Norketotifen

Metabolite of ketotifen

Norketotifen
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Norketotifen is a pharmacologically active metabolite of the drug ketotifen, which is primarily used as an antihistamine and mast cell stabilizer. Norketotifen retains some of the pharmacological properties of its parent compound and contributes to its overall therapeutic effects.

Chemical Structure and Properties

Norketotifen is chemically classified as a piperidine derivative. Its IUPAC name is 4-(1-methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one. The molecular structure of norketotifen includes a thiophene ring fused to a cycloheptane ring, which is a characteristic feature of the ketotifen molecule.

Chemical structure of Norketotifen

Pharmacology

Norketotifen acts as an antagonist at histamine H1 receptors, similar to ketotifen. This action helps in reducing allergic symptoms by preventing the effects of histamine, a compound involved in allergic reactions. Additionally, norketotifen may exhibit anti-inflammatory properties, contributing to its effectiveness in treating allergic conditions.

Metabolism

Norketotifen is formed in the body through the N-demethylation of ketotifen. This metabolic process occurs primarily in the liver, where enzymes such as cytochrome P450 are involved in the conversion. The presence of norketotifen in the bloodstream extends the duration of action of ketotifen, enhancing its therapeutic efficacy.

Clinical Use

While norketotifen itself is not marketed as a separate drug, its presence as a metabolite of ketotifen is significant in the context of ketotifen's clinical use. Ketotifen is used in the management of allergic rhinitis, asthma, and other allergic conditions. The contribution of norketotifen to the overall pharmacological profile of ketotifen is an area of interest in clinical pharmacology.

Safety and Side Effects

The safety profile of norketotifen is closely related to that of ketotifen. Common side effects associated with ketotifen, and by extension norketotifen, include drowsiness, dry mouth, and dizziness. These effects are primarily due to the antihistaminic activity of the compound.

Related Pages

• Ketotifen
• Antihistamine
• Mast cell stabilizer
• Histamine