Clinical data
Trade names Zaditor[1]
AHFS/ Micromedex Detailed Consumer Information
MedlinePlus a604033
  • US: C (Risk not ruled out)
Routes of
Oral (tablets), ophthalmic solution
ATC code R06AX17 (WHO) S01GX08 (WHO)
Legal status
Legal status
  • US: Oral — withdrawn was ℞-only; Eye drops — over-the counter
Pharmacokinetic data
Bioavailability 60%
Protein binding 75%
Metabolism Hepatic
Biological half-life 12 hours
CAS Number 34580-14-8 YesY
PubChem (CID) 3827
DrugBank DB00920 YesY
ChemSpider 3695 YesY
KEGG D01332 YesY
ECHA InfoCard 100.047.349
Chemical and physical data
Formula C19H19NOS
Molar mass 309.426 g/mol
3D model (Jmol) Interactive image

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.


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.


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

See also


  2. 1 2 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. International availability of ketofin Page accessed April 21, 2015
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