| Item |
Information |
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Drug Groups
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approved |
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Description
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A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis. [PubChem] |
| Indication |
Indicated as an add-on or prophylactic oral medication in the chronic treatment of mild atopic asthmatic children. Also used as self-medication for the temporary relief of itching of the eye due to allergic conjunctivitis (ophthalmic). |
| Pharmacology |
Ketotifen is a fast acting non-competitive histamine antagonist. It inhibits the release of mediators from mast cells. It is a non-bronchodilator antiasthmatic drug (when taken orally). |
| Toxicity |
Adverse reactions include headaches, conjunctival injection and rhinitis. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Primarily hepatic. The main metabolite found in both plasma and urine is the inactive ketotifen-N-glucuronide. Nor-ketotifen, the N-demethylated metabolite, and the 10-alpha-hydroxyl derivative are the only other metabolites detectable in human urine. |
| Absorption |
Following oral administration absorption is at least 60% |
| Half Life |
21 hours (for elimination) |
| Protein Binding |
75% |
| External Links |
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