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Metabolite Pharmacokinetics - Europe PMC

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Last Updated: 13 May 2022

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Effect of quercetin on the pharmacokinetics of selexipag and its active metabolite in beagles.

Context Thercetin is a naturally occurring flavonoid with its glycosides, which is consumed at least 100 mg/day in food by an inhibitor cytochrome P450 family 2 subfamily C polypeptide 8. However, it is also unknown if quercetin and selexipag interact, which is also unknown. In beagles, the study investigated the effect of quercetin on the pharmacokinetics of selexipag and ACT-333679. The pharmacokinetics of selexipag and its potential mechanism were investigated by the pharmacokinetic parameters. According to a study conducted by 43. 08% and 26. 92 percent, respectively, treatment with quercetin resulted in an increase in C max and AUC 0-t of selexipag. Discussion and conclusion When co-administration, the study found quercetin could delay the metabolization of selexipag and ACT-333679. Therefore, the medical dose of selexipag should be treated with caution when co-administered with quercetin-rich foods.

Source link: https://europepmc.org/article/MED/34860644


Model-Based Meta-analysis for the Population Pharmacokinetics of Iberdomide and Its Major Active Metabolite in Healthy Subjects and Subjects with Relapse and Refractory Multiple Myeloma

Aim: Based on results from three scientific studies of iberdomide in healthy humans and patients with relapsed and refractory multiple myeloma, a parent-metabolite population pharmacokinetic model of iberdomide was developed, and the effect of socioeconomic and disease-related covariates on popPK parameters was evaluated. Methods of Studying Methods From data from 326 individuals in three scientific studies, nonlinear mixed effects modeling was used to create the popPK model. To link the one-compartment linear elimination metabolite model with the parent model, a first order conversion rate was used. Conclusion In conclusion, the parent-metabolite population pharmacokinetic model adequately portrayed the time course PK results of iberdomide and M12. The model can be used to support the dosing program for a special patient population as well as future iberdomide research design.

Source link: https://europepmc.org/article/PPR/PPR475018


Comparative Pharmacokinetics of Sulfadiazine and Its Metabolite N4-Acetyl Sulfadiazine in Grass Carp (Ctenopharyngodon idella) at Different Temperatures after Oral Administration.

Following a single oral administration of SDZ at 50 mg/kg in grass carp, the plasma pharmacokinetics and tissue disposition of sulfadiazine and its key metabolite, N4-acetyl sulfadiazine, were compared between 18 and 24 °C in this study. The temperature change affected SDZ and ACT-SDZ's pharmacokinetics in plasma and tissues, according to the study. The apparent total body clearance was also increased from 0. 93 to 0. 05 L/kg in plasma, and apparent systemic total body clearance was also increased from 0. 93 to 0. 05 L/kg.

Source link: https://europepmc.org/article/MED/35456543


Pharmacokinetics and anti-liver fibrosis characteristics of amygdalin: Key role of the deglycosylated metabolite prunasin.

Amy and its enzyme metabolite prunasin in vivo have not been investigated and compared, but Pru's Prunasin studies are limited. Purpose: Research seeks to determine whether Amy and its metabolite Pru in vivo and in vitro are physiokinetic, as well as in vitro, and to clarify whether Pru's metabolism is stimulated. The inhibitory effects of Amy and Pru on hepatic stellate cell proliferation and macrophage inflammation in JS1 and RAW 264. 7 cells were determined. The improvement of Amy and Pru on liver fibrosis effects in mice by a CCl 4 -induced liver fibrosis model were thoroughly reviewed by a mouse model. After Amy's oral administration of Amy, the Cmax and AUC of Pru were almost 79. 51-fold higher than those of Amy. The Vmax and K m of Pru were lower than those of Amy in commercial glucosidase and intestinal bacteria, according to the results of enzyme hydrolysis kinetics assay. Amy and Pru were similar in inhibiting the NO production in the RAW264. 7 cell supernatant and the mRNA expression of -SMA and Col1A1 in JS1 cells, according to In vitro cellular assays. Amy and Pru were both shown to have similar success in treating CCl 4-induced liver fibrosis in mice. Conclusions The pharmacokinetic characteristics of Amy and Pru in rat plasma were significantly different. In vivo and vitro, Amy and its deglycosylated metabolite Pru were similar to those in vitro and in vitro.

Source link: https://europepmc.org/article/MED/35247668


Pharmacokinetics of alectinib and its metabolite M4 in a patient with advanced lung adenocarcinoma undergoing hemodialysis: A case report.

This report presents the first comprehensive pharmacokinetic results of alectinib and its derivative M4 in a patient with an anaplastic lymphoma kinase adenocarcinoma undergoing hemodialysis in a patient with an acute lymphoma kinase. The highest detected plasma concentrations of alectinib and M4 were 638 and 82 ng/ml when the patient was given a daily 300 mg bid dose of alectinib were 638 and 82 ng/ml, respectively at steady-state.

Source link: https://europepmc.org/article/MED/35191596

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions