Pharmacokinetics and metabolism in drug design. (2012)

• Record Type: Book
• Other Names: Smith, Dennis A
• 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;
• Edition: 3rd., rev. and updated ed
• Publisher Details: Place of publication not identified : Wiley-VCH
• Publication Date: 2012
• Extent: 1 online resource (268 pages)
• Subjects: 615.7; Pharmacokinetics; Drugs -- Metabolism; Drugs -- Design
• Languages: English
• ISBNs: 9783527645299
• Access Rights: Legal Deposit; Only available on premises controlled by the deposit library and to one user at any one time; The Legal Deposit Libraries (Non-Print Works) Regulations (UK).
• Access Usage: Restricted: Printing from this resource is governed by The Legal Deposit Libraries (Non-Print Works) Regulations (UK) and UK copyright law currently in force.