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 | |
| Identifiers | |
| CAS number | 34580-14-8 |
| ATC code | R06AX17 S01 |
| 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.
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[edit] 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.
[edit] 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.
[edit] References
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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) |
[edit] External links
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