4-Hydroxytertatolol

4-Hydroxytertatolol

4-Hydroxytertatolol is a metabolite of the beta blocker drug tertatolol. It is primarily formed in the liver through the process of oxidation.

Pharmacology

4-Hydroxytertatolol retains the pharmacological activity of its parent compound, tertatolol. It acts as a non-selective beta blocker, inhibiting the action of adrenaline and noradrenaline on beta receptors in the heart and blood vessels. This results in a decrease in heart rate, blood pressure, and myocardial oxygen demand.

Metabolism

The formation of 4-Hydroxytertatolol from tertatolol is mediated by the enzyme cytochrome P450 (CYP2D6). This enzyme is responsible for the oxidation of a wide range of drugs and other xenobiotics. The activity of CYP2D6 can vary greatly between individuals due to genetic polymorphisms, which can affect the rate of 4-Hydroxytertatolol formation and thus the pharmacokinetics and pharmacodynamics of tertatolol.

Clinical significance

The clinical significance of 4-Hydroxytertatolol is primarily related to its role in the metabolism of tertatolol. The formation of this metabolite can be affected by factors such as drug interactions, genetic polymorphisms in CYP2D6, and liver disease. These factors can potentially affect the therapeutic efficacy and safety of tertatolol.

See also

• Tertatolol
• Beta blocker
• Cytochrome P450
• Pharmacokinetics
• Pharmacodynamics