Section 1 Principles of Drug Therapy 1
Chapter 1 Introduction to Pharmacology 1
The Aim of Pharmacology 1
The History of Pharmacology 2
Change of Drug Discovery Strategy 3
Processes of Drug Discovery 3
Preclinical Pharmacology Research（Non-clinical Research） 3
Clinical Trial 4
Chapter 2 Pharmacokinetics 6
Process of Drug in Body 6
Process for Drug Transport across Membranes and Drug Transporters 6
Drug Absorption and Routes of Administration 10
Drug Distribution and Binding to Plasma Protein 13
Drug Metabolism 15
Drug Elimination 19
Kinetic Process of Drug in Body 22
Principles of Pharmacokinetics 22
Pharmacokinetic Parameters and Basic Calculation Equations 26
Chapter 3 Pharmacodynamics 30
Specific Mechanisms of Drug Action 30
Drug-receptor Interactions 30
Effects on Enzymes 37
Effects on Transporters 37
Effects on Structural and Functional Proteins 37
Effects on Genes 38
Common Note Concerning the Drug Mechanism 38
Non-specific Mechanisms of Drug Action 38
Dose-response Relationships 39
Dose-response Relationship Curves 39
Relation between Dose-response 41
Variation in Drug Responsiveness 42
Sources of Inter-individual Variation of Drug Response 43
Section 2 Drugs Affecting the Autonomic Nervous System 47
Chapter 4 Introduction 47
Anatomy and General Functions of Efferent Nervous System 47
Autonomic Nervous System 47
Somatic Motor Nerves 49
Neurotransmitters in the Efferent Nervous System 49
Acetylcholine 50
Norepinephrine 51
Receptors in the Efferent Nervous System 53
Cholinoceptors 53
Adrenoceptors 55
Dopamine Receptors 55
Drugs Affecting the Autonomic Nervous System 55
Agonist and Antagonist Actions at Receptors 55
Interference with Synthesis of the Transmitter 55
Interference with Degradation of the Transmitter 55
Interference with Storage and Release of the Transmitter 56
Classification of Drugs Acting on the Efferent Nervous System 56
Chapter 5 Cholinergic Agonists and Antagonists 59
Muscarinic Agonists 59
Choline Esters 59
Natural Alkaloid Muscarinic Agonists 61
Nicotinic Receptor Agonists 63
Anticholinesterase Agents 63
Hydrolyzation of Acetylcholine by Cholinesterase 63
Reversible and Irreversible Cholinesterase Inhibitors 63
Cholinesterase Regenerators 69
Pralidoxime Chloride 69
Pralidoxime Iodide 70
Muscarinic Acetylcholine Receptor Antagonists 70
Atropine and Related Alkaloids 70
Synthetic and Semisynthetic Substitutes for Belladonna Alkaloids 75
Nicotinic Acetylcholine Receptor Blocking Agents 77
Ganglionic Blocking Agents 77
Skeletal Muscular Relaxants 77
Chapter 6 Adrenergic Agonists and Antagonists 81
Adrenergic Agonists 81
Characteristics of Adrenergic Agonists 81
Agonists for α and β Adrenoceptors 82
Nonselective α Receptor Agonists 84
Selective α1 Receptor Agonists 85
Selective α2 Receptor Agonists 85
Nonselective β Receptor Agonists 85
Selective β1 Receptor Agonists 86
Selective β2 Receptor Agonists 86
Adrenergic Antagonists 86
α Receptor Antagonists 87
β Receptor Antagonists 88
Chapter 7 Local Anesthetics 94
Classifications of Local Anesthetics 94
Individual Local Anesthetics 95
Methods of Administration of Local Anesthesia 96
Adverse Effects of Local Anesthetics 98
Section 3 Drugs Affecting Central Nervous System 99
Chapter 8 Introduction to Central Nervous System 99
Cellular Basis of the CNS 99
Neurons 99
Support Cells 100
Neuronal Circuits 100
Synapse and Synaptic Transmission 101
Blood-brain Barrier 101
Ion Channels ＆ Neurotransmitter in the CNS 101
Ion Channels 101
Central Neurotransmitters and Receptors 102
Actions of Drugs in the CNS 109
Specificity and Nonspecificity of CNS Drug Actions 109
General Characteristics of CNS Drug Actions 110
Chapter 9 General Anesthetics 114
Actions and Mechanism of General Anesthetics 114
Anatomic Sites of Action of General Anesthetics 114
Cellular and Molecular Mechanisms of General Anesthetics 114
Depth of Anesthesia 115
Measurement of Anesthetic Potency 115
Intravenous Anesthetics 116
Common Intravenous Anesthetics 116
Inhalational Anesthetics 117
Common Inhalational Anesthetics 118
Current Clinical Practice 120
Chapter 10 Sedative-hypnotic Drugs 122
