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Produktbild: Pharmacokinetics and Metabolism in Drug Design
Band 51

Pharmacokinetics and Metabolism in Drug Design

Aus der Reihe Methods and Principles in Medicinal Chemistry

Fr. 178.00

inkl. gesetzl. MwSt., Versandkostenfrei

Beschreibung

Produktdetails

Einband

Gebundene Ausgabe

Erscheinungsdatum

04.04.2012

Abbildungen

Tabellen, schwarz-weiss, schwarz-weiss Illustrationen

Herausgeber

Dennis A. Smith + weitere

Verlag

Wiley-VCH

Seitenzahl

268

Maße (L/B/H)

25/17.5/1.9 cm

Gewicht

679 g

Auflage

3rd, rev. and upd. ed.

Sprache

Englisch

ISBN

978-3-527-32954-0

Beschreibung

Produktdetails

Einband

Gebundene Ausgabe

Erscheinungsdatum

04.04.2012

Abbildungen

Tabellen, schwarz-weiss, schwarz-weiss Illustrationen

Herausgeber

Verlag

Wiley-VCH

Seitenzahl

268

Maße (L/B/H)

25/17.5/1.9 cm

Gewicht

679 g

Auflage

3rd, rev. and upd. ed.

Sprache

Englisch

ISBN

978-3-527-32954-0

Herstelleradresse

Wiley-VCH GmbH
product_safety@wiley.com
Wiley-VCH GmbH, Boschstrasse 12, DE-69469 Weinheim

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  • Produktbild: Pharmacokinetics and Metabolism in Drug Design
  • PHYSICOCHEMISTRY

    Physicochemistry and Pharmacokinetics

    Partition and Distribution Coefficients as Measures of Lipophilicity

    Limitations on the Use of 1-Octanol

    Further Understanding of logP

    Alternative Lipophilicity Scales

    Computational Systems to Determine Lipophilicity

    Membrane Systems to Study Drug Behavior

    Dissolution and Solubility

    The BCS Classification and Central Role of Permeability

     

    PHARMACOKINETICS

    Setting the Scene

    Intravenous Administration: Volume of Distribution

    Intravenous Administration: Clearance

    Intravenous Administration: Clearance and Half-life

    Intravenous Administration: Infusion

    Oral Administration

    Repeated Doses

    Development of the Unbound (Free) Drug Model

    Unbound Drug and Drug Action

    Unbound Drug Model and Barriers to Equilibrium

    Pharmacodynamic Models

    Slow Offset Compounds

    Factors Governing Unbound Drug Concentration

     

    ABSORPTION

    The Absorption Process

    Dissolution

    Membrane Transfer

    Barriers to Membrane Transfer

    Prodrugs to Increase Oral Absorption

    Active Transport

    Models for Absorption Estimation

    Estimation of Absorption Potential and other Computational

     

    DISTRIBUTION

    Membrane Transfer Access to the Target

    Brain Penetration

     

    CLEARANCE

    The Clearance Processes

    Role of Transport Proteins in Drug Clearance

    Interplay Between Metabolic and Renal Clearance

    Role of Lipophilicity in Drug Clearance

    Active Metabolites

    Balancing the Rate of Renal and Metabolic clearance and Potency

     

    RENAL CLEARANCE

    Kidney Anatomy and Function

    Lipophilicity and Reabsorption by the Kidney

    Effect of Charge on Renal Clearance

    Plasma Protein Binding and Renal Clearance

    Balancing Renal Clearance and Absorption

    Renal Clearance and Drug Design

     

    METABOLIC (HEPATIC) CLEARANCE

    Symbols

    Function of Metabolism (Biotransformation)

    Cytochrome P450

    Other Oxidative Metabolism Processes

    Oxidative Metabolism and Drug Design

    Nonspecific Esterases

    Prodrugs to Aid Membrane Transfer

    Enzymes Catalyzing Drug Conjugation

    Stability to Conjugation Processes

    Pharmacodynamics and Conjugation

     

    TOXICITY

    Toxicity Findings

    Structure - Toxicity Analyses

    Reactive Metabolite Screening in Drug Discovery

    Structural Alerts/Toxicophores in Drug Design

    Dealing with Reactive Metabolite Positives in Drug Discovery: Risk Assessment Strategies - Effect of Daily Dose

    Dealing with Reactive Metabolite Positives in Drug Discovery: Risk Assessment Strategies - Competing Detoxication Pathways

    Stratification of Toxicity

    Toxicity Prediction: Computational Toxicology

    Toxicogenomics

    Pharmacogenomics

    Enzyme Induction and Drug Design

    Enzyme Inhibition and Drug Design

     

    PREDICTING HUMAN PHARMACOKINETICS

    Objectives of Predicting Human Pharmacokinetics

    Allometric Scaling of Preclinical In Vivo PK Parameters

    Prediction of Human PK Parameters Using In Vitro Data

    Elimination Half-Life

    Moving Forward

     

    ADME SCREENING

    The High-Throughput Synthesis and Screening Trend

    The Concept of ADME Space

    Drug Metabolism and Discovery Screening Sequences

    Physicochemistry

    Absorption/Permeability

    Metabolism, Induction, and Inhibition

    Transporters

    Protein Binding

    Pharmacokinetics