Detail of > 140462-76-6
- CAS Number:
- 140462-76-6
- Name:
Olopatadine hydrochloride
- Formula:
- C21H23NO3·HCl
- Molecular Structure:

- Synonyms:
- Dibenz[b,e]oxepin-2-aceticacid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro-, hydrochloride, (11Z)-(9CI);ALO4943A;Allelock;KW 4679;Dibenz[b,e]oxepin-2-aceticacid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro-, hydrochloride (1:1),(11Z)-;11-((Z)-3-(Dimethylamino)propylidene)-6,11-dihydrodibenz(b,e)oxepin-2-acetic acid, hydrochloride;(Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride;
- Molecular Weight:
- 373.87
- Melting Point:
- 242-245 °C
- Boiling Point:
- 523 °C at 760 mmHg
- Flash Point:
- 270.1 °C
- Appearance:
- White Solid
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Reference
- A comparison of the efficacy and tolerability of olopatadine hydrochloride 0
- A comparison of the efficacy and tolerability of olopatadine hydrochloride 0.1% ophthalmic solution and cromolyn sodium 2% ophthalmic solution in seasonal allergic conjunctivitis. Katelaris, Constance H.; Ciprandi, Giorgio; Missotten, Luc; Turner, F. Darell; Bertin, Donata; Berdeaux, Gilles; Czarny, Daniel; Hall, John H.; McCurrach, Fiona E.; Mitchell, Paul; Stawell, Richard J.; Thomson, George; Weiner, John; West, Robert H.; Goes, Frank M. R.; Marechal-Courtois, Christiane; Missotten, Luc; Pourjavan, Sayeh B.; Riviere, Agnes; Bremond, Dominique; Verin, Philippe; Collum, Amanda; Collum, Luis M. T.; Hurley, Colin; Kearney, Joanne; Khurana, Kavita P.; Ooi, Yeok-See; Cerqueti, Piera M.; Ciprandi, Giorgio; Leonardi, Andrea; Orsoni, Gabriella J.; Secchi, Antonio; de Smet, Marc; Meijer, Frans; Odenthal, T. P.; Reinders, Erik; Dominguez, Dolores S.; Iruzubieta, Jesus M.; Lapuente, Carlos R.; Lopez, Esther C.; Palmer, Ana M.; Parra, Juan C.; Peiro, Jose F.; Sans, Mariano, R.; Pigache, Robert (Department of Clinical Immunology and Allergy, Westmead Hospital, Sydney, Australia). Clinical Therapeutics, 24(10), 1561-1575 (English) 2002 Excerpta Medica, Inc. CODEN: CLTHDG. ISSN: 0149-2918. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 63 Treatments for allergic conjunctivitis have various mechanisms of action. Cromolyn sodium stabilizes conjunctival mast cells by preventing calcium influx across the cell membrane, whereas olopatadine hydrochloride is both an antihistamine and a mast cell stabilizer. This study compared the efficacy and tolerability of olopatadine and cromolyn in controlling the ocular signs and symptoms of seasonal allergic conjunctivitis. This was a multicenter, randomized, double-masked, parallel-group trial. One group instilled olopatadine 0.1% ophthalmic soln. and placebo BID, and the other instilled cromolyn 2% ophthalmic soln. QID, both for 6 wk.Several substances with their cas registry numbers 113806-05-6 and 140462-76-6 may be metioned in this study. The formulation of cromolyn used in this study is currently available only in Europe and Australia. The intent-to-treat efficacy and safety analyses included 185 patients, 91 in the olopatadine group and 94 in the cromolyn group. At 30 min after the first instillation, resp. decreases of ~30% and ~20% were reported in self-rated ocular itching and redness with both treatments; by 4 h, itching had decreased by ~38% in both groups. Differences between treatments were not statistically significant. At 4 h, redness had decreased by ~38% and ~26% in the resp. treatment groups. By day 42, both treatments had produced significant redns. from baseline in ocular signs and symptoms; however, the redns. in itching and redness were significantly greater with olopatadine compared with cromolyn (both variables, P < 0.05). The difference in physicians' impression of overall improvement on days 30 and 42 significantly favored olopatadine over cromolyn (both days, P < 0.05). Most patients (62.2%) had reacted pos. to grass pollen at baseline. The regression slopes correlating itching and redness with pollen count were 5 times lower for olopatadine compared with cromolyn (P = 0.002 and P = 0.016, resp.), indicating that olopatadine's efficacy increased as the pollen count increased. Six weeks' instillation of olopatadine 0.1 % ophthalmic soln. BID had a significantly greater effect on the ocular signs and symptoms of allergic conjunctivitis compared with 6 wk' instillation of cromolyn 2% ophthalmic soln. QID. Both treatments were well tolerated by patients in all age groups; however, olopatadine appeared to have better local tolerability in children aged <11 yr. .
- Clinical efficacy of olopatadine vs
- Clinical efficacy of olopatadine vs. epinastine ophthalmic solution in the conjunctival allergen challenge model. Lanier, Bobby Q.; Finegold, Ira; D'Arienzo, Peter; Granet, David; Epstein, Arthur B.; Ledgerwood, Greg L. (Fort Worth Allergy and Asthma Association, TX, USA). Current Medical Research and Opinion, 20(8), 1227-1233 (English) 2004 LibraPharm Ltd. CODEN: CMROCX. ISSN: 0300-7995. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 63 Olopatadine hydrochloride 0.1% ophthalmic soln. 140462-76-6 and 108929-04-0 are cas registry numbers. These chemicals are also mentioned in this article. (Patanol) and epinastine hydrochloride 0.05% ophthalmic soln. (Elestat) are two topical antiallergic agents. Olopatadine is indicated for the treatment of the signs and symptoms of allergic conjunctivitis that include itching, redness, tearing, lid swelling, and chemosis. Epinastine is indicated for the prevention of itching assocd. with allergic conjunctivitis. This study compared the clin. efficacy of olopatadine and epinastine in the prevention of itching and conjunctival redness in the conjunctival allergen challenge (CAC) model. This was a prospective, randomized, double-masked, contralaterally-controlled, single center allergen challenge study. Ninety-six subjects with a history of allergic conjunctivitis were screened, and the 66 who responded to conjunctival allergen challenge at visits 1 and 2 were randomized into 1 of 3 treatment groups at visit 3 to receive one drop of study medication in each eye: (1) olopatadine in one eye and epinastine in the fellow eye, (2) olopatadine in one eye and placebo in the fellow eye, and (3) epinastine in one eye and placebo in the fellow eye. Five minutes after study drop instillation, subjects were bilaterally challenged with the allergen concn. that had elicited a pos. conjunctival allergic response at Visits 1 and 2. Subjective itching assessments were given at 3 min, 5 min, and 7 min post challenge. Objective redness and chemosis assessments were made at 10 min, 15 min, and 20 min post challenge. Paired sample two-tailed t-tests were performed on the mean scores at each time point to assess statistical significance in the differences between treatments. Fifty-three subjects were randomized into the olopatadine/epinastine treatment group, the primary anal. group. Olopatadine treated eyes exhibited significantly lower mean itching and conjunctival redness scores than the contralateral epinastine treated eyes, -0.19 (p = 0.003) and -0.52 (p < 0.001), resp. Olopatadine treated eyes also exhibited significantly less chemosis -0.24 (p < 0.001), ciliary redness -0.55 (p < 0.001), and episcleral redness -0.58 (p < 0.001) than epinastine treated eyes. Olopatadine is significantly more effective than epinastine in controlling itching, redness and chemosis assocd. with allergic conjunctivitis in the CAC model. .
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