Drug Groups

approved

Description

Emedastine is an antihistamine used in eye drops to treat allergic conjunctivitis. [Wikipedia]

Indication

For the temporary relief of the signs and symptoms of allergic conjunctivitis.

Pharmacology

Emedastine is a relatively selective H₁-receptor antagonist.

Toxicity

Somnolence and malaise have been reported following daily oral administration.

Affected Organisms

Biotransformation

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.

Absorption

Ophthalmic use of emedastine usually does not produce measurable plasma concentrations.

Half Life

The elimination half-life of oral emedastine in plasma is 3-4 hours.

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.

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