The human hepatic metabolism of simvastatin hydroxy acid is …
To identify the cytochrome P450 (CYP) isoforms responsible for the metabolism of simvastatin hydroxy acid (SVA), the most potent metabolite of simvastatin (SV). The metabolism of SVA was characterized in vitro using human liver microsomes and recombinant CYPs.
Pharmacokinetic Aspects of Statins - IntechOpen
2020年3月28日 · Simvastatin, lovastatin, and atorvastatin are metabolized by CYP3A4 isoenzymes, so they will have more significant interactions than fluvastatin, pitavastatin, and rosuvastatin that require CYP2C9.
Detection and characterization of simvastatin and its metabolites …
2022年3月19日 · Simvastatin (SV) is a hypolipidemic agent, and it is the 2nd most widely prescribed lipid-lowering drug. Here, the detection and characterization of SV and its metabolites was studied in selected...
Clinical Pharmacokinetics and Practical Applications of Simvastatin ...
2012年11月9日 · Increasing the dose of simvastatin from 5 to 120mg increases the pharmacological activity in a linear fashion. The several metabolites tend to remain within the liver and the intestines (via biliary excretion). Some gastrointestinal reabsorption of metabolites may …
Comparative Hepatic and Intestinal Metabolism and Pharmacodynamics of ...
2021年8月1日 · Atorvastatin lactone and simvastatin (lactone) showed extensive metabolism [intrinsic clearance (CLint) values of 3700 and 7400 µl/min per milligram], whereas the metabolism of the lactones of 2-hydroxyatorvastatin, 4-hydroxyatorvastatin, and pitavastatin was slower (CLint 20–840 µl/min per milligram).
In vitro metabolism of simvastatin in humans [SBT]identification …
Simvastatin (SV) is a lactone prodrug used for the treatment of hypercholesterolemia. Upon incubation of SV with liver microsomal preparations from human donors, four major metabolic products were formed (3'-hydroxy SV, 6'-exomethylene SV, 3',5'-dihydrodiol SV, and the active hydroxy acid, SVA), tog …
Metabolite Signature of Simvastatin Treatment Involves Multiple ...
Our study reports statistically significant changes in multiple metabolite concentrations in the participants on simvastatin treatment indicating that simvastatin exerts profound pleiotropic effects on different metabolite pathways, affecting not only lipids, but also amino acids, peptides, nucleotides, carbohydrates, co-factors, vitamins, and ...
In Vitro Metabolism of Simvastatin in Humans [sbt]Identification …
1997年10月1日 · Simvastatin (SV) is a lactone prodrug used for the treatment of hypercholesterolemia. Upon incubation of SV with liver microsomal preparations from human donors, four major metabolic products were formed (3′-hydroxy SV, 6′-exomethylene SV, 3′,5′-dihydrodiol SV, and the active hydroxy acid, SVA), together …
In vitro metabolism of simvastatin in humans [SBT]identification …
1997年10月1日 · Three newly identified metabolites of simvastatin hydroxy acid are reported, including two new dihydroxy glutathione adducts and a trihydroxy derivative of SVA, all found in rat bile and only metabolite III was also observed in dog bile.
Clinical pharmacokinetics of statins - PubMed
All statins but pravastatin show highly active metabolites, the pharmacological activity depending on the kinetic profile of both parent compound and active metabolites. Pravastatin has the lowest protein binding (50% vs. > 90%) and is eliminated by both metabolism and renal excretion.