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Pharmacokinetics and Pharmacodynamics for Chemists

Type	Webinar
Language	English
Date	September 24, 2009 from 11:00 am to 12:15 pm
Venue	Eastern Time , US
Chemistry Specialties	other
Chemistry Techniques	other
Contact	American Chemical Society 1155 Sixteenth Street, NW Washington, DC 20036 US (800) 227-5558 shortcourses@acs.org
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by Daniel Fishman — last modified 05-26-09 05:33 AM

This course will meet for six online sessions of one hour and 15 minutes each. September 24; October 1, 8, 15, 22, 29. This course presents the fundamentals of Pharmacokinetics and Pharmacodynamics as they apply to the chemical structure of drugs. There will be specific discussion of the role of medicinal chemistry in the drug discovery process; how chemical structure affects the absorption, distribution, metabolism and excretion (ADME properties) of drugs; and drug affinity and efficacy (Pharmacodynamics). In addition, students will learn the essentials of interpreting pharmacokinetic data from animal studies for prediction of first dose in humans and therapeutic use of drugs. By the end of this course, students should be able to understand the role of the medicinal chemist in the process of drug discovery and development. This course is centered on gaining an understanding of in vitro PK assay data (Caco-2, MDCK, PAMPA, microsomes, hepatocytes etc) to predict in vivo PK and optimize drug ADME properties. In vivo data interpretation (scaling from animal to humans, allometric plots) will be discussed with specific examples of the role of pharmacokinetics in drug development.

Key Topics * Hands-on exercises in PK to gain proficiency in PK analyses * Principles of first-order (linear) kinetics and comparison with non-linear processes. * Linkage of physicochemical properties of molecules and ADME properties * Use of in vitro data (absorption Caco-2, PAMPA / metabolism microsomes, S9, hepatocytes) to predict PK in humans * Discussion of in silico solutions to ADME problems * Meaning and application of compartmental (vs. non-compartmental) models and their analysis. * How ADME characteristics affect dosing and how drugs are used (i.e. once a day oral) * Definition, measurement and inter-relationships among apparent volume of distribution, plasma protein binding, clearance and half-life. * Critical issues in drug candidate selection. * Factors affecting oral drug absorption and bioavailability. * Relationships between PK and PD / system-independent measurement of drug activity * pK-PD interface: drug requirements for activity in open (in vivo) systems * Allometric scaling / interpretation of in vivo PK data

Session titles

* Basic Principles: Michaelis-Menten Kinetics, curve fitting, mass action * Chemical properties of drugs: pKa, solubility, lipophilicity, stereochemistry,mol. weight * ADME: Introduction to PK + Absorption Principles * Protein Binding, Drug Metabolism (CYP450 activity, induction, drug-drug interactions) * Clearance: Hepatic and Renal * Compartmental analysis, Volume of Distribution, Half-Life, Oral Bioavailability * Multiple Dose regimens: dose-interval, non-linear Pharmacokinetics * Emphasis on in vitro data to predict in vivo PK: Caco-2, MDCK, PAMPA, microsomes, hepatocytes, many more * Interpretation of in vivo Pharmcokinetic data/Allometry/first time dose in humans * Predictive PK: 17 hands-on exercises done throughout class on minimal data to predict good/bad PK * PK-Pharmacodynamics interface: Basic Pharmacological principles for quantifying biological target activity

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