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| Formula | C17 H26 N4 O |
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Emedastine (trade nameEmadine) is a second generationantihistamine used ineye drops to alleviate the symptoms ofallergic conjunctivitis.[1] It acts as aH1 receptor antagonist. It works by blocking the action ofhistamine that causes allergic symptoms. It is used in form of the difumarate.[2] The emedastine difumarate is a white, crystalline, water-soluble fine powder. Emedastine eye drops is usually applied twice a day to the affected eye. When the patients with allergic conjunctivitis were treated with 0.05% emedastine difumarate ophthalmic solution for six weeks, the signs and symptoms such as redness, itching and swelling of the eyes were relieved. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors. This drug was developed byAlcon, which is global medical company specializing in eye care products.
Emedastine is significantly selective to H1 histamine receptors (Ki = 1.3 nM), whereas its affinities for other histamine receptors were low (H2: Ki = 49067 nM and H3: Ki = 12430 nM) ubin vitro study. Topical ocular administration of emedastine inhibits histamine-stimulated vascular permeability in the conjunctiva as a concentration-dependent manner inin vitro study.
The human oral bioavailability is approximately 50% and maximum plasma concentration was achieved within 1–2 hours after dosing. Emedastine is mainly metabolized by the liver. There are two primary metabolites: 5-hydroxyemedastine and 6-hydroxyemedastine. They are excreted in the urine as both free and conjugated forms. The 5'-oxoanalogs of 5-hydroxyemedastine, 6-hydroxyemedastine and theN-oxide are also formed as minor metabolites. The elimination half-life of oral emedastine in plasma is 3–4 hours, whereas that of topical emedastine is 10 hours. 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.[3]
Emedastine should not be used in patients who are hypersensitive to emedastine or any other excipients of the preparation.Benzalkonium chloride contained in the bottle of emedastine solution can discolor softcontact lenses, so people who wear contact lenses should be careful using it.
The most common adverse effect was headache (11%). The other minor adverse effects encountered in less than 5% of patients wereasthenia, burning or stinging sensation, unpleasant taste, blurred vision, eye dryness and tearing.
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