Ketotifen

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Ketotifen
Ketotifen structure.svg
Systematic (IUPAC) name
4-(1-Methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
Clinical data
AHFS/Drugs.com Micromedex Detailed Consumer Information
MedlinePlus a604033
Pregnancy cat. C (US)
Legal status Oral - Prescription; Eye Drops - OTC (US)
Routes Oral, Eye Drops
Pharmacokinetic data
Bioavailability 60%
Protein binding 75%
Metabolism Hepatic
Half-life 12 Hours
Identifiers
CAS number 34580-14-8 YesY
ATC code R06AX17 S01GX08
PubChem CID 3827
DrugBank DB00920
ChemSpider 3695 YesY
UNII HBD503WORO YesY
KEGG D01332 YesY
ChEMBL CHEMBL534 YesY
Chemical data
Formula C19H19NOS 
Mol. mass 309.426 g/mol
 YesY (what is this?)  (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,[1] or the itchy red eyes caused by allergies. In its oral form, it is used to prevent asthma attacks.

Uses[edit]

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.[1] The mean elimination half life is 12 hours.[2] 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.[3]

Side effects[edit]

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

Brands[edit]

Ketotifen is marketed as ophthalmic solutions under the brand names Zaditor, Zaditen,[4] Alaway, Zyrtec Itchy-Eye Drops, and Claritin Eye. A generic version of Novartis' Zaditor, ketotifen fumarate ophthalmic solution, 0.025%, is available. Generic Zaditor is made by Alcon Laboratories Apotex, Inc.and Akorn, Inc.

Bausch & Lomb makes a brand-name version (Alaway®) that is equivalent to Zaditor.

See also[edit]

References[edit]

  1. ^ a b Zaditor prescribing information Novartis
  2. ^ 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. 
  3. ^ 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. 
  4. ^ Novartis Pharmaceuticals, Alphabetically, beginning with Z.

External links[edit]