171. Basic Concepts In Pharmacology

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171. Basic Concepts In Pharmacology

171. Basic Concepts In Pharmacology

 

 

CATEGORY: Medical & Medicine – 500 Courses

COURSE NUMBER: 171

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Syllabus

Preface xiii

PART II
DRUGS THAT AFFECT THE
AUTONOMIC NERVOUS SYSTEM
6. REVIEW OF THE AUTONOMIC
NERVOUS SYSTEM 29
Why Include This Material? 29
Relevant Anatomy 30
Synthesis, Storage, Release, and
Removal of Transmitters 32
Receptors 34
General Rules of Innervation 35
Presynaptic Receptors 37
7. CHOLINERGIC AGONISTS 38
Organization of Class 38
Direct Cholinergic Agonists 39
Cholinesterase Inhibitors 40
8. CHOLINERGIC ANTAGONISTS 43
Organization of Class 43
Muscarinic Antagonists 43
Ganglionic Blockers 45
Neuromuscular Blockers 45
9. ADRENERGIC AGONISTS 47
Organization of Class 47
Direct-Acting Agonists 48
Dopamine 49
Indirect-Acting Agents 50
Cardiovascular Effects of Norepinephrine,
Epinephrine, and Isoproterenol 50

1. WHERE TO START 1
PART I
GENERAL PRINCIPLES
2. RECEPTOR THEORY 5
Agonists 5
Efficacy and Potency 6
Therapeutic Index 7
Antagonists 7
Inverse Agonists 9
3. ABSORPTION, DISTRIBUTION,
AND CLEARANCE 11
First-Pass Effect 11
How Drugs Cross Membranes 11
Bioavailability 13
Total Body Clearance 14
4. PHARMACOKINETICS 16
Volume of Distribution 16
First-Order Kinetics 17
Zero-Order Kinetics 19
Steady-State Concentration 20
Time Needed to Reach Steady State 21
Loading Dose 22
5. DRUG METABOLISM AND RENAL
ELIMINATION 24
Liver Metabolism 24
Renal Excretion 25

10. ADRENERGIC ANTAGONISTS 52
Organization of Class 52
Central Blockers 52
` -Blockers 52
a-Blockers 54
Mixed `- and a-Blockers 55
PART III
DRUGS THAT AFFECT THE
CARDIOVASCULAR SYSTEM
11. ANTIHYPERTENSIVE DRUGS 59
Organization of Class 59
Diuretics 60
Drugs That Interfere With the
Renin-Angiotensin System 62
Angiotensin-Converting Enzyme (ACE)
Inhibitors 62
Angiotensin II Receptor Blockers (ARBs) 63
Selective Aldosterone Receptor Antagonists 64
Direct Renin Inhibitor (DRI) 64
Calcium Channel Blockers 64
Nitrates 65
Other Direct Vasodilators 66
`- and a-Blockers 66
Clonidine 67
12. DRUGS USED IN ISCHEMIC HEART
DISEASE AND CONGESTIVE
HEART FAILURE 69
Ischemic Heart Disease 69
Congestive Heart Failure 69
Reduction of Cardiac Workload 70
Control of Excessive Fluid 70
Enhancement of Contractility 71
Cardiac Glycosides 71
Sympathomimetics 72
Phosphodiesterase Inhibitors 72
Ranolazine 72
13. ANTIARRHYTHMIC DRUGS 73
Organization of Class 73
Class I Drugs (Sodium Channel Blockers) 74
Class II Drugs (β-Blockers) 75
Class III Drugs (Potassium Channel Blockers) 76
Class IV Drugs (Calcium Channel Blockers) 77
Other Antiarrhythmic Drugs 78
Drugs That Increase Heart Rate 78
14. DRUGS THAT AFFECT BLOOD 79
Organization of Class 79
Antiplatelet Agents 79
Anticoagulants 81

Thrombolytic Drugs 83
Phosphodiesterase Inhibitors 84
Drugs Used in the Treatment of Anemia 84
15. LIPID-LOWERING DRUGS 86
Organization of Class 86
Additional Explanation of Mechanisms 87
PART IV
DRUGS THAT ACT ON THE CENTRAL
NERVOUS SYSTEM
16. DRUGS USED IN DEMENTIA 91
Organization of Class 91
Cholinesterase Inhibitors 91
NMDA Blocker 92
17. ANXIOLYTIC AND HYPNOTIC DRUGS 93
Tolerance and Dependence 93
Organization of Class 94
Barbiturates 95
Benzodiazepines 96
Buspirone 98
Benzodiazepine Receptor Agonists 98
Melatonin Receptor Agonist 98
18. DRUGS USED IN MOOD DISORDERS 100
Organization of Class 100
Serotonin-Specific Reuptake Inhibitors (SSRIs) 101
Serotonin/Norepinephrine Reuptake
Inhibitors (SNRIs) 102
Heterocyclics/TCAs 102
Monoamine Oxidase (MAO) Inhibitors 103
Other Antidepressants 104
Drugs Used in Bipolar Disorder 105
19. ANTIPSYCHOTICS OR NEUROLEPTICS 106
Organization of Class 106
Typical Antipsychotics (First Generation) 107
Serotonin-Dopamine Antagonists (Second
Generation) 108
Neuroleptic Malignant Syndrome 109
20. DRUGS USED IN PARKINSON DISEASE 110
Organization of Class 110
Dopamine Replacement Therapy 111
Dopamine Agonist Therapy 112
Anticholinergic Therapy 112
21. ANTIEPILEPTIC DRUGS 113
Organization of Class 113
Important Details About the Most
Important Drugs 114
Other Drugs to Consider 115

