Pharmacokinetics and Metabolism in Drug Design / Methods and Principles in Medicinal Chemistry Bd.29 (PDF)

PHYSICOCHEMISTRY Partition and Distribution Coefficient as Measures of Lipophilicity Limitations on the Use of Octanol Further Understanding of log P Alternative Lipophilicity Scales Computational Approaches to Lipophilicity Membrane Systems to Study Drug Behaviour NEW: Dissolution and Solubility NEW: Ionisation (pKa) PHARMACOKINETICS Intravenous Administration: Volume of Distribution Intravenous Administration: Clearance 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 Slow Offset Compounds Factors Governing Unbound Drug Concentration ABSORPTION The Absorption Process Dissolution Membrane Transfer Barriers to Membrane Transfer Models for Absorption Estimation Estimation of Absorption Potential Computational Approaches DISTRIBUTION Membrane Transfer Access to the Target Brain penetration Volume of Distribution and Duration Distribution and Tmax CLEARANCE The Clearance Processes Role of Transport Proteins in Drug Clearance Interplay Between Metabolic and Renal Clearance Role of Lipophilicity in Drug Clearance 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 Function of Metabolism (Biotransformation) Cytochrome P450 Other oxidative processes Oxidative Metablism and Drug Design Non-Specific Esterases Prodrugs to Aid Membrane Transfer Enzymes Catalysing Drug Conjugation Stability to Conjugation Processes Pharmacodynamics and Conjugation TOXICITY Toxicity Findings Importance of dose size Toxicity of selected compound classes Stratification of Toxicity Toxicity Prediction - Computational Toxicology Toxicogenomics Enzyme Induction (CYP3A4) and Drug Design Enzyme Inhibition and Drug Design

The authors are leading scientists in the Drug Metabolism department of Pfizer, one of the top five pharmaceutical companies in the world.

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