Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2017 Publisher: Bausch & Lomb UK Limited, Bausch & Lomb House, 106 London Road, Kingston-Upon-Thames, Surrey, UK, KT2 6TN
Pharmacotherapeutic group: Corticosteroids, plain
ATC code: S01BA04
The actions of corticosteroids are mediated by the binding of the corticosteroid molecules to receptor molecules located within sensitive cells. Corticosteroid receptors are present in human trabecular meshwork cells and in rabbit iris ciliary body tissue.
Prednisolone, in common with other corticosteroids, will inhibit phospholipase A2 and thus decrease prostaglandin formation.
The activation and migration of leucocytes will be affected by prednisolone. A 1% solution of prednisolone has been demonstrated to cause a 5.1% reduction in polymorphonuclear leucocyte mobilisation to an inflamed cornea. Corticosteroids will also lyse and destroy lymphocytes. These actions of prednisolone all contribute to its anti-inflammatory effect.
The oral availability, distribution and excretion of prednisolone is well documented. A figure of 82 ± 13% has been quoted as the oral availability and 1.4 ± 0.3ml/min/kg as the clearance rate. A half life of 2.1-4.0 hours has been calculated.
With regard to ocular pharmacokinetics, prednisolone sodium phosphate is a highly water soluble compound and is almost lipid insoluble. Therefore, theoretically it should not penetrate the intact corneal epithelium. Nevertheless, 30 minutes after instillation of a drop of 1% drug, corneal concentrations of 10µg/g and aqueous levels of 0.5µg/g have been attained. When a 0.5% solution was instilled in rabbit eyes every 15 minutes for an hour, an aqueous concentration of 2.5µg/ml was measured. Considerable variance exists in the intraocular penetration of prednisolone depending on whether the cornea is normal or abraded.
It can be seen that only low levels of prednisolone will be absorbed systemically, particularly where the cornea is intact.
Any prednisolone which is absorbed will be highly protein-bound in common with other corticosteroids.
The use of prednisolone in ophthalmology is well-established. Little specific toxicology work has been reported, however, the breadth of clinical experience confirms its suitability as a topical ophthalmic agent.
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