, psoriasis, rheumatoid arthritis, dry eye diseaseRegulated by MHRA
Requires therapeutic drug monitoring due to narrow therapeutic index; contraindicated in uncontrolled hypertension and severe renal impairment.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Cyclosporine?
Cyclosporine A is a cyclic undecapeptide immunosuppressant used to prevent organ transplant rejection and treat autoimmune conditions; it acts via calcineurin inhibition.
What is Cyclosporine used for?
Cyclosporine is educationally associated with: Dry eye disease, Plaque psoriasis, Dry eye disease (topical), Nephrotic syndrome, Rheumatoid arthritis, Severe plaque psoriasis, Organ transplant prophylaxis, Prevention of solid organ transplant rejection, Atopic dermatitis. Educational only — not medical advice.
How is Cyclosporine administered?
Recorded routes of administration: Intravenous, Ophthalmic, Oral, Topical.
What are the potential side effects of Cyclosporine?
Reported adverse effects include: Hypertension, Hirsutism, Tremor, Increased infection risk, Gingival hyperplasia, Neurotoxicity (tremor, headache, paresthesia), Increased risk of infection and malignancy, Nephrotoxicity, Hyperlipidemia. This list is not exhaustive — consult a qualified clinician.
Who should avoid Cyclosporine?
Recorded contraindications: Concurrent use of potassium-sparing diuretics, Hypersensitivity to cyclosporine, Live vaccines, Active malignancy or history of malignancy (for non-transplant use), Renal impairment (for non-transplant indications), Severe renal impairment (CrCl <30 mL/min), Hypersensitivity to cyclosporine or polyoxyethylated castor oil (IV formulation), Uncontrolled hypertension. Consult a qualified clinician before use.