Elestat
Elestat - General Information
Elestat is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Pharmacology of Elestat
Elestat is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Elestat is indicated for the prevention of itching associated with allergic conjunctivitis. Elestat is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Elestat is selective for the histamine H1-receptor and has affinity for the histamine H2 receptor. Elestat also possesses affinity for the a1-, a2-, and 5-HT2 -receptors. Elestat does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.
Elestat for patients
Information for Patients: Patients should be advised not to wear a contact lens if their eye is red. ELESTAT™ should not be used to treat contact lens related irritation. The preservative in ELESTAT™, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed prior to instillation of ELESTAT™ and may be reinserted after 10 minutes following its administration.
Patients should be instructed to avoid allowing the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to avoid contamination of the solution by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions.
Bottle should be kept tightly closed when not in use.
Elestat Interactions
None Reported
Elestat Contraindications
ELESTAT™ ophthalmic solution is contraindicated in those patients who have shown hypersensitivity to epinastine or to any of the other ingredients.
Additional information about Elestat
Elestat Indication: For the prevention of itching associated with allergic conjunctivitis.
Mechanism Of Action: Elestat has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Epinastine
Synonyms: Epinastina [Spanish]; Epinastinum [Latin]
Drug Category: Antihistamines; Ophthalmics
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Epinastine: Elestat;
Absorption: The absolute bioavailability of epinastine is about 40%.
Toxicity (Overdose): Not Available
Protein Binding: 64%
Biotransformation: Mainly excreted unchanged, less than 10% metabolized.
Half Life: 12 hours
Dosage Forms of Elestat: Solution / drops Ophthalmic
Chemical IUPAC Name: Not Available
Chemical Formula: C16H15N3
Epinastine on Wikipedia: https://en.wikipedia.org/wiki/Epinastine
Organisms Affected: Humans and other mammals
