Emedastine

Soluble (difumarate formulation)

1.44e+00 g/L

Breast Feeding; Lactation; Milk, Human; Antihistamines

EMA approved medicines: Human medicine

S01GX06

S - Sensory organs

QS - Sensory organs

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 exert negligible effects on adrenergic, dopaminergic and serotonin receptors.

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EMEDASTINE

Mechanisms of Action [MoA] - Histamine H1 Receptor Antagonists

Established Pharmacologic Class [EPC] - Histamine-1 Receptor Inhibitor

Emedastine is a Histamine-1 Receptor Inhibitor. The mechanism of action of emedastine is as a Histamine H1 Receptor Antagonist.

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.

Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475)

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

Following oral administration, approximately 44% of the total dose can be recovered in the urine over the 24-hour period, with only 3.6% of the dose excreted as unchanged form. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms.