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Biochemical Pharmacology Lecture Notes
Shubham Goyal

Biochemical Pharmacology Lecture Notes

Shubham Goyal | 22-Jan-2016 |
Pharmacokinetics , Drug distribution , Pharmacodynamics , Some aspects of calcium pharmacology , Some aspects of neurophysiology relevant to pharmacology , G protein-coupled receptors , Drugs that act on sodium and potassium channels , The ionic basis of cell excitation , Pharmacology of cholinergic synapses , Pharmacology of catecholamines and of serotonin , Pharmacology of nitric oxide (NO) , Pharmacology of Eicosanoids , Some principles of cancer pharmacotherapy ,

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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
3.2.4. Example: Inhibition of a-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 . . . . . . 65
7.3. Pharmacologically important neurotransmitters and their receptors . . . . . . . . . . . . . . . . . . 65
7.4. Neurotransmitter receptors 67
7.5. Overview of the autonomic nervous system . . . 68
Chapter 8. G protein-coupled receptors . . . . . . . . . . . . . . . . . 72
8.1. Structure and function of G protein-coupled receptors . . . . . . . . . . . 72
8.2. The complexity of G protein signalling . . . . . . . 74
8.3. Agonist-specific coupling . . 74
8.4. GPCR oligomerization . . . . . 75
8.5. ‘Allosteric’GPCR agonists and antagonists . . . 75
Chapter 9. Pharmacology of cholinergic synapses . . . . . . 78
9.1. Structure and function of the nicotinic acetylcholine receptor . . . . 78
9.1.1. Overall structure . 78
9.1.2. Location of the acetylcholine binding site . . . . . . . . . . . . . . 79
9.1.3. The nature of the receptor-ligand interaction . . . . . . . . . . . 80
9.1.4. Receptor desensitization . . . . . . . . . . . . . 81
9.2. Cholinergic agonists . . . . . . . 82
9.2.1. Muscarinic agonists . . . . . . . . . . . . . . . . . . 83
9.2.2. Nicotinic agonists 83
9.3. Cholinergic antagonists . . . . 84
9.3.1. Muscarinic antagonists . . . . . . . . . . . . . . 84
9.3.2. Nicotinic antagonists . . . . . . . . . . . . . . . . . 84
9.3.3. Muscle relaxants . 85
9.3.4. Nicotinic antagonists used as muscle relaxants . . . . . . . . . 85
9.3.5. Depolarizing muscle relaxants . . . . . . . 85
9.4. Cholinesterase antagonists . 86
9.4.1. Chemical groups of cholinesterase inhibitors . . . . . . . . . . . 87
9.4.2. Applications of cholinesterase inhibitors . . . . . . . . . . . . . . . . 88
Chapter 10. Pharmacology of catecholamines and of serotonin . . . . . . . . . . . 90
10.1. Biosynthesis and degradation of catecholamines . . . . . . . . . . . . . . . . 90
10.2. Pharmacokinetic aspects . . 91
10.3. Drug targets in catecholaminergic synapses . . 91
10.4. Adrenergic receptor agonists and antagonists 92
10.4.1. Physiological effects of a- and b-selective adrenergic agonists . . . . . . . . . . . 92
10.4.2. Physiological effects of a2-adrenergic agonists . . . . . . . . 92
10.4.3. b-Adrenergic agonists . . . . . . . . . . . . . . 94
10.4.4. a-Adrenergic antagonists . . . . . . . . . . 94
10.4.5. b-Adrenergic antagonists . . . . . . . . . . . 94
10.5. Inhibitors of presynaptic transmitter reuptake . . . . . . . . . . . . . . . . . . . 95
10.6. Inhibition of vesicular storage . . . . . . . . . . . . . . . 96
10.7. Indirect sympathomimetics . . . . . . . . . . . . . . . . . . . 97
10.8. L-DOPA and carbidopa in the therapy of Parkinson’s disease . . 99
10.9. ‘False transmitters’. . . . . . . . 99
10.10. Cytotoxic catecholamine analogs . . . . . . . . . . . 99
10.11. Monoamine oxidase inhibitors . . . . . . . . . . . . . . 100
Chapter 11. Pharmacology of nitric oxide (NO) . . . . . . . . 103
11.1. Vascular effects of nitric oxide . . . . . . . . . . . . . . . 103
11.2. Nitric oxide synthase and its isoforms . . . . . . . 104
11.3. Biochemical mechanisms of NO signalling . . 105
11.4. Role of NO in macrophages . . . . . . . . . . . . . . . . . . 108
11.5. NO releasing drugs . . . . . . . 109
11.6. NOS inhibitors . . . . . . . . . . . . 110
Chapter 12. Pharmacology of Eicosanoids . . . . . . . . . . . . . . 112
12.1. Biosynthesis of eicosanoids . . . . . . . . . . . . . . . . . . 112
12.2. Cyclooxygenase inhibitors . . . . . . . . . . . . . . . . . . . 115
12.3. Lipoxygenases and related drugs . . . . . . . . . . . . . 117
Chapter 13. Some principles of cancer pharmacotherapy . . . . . . . . . . . . . . . . . 122
13.1. Cell type-specific antitumor drugs . . . . . . . . . . . 123
13.2. The cell cycle . . . . . . . . . . . . . 124
13.3. Alkylating agents . . . . . . . . . 124
13.4. Antibiotics . . . . . . . . . . . . . . . . 126
13.5. Antimetabolites . . . . . . . . . . . 126
13.6. Inhibitors of mitosis . . . . . . 128
13.7. Monoclonal antibodies in tumour therapy . . . 129

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