Ketotifen

Ketotifen

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Systematic (IUPAC) name
4-(1-methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
Clinical data
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	Oral, Eye Drops
Legal status
Legal status	US: OTC Oral - Prescription, Eye Drops - OTC
Pharmacokinetic data
Bioavailability	60%
Protein binding	75%
Metabolism	Hepatic
Biological half-life	12 Hours
Identifiers
CAS Number	34580-14-8
ATC code	R06AX17 (WHO) S01GX08
PubChem	CID 3827
DrugBank	APRD01061
Chemical data
Formula	C19H19NOS
Molar mass	309.426 g/mol[[]]
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Ketotifen fumarate 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.

The drug is marketed as ophthalmic solutions under the brand names Zaditor/Zaditen (Novartis), Alaway (Bausch and Lomb), Zyrtec Itchy-Eye Drops, and Claritin Eye.

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 three. The mean elimination half life is 12 hours. 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 due to its phosphodiesterase inhibition, since a phosphodiesterase enzyme is involved in their feedback/homeostatic pathway.

External links

• Zaditor web site
• Alaway web site

bg:Кетотифен th:คีโตติเฟน