Sources of interindividual variability in IVIVE of clearance: an investigation into the prediction of benzodiazepine clearance using a mechanistic population-based pharmacokinetic model

No abstract is available for this paper.

• Publication year

  2011

• Venue

  Xenobiotica; the fate of foreign compounds in biological systems

• Publication date

  2011-07-06

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.3109/00498254.2011.560294PMID 21434772
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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• Prediction of Human Metabolic Clearance from In Vitro Systems: Retrospective Analysis and Prospective View

  2010influential reference
• Estimation of the interindividual variability of cytochrome 2D6 activity from urinary metabolic ratios in the literature.

  2010cited by this paper
• Determination of a quantitative relationship between hepatic CYP3A5*1/*3 and CYP3A4 expression for use in the prediction of metabolic clearance in virtual populations

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  2010cited by this paper
• Semiphysiologically Based Pharmacokinetic Models for the Inhibition of Midazolam Clearance by Diltiazem and Its Major Metabolite

  2009cited by this paper
• The Simcyp population-based ADME simulator.

  2009cited by this paper
• In vitro and in vivo glucuronidation of midazolam in humans.

  2009cited by this paper
• The Simcyp® Population-based ADME Simulator

  2009cited by this paper
• Evaluation of Recombinant Cytochrome P450 Enzymes as an in Vitro System for Metabolic Clearance Predictions

  2009cited by this paper
• Methods for predicting in vivo pharmacokinetics using data from in vitro assays.

  2008cited by this paper
• A novel screening strategy to identify ABCB1 substrates and inhibitors

  2008cited by this paper
• Covariation of Human Microsomal Protein Per Gram of Liver with Age: Absence of Influence of Operator and Sample Storage May Justify Interlaboratory Data Pooling

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• Interaction Profile of Armodafinil with Medications Metabolized by Cytochrome P450 Enzymes 1A2, 3A4 and 2C19 in Healthy Subjects

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• Comparison of different approaches to predict metabolic drug–drug interactions

  2007cited by this paper
• Simulation and prediction of in vivo drug metabolism in human populations from in vitro data

  2007cited by this paper
• Prediction of intestinal first-pass drug metabolism.

  2007cited by this paper
• Pomegranate Juice Does Not Impair Clearance of Oral or Intravenous Midazolam, a Probe for Cytochrome P450‐3A Activity: Comparison With Grapefruit Juice

  2007cited by this paper
• Approach to predict the contribution of cytochrome P450 enzymes to drug metabolism in the early drug-discovery stage: The effect of the expression of cytochrome b5 with recombinant P450 enzymes

  2007cited by this paper
• Relative roles of CYP2C19 and CYP3A4/5 in midazolam 1′-hydroxylation

  2007cited by this paper
• Effect of Polymorphic CYP3A5 Genotype on the Single‐Dose Simvastatin Pharmacokinetics in Healthy Subjects

  2007cited by this paper
• Scaling factors for the extrapolation of in vivo metabolic drug clearance from in vitro data: reaching a consensus on values of human microsomal protein and hepatocellularity per gram of liver.

  2007cited by this paper
• EFFECT OF CYP3A5 POLYMORPHISM ON TACROLIMUS METABOLIC CLEARANCE IN VITRO

  2006cited by this paper
• Intestinal and Hepatic Metabolic Activity of Five Cytochrome P450 Enzymes: Impact on Prediction of First-Pass Metabolism

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• Characterization of the Rhesus Monkey CYP3A64 Enzyme: Species Comparisons of CYP3A Substrate Specificity and Kinetics Using Baculovirus-Expressed Recombinant Enzymes

  2006cited by this paper
• Prediction of in vivo drug clearance from in vitro data. I: Impact of inter-individual variability

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• Comparative analysis of substrate and inhibitor interactions with CYP3A4 and CYP3A5

  2006cited by this paper
• Pharmacokinetics of an Extended Release Formulation of Alprazolam (Xanax XR) in Healthy Normal Adolescent and Adult Volunteers

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• Enzymatic characteristics of CYP3A5 and CYP3A4: A comparison of in vitro kinetic and drug–drug interaction patterns

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• Activity of CYP2E1 and CYP3A enzymes in adults with moderate alcohol consumption: A comparison with nonalcoholics

  2005cited by this paper
• Kinetics and Dynamics of Intravenous Adinazolam, N‐Desmethyl Adinazolam, and Alprazolam in Healthy Volunteers

  2005cited by this paper
• Textbook of Medical Physiology

  2005cited by this paper
• Microsomal prediction of in vivo clearance and associated interindividual variability of six benzodiazepines in humans

  2005cited by this paper
• Influence of dosing regimen on alprazolam and metabolite serum concentrations and tolerance to sedative and psychomotor effects

  2005cited by this paper
• Predicting in vivo drug interactions from in vitro drug discovery data

  2005cited by this paper
• Changes in liver volume from birth to adulthood: A meta‐analysis

  2005influential reference
• Oral administration of a low dose of midazolam (75 μg) as an in vivo probe for CYP3A activity

  2004cited by this paper
• Oral administration of a low dose of midazolam (75 microg) as an in vivo probe for CYP3A activity.

