Clearance concepts in pharmacokinetics
No abstract listed.
Effect of perfusion rate and distribution factors on drug elimination kinetics in a perfused organ system
Application of clearance concepts to some literature data on drug metabolism in the isolated perfused liver preparation and in vivo
Pharmacokinetic basis for the influence of route of administration on the area under the plasma concentration-time curve
THE RENAL CLEARANCES OF SUBSTITUTED HIPPURIC ACID DERIVATIVES AND OTHER AROMATIC ACIDS IN DOG AND MAN
The effects of epoprostenol on drug disposition. I: A pilot study of the pharmacokinetics of digoxin with and without epoprostenol in patients with congestive heart failure
Moments of physiological transit time distributions and the time course of drug disposition in the body
Model independent derivation of general equations for the "first-pass" effect and extra-hepatic drug elimination
Induction of drug metabolism in man after rifampicin treatment measured by increased hexobarbital and tolbutamide clearance
Hepatic clearance of gitoxin: pharmacokinetic study on rabbit isolated liver. Influence of protein binding and comparison with digoxin
Application of physiologically based pharmacokinetic modeling and clearance concept to drugs showing transporter-mediated distribution and clearance in humans
Differential effect of biliary and micronodular cirrhosis on oxidative drug metabolism. In vivo-in vitro correlations of dextromethorphan metabolism in rat models
Application of clearance concepts to some literature data on drug metabolism in the isolated perfused liver preparation and in vivo
Pharmacokinetics of the enantiomers of hexobarbital studied in the same intact rat and in the same isolated perfused rat liver
Action by the lungs on circulating xenobiotic agents, with a case study of physiologically based pharmacokinetic modeling of benzo(a)pyrene disposition
Effect of fasting, induction, sex and age on clearance of benz(a)anthracene and chrysene by isolated perfused rat liver
Applications and prospects for physiologically based pharmacokinetic (PB-PK) models involving pharmaceutical agents
Effects of variability in hepatic clearance on the bioequivalence parameters of a drug and its metabolite: simulations using a pharmacostatistical model
'Albumin-receptor' uptake kinetics do not require an intact lobular architecture and are not specific for albumin
The effects of diet, aging and disease-states on presystemic elimination and oral drug bioavailability in humans
In vivo determination of drug kinetic linearity and individual organ elimination by the accelerated infusion technique
Interplay of drug metabolism and transport: a real phenomenon or an artifact of the site of measurement?
Controlling in vivo stability and biodistribution in electrostatically assembled nanoparticles for systemic delivery
Stereoselective central nervous system effects of the R- and S-isomers of the GABA uptake blocker N-(4, 4-di-(3-methylthien-2-yl)but-3-enyl) nipecotic acid in the rat
A study of factors influencing drug disposition in chronic liver disease, using the model drug (+)-propranolol
Biological determinants of propranolol disposition in normal subjects and patients with cirrhosis [proceedings
Reduction of oral bioavailability of lignocaine by induction of first pass metabolism in epileptic patients
Liver blood flow, antipyrine clearance, and antipyrine metabolite formation clearance in patients with chronic active hepatitis and alcoholic cirrhosis
Hepatic elimination of indocyanine green with special reference to distribution kinetics and the influence of plasma protein binding
Impact of ignoring extraction ratio when predicting drug-drug interactions, fraction metabolized, and intestinal first-pass contribution
Pharmacokinetics and pharmacodynamics of intravenous midazolam in patients with severe alcoholic cirrhosis
Quantitative prediction of in vivo drug clearance and drug interactions from in vitro data on metabolism, together with binding and transport
Increased clearance of antipyrine and d-propranolol after phenobarbital treatment in the monkey. Relative contributions of enzyme induction and increased hepatic blood flow
Verapamil favorably influences hepatic microvascular exchange and function in rats with cirrhosis of the liver
Time-variant increase in methylprednisolone clearance in patients with acute respiratory distress syndrome: a population pharmacokinetic study
Benet L Z and Galeazzi R L: noncompartmental determination of the steady-state volume of distribution, J Pharm Sci 68, 1071-1074, 1979--the backstory
Nonlinear mixed effects model analysis of the pharmacokinetics of aripiprazole in healthy Japanese males
The role of pharmacokinetic studies in drug discovery: where are we now, how did we get here and where are we going?
