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OLPATADINE
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.[1] It is also available as an oral tablet in Japan under the tradename Allelock, manufactured by Kyowa Hakko Kogyo.[2]
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).[3]
Olopatadine was developed by Kyowa Hakko Kogyo.[4]
Side Effects
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.
Synthesis
Olopatadine synthesis:[5]
References
- 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.
- Jump up^ 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.”.
- Jump up^ Kyowa Hakko Kogyo Co., Ltd. (2002). “Company History”.Company Information. Kyowa Hakko Kogyo Co., Ltd. Retrieved16 September 2010.
- Jump up^ 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.
External links
| Systematic (IUPAC) name | |
|---|---|
|
{(11Z)-11-[3-(dimethylamino)propylidene]-6,11-
dihydrodibenzo[b,e]oxepin-2-yl}acetic acid |
|
| Clinical data | |
| Trade names | Patanol and others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a602025 |
| Pregnancy category |
|
| Routes of administration |
Ophthalmic, intranasal, oral |
| Pharmacokinetic data | |
| Biological half-life | 3 hours |
| Identifiers | |
| CAS Number | 113806-05-6 |
| ATC code | S01GX09 (WHO)R01AC08 (WHO) |
| PubChem | CID 5281071 |
| DrugBank | DB00768 |
| ChemSpider | 4444528 |
| UNII | D27V6190PM |
| KEGG | D08293 |
| ChEMBL | CHEMBL1189432 |
| Chemical data | |
| Formula | C21H23NO3 |
| Molar mass | 337.412 g/mol |
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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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