Olopatadine

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Olopatadine
Olopatadine.svg
Clinical data
Trade namesPatanol and others
AHFS/Drugs.comMonograph
MedlinePlusa602025
License data
Pregnancy
category
  • C
Routes of
administration
Eye drops, intranasal, by mouth
ATC code
Pharmacokinetic data
Elimination half-life3 hours
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard100.133.834 Edit this at Wikidata
Chemical and physical data
FormulaC21H23NO3
Molar mass337.412 g/mol g·mol−1
3D model (JSmol)
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Olopatadine is an antihistamine (as well as anticholinergic and mast cell stabilizer), sold as an eye drop, nasal spray, and pill. It is used to treat itching associated with allergic conjunctivitis (eye allergies).[1]

There is potential for olopatadine as a treatment modality for steroid rebound (red skin syndrome).[2]

Olopatadine was patented in 1986 by Kyowa Hakko Kogyo and came into medical use in 1997.[3] In 2016 it was the 269th most prescribed medication in the United States with more than a million prescriptions.[4]

Side effects[edit]

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, taste perversion, and vomiting.

Chemistry[edit]

Synthesis[edit]

Olopatadine synthesis:[5]

Pharmacology[edit]

Pharmacodynamics[edit]

Olopatadine acts as a selective antagonist of the histamine H1 receptor, thus stabilizing mast cells and inhibiting histamine release.

Brand names[edit]

Brand names include Pazeo, Pataday, Patanol S, Patanol, Opatanol, Olopat, Patanase.[6] It is also available as an oral tablet in Japan under the tradename Allelock, manufactured by Kyowa Hakko Kogyo.[7]

References[edit]

  1. ^ Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A (2015). "Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis". Cochrane Database Syst Rev. 6 (6): CD009566. doi:10.1002/14651858.CD009566.pub2. PMID 26028608.CS1 maint: Uses authors parameter (link)
  2. ^ 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". Clin Exp Allergy. 35 (1): 97–103. doi:10.1111/j.1365-2222.2005.02147.x. PMID 15649273.
  3. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 549. ISBN 9783527607495.
  4. ^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
  5. ^ 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): 941–946. doi:10.1021/jm00229a017.
  6. ^ Drugs.com, Alcon's Patanase Nasal Spray Approved by FDA for Treatment of Nasal Allergy Symptoms
  7. ^ Kyowa Hakko Kogyo Co., Ltd. (2007). "ALLELOCK Tablets 2.5 & ALLELOCK Tablets 5 (English)" (PDF). Retrieved 2008-08-10.

External links[edit]