Alpha 1-acid glycoprotein-binding as a factor in age-related changes in the pharmacokinetics of trimethoprim in piglets
Role of oxidation polymorphism on blood and urine concentrations of amitriptyline and its metabolites in man
The effect of chlorpyrifos on thermogenic capacity of bank voles selected for increased aerobic exercise metabolism
Species differences in the metabolism of the antitumour agent 5,6-dimethylxanthenone-4-acetic acid in vitro: implications for prediction of metabolic interactions in vivo
The successes and failures of physiologically based pharmacokinetic modeling: there is room for improvement
Effect of microcirculatory heterogeneity on the determination of pharmacokinetic parameters: implications for risk assessment
Sandwich-cultured hepatocytes: utility for in vitro exploration of hepatobiliary drug disposition and drug-induced hepatotoxicity
The effect of intercellular distribution of drug-metabolizing enzymes on the kinetics of stable metabolite formation and elimination by liver: first-pass effects
Correlation of the intrinsic clearance of donepezil (Aricept) between in vivo and in vitro studies in rat, dog and human
A valid equation for the well-stirred perfusion limited physiologically based pharmacokinetic model that consistently accounts for the blood-tissue drug distribution in the organ and the corresponding valid equation for the steady state volume of distribution
Conceptual underestimation of the total body clearance by the sum of clearances of individual organs in physiologically based pharmacokinetics
Prediction of the possibility of the secondary peaks of iv bolus drug plasma concentration time curve by the model that directly takes into account the transit time through the organ
Prediction of the human oral bioavailability by using in vitro and in silico drug related parameters in a physiologically based absorption model
Prediction of the in vitro intrinsic clearance determined in suspensions of human hepatocytes by using artificial neural networks
Optimization of an isolated perfused rainbow trout liver model: Clearance studies with 7-ethoxycoumarin
Analysis of the impact of controlled release formulations on oral drug absorption, gut wall metabolism and relative bioavailability of CYP3A substrates using a physiologically-based pharmacokinetic model
Evaluation of a basic physiologically based pharmacokinetic model for simulating the first-time-in-animal study
Prediction of drug bioavailability in humans using immobilized artificial membrane phosphatidylcholine column chromatography and in vitro hepatic metabolic clearance
Prediction of human pharmacokinetics--evaluation of methods for prediction of hepatic metabolic clearance
On the observed large interspecies overprediction of human clearance ("vertical allometry") of UCN-01: further support for a proposed model based on plasma protein binding
Clinical significance of organic anion transporting polypeptides (OATPs) in drug disposition: their roles in hepatic clearance and intestinal absorption
Postoperative morphine concentration in infants with or without biliary atresia and its association with hepatic blood flow
Metabolic activation of phenanthrene by human and mouse cytochromes P450 and pharmacokinetics in CYP1A2 knockout mice
Influence of food on the absorption of the p-chlorophenolic ester of chlorophenoxyisobutyric acid in man
Pharmacokinetic and pharmacodynamic alterations of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors: drug-drug interactions and interindividual differences in transporter and metabolic enzyme functions
In vitro-in vivo extrapolation of quantitative hepatic biotransformation data for fish. I. A review of methods, and strategies for incorporating intrinsic clearance estimates into chemical kinetic models
Sex difference in antipyrine 3-hydroxylation. An in vivo-in vitro correlation of antipyrine metabolism in two rat strains
Metabolism of antipyrine in vivo in two rat models of liver cirrhosis. Its relationship to intrinsic clearance in vitro and microsomal membrane lipid composition
Intracellular binding is an important determinant of the avid hepatic uptake of the high clearance drug omeprazole
6-[18F]fluoro-L-dihydroxyphenylalanine metabolism and positron emission tomography after catechol-O-methyltransferase inhibition in normal and hemiparkinsonian monkeys
Hepatic extraction of chenodeoxycholic acid in dogs chronically intoxicated with dimethylnitrosamine
Selective effects of a bacterial infection (Actinobacillus pleuropneumoniae) on the hepatic clearances of caffeine, antipyrine, paracetamol, and indocyanine green in the pig
Using human recombinant UDP-glucuronosyltransferase isoforms and a relative activity factor approach to model total body clearance of laropiprant (MK-0524) in humans
Kinetics of hepatic transport of 4-methylumbelliferone in rats. Analysis by multiple indicator dilution method
Studies on the reliability of a bihyperbolic functional absorption model. I. Ring-substituted anilines
Axial tissue diffusion can account for the disparity between current models of hepatic elimination for lipophilic drugs
Effects of perfusate flow rate on measured blood volume, disse space, intracellular water space, and drug extraction in the perfused rat liver preparation: characterization by the multiple indicator dilution technique
General treatment of mean residence time, clearance, and volume parameters in linear mammillary models with elimination from any compartment