  2004cited by this paper
• Intravenous and oral alfentanil as in vivo probes for hepatic and first‐pass cytochrome P450 3A activity: Noninvasive assessment by use of pupillary miosis

  2004cited by this paper
• Predicting drug clearance from recombinantly expressed CYPs: intersystem extrapolation factors

  2004cited by this paper
• Pharmacokinetics and pharmacodynamics of alprazolam after oral and IV administration

  2004cited by this paper
• Kinetics and EEG Effects of Midazolam during and after 1‐Minute, 1‐Hour, and 3‐Hour Intravenous Infusions

  2004cited by this paper
• Validated assays for human cytochrome P450 activities.

  2004cited by this paper
• EVIDENCE OF SIGNIFICANT CONTRIBUTION FROM CYP3A5 TO HEPATIC DRUG METABOLISM

  2004cited by this paper
• UTILITY OF RECOMBINANT ENZYME KINETICS IN PREDICTION OF HUMAN CLEARANCE: IMPACT OF VARIABILITY, CYP3A5, AND CYP2C19 ON CYP3A4 PROBE SUBSTRATES

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  2004cited by this paper
• In vivo comparisons of constitutive cytochrome P450 3A activity assessed by alprazolam, triazolam, and midazolam

  2004influential reference
• A pharmacokinetic and pharmacodynamic evaluation of the combined administration of alprazolam and fluvoxamine

  2004cited by this paper
• Comparison of alprazolam plasma levels in normal Asian and Caucasian male volunteers

  2004cited by this paper
• Inter-individual variability in levels of human microsomal protein and hepatocellularity per gram of liver.

  2003cited by this paper
• Cytochrome P450 inhibition using recombinant proteins and mass spectrometry/multiple reaction monitoring technology in a cassette incubation.

  2003cited by this paper
• In vitro inhibitory effect of 1-aminobenzotriazole on drug oxidations catalyzed by human cytochrome P450 enzymes: a comparison with SKF-525A and ketoconazole.

  2003cited by this paper
• Pharmacokinetic and Pharmacodynamic Interactions of Oral Midazolam with Ketoconazole, Fluoxetine, Fluvoxamine, and Nefazodone

  2003cited by this paper
• Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR‐1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus

  2003influential reference
• Comparative analysis of CYP3A expression in human liver suggests only a minor role for CYP3A5 in drug metabolism.

  2003cited by this paper
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• The effect of age, sex, and rifampin administration on intestinal and hepatic cytochrome P450 3A activity

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• Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7.

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• In Vitro/in Vivo scaling of alprazolam metabolism by CYP3A4 and CYP3A5 in humans

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  2001influential reference
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  2001influential reference
• Alprazolam‐ritonavir interaction: Implications for product labeling

  2000cited by this paper
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  1998cited by this paper
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  1998cited by this paper
• Development of a comprehensive panel of antibodies against the major xenobiotic metabolising forms of cytochrome P450 in humans.

  1998influential reference
• Inhibition of triazolam clearance by macrolide antimicrobial agents: In vitro correlates and dynamic consequences

  1998cited by this paper
• Ketoconazole inhibition of triazolam and alprazolam clearance: Differential kinetic and dynamic consequences

  1998cited by this paper
• The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data.

  1997cited by this paper
• Triazolam is ineffective in patients taking rifampin

  1997cited by this paper
• Incorporation of in vitro drug metabolism data into physiologically-based pharmacokinetic models.

  1997cited by this paper
• Pharmacokinetics and Psychomotor Performance of Alprazolam: Concentration—Effect Relationship

  1997cited by this paper
• Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism.

  1997influential reference
• Diltiazem enhances the effects of triazolam by inhibiting its metabolism

  1996cited by this paper
• Oral first‐pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A‐mediated metabolism

  1996cited by this paper
• The Effect of the Systemic Antimycotics, Itraconazole and Fluconazole, on the Pharmacokinetics and Pharmacodynamics of Intravenous and Oral Midazolam

  1996cited by this paper
• Coadministration of nefazodone and benzodiazepines: II. A pharmacokinetic interaction study with triazolam.

  1995cited by this paper
• Pharmacokinetics and pharmacodynamics of triazolam after two intermittent doses in obese and normal-weight men.

  1995influential reference
• Coadministration of nefazodone and benzodiazepines: III. A pharmacokinetic interaction study with alprazolam.

  1995cited by this paper
• Azithromycin does not increase plasma concentrations of oral midazolam.

  1995cited by this paper
• Triazolam pharmacokinetics after intravenous, oral, and sublingual administration.

  1995influential reference
• Interaction between grapefruit juice and midazolam in humans

  1995cited by this paper
• Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians.

  1994influential reference
• A potentially hazardous interaction between erythromycin and midazolam.

  1993cited by this paper
• Pharmacokinetic‐pharmacodynamic modeling of the central nervous system effects of midazolam and its main metabolite α‐hydroxymidazolam in healthy volunteers

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