دورية أكاديمية
Rerouting cardiovascular management following gastric bypass surgery: Dose optimization of carvedilol using population-based analysis.
| العنوان: | Rerouting cardiovascular management following gastric bypass surgery: Dose optimization of carvedilol using population-based analysis. |
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| المؤلفون: | Yamamoto PA; Center for Pharmacometrics and Systems Pharmacology, College of Pharmacy, University of Florida, Orlando, FL, USA.; School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo (USP), Ribeirão Preto, SP, Brazil., Vozmediano V; Center for Pharmacometrics and Systems Pharmacology, College of Pharmacy, University of Florida, Orlando, FL, USA., Cristofoletti R; Center for Pharmacometrics and Systems Pharmacology, College of Pharmacy, University of Florida, Orlando, FL, USA., Jiang J; Cancer Genetics Research Complex, College of Pharmacy, University of Florida, Gainesville, FL, USA., Schmittgen TD; Cancer Genetics Research Complex, College of Pharmacy, University of Florida, Gainesville, FL, USA., de Gaitani CM; School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo (USP), Ribeirão Preto, SP, Brazil., Kemp R; School of Medicine of Ribeirão Preto, University of São Paulo (USP), Ribeirão Preto, SP, Brazil., Sankarankutty AK; School of Medicine of Ribeirão Preto, University of São Paulo (USP), Ribeirão Preto, SP, Brazil., Dos Santos JS; School of Medicine of Ribeirão Preto, University of São Paulo (USP), Ribeirão Preto, SP, Brazil., Salgado Junior W; School of Medicine of Ribeirão Preto, University of São Paulo (USP), Ribeirão Preto, SP, Brazil., de Moraes NV; Center for Pharmacometrics and Systems Pharmacology, College of Pharmacy, University of Florida, Orlando, FL, USA. |
| المصدر: | British journal of clinical pharmacology [Br J Clin Pharmacol] 2024 Sep; Vol. 90 (9), pp. 2223-2235. Date of Electronic Publication: 2024 Jun 09. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Wiley-Blackwell Country of Publication: England NLM ID: 7503323 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1365-2125 (Electronic) Linking ISSN: 03065251 NLM ISO Abbreviation: Br J Clin Pharmacol Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Wiley-Blackwell Original Publication: London, Macmillan Journals Ltd. |
| مواضيع طبية MeSH: | Carvedilol*/administration & dosage , Carvedilol*/pharmacokinetics , Gastric Bypass*/adverse effects , Models, Biological* , Propanolamines*/pharmacokinetics , Propanolamines*/administration & dosage , Carbazoles*/administration & dosage , Carbazoles*/pharmacokinetics, Humans ; Male ; Female ; Adult ; Middle Aged ; Multidrug Resistance-Associated Protein 2 ; Adrenergic beta-Antagonists/pharmacokinetics ; Adrenergic beta-Antagonists/administration & dosage ; Dose-Response Relationship, Drug ; Biological Availability ; Multidrug Resistance-Associated Proteins/metabolism ; Multidrug Resistance-Associated Proteins/genetics ; Obesity/surgery ; Heart Rate/drug effects ; Administration, Oral ; Aged |
| مستخلص: | Aims: A population-based pharmacokinetic (PK) modeling approach (PopPK) was used to investigate the impact of Roux-en-Y gastric bypass (RYGB) on the PK of (R)- and (S)-carvedilol. We aimed to optimize carvedilol dosing for these patients utilizing a pharmacokinetic/pharmacodynamic (PK/PD) link model. Methods: PopPK models were developed utilizing data from 52 subjects, including nonobese, obese, and post- RYGB patients who received rac- carvedilol orally. Covariate analysis included anthropometric and laboratory data, history of RYGB surgery, CYP2D6 and CYP3A4 in vivo activity, and relative intestinal abundance of major drug- metabolizing enzymes and transporters. A direct effect inhibitory E Results: A 2-compartmental model with linear elimination and parallel first-order absorptions best described (S)-carvedilol PK. RYGB led to a twofold reduction in relative oral bioavailability compared to nonoperated subjects, along with delayed absorption of both enantiomers. The intestinal ABCC2 mRNA expression increases the time to reach the maximum plasma concentration. The reduced exposure (AUC) of (S)-carvedilol post-RYGB corresponded to a 33% decrease in the predicted area under the effect curve (AUEC) for the 24-hour β-blocker response. Simulation results suggested that a 50-mg daily dose in post-RYGB patients achieved comparable AUC and AUEC to 25-mg dose in nonoperated subjects. Conclusion: Integrated PK/PD modeling indicated that standard dosage regimens for nonoperated subjects do not provide equivalent β-blocking activity in RYGB patients. This study highlights the importance of personalized dosing strategies to attain desired therapeutic outcomes in this patient cohort. (© 2024 British Pharmacological Society.) |
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| معلومات مُعتمدة: | 18/06569-9 Fundação de Amparo à Pesquisa do Estado de São Paulo; Finance Code 001 Coordenação de Aperfeiçoamento de Pessoal de Nível Superior |
| فهرسة مساهمة: | Keywords: carvedilol; gastric bypass; pharmacokinetics; population‐based analysis |
| المشرفين على المادة: | 0K47UL67F2 (Carvedilol) 0 (Propanolamines) 0 (Carbazoles) 0 (Multidrug Resistance-Associated Protein 2) 0 (ABCC2 protein, human) 0 (Adrenergic beta-Antagonists) 0 (Multidrug Resistance-Associated Proteins) |
| تواريخ الأحداث: | Date Created: 20240609 Date Completed: 20240829 Latest Revision: 20240829 |
| رمز التحديث: | 20240830 |
| DOI: | 10.1111/bcp.16129 |
| PMID: | 38852609 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1365-2125 |
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| DOI: | 10.1111/bcp.16129 |