lec 4 and 5

lec 4 and 5 - Introductory Pharmacology Chemical properties...

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Introductory Pharmacology Chemical properties of Relevance to Pharmacology Lecture 4 & 5 Combined: April 6 & 8, 2009 With Schild equation troduction to Bioassays, Dose response and Introduction to Bioassays, Dose response and Quantitative Analysis of Drug Responses Receptor Quantitative Kinetics / Equilibrium Binding p Q / q g Effects of Competitive and Noncompetitive Antagonists eceptor Modulation Receptor Modulation
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Chemical and physicochemical properties of drugs or chemicals determining drug / chemical efficacy or toxicity “exerting an action” ) type of interaction with target sites (f) type of interaction with target sites “irreversible”: covalent bonding “ eversible”: ionic interaction, hydrophobic interaction, reversible : ionic interaction, hydrophobic interaction, hydrogen bond formation, van der Waals interactions CONSIDER IMPORTANCE OF REVERSIBILITY (g) stereochemistry “selectivity of fit”: defines the “receptor” construct of pharmacology, may be important in binding to enzymes From prior lecture slide set
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Chemical and physicochemical properties of drugs or chemicals determining drug / chemical efficacy or toxicity “ etting to & exerting an action” getting to & exerting an action ( h) molecular stability stability to local environment often determines route of drug administration, example acid labile drugs like eptides peptides (i) molecular reactivity–does it have sites that are highly reactive (j) must it undergo chemical reaction to form the “active” substance (e.g., prodrugs) acetaminophen (Tylenol) the product of hepatic metabolism of phenacetin – LOOK UP From prior lecture slide set
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Relating chemical and physicochemical properties of rugs/chemicals to biological responses drugs/chemicals to biological responses The Bioassay –uses living systems > i” “i it
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lec 4 and 5 - Introductory Pharmacology Chemical properties...

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