SEE FOR SYNTHESIS http://www.allfordrugs.com/2016/08/10/olopatadine/
Olopatadine hydrochloride is an antihistamine (as well as anticholinergic and mast cell stabilizer), sold as a prescription eye dropmanufactured by Alcon in one of three strengths: 0.7% solution or Pazeo in the US, 0.2% solution or Pataday (also called Patanol Sin some countries), and 0.1% or Patanol (also called Opatanol in some countries). It is used to treat itching associated with allergicconjunctivitis (eye allergies). A decongestant nasal spray formulation is sold as Patanase, which was approved by the FDA on April 15, 2008. It is also available as an oral tablet in Japan under the tradename Allelock, manufactured by Kyowa Hakko Kogyo.
It should not be used to treat irritation caused by contact lenses. The usual dose for Patanol is 1 drop in each affected eye 2 times per day, with 6 to 8 hours between doses. Both Pazeo and Pataday are dosed 1 drop in each eye daily.
There is potential for Olopatadine as a treatment modality for steroid rebound (red skin syndrome).
Olopatadine was developed by Kyowa Hakko Kogyo.
Some known side effects include headache (7% of occurrence), eye burning and/or stinging (5%), blurred vision, dry eyes, foreign body sensation, hyperemia, keratitis, eyelid edema, pruritus, asthenia, sore throat (pharyngitis), rhinitis, sinusitis, and taste perversion.
- Drugs.com, Alcon’s Patanase Nasal Spray Approved by FDA for Treatment of Nasal Allergy Symptoms
- Kyowa Hakko Kogyo Co., Ltd. (2007). “ALLELOCK Tablets 2.5 & ALLELOCK Tablets 5 (English)” (PDF). Retrieved2008-08-10.
- Tamura T; Matsubara M; Hasegawa K; Ohmori K; Karasawa A. (2005). “Olopatadine hydrochloride suppresses the rebound phenomenon after discontinuation of treatment with a topical steroid in mice with chronic contact hypersensitivity.”.
- Kyowa Hakko Kogyo Co., Ltd. (2002). “Company History”.Company Information. Kyowa Hakko Kogyo Co., Ltd. Retrieved16 September 2010.
- Ueno, K.; Kubo, S.; Tagawa, H.; Yoshioka, T.; Tsukada, W.; Tsubokawa, M.; Kojima, H.; Kasahara, A. (1976). “6,11-Dihydro-11-oxodibenz[b,e]oxepinacetic acids with potent antiinflammatory activity”. Journal of Medicinal Chemistry. 19 (7): 941.doi:10.1021/jm00229a017.
|Systematic (IUPAC) name|
|Trade names||Patanol and others|
|Ophthalmic, intranasal, oral|
|Biological half-life||3 hours|
|ATC code||S01GX09 (WHO)R01AC08 (WHO)|
|Molar mass||337.412 g/mol|