Ciclosporin

Ciclosporin
ATC Code L04AD01, S01XA18
Formula C62H111N11O12
Molar Mass (g·mol−1) 1202,61
Physical State solid
Density (g·cm−3) 1.0
Melting Point (°C) 148 – 151
Boiling Point (°C) 1293,8 (+/- 65)
PKS Value -2,4; 11,83
CAS Number 59865-13-3
PUB Number 5284373
Drugbank ID DB00091

Basics

Ciclosporin is an immunosuppressant and is mainly used after organ transplantation to prevent rejection reactions. For this purpose, a high dose is started initially, reduced over several months, and then a low maintenance dose must be taken for the rest of the patient's life. Another possible application is autoimmune diseases such as psoriasis, glomerulonephritis or inflammatory bowel diseases such as ulcerative colitis. In the case of inflammation of the conjunctiva or cornea of the eye, ciclosporin can also be applied as a cream.

Pharmacology

Pharmacodynamics

The immunosuppressant binds to cyclophilin and the resulting complex inhibits the activity of calcineurin. This regulates the release of inflammatory cytokines. Thus, ciclosporin inhibits the activity of T cells and the normally resulting immune response. The full effect unfolds only after three months of intake.

Pharmacokinetics

Maximum plasma levels are reached after approximately one hour. The immunosuppressant is metabolized via the cytochrome P450 system, primarily via CYP3A4. It is eliminated particularly via bile, with a half-life of approximately 6 hours.

Drug Interactions

Concomitant use of drugs that affect this enzyme CYP3A4 may alter the efficacy of ciclosporin. Thus, inducers of CYP3A4, such as rifampicin or dexamethasone, may reduce the efficacy of immunosuppression, while inhibitors such as fluconazole or verapamil may reduce degradation and thus increase side effects.

Toxicity

Side effects
Sehr häufig treten Kopfschmerzen, erhöhte Blutfette und Blutdruckwerte sowie Störungen der Nierenfunktion auf. Weitere häufige Nebenwirkungen sind Leberfunktionsstörungen, Elektrolytstörungen, Muskelkrämpfe und Magen-Darm-Beschwerden.

Many of these complaints can usually be alleviated by dose reduction.

Toxicological data
Durch die Schwächung des Immunsystems besteht bei Einnahme von Ciclosporin eine erhöhte Infektgefahr. Bei Transplantationspatienten liegt zudem das Krebsrisiko 3- bis 5-mal höher als in der Normalbevölkerung.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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