Theoretical considerations in the calculation of bioavailability of drugs exhibiting Michaelis-Menten elimination kinetics
Effect of plasma protein binding on drug disposition in muscle tissue: application of statistical moment analysis and network theory to in situ local single-pass perfusion system
Influence of plasma protein binding kinetics on hepatic clearance assessed from a "tube" model and a "well-stirred" model
Models of hepatic elimination: comparison of stochastic models to describe residence time distributions and to predict the influence of drug distribution, enzyme heterogeneity, and systemic recycling on hepatic elimination
Prediction of hepatic first-pass metabolism and plasma levels following intravenous and oral administration of barbiturates in the rabbit based on quantitative structure-pharmacokinetic relationships
Importance of "first-pass elimination" for interindividual differences in steady-state concentrations of the adrenergic beta-receptor antagonist alprenolol
A new method for assessment of drug disposition in muscle: application of statistical moment theory to local perfusion systems
Physiological modeling of drug and metabolite: disposition of oxazepam and oxazepam glucuronides in the recirculating perfused mouse liver preparation
Prediction of the disposition of beta-lactam antibiotics in humans from pharmacokinetic parameters in animals
An integrated approach to pharmacokinetic analysis for linear mammillary systems in which input and exit may occur in/from any compartment
Applications of a recirculatory stochastic pharmacokinetic model: limitations of compartmental models
Hepatic clearance of drugs. I. Theoretical considerations of a "well-stirred" model and a "parallel tube" model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance
Hepatic clearance of drugs. II. Experimental evidence for acceptance of the "well-stirred" model over the "parallel tube" model using lidocaine in the perfused rat liver in situ preparation
Hepatic clearance of drugs. III. Additional experimental evidence supporting the "well-stirred" model, using metabolite (MEGX) generated from lidocaine under varying hepatic blood flow rates and linear conditions in the perfused rat liver in situ preparation
Protein binding and hepatic clearance: discrimination between models of hepatic clearance with diazepam, a drug of high intrinsic clearance, in the isolated perfused rat liver preparation
An understanding of the role of enzyme localization of the liver on metabolite kinetics: a computer simulation
A comparative investigation of hepatic clearance models: predictions of metabolite formation and elimination
A dispersion model of hepatic elimination: 3. Application to metabolite formation and elimination kinetics
Contribution of intestinal cytochrome p450-mediated metabolism to drug-drug inhibition and induction interactions
Drug-drug interactions mediated through P-glycoprotein: clinical relevance and in vitro-in vivo correlation using digoxin as a probe drug
Influence of hypoxia on the metabolism and excretion of misonidazole by the isolated perfused rat liver--a model system
Use of HμREL Human Coculture System for Prediction of Intrinsic Clearance and Metabolite Formation for Slowly Metabolized Compounds
Prediction of in vivo developmental toxicity by combination of Hand1-Luc embryonic stem cell test and metabolic stability test with clarification of metabolically inapplicable candidates
Comparison of trout hepatocytes and liver S9 fractions as in vitro models for predicting hepatic clearance in fish
Hepatic clearance of 6 polycyclic aromatic hydrocarbons by isolated perfused trout livers: prediction from in vitro clearance by liver S9 fractions
The influence of Bacillus piliformis (Tyzzer) infections on the reliability of pharmacokinetic experiments in mice
Inhibition of glucuronidation and oxidative metabolism of buprenorphine using GRAS compounds or dietary constituents/supplements: in vitro proof of concept
Unequivocal evidence supporting the segregated flow intestinal model that discriminates intestine versus liver first-pass removal with PBPK modeling
Kinetics of peritoneal drug transport in rats: an application of the pore theory of transcapillary exchange
Clinical applicability of current pharmacokinetic models: splanchnic elimination of 5-fluorouracil in cancer patients
The role of hepatic biotransformation in mediating the acute toxicity of the phosphorothionate insecticide chlorpyrifos
In vitro-in vivo extrapolation of hepatic clearance involving active uptake: theoretical and experimental aspects
Use of unbound drug concentration in blood to discriminate between two models of hepatic drug elimination
Comment on: "Challenges in Individualizing Drug Dosage for Intensive Care Unit Patients: Is Augmented Renal Clearance What We Really Want to Know? Some Suggested Management Approaches and Clinical Software Tools"
The ontogeny and population variability of human hepatic dihydronicotinamide riboside:quinone oxidoreductase (NQO2)
Commentary on "The Universally Unrecognized Assumption in Predicting Drug Clearance and Organ Extraction Ratio"
New Perspectives in Clinical Pharmacokinetics-1: the Importance of Updating the Teaching in Pharmacokinetics that both Clearance and Elimination Rate Constant Approaches Are Mathematically Proven Equally Valid
Predicting Pharmacokinetics/Pharmacodynamics in the Individual Patient: Separating Reality From Hype.
