Ciclosporin
Chemical compound / From Wikipedia, the free encyclopedia
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Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. It is taken orally or intravenously for rheumatoid arthritis, psoriasis, Crohn's disease, nephrotic syndrome, eczema, and in organ transplants to prevent rejection.[12][13] It is also used as eye drops for keratoconjunctivitis sicca (dry eyes).[14]
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Pronunciation | /ˌsaɪkləˈspɔːrɪn/[1] |
Trade names | Neoral, Sandimmune, Restasis, Gengraf, other |
Other names | cyclosporin, ciclosporin A,[2] cyclosporine A, cyclosporin A (CsA), cyclosporine (USAN US) |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601207 |
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Routes of administration | by mouth, intravenous (IV), eye drops |
Drug class | Calcineurin inhibitor |
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Bioavailability | variable |
Metabolism | Liver CYP3A4 |
Elimination half-life | variable (about 24 hours) |
Excretion | Bile duct |
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ECHA InfoCard | 100.119.569 |
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Formula | C62H111N11O12 |
Molar mass | 1202.635 g·mol−1 |
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Common side effects include high blood pressure, headache, kidney problems, increased hair growth, and vomiting.[13] Other severe side effects include an increased risk of infection, liver problems, and an increased risk of lymphoma.[13] Blood levels of the medication should be checked to decrease the risk of side effects.[13] Use during pregnancy may result in preterm birth; however, ciclosporin does not appear to cause birth defects.[15]
Ciclosporin is believed to work by decreasing the function of lymphocytes.[13] It does this by forming a complex with cyclophilin to block the phosphatase activity of calcineurin, which in turn decreases the production of inflammatory cytokines by T-lymphocytes.[16]
Ciclosporin was isolated in 1971 from the fungus Tolypocladium inflatum and came into medical use in 1983.[17] It is on the World Health Organization's List of Essential Medicines.[18][19] In 2021, it was the 175th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[20][21] It is available as a generic medication.[22]