This course covers the chemical and biological analysis of the metabolism and distribution of drugs, toxins and chemicals in animals and humans, and the mechanism by which they cause therapeutic and toxic responses. Metabolism and toxicity as a basis for drug development is also covered.

Syllabus

Overview

This course covers the chemical and biological analysis of the metabolism and distribution of drugs, toxins and chemicals in animals and humans, and the mechanism by which they cause therapeutic and toxic responses. Metabolism and toxicity as a basis for drug development, metabolic polymorphisms and biomarkers of exposure are also covered.

Texts

Required

 Golan, David E., Editor-in-chief; Armen H. Tashjian, Deputy Editor; Ehrin J. Armstrong, et al., eds. Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. Baltimore, MD: Lippincott Williams & Wilkins, 2004. ISBN: 9780781746786.

Recommended

 Klaassen, Curtis D., ed. Casarett and Doull's Toxicology: The Basic Science of Poisons. 6th ed. New York, NY: McGraw-Hill Medical Pub Division, 2001. ISBN: 9780071347211.

The Biochemistry you need to know or learn for this course

• Structures and Functional Groups
  • Carboxylic Acids
  • Aldehydes
  • Ketones
  • Aromatic Molecules/Heterocycles
  • Esters
  • Amides
  • Thiols (Sulfhydryls)
  • Epoxides
• Nucleophiles/Electrophiles
• Bonding
  • Covalent Bonds
  • Coordinate Covalent Bonds
  • Ionic Bonds
  • Hydrogen Bonding
  • Van Der Waal's Interactions
• Reduction/Oxidation
• Thermodynamics and Equilibria
• Acid/Base Chemistry
• Reaction Kinetics and Mechanisms
  • Zero-, First- and Second-Order Reaction Kinetics
  • S_N1 and S_N2 Nucleophilic Substitution Mechanisms
  • Michael Acceptors
• Enzymes
  • Kinetics
  • Cofactors: NAD+/NADH; FAD/FADH; FMN; Coenzyme A/acetyl CoA; UDP-Glucuronic Acid; ATP; GTP; cAMP; cGMP; PAPS (3'-phosphoadenosine-5'-phosphosulfate); s-adenosylmethionine (SAM); Glutathione
• Lipids
  • Membrane Structure
  • Types of Lipid: Fatty Acids (Arachadonic Acid); Triglycerides; Cholesterol; Phospholipids
• Mitochondrial Structure and Function
• Metabolism and ATP Generation
• DNA Structure
  • Bases, Nucleosides, Nucleotides
  • Primary, Secondary Structure
• Proteins/Peptides
  • Amino Acid Structure and Side Chain Chemistry
  • Peptide Bonds
  • Glutathione

Recitations

There will be a recitation session offered throughout the term. Several of these sessions will consist of seminars presented by scientists from local pharmaceutical and biotechnology companies. The other sessions will be run by the TA and will entail answering questions relating to the lecture material, homework assignments, and projects and providing background help with concepts in several areas, including elements of chemistry and biochemistry.

Homework Assignments and Readings

Additional assignments will include:

1. specific papers and book chapters;
2. problem sets associated with the reading; and
3. problem sets relevant to lecture material.

The homework is due as noted in the lecture schedule. There is a 20% reduction in the grade for each day the assignment is late.

Quizzes

There will be two quizzes during the term. All are non-comprehensive, in-class quizzes given during the regular lecture period. There is no final examination.

Team Projects

The class will be divided into groups of 3-5 students (depending on class size) to work as a team on a project to investigate a drug. The investigation will center on concepts developed during the term, with emphasis on understanding drug mechanisms and the successful development of drugs.

Grading Policy

Percentage contributions to the final grade are as follows:

Calendar

PCD = Prof. Peter Dedon
SRT = Prof. Steven Tannenbaum