Benzodiazepines 122
Chemistry 122
Pharmacokinetics 122
Mechanism of Action 124
Pharmacological Effects and Therapeutic Uses 124
Adverse Effects 125
New Generation Sedative-hypnotic Drugs 126
Novel Benzodiazepine Receptor Agonists 126
Barbiturates and Other Hypnotics 128
Chapter 11 Antiepileptics 132
Classification of Epilepsy 132
Pathogenesis of Epilepsy 133
Antiepileptic Drugs 133
Chapter 12 Antipsychotics and Antidepressants 135
Antipsychotic Drugs 135
Classification of Antipsychotic Drugs 136
First-generation Antipsychotics 136
Second-generation Antipsychotics 140
Antidepressants 142
Classification of Antidepressants 142
Selective Serotonin Reuptake Inhibitors （SSRIs） 142
Serotonin/Norepinephrine Reuptake Inhibitors （SNRIs） 144
Norepinephrine Reuptake Inhibitors （NRIs） 145
5-HT2 Receptor Antagonist 145
Monoamine Oxidase Inhibitors （MAOIs） 145
Other Antidepressants 146
Drugs for Bipolar Disorder 147
Antianxiety Drugs 147
Chapter 13 Analgesics 150
Opioid Receptor and Mechanism of Action 150
Opioid Receptors 150
Endogenous Opioid Peptides 150
Mechanism of Action 151
Morphine and Opioid Agonists 151
Structure-activity Relationship 151
Pharmacokinetics 151
Pharmacodynamics 152
Therapeutic Uses 152
Adverse Effects 153
Contraindications 153
Other Opioid Receptor Agonists 153
Strong Agonists 153
Moderate Agonists 154
Mixed Agonist-antagonist 154
Opioid Receptor Antagonists 154
Chapter 14 Drugs for Neurodeg-enerative Diseases 155
Anti-Parkinson Drugs 155
Classification of Anti-Parkinson Drugs 156
DA Precursor 157
Levodopa Degradation Inhibitors 158
DA Receptor Agonists 158
Selective MAO-B Inhibitors 160
COMT Inhibitors 160
N-methyl-D-aspartate （NMDA） Receptor Antagonist 160
Antimuscarinic Agents 161
Drugs for Alzheimer’s Disease 161
Acetylcholinesterase （AChE） Inhibitors 162
NMDA Receptor Antagonist 163
Chapter 15 Central Nervous System Stimulants 166
Drugs Mainly Acting on the Cortex 166
Drugs Stimulating Respiratory Center 166
Section 4 Cardiovascular Pharmacology 169
Chapter 16 Diuretics 169
Definition and Classification of Diuretics 169
Physiological Basis of Diuretics 169
Glomerular Filtration 169
Reabsorption and Secretion of Substances in Renal Tubules 170
Common Diuretics 172
High Efficacy Diuretics （Loop Diuretics） 172
Moderate Efficacy Diuretics （Thiazides or Thiazide-like Diuretics） 174
Low Efficacy Diuretics 176
Dehydrants 177
Chapter 17 Anti hypertensive Drugs 179
Classification of Antihypertensive Agents 179
Drugs that Interfere with Renin-angiotensin System 180
ACE Inhibitors 181
Angiotensin Ⅱ Receptor Blockers 183
Renin Inhibitor 184
Calcium Channel Blockers 184
Diuretics 186
Sympathetic Nervous System Inhibitors 186
β Adrenoceptor Blockers 186
α Adrenoceptor Blockers 187
α-/β Adrenoceptor Blocking Agents 188
Centrally Acting Adrenergic Drugs 188
Vasodilators 189
Combination Therapy of Hypertension 190
Chapter 18 Antianginal Drugs 192
Organic Nitrates 194
Chemistry 194
Pharmacokinetics 194
Pharmacodynamics 194
Mechanism of Action 195
Therapeutic Uses 195
Adverse Effects and Drug Interactions 196
β Blockers 197
Pharmacodynamics 197
Therapeutic Uses 197
Adverse Effects and Drug Interactions 197
Calcium Channel Blockers 198
Pharmacodynamics 198
Therapeutic Uses and Adverse Effects 198
Other Antianginal Drugs 199
Chapter 19 Drugs Used in Congestive Heart Failure 201
Drug Classification 201
Representative Drugs Used in Congestive Heart Failure 202
Diuretics 202
Vasodilators 202
Renin-angiotensin-aldosterone Axis Antagonists 203
β Adrenergic Receptor Antagonists 203
Cardiac Glycosides 203
β Adrenergic and Dopaminergic Agonists 205
Phosphodiesterase （PDE） Inhibitors 205
Chapter 20 Anti-arrhythmic Drugs 208
Electrophysiology of Normal Cardiac Rhythm 208
Ionic Basis of Membrane Electrical Activity 209
Automaticity， Conduction，and Refractoriness 209
Mechanisms of Cardiac Arrhythmias 210
Re-entry 210
Enhanced Automaticity 211
Afterdepolarization 211
Mechanisms of Anti-arrhythmic Drugs 211
Slowing Automatic Rhythms 211
Inhibiting Afterdepolarizations and Triggered Activity 212
