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Ketotifen

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This is an old revision of this page, as edited by 198.52.13.15 (talk) at 21:31, 24 October 2016 (added that in the US the oral form was withdrawn from market however the eye drops are still avabile with out a prescription). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Ketotifen
Clinical data
Trade namesZaditor[1]
AHFS/Drugs.comMicromedex Detailed Consumer Information
MedlinePlusa604033
Routes of
administration		Oral (tablets), ophthalmic solution
ATC code
Legal status
Legal status
  • US: Oral — withdrawn was ℞-only; Eye drops — over-the counter
Pharmacokinetic data
Bioavailability60%
Protein binding75%
MetabolismHepatic
Elimination half-life12 hours
Identifiers
  • 4-(1-Methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.047.348 Edit this at Wikidata
Chemical and physical data
FormulaC19H19NOS
Molar mass309.426 g/mol g·mol−1
3D model (JSmol)
  • O=C3c1sccc1C(\c2c(cccc2)C3)=C4/CCN(C)CC4
  • InChI=1S/C19H19NOS/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19/h2-5,8,11H,6-7,9-10,12H2,1H3 checkY
  • Key:ZCVMWBYGMWKGHF-UHFFFAOYSA-N checkY
  (verify)

Ketotifen is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt with fumaric acid, ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis,[2] or the itchy red eyes caused by allergies. In its oral form, it is used to prevent asthma attacks.

Uses

Ketotifen relieves and prevents eye itchiness and/or irritation associated with most seasonal allergies. It starts working within minutes after administering the drops. The drug has not been studied in children under three.[2] The mean elimination half life is 12 hours.[3] Besides its anti-histaminic activity, it is also a functional leukotriene antagonist and a phosphodiesterase inhibitor.

The drug may also help relieve the symptoms of irritable bowel syndrome.[4]

Side effects

Side effects include drowsiness, weight gain, dry mouth, irritability, and increased nosebleeds.

Brands

Ketotifen is marketed under many brand names worldwide.[5]

See also

References

  1. ^ http://www.webmd.com/drugs/2/drug-17484/zaditor-opht/details
  2. ^ a b Zaditor prescribing information Novartis
  3. ^ Grahnén A; Lönnebo A; Beck O; Eckernäs SA; Dahlström B; Lindström B (May 1992). "Pharmacokinetics of ketotifen after oral administration to healthy male subjects". Biopharm Drug Dispos. 13 (4): 255–262. doi:10.1002/bdd.2510130404. PMID 1600111.
  4. ^ Klooker, TK; Braak, B; Koopman, KE; Welting, O; Wouters, MM; Van Der Heide, S; Schemann, M; Bischoff, SC; et al. (2010). "The mast cell stabiliser ketotifen decreases visceral hypersensitivity and improves intestinal symptoms in patients with irritable bowel syndrome". Gut. 59 (9): 1213–21. doi:10.1136/gut.2010.213108. PMID 20650926.
  5. ^ drugs.com International availability of ketofin Page accessed April 21, 2015
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