Effect of CYP2C9 Polymorphisms on the Pharmacokinetics of Indomethacin During Pregnancy

التفاصيل البيبلوغرافية
العنوان: Effect of CYP2C9 Polymorphisms on the Pharmacokinetics of Indomethacin During Pregnancy
المؤلفون: Raman Venkataramanan, Sherif Z. Abdel-Rahman, Maged M. Costantine, Poonam Shah, Shannon M. Clark, Erik Rytting, Meixiang Xu, Steve N. Caritis, Xiaoming Wang, Holly West, Gary D.V. Hankins, Mansi Shah, Tatiana N. Nanovskaya, Mahmoud Ahmed
المصدر: European journal of drug metabolism and pharmacokinetics. 44(1)
سنة النشر: 2018
مصطلحات موضوعية: Adult, Tocolytic agent, Adolescent, Clinical chemistry, Metabolite, Buccal swab, Indomethacin, Pharmacology, 030226 pharmacology & pharmacy, Article, 03 medical and health sciences, chemistry.chemical_compound, Young Adult, 0302 clinical medicine, Pharmacokinetics, Polymorphism (computer science), Pregnancy, Genotype, Medicine, Humans, Pharmacology (medical), CYP2C9, Cytochrome P-450 CYP2C9, Polymorphism, Genetic, business.industry, Anti-Inflammatory Agents, Non-Steroidal, chemistry, 030220 oncology & carcinogenesis, Female, business
الوصف: BACKGROUND AND OBJECTIVE: CYP2C9 catalyzes the biotransformation of indomethacin to its inactive metabolite O-desmethylindomethacin (DMI). The aim of this work was to determine the effect of CYP2C9 polymorphisms on indomethacin metabolism in pregnant women. METHODS: Plasma concentrations of indomethacin and DMI at steady state were analyzed with a validated LC-MS/MS method. DNA was isolated from subject blood and buccal smear samples. Subjects were grouped by genotype for comparisons of pharmacokinetic parameters. RESULTS: For subjects with the *1/*2 genotype, the mean CL/F(ss) of indomethacin was 13.5 ± 7.7 L/h (n=4) and the mean metabolic ratio (AUC(DMI)/AUC(indomethacin)) was 0.291 ± 0.133. For subjects with the *1/*1 genotype, these values were 12.4 ± 2.7 L/h and 0.221 ± 0.078, respectively (n=14). Of note, we identified one subject who was a carrier of both the *3 and *4 alleles, resulting in an amino acid change (I359P) which has not been reported previously. This subject had a metabolic ratio of 0.390 and a steady-state apparent oral clearance of indomethacin (24.3 L/h) that was nearly double the wild-type clearance. CONCLUSION: Although our results are limited by sample size and are not statistically significant, these data suggest that certain genetic polymorphisms of CYP2C9 may lead to an increased metabolic ratio and an increase in the clearance of indomethacin. More data are needed to assess the impact of CYP2C9 genotype on the effectiveness of indomethacin as a tocolytic agent.
تدمد: 2107-0180
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c16546bf0c164166fb1feb74b4caac9
https://pubmed.ncbi.nlm.nih.gov/30159654
Rights: OPEN
رقم الانضمام: edsair.doi.dedup.....3c16546bf0c164166fb1feb74b4caac9
قاعدة البيانات: OpenAIRE