The preclinical pharmacology and pharmacokinetic properties of (2R)-6-methoxy-8-(4-methylpiperazin-1-yl)-N-(4-morpholin-4-ylphenyl)chromane-2-carboxamide (AZD3783), a potent 5-hydroxytryptamine 1B (5-HT(1B)) receptor antagonist, were characterized as part of translational pharmacokinetic/pharmacodynamic hypothesis testing in human clinical trials. The affinity of AZD3783 to the 5-HT(1B) recepto...

the aim of this study was to investigate the pharmacokinetic profiles of baicalin, wogonoside, baicalein and wogonin after oral administration of pure baicalin, radix scutellariae and scutellariae-paeoniae couple extracts were administered and the pharmacokinetics profiles were compared between normal and ulcerative colitis rats. the plasma concentrations of the four flavonoids were determined ...

Although clinical responses in liquid tumors and certain lymphomas have been reported, the clinical efficacy of histone deacetylase inhibitors in solid tumors has been limited. This may be in part due to the poor pharmacokinetic of these drugs, resulting in inadequate tumor concentrations of the drug. SB939 is a new hydroxamic acid based histone deacetylase inhibitor with improved physicochemic...

Protein binding significantly influences pharmacokinetic properties of drug distribution. Albumin accounts for approximately 60% of the total plasma protein by mass, thereby making it the major protein in the body. Hypoalbuminemia, a type of hypoproteinemia, is a condition of abnormally low blood albumin levels. Hypoaluminemia causes pharmacokinetic issues in regards to dosing a patient's medic...

There are several excellent alternatives to warfarin on the horizon for atrial fibrillation. Results from the trials, as well as pharmacokinetic data from the edoxaban studies, suggest that dose selection, based on pharmacokinetic and pharmacodynamic properties, is a critical component in the development of novel anticoagulants. Greater flexibility in dosing with edoxaban and the opportunity fo...

The aim of this study was to characterize the effect of typhoid fever on pharmacokinetic parameters of levofloxacin (LF) and compare the pharmacokinetic parameters of the said antibiotic in healthy human volunteers and patients with typhoid fever. Total of 12 subjects were divided into two groups “A” (healthy volunteers) and “B” (typhoid patients). Single oral dose of LF 500 mg was given and 5 ...

INTRODUCTION Childhood obesity is common and results in substantial morbidity. The most commonly prescribed drugs in obese children are antibiotics. However, physiologic changes associated with childhood obesity can alter antibiotic pharmacokinetics and optimal body size measures to guide dosing in his population are ill defined. This combination can result in therapeutic failures or drug-relat...

We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data. This data set provides the drug metabolism scientist with a robust and accurate resource suitable for a number of applications, including in silico modeling, in vitro-in vivo scaling, and phy...

the objective of the present study was to evaluate the pharmacokinetic parameters and bioavailability of a selective histamine (h1)-receptor antagonist, cetirizine hydrochloride (ctz), following administration of a single oral dose of the drug. the properties of a test compound were compared with those of a reference product in a randomized cross-over study in 12 volunteers. blood samples were ...

The COVID-19 pandemic triggering acute respiratory syndrome is a major global health concern. SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) enzyme regulating viral replication has been evaluated as potential therapeutic target for inhibition of the infection SARS-CoV-2. In this study, we ability drug inhibitors by using molecular docking in silico model. Lipinski’s rule Five was used to evalua...