Products
Ciclosporin eye drops were approved in the EU in 2015 and in many countries in 2016 (Ikervis). They have been registered in the United States since 2009 (Restasis).
Structure and properties
Ciclosporin (C62H111N11O12, Mr = 1203 g/mol) exists as a white powder that is practically insoluble in water. It is extracted from the mushroom ( chamois) or produced by other methods. The fungus was originally found by a Sandoz employee in a soil sample from Norway. Ciclosporin is a lipophilic cyclic polypeptide consisting of 11 amino acids (undecapeptide).
Effects
Ciclosporin (ATC S01XA18) has immunosuppressive and anti-inflammatory properties. It blocks the formation and release of proinflammatory cytokines such as interleukin 2. Ciclosporin is mainly effective against lymphocytes (T cells). The effects are due to inhibition of the calcium-dependent phosphatase calcineurin, which is involved in gene activation and transcription of inflammatory mediators.
Indications
For the treatment of severe keratitis in adults with dry eyes who have not improved despite treatment with tear substitutes
Dosage
According to the SmPC. The drops are placed in the affected eyes once daily before bedtime.
Contraindications
- Hypersensitivity
- Acute or suspected infection in or around the eye
For complete precautions, see the drug label.
Interactions
Co-administration of glucocorticoid eye drops may increase immunosuppressive effects.
Adverse effects
The most common possible adverse effects include ocular pain, ocular irritation, lacrimation, ocular hyperemia, and eyelid erythema.
