Population pharmacokinetic analysis of tramadol and O -desmethyltramadol with genetic polymorphism of CYP2D6

• Published in: Drug design, development and therapy Vol. 13; pp. 1751 - 1761
• Main Authors: Lee, Joomi, Yoo, Hee-Doo, Bae, Jung-Woo, Lee, Sooyeun, Shin, Kwang-Hee
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01.05.2019; Taylor & Francis Ltd; Dove; Dove Medical Press
• Subjects: Administration, Oral; Adult; Analgesics; Analysis; CYP2D6 protein; CYP2D610; Cytochrome; Cytochrome P-450; Cytochrome P-450 CYP2D6 - genetics; Cytochrome P450; Cytochromes P450; Dosage; Dose-Response Relationship, Drug; Enzymes; Gene polymorphism; Genetic aspects; Genetic polymorphisms; Genotype; Healthy Volunteers; Humans; Male; Metabolites; Narcotics; Neuralgia; Nonlinear Dynamics; O-desmethyltramadol; Opioid receptors; Original Research; Pain; Pharmacodynamics; Pharmacokinetics; Pharmacology; Polymorphism; Polymorphism, Genetic - genetics; Population; population model; Republic of Korea; Tramadol; Tramadol - administration & dosage; Tramadol - analogs & derivatives; Tramadol - metabolism; Tramadol - pharmacokinetics; Young Adult; Republic of Korea; Iran; South Korea; United States > US; pharmacokinetics; tramadol; population pharmacokinetic model; CYP2D610; O-desmethyltramadol; genetic polymorphism

Tramadol is widely used to treat acute, chronic, and neuropathic pain. Its primary active metabolite, desmethyltramadol (M1), is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to M1 mainly by the cytochrome P450 (CYP) 2D6 enzyme, and to other metabolit...