Reliability of In Vitro Methods Used to Measure Intrinsic Clearance of Hydrophobic Organic Chemicals by Rainbow Trout: Results of an International Ring Trial
Unrepaired Tetralogy of Fallot-related Pathophysiologic Changes Reduce Systemic Clearance of Etomidate in Children
Michaelis-Menten elimination kinetics: areas under curves, steady-state concentrations, and clearances for compartment models with different types of input
Theoretical decrease in systemic availability with decrease in input rate at steady-state for first-pass drugs
Comparison of nonlinear pharmacokinetic parameters estimated from the sinusoidal perfusion and venous equilibrium models
Single intravenous dose and steady-state oral dose pharmacokinetics of nicardipine in healthy subjects
Single photon emission computed tomography to determine effective hepatic blood flow and intrahepatic shunting
A carrier-protein receptor is not a prerequisite for avid hepatic elimination of highly bound compounds: a study of propranolol elimination by the isolated perfused rat liver
Recovery of liver function in partially hepatectomized rats evaluated by aminopyrine demethylation capacity
Hepatic enzyme activity is the major factor determining elimination rate of high-clearance drugs in cirrhosis
Modeling of substrate elimination by the liver: has the albumin receptor model superseded the well-stirred model?
Introduction of quantitative methods in pharmacology and clinical pharmacology: a historical overview
Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERα covalent antagonist (SERCA)
Intra-arterial administration of hexobarbital enantiomers to the rat: disposition and estimation of apparent extraction ratio
Technical and physiological background of plasma volume measurement with indocyanine green: a clarification of misunderstandings
Interpretation of Non-Clinical Data for Prediction of Human Pharmacokinetic Parameters: In Vitro-In Vivo Extrapolation and Allometric Scaling
Prediction of Human Nonlinear Pharmacokinetics of a New Bcl-2 Inhibitor Using PBPK Modeling and Interspecies Extrapolation Strategy
Prediction of the pharmacokinetics of atorvastatin, cerivastatin, and indomethacin using kinetic models applied to isolated rat hepatocytes
Assessment of the impact of CYP3A polymorphisms on the formation of α-hydroxytamoxifen and N-desmethyltamoxifen in human liver microsomes
Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulation Approaches: A Systematic Review of Published Models, Applications, and Model Verification
Utility of in vitro systems and preclinical data for the prediction of human intestinal first-pass metabolism during drug discovery and preclinical development
A perspective on the prediction of drug pharmacokinetics and disposition in drug research and development
In vitro characterization of sarizotan metabolism: hepatic clearance, identification and characterization of metabolites, drug-metabolizing enzyme identification, and evaluation of cytochrome p450 inhibition
A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum
Comparative pharmacokinetics and pharmacodynamics of the advanced Retinol-Binding Protein 4 antagonist in dog and cynomolgus monkey
Formed and preformed metabolite excretion clearances in liver, a metabolite formation organ: studies on enalapril and enalaprilat in the single-pass and recirculating perfused rat liver
Metabolic Stability Assessment of New PARP Inhibitor Talazoparib Using Validated LC-MS/MS Methodology: In silico Metabolic Vulnerability and Toxicity Studies
Two-compartment dispersion model for analysis of organ perfusion system of drugs by fast inverse Laplace transform (FILT)
Expert Discussion of the Role of Rate Constant Versus Clearance Approaches to Define Drug Pharmacokinetics: Theoretical and Clinical Considerations.
In vitro hepatic oxidative metabolism of antipyrine, phenytoin and phenylbutazone in uraemic rabbits
Pharmacokinetics and biopharmaceutics of some adrenergic beta-receptor antagonists with special emphasis on alprenolol and metoprolol
Models of hepatic drug clearance: discrimination between the 'well stirred' and 'parallel-tube' models
Accumulation and clearance of capsanthin in blood plasma after the ingestion of paprika juice in men
Introduction of a composite parameter to the pharmacokinetics of venlafaxine and its active O-desmethyl metabolite
Drug absorption and hepatic drug metabolism in patients with different types of intestinal shunt operation for obesity. A study with phenazone
Characterization of Pharmacokinetics in the Göttingen Minipig with Reference Human Drugs: An In Vitro and In Vivo Approach
Author's Reply to Proost: "Challenges in Individualizing Drug Dosage for Intensive Care Unit Patients"
The impact of desorption kinetics from albumin on hepatic extraction efficiency and hepatic clearance: a model study
Relevance of In Vitro Metabolism Models to PET Radiotracer Development: Prediction of In Vivo Clearance in Rats from Microsomal Stability Data
Towards human ex vivo organ perfusion models to elucidate drug pharmacokinetics in health and disease
Galactose removal kinetics during hypoxia in perfused pig liver: reduction of Vmax, but not of intrinsic clearance Vmax/Km
Investigating the Theoretical Basis for In Vitro-In Vivo Extrapolation (IVIVE) in Predicting Drug Metabolic Clearance and Proposing Future Experimental Pathways.
