Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux]

Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux] Publisher Pubmed

Rouini MR¹ ; Afshar M^{1, 2}

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1. Biopharmaceutics and pharmacokinetics division, department of pharmaceutics, faculty of pharmacy, Tehran university of medical sciences, P.O. Box 14155-6451, Tehran, Iran
2. Department of pharmaceutics, pharmaceutical sciences branch, Islamic Azad university (IAUPS), Tehran, 193956466, Iran

Source: Therapie Published:2017

Abstract

Aim of the study Propafenone (PPF) is an antiarrhythmic drug, metabolized mainly by CYP2D6 to 5-hydroxypropafenone (5OH-PPF) and by CYP3A4 to norpropafenone (NOR-PPF). CYP2D6 shows a high degree of genetic polymorphism which is associated with diminished antiarrhythmic efficacy or cardiac seizures/cardiotoxicity. This study aimed to investigate the effect of the CYP2D6 polymorphism on the pharmacokinetics of PPF and its two main metabolites. The usefulness of PPF/5OH-PPF ratio for CYP2D6 phenotyping in healthy adults was also evaluated. Methods Twelve healthy volunteers, 3 poor metabolizers (PM), 2 intermediate metabolizers (IM) and seven extensive metabolizers (EM) received an oral dose of PPF. Concentrations of PPF and its metabolites were analyzed in serum samples over 27 h. Results The PPF/5OH-PPF ratio distinguished EMs from PMs, but not from IMs. In PMs, the mean transit time (MTT) values were almost the same for PPF and NOR-PPF and much higher than those of EMs and IMs. 5OH-PPF was not detected in EMs. Mean MTT values of 5OH-PPF and NOR-PPF in IMs were 5.27- and 1.52-fold higher than those of EMs. Conclusion A single time point serum PPF-MR approach is a useful tool to identify PMs. CYP2D6 polymorphism significantly affects the pharmacokinetics of PPF and its two metabolites. © 2016 Societe francaise de pharmacologie et de therapeutique

Style	Citing Format
MLA	Rouini MR, Afshar M. "Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux]." Therapie, vol. 72, no. 3, 2017, pp. 373-382.
APA	Rouini MR, Afshar M (2017). Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux]. Therapie, 72(3), 373-382.
Chicago	Rouini MR, Afshar M. "Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux]." Therapie 72, no. 3 (2017): 373-382.
Harvard	Rouini MR, Afshar M (2017) 'Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux]', Therapie, 72(3), pp. 373-382.
Vancouver	Rouini MR, Afshar M. Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux]. Therapie. 2017;72(3):373-382.
BibTex	@article{ author = {Rouini MR and Afshar M}, title = {Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux]}, journal = {Therapie}, volume = {72}, number = {3}, pages = {373-382}, year = {2017} }
RIS	TY - JOUR AU - Rouini MR AU - Afshar M TI - Effect of Cyp2d6 Polymorphisms on the Pharmacokinetics of Propafenone and Its Two Main Metabolites; [Effet De Polymorphismes Cyp2d6 Sur La Pharmacocinetique De La Propafenone Et Ses Deux Metabolites Principaux] JO - Therapie VL - 72 IS - 3 SP - 373 EP - 382 PY - 2017 ER -

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