000000000000 Matthew Lang

000000000000 Matthew Lang - 20.201 Mechanisms of Drug...

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20.201 Mechanisms of Drug Action Lecture #1 9/7/05 Instructors Prof. Peter Dedon Prof. Steven Tannenbaum Monday and Wednesday 1:30-3:00 pm Recitations on Friday 1:30-2:30 pm 1
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Course Objectives • Develop an understanding of the scientific basis for drug development and drug mechanisms • Develop an appreciation for the role of pharmacokinetics, drug metabolism and drug interactions in the mechanisms of action of drugs • Understand the balance between pharmacogenetics, toxicity and therapeutic outcome associated with any drug 2
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What is the “mechanism of action of a drug?” • Popular misconception: the mechanism of action of a drug is its interaction with a specific receptor • This is termed, “pharmacodynamics” • A drug, by definition, is a chemical agent that is both safe and efficacious in the treatment of a human disease • If a chemical agent never reaches its receptor target, then it is not a drug and it has no “mechanism of action” 3
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The mechanism of action of a drug involves every aspect of its fate • The less appreciated facet of a drug’s mechanism of action is its “pharmacokinetics” • “Pharmacokinetics” and “pharmacodynamics” are the two foundations of a drug’s mechanism of action • Pharmacokinetics, in its broadest definition, involves: ~ Uptake = absorption ~ Distribution ~ Metabolism ~ Elimination ~ Toxicology (politically correct: “Drug Safety”) A D M E T 4
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Topics Covered First half of term : • Role of drug structure and drug transport proteins in uptake and distribution • Kinetics of drug behavior in the human body • Metabolism: ~ chemical alterations of drugs ~ generation of toxic metabolites ~ metabolic activation of drugs • Drug interactions leading to toxicity • Drug-receptor interactions 5
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Topics Covered Second half of term : • Apply basic concepts to case studies of specific drugs • Pharmacogenetics and biological variability in drug action • The science of clinical trials for drug candidates 6
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Omeprazole N N H N S O OCH 3 CH 3 H 3 C H 3 CO N S OH OCH 3 CH 3 H 3 C +H + N HN OCH 3 N S OCH 3 CH 3 H 3 C N N OCH 3 N S OCH 3 CH 3 H 3 C NH N OCH 3 + + + ENZ-SH S-ENZ N N H N S O OCH 3 CH 3 H 2 C H 3 CO HO 5-hydroxyomeprazole N N H
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000000000000 Matthew Lang - 20.201 Mechanisms of Drug...

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