4612 T3D4558 Azelastine Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista&#174;. Dymista&#174; is indicated in patient over 12 years old for symptomatic relief of seasonal allergic rhinitis. 58581-89-8 2267 C22H24ClN3O White powder. 225 °C (hydrochloride salt) Sparingly soluble (hydrochloride salt) Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration. Azelastine competes with histamine for the H1-receptor sites on effector cells and acts as an antagonist by inhibiting the release of histamine and other mediators involved in the allergic response. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity. Route of Elimination: Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system. Half Life: Elimination half-life (based on intravenous and oral administration) is 22 hours. Elimination half-life of the active metabolite, desmethylazelastine, is 54 hours (after oral administration of azelastine). No indication of carcinogenicity to humans (not listed by IARC). For the symptomatic treatment of seasonal allergic rhinitis and non-allergic rhinitis, as well as symptomatic relief of ocular itching associated with allergic conjunctivitis. 2014-08-30T21:04:10Z 2026-05-14T16:54:33Z Azelastine C07768 2950 DB00972 true CN1CCCC(CC1)N1N=C(CC2=CC=C(Cl)C=C2)C2=CC=CC=C2C1=O C22H24ClN3O InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3 MBUVEWMHONZEQD-UHFFFAOYSA-N 381.898 381.160790112 Exogenous Solid 4.9 CHEMBL639 2180 <p>Yutaka Morita, Noritoshi Koyama, Shigemitsu Ohsawa, &#8220;Methods employing stable preparation containing azelastine hydrochloride.&#8221; U.S. Patent US6117864, issued December, 1990.</p> CHEM003518 DTXSID6022638 NS00003187 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one 35.910000000000004 110.51540000000003 41.539291345321864 3 3 0 8.876474536708875 1 4 3.81 -4.62 9.20e-03 g/l