22. NARCOTICS (OPIATES) 117
Organization of Class 117
Actions of Morphine and the Other Agonists 118
Distinguishing Features of Some Agonists 119
Opioid Antagonists 120
Opioid Agonist-Antagonists 121
23. GENERAL ANESTHETICS 122
Organization of Class 122
Uptake and Distribution of Inhalational
Anesthetics 123
Elimination of Inhalational Anesthetics 124
Potency of General Anesthetics 124
Specific Gases and Volatile Liquids 124
Specific Intravenous Agents 125
24. LOCAL ANESTHETICS 126
Organization of Class 126
Mechanism of Action 127
Special Features About Individual Agents 127
PART V
CHEMOTHERAPEUTIC AGENTS
25. INTRODUCTION TO CHEMOTHERAPY 131
Approach to the Antimicrobials 131
General Principles of Therapy 131
Definitions 132
Important Concepts to Understand 132
Classification of Antimicrobials 134
26. INHIBITORS OF CELL WALL SYNTHESIS 136
General Features 136
β-Lactams 136
Penicillins 138
Cephalosporins 139
Carbapenems 140
Monobactams (Aztreonam) 140
Other Inhibitors of Cell Wall Synthesis 141
Vancomycin 141
Bacitracin 141
Fosfomycin 141
Daptomycin 141
27. PROTEIN SYNTHESIS INHIBITORS 142
General Features 142
Aminoglycosides 142
Tetracyclines 143
Macrolides 144
Streptogramins and Oxazolidinones 145
Chloramphenicol 146
Clindamycin 146

28. FOLATE ANTAGONISTS 147
Mechanism of Action 147
Selected Features 148
29. QUINOLONES AND URINARY TRACT
ANTISEPTICS 149
Drugs in This Group 149
Quinolones 149
Methenamine 150
30. DRUGS USED IN TUBERCULOSIS AND
LEPROSY 151
Organization of Class 151
Isoniazid 152
Rifampin 152
Pyrazinamide 153
Ethambutol 153
Dapsone 153
31. ANTIFUNGAL DRUGS 155
Organization of Class 155
Azole Antifungals 156
Polyene Antifungals 157
Echinocandins 158
Terbinafine 158
32. ANTHELMINTIC DRUGS 159
Organization of Class 159
Drugs Used Against Cestodes and
Trematodes 159
Drugs Used Against Nematodes 160
Drugs Used Against Filaria 160
33. ANTIVIRAL DRUGS 162
Organization of Class 162
Anti-HIV Drugs 163
Drugs Used in Influenza 164
Other Antivirals 165
34. ANTIPROTOZOAL DRUGS 166
Organization of Class 166
Metronidazole 167
Antimalarial Agents 167
Therapeutic Considerations 168
Special Features 168
35. ANTICANCER DRUGS 170
Organization of Class 170
Terminology and General Principles
of Therapy 171
Adverse Effects 173
Cytotoxic Drugs 174
Alkylating Agents 174
Antimetabolites 175
Antibiotics and Other Natural Products 176

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xii Contents
Antibodies 178
Other Cytotoxic Drugs 178
Hormonal Agents 179
Kinase Inhibitors 180
Miscellaneous Agents 180
PART VI
DRUGS THAT AFFECT THE
ENDOCRINE SYSTEM
36. ADRENOCORTICAL HORMONES 185
Organization of Class 185
Glucocorticoids 187
Mineralocorticoids 188
Inhibitors of Adrenocorticoid Synthesis 188
37. SEX STEROIDS 189
Organization of Class 189
Estrogens 191
Antiestrogens 191
Progestins 192
Antiprogestins 192
Oral Contraceptives 192
Androgens 193
Antiandrogens 194
GnRH Agonists and Antagonists 194
PDE5 Inhibitors 195
38. THYROID AND PARATHYROID DRUGS 196
Organization of Class 196
Thyroid Replacement Therapy 197
Drugs That Are Thyroid Downers 197
Parathyroid Drugs 197
39. INSULIN, GLUCAGON, AND ORAL
HYPOGLYCEMIC DRUGS 199
Organization of Class 199
Insulins 200
Oral Hypoglycemic Agents 201
PART VII
MISCELLANEOUS DRUGS
40. HISTAMINE AND ANTIHISTAMINES 205
Organization of Class 205
H1
Receptor Antagonists 205

41. RESPIRATORY DRUGS 208
Organization of Class 208
a-Agonists 209
Leukotriene Modifiers 209
Methylxanthines 210
Cholinergic Antagonists 210
Cromolyn and Omalizumab 210
Pulmonary Hypertension 210
42. DRUGS THAT AFFECT THE GI TRACT 212
Organization of Class 212
Drugs That Act in the Upper GI Tract 212
Drugs That Act in the Lower GI Tract 213
43. NONNARCOTIC ANALGESICS AND
ANTI-INFLAMMATORY DRUGS 216
Organization of Class 216
Nonsteroidal Anti-Inflammatory
Drugs 216
Cox-2 Inhibitors 218
Salicylates, Including Aspirin 218
Acetaminophen 220
Other Drugs for Arthritis 220
Antigout Agents 221
Drugs Used in the Treatment of Headaches 222
44. IMMUNOSUPPRESSIVES 223
Organization of Class 223
Calcineurin Inhibitors 223
Mycophenolate Mofetil and
Azathioprine 224
Monoclonal Antibodies 224
45. DRUGS USED IN OSTEOPOROSIS 225
Organization of Class 225
Bisphosphonates 226
Selective Estrogen Receptor Modulators 226
Estrogens 226
Parathyroid Hormone 227
Calcitonin 227
Other Agents 227
46. TOXICOLOGY AND POISONING 228
Principles of Toxicology 228
General Principles in the Treatment of
Poisoning 228
Specific Antidotes 229
Index 231

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