دورية أكاديمية

Effects of CYP2D6 *10 and *41 Variants in Healthy Chinese Men on the Pharmacokinetics of Dapoxetine.

التفاصيل البيبلوغرافية
العنوان: Effects of CYP2D6 *10 and *41 Variants in Healthy Chinese Men on the Pharmacokinetics of Dapoxetine.
المؤلفون: Wang Z; School of Pharmacy Lanzhou University, Lanzhou, Gansu, China., Gao Y; School of Pharmacy Lanzhou University, Lanzhou, Gansu, China., Ji X; School of Pharmacy Lanzhou University, Lanzhou, Gansu, China., Wu T; School of Pharmacy Lanzhou University, Lanzhou, Gansu, China., Pu L; School of Pharmacy Lanzhou University, Lanzhou, Gansu, China., Qiu W; National Drug Clinical Trial Institution, Lanzhou University Second Hospital, Lanzhou, Gansu, China.; Pharmacy Department, Lanzhou University Second Hospital, Lanzhou, Gansu, China.
المصدر: Journal of clinical pharmacology [J Clin Pharmacol] 2024 May; Vol. 64 (5), pp. 601-608. Date of Electronic Publication: 2024 Jan 04.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Wiley Country of Publication: England NLM ID: 0366372 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1552-4604 (Electronic) Linking ISSN: 00912700 NLM ISO Abbreviation: J Clin Pharmacol Subsets: MEDLINE
أسماء مطبوعة: Publication: 2013- : Oxford : Wiley
Original Publication: Stamford, Conn., Hall Associates.
مواضيع طبية MeSH: Cytochrome P-450 CYP2D6*/genetics , Cytochrome P-450 CYP2D6*/metabolism , Benzylamines*/pharmacokinetics , Benzylamines*/administration & dosage , Benzylamines*/blood , Naphthalenes*/pharmacokinetics , Naphthalenes*/administration & dosage , Selective Serotonin Reuptake Inhibitors*/pharmacokinetics , Selective Serotonin Reuptake Inhibitors*/blood , Selective Serotonin Reuptake Inhibitors*/administration & dosage , Asian People*/genetics , Genotype*, Humans ; Male ; Adult ; Young Adult ; Polymorphism, Genetic ; Area Under Curve ; Healthy Volunteers ; East Asian People
مستخلص: Dapoxetine is a selective serotonin reuptake inhibitor (SSRI) used to treat premature ejaculation (PE), and is mainly metabolized by CYP2D6, CYP3A4, and flavin-containing monooxygenase 1. The purpose of the study was to evaluate the effect of CYP2D6 polymorphism on the pharmacokinetics of dapoxetine in healthy Chinese men. Thirty-nine subjects who received a single oral dose of 30 mg dapoxetine hydrochloride were classified based on their CYP2D6 genotype: *1/*1 (n = 9), *1/*41 (n = 1), *1/*10 (n = 12), *10/*41 (n = 3), or *10/*10 (n = 14). The difference in pharmacokinetic parameters between different genotype groups was analyzed and then scored according to the activity score system. Compared with the wild-type subjects of CYP2D6 *1/*1, the peak plasma concentration (C max ) and the area under the plasma drug concentration-time curve (AUC inf ) of dapoxetine in the *10/*10 and *10/*41 groups were notably increased (P ≤ .05). Significant differences in C max , AUC, volume of distribution/bioavailability (V/F) and clearance/bioavailability (CL/F) were observed among dapoxetine activity score groups (P ≤ .05). The AUC inf was increased significantly (154% and 89.73%, P ≤ .05) and the C max was increased significantly (73.45% and 42.67%, P ≤ .05) in CYP2D6 *10/*41 subjects, compared with CYP2D6 *1/*1 and *1/*10 subjects. The results obtained indicated that CYP2D6 *10 and *41 polymorphisms have significant effects on the pharmacokinetic properties of dapoxetine.
(© 2023, The American College of Clinical Pharmacology.)
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فهرسة مساهمة: Keywords: CYP2D6 *10; CYP2D6 *41; activity score; dapoxetine; pharmacokinetics; premature ejaculation
المشرفين على المادة: GB2433A4M3 (dapoxetine)
EC 1.14.14.1 (Cytochrome P-450 CYP2D6)
0 (Benzylamines)
0 (Naphthalenes)
0 (Selective Serotonin Reuptake Inhibitors)
تواريخ الأحداث: Date Created: 20231207 Date Completed: 20240424 Latest Revision: 20240508
رمز التحديث: 20240509
DOI: 10.1002/jcph.2391
PMID: 38059315
قاعدة البيانات: MEDLINE