Course Catalog

Pharmacokinetics and Pharmacodynamics for Chemists Online Short Course

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.

Course Details

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

Information

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.

Who Should Attend

Chemical scientists who have little or no formal training in physiology, pharmacology, or medicinal chemistry. Registrants should have a firm grasp of organic chemistry and the equivalent of an introductory course in physical chemistry and biochemistry. Course is ideal for scientists in the pharmaceutical, chemical and cosmetic industries needing a basic understanding of PK/PD concepts and illustration of practical applications. Others who would benefit are toxicologists, regulatory affairs and clinical professionals.

Benefits

  • Master the language and terminology of pharmacology and medicinal chemistry
  • Learn the relationship between the chemical structure of drugs and how they affect drug absorption, distribution, metabolism and excretion.
  • Learn how pharmacology can be used to study a drug’s mechanisms of action.
  • Learn what in vitro assays can be used to yield important ADME data early in discovery programs
  • Learn how to apply in vitro ADME assay data (Caco-2, liver microsomes, Clog P) to predict drug-like behavior
  • Learn how to interpret Pharmacokinetic data from in vivo animal studies to predict first time dose in humans / dosage regimens

Agenda

  • 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

 

Course Locations

Date

August 11 - September 15, 2015

This course will meet for six online sessions at 12:30 PM – 1:45 PM on the following dates:

Tuesdays
August 11
August 25
Septmeber 1
September 8
September 15

Attendance at scheduled class times is NOT required. Registered participants can attend the course by viewing session recordings.

Register Online Register Via Mail

Venue

Online

Each person attending must register individually for this course

The course fee includes a electronic access to the course materials.

Four for three! Register four people for one course, one person for four courses, or any combination in between, and the fifth registration is free! This offer can only be used in conjunction with online registrations and cannot be combined with any other offer. All courses must be completed in the same calendar year. All four registrations must be received by our offices on the same day. Note: This discount is only available if you register by fax, mail or phone and mention this discount.


Pricing
  Member Non-Member
Standard $1,095 per person $1,295 per person

System Requirements
You need a high-speed connection to the Internet and an up-to-date
version of your web browser. The audio portion of the live session
will be provided via VOIP and US toll-free conference call. VOIP is
dependent on the quality and speed of your internet connection so
a high-speed connection is strongly recommended. Those choosing to
use VOIP should also have a headset or microphone in order to
interact with the instructor. If not, we recommend you choose
the telephone option, or contact us
to purchase a headset for $5.

Date

October 20 - November 24, 2015

This course will meet for six online sessions at 12:30 PM – 1:45 PM on the following dates:

Tuesdays

October 20
October 27
November 3
November 10
November 17
November 24

Attendance at scheduled class times is NOT required. Registered participants can attend the course by viewing session recordings.

Register Online Register Via Mail

Venue

Online

Each person attending must register individually for this course

The course fee includes a electronic access to the course materials.

Four for three! Register four people for one course, one person for four courses, or any combination in between, and the fifth registration is free! This offer can only be used in conjunction with online registrations and cannot be combined with any other offer. All courses must be completed in the same calendar year. All four registrations must be received by our offices on the same day. Note: This discount is only available if you register by fax, mail or phone and mention this discount.


Pricing
  Member Non-Member
Standard $1,095 per person $1,295 per person

System Requirements
You need a high-speed connection to the Internet and an up-to-date
version of your web browser. The audio portion of the live session
will be provided via VOIP and US toll-free conference call. VOIP is
dependent on the quality and speed of your internet connection so
a high-speed connection is strongly recommended. Those choosing to
use VOIP should also have a headset or microphone in order to
interact with the instructor. If not, we recommend you choose
the telephone option, or contact us
to purchase a headset for $5.

About the Instructor

  • Terry Kenakin

    has spent 32 years in industrial drug discovery, has won numerous awards for pharmacological research (Gaddum Memorial Award: 2014, Ariens Award: 2011, Poulsson Medal: 2008, IUPHAR Analytical Pharmacology Award: 2006), authored over 250 peer reviewed papers and reviews and written 10 books on Pharmacology.He also is Editor-in-Chief of Journal of Receptors and Signal Transduction and Co-Editor-in-Chief of Current Opinion in Pharmacology. He currently is Professor of Pharmacology at the University of North Carolina School of Medicine, Chapel Hill NC.