Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2020 Publisher: Novartis Pharmaceuticals UK Limited, 2nd Floor, The WestWorks Building, White City Place, 195 Wood Lane, London, W12 7FQ, United Kingdom
Pharmacotherapeutic Group: Ophthalmologicals: Anti-inflammatory Agents
ATC Code: S01BA01
Dexamethasone has been demonstrated by animal and human studies based on oral application to possess approximately six to seven times the potency of prednisolone and at least 30 times the potency of cortisone. The potency of the compound is accomplished by the addition of a methyl radical and a fluorine atom to the prednisolone radical.
Dexamethasone is absorbed rapidly after oral administration with a half-life of about 190 minutes. Sufficient absorption may occur after topical application to the skin and eye to produce systemic effects. In plasma dexamethasone protein binding is less than for most other corticosteroids. Corticosteroids diffuse into tissue fluids and cerebrospinal fluid but transplacental diffusion in significant amounts has not been demonstrated. Corticosteroids are metabilised in the liver the kidney and excrete in the urine. Metabolism is similar to other corticosteroids. Intraocular penetration occurs in significant amounts and contributes to the effectiveness of dexamethasone in anterior segment inflammatory disease.
Repeat dose topical ocular safety studies with dexamethasone in rabbits have shown systemic corticosteroid effects. Such effects are considered to be unlikely when MAXIDEX is used as recommended.
Dexamethasone was clastogenic in the in vitro human lymphocyte assay and in vivo in the mouse micronucleus assay at doses in excess of those obtained following topical application. Conventional carcinogenicity studies with MAXIDEX have not been performed.
Dexamethasone has been found to be teratogenic in animal models. Dexamethasone induced abnormalities of fetal development including cleft palate, intra-uterine growth retardation and effects on brain growth and development. The ocular administration of 0.1% dexamethasone also resulted in fetal anomalies in rabbits. Dexamethasone had no adverse effects on female fertility in a chorionic gonadotropin primed rat model.
There are no other preclinical data of relevance to the prescriber which are additional to that included in other sections of the SPC.
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