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PharmacologyNotes - Biochemical Pharmacology Lecture Notes...

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Biochemical Pharmacology Lecture Notes Michael Palmer, Department of Chemistry, University of Waterloo, Canada Third edition, January 2007
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Contents About these notes ...................................................................................................... vi Chapter 1 . Introduction ............................................................................................... 1 1.1. What are drugs? . ........................................................................................... 1 1.2. Drugs and drug target molecules . ......................................................................... 2 1.3. Drug molecules may or may not have physiological counterparts . ....................................... 3 1.4. Synthetic drugs may exceed the corresponding physiological agonists in selectivity . ................... 4 1.5. Metabolism of physiological mediators and of drugs . .................................................... 5 1.6. Strategies of drug development . ........................................................................... 5 Chapter 2 . Pharmacokinetics ......................................................................................... 9 2.1. Drug application and uptake . .............................................................................. 9 2.1.1. Oral drug application . 9 2.1.2. Intravenous drug application . ................................................................... 10 2.1.3. Other routes of drug applicaton . ................................................................ 11 2.2. Drug distribution . .......................................................................................... 12 2.2.1. Vascular permeability; the blood brain barrier . ................................................. 12 2.2.2. Drug hydrophobicity and permeation across membranes . ...................................... 12 2.2.3. L-DOPA as an example of drug distribution facilitated by specific transport . ................. 14 2.2.4. The ‘volume of distribution’. .................................................................... 14 2.2.5. Protein binding . .................................................................................. 15 2.2.6. Kinetics of drug distribution . 15 2.3. Drug elimination: Kidneys . ............................................................................... 16 2.3.1. Kidney anatomy and function . .................................................................. 16 2.3.2. Filtration, secretion, reuptake . 18 2.3.3. Examples . ........................................................................................ 20 2.4. Drug elimination: Metabolism . 21 2.4.1. Example: Metabolism of phenobarbital and of morphine . ..................................... 21 2.4.2. Cytochrome P450 enzymes . ..................................................................... 22 2.4.3. Overview of drug conjugation reactions . ....................................................... 23 2.4.4. Glucuronidation . ................................................................................. 24 2.4.5. Glutathione conjugation . ........................................................................ 24 2.4.6. Acetylation . ...................................................................................... 25 2.4.7. Other reactions in drug metabolism . ............................................................ 25 Chapter 3 . Pharmacodynamics ....................................................................................... 27 3.1. Classes of drug receptors . 27 3.2. Mechanisms and kinetics of drug receptor interaction . ................................................... 28 3.2.1. Mass action kinetics of drug-receptor binding . 28 3.2.2. Reversible inhibition . ............................................................................ 28 3.2.3. Irreversible inhibition . 29
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3.2.4. Example: Inhibition of α -adrenergic receptors by tolazoline and phenoxybenzamine . ....... 30 3.3. Drug dose-effect relationships in biochemical cascades . ................................................. 31 3.4. Spare receptors . ............................................................................................ 33 3.5. Potency and efficacy . ...................................................................................... 33 3.6. Partial agonism and the two-state model of receptor activation . ......................................... 34 3.7. Toxic and beneficial drug effects . ......................................................................... 35 Chapter 4 . The ionic basis of cell excitation 38 4.1. Ion gradients across the cell plasma membrane . .......................................................... 38 4.2. The physics of membrane potentials . ..................................................................... 39 4.3. Voltage-gated cation channels and the action potential . .................................................. 41 4.4. The origin of cell excitation . .............................................................................. 43 4.5. Anion channels . 44 Chapter 5 . Drugs that act on sodium and potassium channels .................................................... 47 5.1. Local anesthetics . .......................................................................................... 48 5.2. Sodium channel blockers as antiarrhythmic agents . ...................................................... 50 5.3. Sodium channel blockers in epilepsia . .................................................................... 51 5.4. Potassium channel blockers. ............................................................................... 52 5.5. Potassium channel openers . 53 Chapter 6 . Some aspects of calcium pharmacology ................................................................ 55 6.1. Calcium in muscle cell function . .......................................................................... 55 6.2. Calcium channel blockers . ................................................................................ 57 6.3. Digitalis (foxglove) glycosides . ........................................................................... 58 6.4. Calcium-dependent signaling by adrenergic receptors . ................................................... 60 Chapter 7 . Some aspects of neurophysiology relevant to pharmacology 63 7.1. Structure and function of synapses . ....................................................................... 64 7.2. Mechanisms of drug action on synapses .
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This note was uploaded on 09/22/2011 for the course CHEM 333 taught by Professor Michaelpalmer during the Winter '07 term at Waterloo.

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PharmacologyNotes - Biochemical Pharmacology Lecture Notes...

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