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Olopatadine

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Olopatadine.svg

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

  1.  Drugs.com, Alcon’s Patanase Nasal Spray Approved by FDA for Treatment of Nasal Allergy Symptoms
  2.  Kyowa Hakko Kogyo Co., Ltd. (2007). “ALLELOCK Tablets 2.5 & ALLELOCK Tablets 5 (English)” (PDF). Retrieved2008-08-10.
  3. 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.”.
  4. Jump up^ Kyowa Hakko Kogyo Co., Ltd. (2002). “Company History”.Company Information. Kyowa Hakko Kogyo Co., Ltd. Retrieved16 September 2010.
  5. 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

 

 

Olopatadine
Olopatadine.svg
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
  • C
Routes of
administration
Ophthalmic, intranasal, oral
Pharmacokinetic data
Biological half-life 3 hours
Identifiers
CAS Number 113806-05-6 Yes
ATC code S01GX09 (WHO)R01AC08 (WHO)
PubChem CID 5281071
DrugBank DB00768 Yes
ChemSpider 4444528 Yes
UNII D27V6190PM Yes
KEGG D08293 Yes
ChEMBL CHEMBL1189432 
Chemical data
Formula C21H23NO3
Molar mass 337.412 g/mol

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Filed under: Uncategorized Tagged: Olopatadine

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