10-Hydroxyketotifen
Chemical compound
10-Hydroxyketotifen is a chemical compound that is a metabolite of the drug ketotifen. Ketotifen is an antihistamine and mast cell stabilizer used primarily in the treatment of allergic conditions such as asthma and allergic rhinitis.
Chemical Structure and Properties
10-Hydroxyketotifen is characterized by the presence of a hydroxyl group attached to the ketotifen molecule. This modification occurs during the metabolic processing of ketotifen in the body. The chemical structure of 10-Hydroxyketotifen can be represented by the molecular formula C19H19NO3.
Pharmacology
As a metabolite of ketotifen, 10-Hydroxyketotifen retains some of the pharmacological properties of its parent compound. Ketotifen functions by blocking histamine H1 receptors and stabilizing mast cells, thereby preventing the release of inflammatory mediators. The role of 10-Hydroxyketotifen in the pharmacological activity of ketotifen is primarily as a byproduct of its metabolism, and it may contribute to the overall antihistaminic effects observed in patients.
Metabolism
Ketotifen undergoes extensive metabolism in the liver, where it is converted into several metabolites, including 10-Hydroxyketotifen. The metabolic pathway involves the action of liver enzymes that introduce a hydroxyl group into the ketotifen molecule, resulting in the formation of 10-Hydroxyketotifen. This process is part of the body's mechanism to increase the solubility of the compound, facilitating its excretion.
Clinical Significance
The presence of 10-Hydroxyketotifen in the body is indicative of the metabolic processing of ketotifen. While the metabolite itself is not used therapeutically, understanding its formation and excretion can provide insights into the pharmacokinetics of ketotifen. Monitoring levels of 10-Hydroxyketotifen may be relevant in pharmacokinetic studies and in assessing the metabolic profile of ketotifen in different populations.
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Contributors: Prab R. Tumpati, MD