Olopatadine
Olopatadine
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Clinical data |
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Trade names |
Patanol and others |
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AHFS/Drugs.com |
Monograph |
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MedlinePlus |
a602025 |
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Pregnancy category |
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Routes of administration |
Ophthalmic, intranasal, oral |
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ATC code |
S01GX09 (WHO) R01AC08 (WHO) |
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Pharmacokinetic data |
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Biological half-life |
3 hours |
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Identifiers |
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- {(11Z)-11-[3-(dimethylamino)propylidene]-6,11-
dihydrodibenzo[b,e]oxepin-2-yl}acetic acid
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CAS Number |
113806-05-6 Y |
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PubChem (CID) |
5281071 |
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DrugBank |
DB00768 Y |
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ChemSpider |
4444528 Y |
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UNII |
D27V6190PM Y |
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KEGG |
D08293 Y |
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ChEMBL |
CHEMBL1189432 N |
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ECHA InfoCard |
100.133.834 |
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Chemical and physical data |
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Formula |
C21H23NO3 |
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Molar mass |
337.412 g/mol |
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3D model (Jmol) |
Interactive image |
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O=C(O)Cc2ccc1OCc3c(C(\c1c2)=C\CCN(C)C)cccc3
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InChI=1S/C21H23NO3/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24)/b18-8- YKey:JBIMVDZLSHOPLA-LSCVHKIXSA-N Y
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NY (what is this?) (verify) |
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Olopatadine hydrochloride is an antihistamine (as well as anticholinergic and mast cell stabilizer), sold as a prescription eye drop manufactured by Alcon in one of three strengths: 0.7% solution or Pazeo in the US, 0.2% solution or Pataday (also called Patanol S in some countries), and 0.1% or Patanol (also called Opatanol in some countries). It is used to treat itching associated with allergic conjunctivitis (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]
See also
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). Retrieved 2008-08-10.
- ↑ 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. Retrieved 16 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.
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| ChAT |
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| AChE | |
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| BChE |
- Inhibitors: Cymserine
- Many of the AChE inhibitors listed above
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Receptor (ligands) | H1 |
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| H2 | |
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| H3 | |
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| H4 | |
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Transporter (inhibitors) | |
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Enzyme (inhibitors) | |
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Others | |
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