| Item |
Information |
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Drug Groups
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approved |
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Description
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Rimexolone is a glucocorticoid steroid used to treat inflammation in the eye. It is marketed as a 1% eye drop solution under the trade name Vexol |
| Indication |
For the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis. |
| Pharmacology |
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. |
| Toxicity |
Symptoms of overdose include retinal toxicity, glaucoma, and subcapsular cataract. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
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. |
| Absorption |
Systemically absorbed. |
| Half Life |
The serum half-life of rimexolone could not be reliably estimated due to the large number of samples below the quantitation limit of the assay (80 pg/mL). However, based on the time required to reach steady-state, the half-life appears to be short (1-2 hours). |
| Elimination |
Following IV administration of radio-labelled rimexolone to rats, greater than 80% of the dose is excreted via the feces as rimexolone and metabolites. |
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