Two compartment analysis of plasma elimination of phenazone in normals and in patients with cirrhosis of the liver
Absorption and metabolism of hexamethylmelamine and pentamethylmelamine in rat everted perfused gut segments: correlation with in-vivo data
Evaluation of the Disconnect between Hepatocyte and Microsome Intrinsic Clearance and In Vitro In Vivo Extrapolation Performance
LC-MS/MS Estimation of the Anti-Cancer Agent Tandutinib Levels in Human Liver Microsomes: Metabolic Stability Evaluation Assay
Role of pharmacokinetic consideration for the development of drug delivery systems: A historical overview
Prediction of Oral Pharmacokinetics Using a Combination of In Silico Descriptors and In Vitro ADME Properties.
Comparative Assessment of Extrapolation Methods Based on the Conventional Free Drug Hypothesis and Plasma Protein-Mediated Hepatic Uptake Theory for the Hepatic Clearance Predictions of Two Drugs Extensively Bound to Both the Albumin And Alpha-1-Acid Glycoprotein.
Establishing the dose-dependent daily variations of a low molecular weight heparin (Fraxiparine) through a population approach analysis in the rat
An examination of protein binding and protein-facilitated uptake relating to in vitro-in vivo extrapolation
GABAA receptor activity modulating piperine analogs: In vitro metabolic stability, metabolite identification, CYP450 reaction phenotyping, and protein binding
In vitro-in vivo extrapolation of quantitative hepatic biotransformation data for fish. II. Modeled effects on chemical bioaccumulation
Impact of hepatic uptake transporters on pharmacokinetics and drug-drug interactions: use of assays and models for decision making in the pharmaceutical industry
Relevance of desorption kinetics and permeability for in vitro-based predictions of hepatic clearance in fish.
There is Only One Valid Definition of Clearance: Critical Examination of Clearance Concepts Reveals the Potential for Errors in Clinical Drug Dosing Decisions.
Evaluation and comparison of in vitro intrinsic clearance rates measured using cryopreserved hepatocytes from humans, rats, and rainbow trout.
Recent developments in in vitro and in vivo models for improved translation of preclinical pharmacokinetics and pharmacodynamics data.
Pharmacokinetic aspects of sulfobromophthalein transport in chronically carbon tetrachloride-intoxicated rats
The Physical Adsorption of Gelatinized Starch with Tannic Acid Decreases the Inhibitory Activity of the Polyphenol against α-Amylase.
A Validated LC-MS/MS Assay for the Simultaneous Quantification of the FDA-Approved Anticancer Mixture (Encorafenib and Binimetinib): Metabolic Stability Estimation.
Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.
STING Receptor Agonists
Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.
Chronic Fatigue Syndrome
Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.
Spatio-Temporal Regulation of DNA Repair
DNA repair is a complex process regulated by several different classes of enzymes, including ligases, endonucleases, and polymerases. This feed focuses on the spatial and temporal regulation that accompanies DNA damage signaling and repair enzymes and processes.
Glut1 deficiency, an autosomal dominant, genetic metabolic disorder associated with a deficiency of GLUT1, the protein that transports glucose across the blood brain barrier, is characterized by mental and motor developmental delays and infantile seizures. Follow the latest research on Glut1 deficiency with this feed.
Hereditary Sensory Autonomic Neuropathy
Hereditary Sensory Autonomic Neuropathies are a group of inherited neurodegenerative disorders characterized clinically by loss of sensation and autonomic dysfunction. Here is the latest research on these neuropathies.
Separation anxiety is a type of anxiety disorder that involves excessive distress and anxiety with separation. This may include separation from places or people to which they have a strong emotional connection with. It often affects children more than adults. Here is the latest research on separation anxiety.
Neural Activity: Imaging
Imaging of neural activity in vivo has developed rapidly recently with the advancement of fluorescence microscopy, including new applications using miniaturized microscopes (miniscopes). This feed follows the progress in this growing field.
Applications of Molecular Barcoding
The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.