| Indication | For the temporary relief of the signs and symptoms of allergic conjunctivitis. |
| Pharmacodynamics | Emedastine is a relatively selective H1-receptor antagonist. |
| Mechanism of action | Emedastine is a relatively selective, histamine H1 antagonist. In vitro examinations of emedastine's affinity for histamine receptors demonstrate relative selectivity for the H1 histamine receptor. In vivo studies have shown concentration-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva following topical ocular administration. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors. |
| Absorption | Ophthalmic use of emedastine usually does not produce measurable plasma concentrations. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism | Two primary metabolites, 5-hydroxyemedastine and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5'-oxoanalogs of 5-hydroxyemedastine and 6-hydroxy-emedastine and the N-oxide are also formed as minor metabolites. |
| Route of elimination | Approximately 44% of the oral dose is recovered in the urine over 24 hours with only 3.6% of the dose excreted as parent drug. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. |
| Half life | The elimination half-life of oral emedastine in plasma is 3-4 hours. |
| Clearance | Not Available |
| Toxicity | Somnolence and malaise have been reported following daily oral administration. |
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