Epinastine

• 9,13 b -dihydro -1H- dibenz [c, f] imidazo [ 1,5-a] azepine -3-amine
• (RS )-3- amino-9, 13b -dihydro -1H- dibenz [c, f] imidazo [ 1,5-a] azepine
• Latin: Epinastinum

• C16H15N3 ( epinastine )
• C16H15N3 · HCl ( epinastine · monohydrochloride )
• C16H15N3 · HBr ( epinastine · monohydrobromide )

• 80012-43-7 ( epinastine )
• 108929-04-0 ( epinastine · monohydrochloride )
• 127786-29-2 ( epinastine · monohydrobromide )

• R06AX24
• S01GX10

H1 - antihistamines

Antagonist of H1 receptors

• 249.32 g · mol -1 ( epinastine )
• 285.77 g · mol -1 ( epinastine · monohydrochloride )

• 205-208 ° C
• 273-275 ° C ( epinastine · monohydrochloride )
• 284-286 ° C ( epinastine · monohydrobromide )

Insoluble in water (1.86 mg · l-1 at 25 ° C)

Risk

192 mg · kg -1 ( LD50, Rat, oral, monohydrochloride )

Template: Infobox chemical / molecular formula search available

Epinastine is a drug which is used as an antihistamine for the relief of symptoms of allergic conjunctivitis.

Effect

The active ingredient occupies the histamine binding sites in the body, thus reducing the allergic reaction. It is a potent antagonist (more precisely, an inverse agonist ) of H1 receptors (H1- antihistamines ), and does not penetrate the blood- brain barrier. In addition, the drug is mast cell- stabilizing effect. Dosing is 2 times a day 1 drop in the eye.

Side effects

Observed side effect is irritation of the eyes. It has no effect on the central nervous system.

Stereochemistry

Medicines containing the drug as a racemate ( 1:1 mixture of enantiomers), with fundamental reasons the use of better and have fewer side effects active enantiomer would be preferable.