Zaditor  

Ketotifen

Systematic (IUPAC) name
4-(1-methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
Identifiers
CAS number	34580-14-8
ATC code	R06AX17 S01GX08
PubChem	3827
DrugBank	APRD01061
Chemical data
Formula	C19H19NOS
Mol. mass	309.426 g/mol
Pharmacokinetic data
Bioavailability	60%
Protein binding	75%
Metabolism	Hepatic
Half life	12 Hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status	?(US) Oral - Prescription, Eye Drops - OTC
Routes	Oral, Eye Drops
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Ketotifen fumarate (ophthalmic solutions marketed under the brand name Zaditor (Novartis), Alaway (Bausch and Lomb)), Zyrtec Itchy-Eye Drops, and Claritin Eye, is a second-generation H₁-antihistamine/mast cell stabilizer available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis, or the itchy red eyes caused by allergies. In its oral form, it is used to prevent asthma attacks. Side effects include drowsiness, weight gain, dry mouth, irritability, and increased nosebleeds.

General Information

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

Besides its anti-histaminic activity, it is also a functional leukotriene antagonist and a phosphodiesterase inhibitor.

Off-Label Use

Ketotifen is used to up-regulate Beta-2 adrenergic receptors down-regulated by Beta-2 adrenergic agonists. It upregulates adrenergic receptors thanks to its phosphodiesterase inhibition, since a phosphodiesterase enzyme is involved in their feedback/omeostatic pathway.

References

This article includes a list of references, related reading or external links, but its sources remain unclear because it lacks inline citations. Please improve this article by introducing more precise citations where appropriate. (June 2009)

External links

• Zaditor web site
• Alaway web site

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