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[资源] Pharmacokinetics and Metabolism in Drug Design (3rd edition)

Pharmacokinetics and Metabolism in Drug Design,3rd Edition
Editor(s): Dennis A. Smith, Charlotte Allerton, Amit S. Kalgutkar, Han van de Waterbeemd, Don K. Walker
Wiley-VCH Verlag GmbH & Co. KGaA
Published Online: 20 APR 2012 03:48AM EST
Print ISBN: 9783527329540
Online ISBN: 9783527645763
DOI: 10.1002/9783527645763

Table of Contents

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

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