Advanced searches left 3/3

Metabolite Pharmacokinetics - Wiley Online Library

Summarized by Plex Scholar
Last Updated: 13 May 2022

* If you want to update the article please login/register

Development and validation of an LC–MS/MS method for simultaneous determination of remdesivir and its hydrolyzed metabolite and nucleoside, and its application in a pharmacokinetic study of normal and diabetic nephropathy mice

It is the first antiviral drug on the U. S. Food and Drug Administration for the treatment of COVID 19-19. 19 To improve RV in mouse blood, the phosphatase inhibitor PhosSTOP and carboxylesterase inhibitor 5,5′dithiobis2–nitrobenzoic acid were used here. After intravenous injection of RDV at 20 mg/kg, normal and diabetic nephropathy DBA/2 J mice, this technique was successfully used to analyze RDV, RM442, and RN in the blood of healthy and diabetic nephropathy DBA/2 J mice. There was a significant difference between the normal and diabetic nephropathy mice under the concentration-time curve, which revealed a significant difference.

Source link: https://onlinelibrary.wiley.com/doi/10.1002/bmc.5380


Pharmacokinetics of Daprodustat and Metabolites in Individuals with Normal and Impaired Hepatic Function

In participants with mild and moderate hepatic impairment, respectively, compared to controls, there were 1. 5 and 2. 0 fold greater daprostat Cmax and area under the curve exposures in participants with mild and moderate hepatic impairment, respectively, as well as controls; Cmax in mild hepatic impairment was comparable to controls. In comparison to hepaticimpaired participants, matched controls were 0. 3-fold less and 2. 2 percent higher. Compared to matched controls, Daprodustat use was elevated in participants with moderate and mild hepatic impairment, relative to matched controls; however, no significant differences in EPO were found and no new safety concerns were raised; however, no new safety issues were raised.

Source link: https://onlinelibrary.wiley.com/doi/10.1002/cpdd.1090


Effects of elagolix on the pharmacokinetics of omeprazole and its metabolites in healthy premenopausal women

This review examined the effects of repeated doses of elagolix on the pharmacokinetics of omeprazole and its metabolites in healthy premenopausal female subjects. On day 1 and day 11, and in oral and oral doses of elagolix twice daily, the adult premenopausal female subjects were given a single oral dose of omeprazole on day 1 and day 11 and then, as well as oral doses of elagolix twice daily on days 3–11. After dosing on days 1 and 11, serial blood samples for assay of omeprazole and its metabolites were collected for 24 h. The elagolix 300 mg tablete dosage twice a day for nine days increased omeprazole exposure by 1. 8 percent and reduced the metabolite-to-parent ratio by 60%. In CYP2C19 extensive and intermediate metabolism testers, the omeprazole exposures increased by 22% to 2. 5 fold, but poor metabolizer subjects showed decreased omeprazole exposures by 40%. Omeprazole may cause drug interactions due to several mechanisms other than CYP2C19-mediated metabolism, causing confusion in the interpretation of results from omeprazole DDI studies.

Source link: https://onlinelibrary.wiley.com/doi/10.1111/cts.13247


Comparative analysis of absorbed ingredients and metabolites, and pharmacokinetic studies of Zhimu–Huangbai herb pair in the plasma of normal and type 2 diabetes mellitus rats by UHPLC‐linear trap quadrupole‐orbitrap MS and LC‐MS/MS

Seven key bioactive ingredients in normal and type 2 diabetes mellitus rats were found and validated in pharmacokinetic comparative research of seven key bioactive components. The plasma of type 2 diabetes mellitus rats was significantly different from those in normal rats, according to partial pharmacokinetic parameters. This is the first comparison of absorbent components and metabolites of Zhimu-Huangbai's herb pair, as well as its use in pharmacokinetic studies of type 2 diabetes mellitus rats, to our knowledge.

Source link: https://onlinelibrary.wiley.com/doi/10.1002/jssc.202100582


Effects of Renal Impairment on the Pharmacokinetics of Abrocitinib and Its Metabolites

Following a 200-mg oral dose, a nonrandomized, open-label, single-dose study looked at the effects of renal impairment on absorption, stability, and tolerability of abrocitinib and its metabolites. According to subjects with moderate renal impairment vs. normal renal function, the GMRs of unbound area under the concentration time curve were 210. 20 and 133. 87, respectively. Patients with moderate to severe renal impairment were prone to more abductinib-active moiety, which means that abrocitinib doses should be reduced by half for patients with moderate or severe renal impairment.

Source link: https://onlinelibrary.wiley.com/doi/10.1002/jcph.1980

* 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