Ciclosporin
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| Pronunciation | /ˌsaɪkləˈspɔːrɪn/[1] |
| Trade names | Sandimmune, others |
| 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 | Oral, intravenous (IV), eye drops |
| Drug class | Calcineurin inhibitor |
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| Pharmacokinetic data | |
| Bioavailability | variable |
| Metabolism | Liver CYP3A4 |
| Elimination half-life | variable (about 24 hours) |
| Excretion | Bile duct |
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| ECHA InfoCard | 100.119.569 |
| Chemical and physical data | |
| Formula | C62H111N11O12 |
| Molar mass | 1202.635 g·mol−1 |
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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.[13][14] It is also used as eye drops for keratoconjunctivitis sicca (dry eyes).[15]
Common side effects include high blood pressure, headache, kidney problems, increased hair growth, and vomiting.[14] Other severe side effects include an increased risk of infection, liver problems, and an increased risk of lymphoma.[14] Blood levels of the medication should be checked to decrease the risk of side effects.[14] Use during pregnancy may result in preterm birth; however, ciclosporin does not appear to cause birth defects.[16]
Ciclosporin is believed to work by decreasing the function of lymphocytes.[14] 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.[17]
Ciclosporin was isolated in 1971 from the fungus Tolypocladium inflatum and came into medical use in 1983.[18] It is on the World Health Organization's List of Essential Medicines.[19][20] In 2022, it was the 185th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[21][22] It is available as a generic medication.[23]
- ^ "cyclosporin". Dictionary.com Unabridged. Random House. n.d. Archived from the original on 18 November 2010. Retrieved 13 July 2011.
- ^ Laupacis A, Keown PA, Ulan RA, McKenzie N, Stiller CR (May 1982). "Cyclosporin A: a powerful immunosuppressant". Canadian Medical Association Journal. 126 (9): 1041–6. PMC 1863293. PMID 7074504.
- ^ "Regulatory Decision Summary for Restasis Multidose". Drug and Health Product Register. 23 October 2014. Archived from the original on 7 June 2022. Retrieved 7 June 2022.
- ^ "Regulatory Decision Summary for Verkazia". Drug and Health Product Register. 23 October 2014. Archived from the original on 7 June 2022. Retrieved 7 June 2022.
- ^ "Health product highlights 2021: Annexes of products approved in 2021". Health Canada. 3 August 2022. Retrieved 25 March 2024.
- ^ Cite error: The named reference
Neoral FDA labelwas invoked but never defined (see the help page). - ^ Cite error: The named reference
Sandimmune FDA labelwas invoked but never defined (see the help page). - ^ Cite error: The named reference
Restasis FDA labelwas invoked but never defined (see the help page). - ^ "Vevye- cyclosporine ophthalmic solution solution/ drops". DailyMed. 26 May 2023. Archived from the original on 29 August 2023. Retrieved 29 August 2023.
- ^ "Ikervis". European Medicines Agency. 17 September 2018. Archived from the original on 13 August 2022. Retrieved 27 February 2023.
- ^ Cite error: The named reference
Vevizye EPARwas invoked but never defined (see the help page). - ^ "Vevizye PI". Union Register of medicinal products. 23 September 2024. Retrieved 27 September 2024.
- ^ World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. p. 221. hdl:10665/44053. ISBN 9789241547659.
- ^ a b c d e "Cyclosporine". The American Society of Health-System Pharmacists. Archived from the original on 17 October 2016. Retrieved 8 December 2016.
- ^ "Cyclosporine eent". The American Society of Health-System Pharmacists. Archived from the original on 13 January 2016. Retrieved 8 December 2016.
- ^ "Cyclosporine Use During Pregnancy". Drugs.com. Archived from the original on 14 September 2017. Retrieved 20 December 2016.
- ^ Cite error: The named reference
Matsuda_2000was invoked but never defined (see the help page). - ^ Watts R, Clunie G, Hall F, Marshall T (2009). Rheumatology. Oxford University Press. p. 558. ISBN 978-0-19-922999-4. Archived from the original on 5 November 2017.
- ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Cyclosporine Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
- ^ "FDA Approves First Generic of Restasis". U.S. Food and Drug Administration (FDA) (Press release). 2 February 2022. Archived from the original on 2 February 2022. Retrieved 3 February 2022.