RIMEXOLONE (100 MG)

Absorption

Systemically absorbed.

Toxicity

Symptoms of overdose include retinal toxicity, glaucoma, and subcapsular cataract.

Description

Rimexolone, an ophthalmic corticosteroid, was launched in 1995 in the U.S.A. for the treatment of postoperative inflammation following ocular surgery and anterior uveitis. Rimexolone has high corticoid receptor affinity and is a potent local antiinflammatory agent with minimal systemic effects and virtually no atrophogenic action in many animal models studied, unique among a wide range of topical steroids. Rapid onset, long duration of action plus a superior safety profile are characteristics of rimexolone. It was also approved in Europe for the treatment of rheumatoid arthritis and is currently in clinical trials for tendinitis and osteoarthritis.

Originator

Akzo (Netherlands)

The Uses of RIMEXOLONE (100 MG)

Anti-inflammatory (local).

Background

Rimexolone is a 1% eye drop solution is a glucocorticoid steroid. It is used to treat inflammation in the eye. It is marketed as Vexol.

Indications

For the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis.

Definition

ChEBI: Rimexolone is a 20-oxo steroid.

brand name

Vexol (Alcon).

General Description

Rimexolone, 11β-hydroxy-16α,17α-dimethyl-17-(1-oxopropyl)androsta-1,4-diene-3-one,like medrysone and fluorometholone, lacks the C21 OHgroup. In addition, rimexolone has an additional methylgroup in the 17 -position, a site where an OH group is typicallyfound. Rimexolone is available as a suspension forophthalmic use.

Pharmacokinetics

Rimexolone is a glucocorticoid corticosteroid for systemic use. Corticosteroids suppress the inflammatory response to a variety of inciting agents of a mechanical, chemical, or immunological nature. They inhibit edema, cellular infiltration, capillary dilatation, fibroblastic proliferation, deposition of collagen and scar formation associated with inflammation.

Metabolism

Undergoes extensive metabolism. Following intravenous administration of radiolabeled rimexolone in rats, more than 80% of the dose was excreted in the feces as rimexolone and metabolites. Metabolites have been shown to be either less active than rimexolone or inactive in human glucocorticoid receptor binding assays.