Inhibiting Re-entry 212
Classification of Anti-arrhythmic Drugs 212
Ⅰ Na＋ Channel Blockers 212
Ⅱβ Adrenoceptor Antagonists 213
Ⅲ Drugs Prolonging Action Potential Duration 213
Ⅳ Ca2＋Channel Blockers 213
Representative Anti-arrhythmic Drugs 213
Chapter 21 Drugs for Hyperlipidemia and Atherosclerosis 217
Pathophysiology of Hyperlipidemia 217
Normal Lipoprotein Metabolism 217
Lipoprotein Disorders 218
Dietary Management of Hyperlipidemia 219
Drugs Used in Hyperlipidemia 220
HMG-CoA Reductase Inhibitors 220
Bile Acid-binding Resins 223
Cholesterol Absorption Inhibitor 224
Fibrates 224
Nicotinic Acid 226
Antioxidants 226
Polyunsaturated Fatty Acids 227
n-3（or ω-3） -type of PUFAs 227
n-6（or ω-6） -type of Fatty Acids 227
Combined Use of Antihyperlipidemic Drugs 228
Section 5 Inflammation， Immunomodulation and Autacoid Pharmacology 231
Chapter 22 NSAIDs and Drugs for Gout 231
Non-steroidal Anti-inflammatory Drugs 231
Pharmacodynamics 233
Adverse Effects 233
Non-selective COX Inhibitors 234
Salicylic Acids 234
Anilines 236
Pyrazolones 237
Indoles 237
Phenylacetic Acids 237
Propionic Acids 238
Oxicams 239
Selective COX-2 Inhibitors 240
Compound Preparations of NSAIDs 241
Choice of NSAIDs 241
Antirheumatic Drugs 241
Drugs Used in Gout 242
Chapter 23 Immunomodulators 246
Immune and Immune Response 246
Immune Response 246
Immunopathogenesis Response 246
Immunosuppressive Agents 247
Glucocorticoid Hormones 248
Calcineurin Inhibitors 249
Antiproliferative/Anti metabolic Agents 251
Antibody 254
Other Immunosuppressive Agents 256
Immunopotentiating Agents 256
Chapter 24 Histamine Antagonists 261
Histamine 261
Distribution of Histamine 261
Synthesis and Metabolism of Histamine 261
Release of Histamine 262
Histamine Receptors 262
Pharmacodynamics 262
Clinical Use of Histamine 262
H1 Receptor Antagonists 262
Pharmacodynamics 263
Pharmacokinetics 264
H2 Receptor Antagonists 264
Pharmacodynamics 264
Pharmacokinetics 265
Adverse Effects 265
Drug Interactions 266
Therapeutic Uses 266
H3 and H4 Receptor Antagonists 266
Chapter 25 Autacoids Pharmacology 268
Membrane Phospholipid Metabolites and Inhibitors 268
Prostaglandins 268
Leukotrienes and Antagonists 270
Platelet Activating Factors 270
5-Hydroxytryptamine 271
5-Hydroxytryptamine and Its Receptors 271
5-HT Receptor Agonists 272
5-HT Receptor Antagonists 273
Polypeptide Drugs 273
Kinins 273
Endothelins 274
Substance P 275
Natriuretic Peptides 275
Angiotensin and Related Drugs 276
Drugs Affecting Adenosine 276
Adenosine and the Receptors 276
Adenosine—Effects and Related Drugs 276
Nitric Oxide Pharmacology 276
Production of NO 276
Pharmacological Effects of Nitric Oxide 277
NO and Related Drugs 278
Chapter 26 Adrenocorticosteriods 280
Chemistry 280
Glucocorticoids 281
Pharmacokinetics 281
Pharmacodynamics 282
Therapeutic Uses 285
Adverse Effects 286
Contraindications 287
Mineralocorticoids 287
Inhibitors of Biosynthesis and Function of Adrenocorticosteroids 287
Chapter 27 Insulin and Other Hypoglycemic Drugs 289
Diabetes 289
Insulin 289
Chemistry 289
Insulin Preparations 290
Pharmacokinetics 290
Pharmacodynamics 291
Therapeutic Uses 293
Adverse Effects 293
Insulin Secretagogues and Other Hypoglycemic Agents 293
Insulin Secretagogues ： Sulfonylureas 294
Insulin Secretagogues ： Repaglinide and Nateglinide 295
Insulin Sensitizer ： Thiazolidinediones 296
α-Glucosidase Inhibitors 297
Glucagon-like Polypeptide-1 （GLP-1）Receptor Agonists 297
Dipeptidyl Peptidase-4 （DPP-4）Inhibitors 297
Amylin Analog 298
Bile Acid Sequestrants 298
Section 6 Endocrine Drugs 301
Chapter 28 Thyroid and Antithyroid Drugs 301
Thyroid Hormone 301
Synthesis and Secretion 301
Treatments of Hyperthyroidism 303
Chapter 29 Pituitary Hormones and Their Hypothalamic Regulators 305
Anterior Pituitary Hormones and Their Hypothalamic Regulators 306
Adrenocorticotropic Hormone 306
Growth Hormone （Somatotropin） and Somatostatin 306
Gonadotropin-releasing Hormone （GnRH）and Its Analogs 306
Follicle-stimulating Hormone （FSH） ，Luteinizing Hormone and Their Analogs 307
Menotropins and Chorionic Gonadotrophin 307
Posterior Pituitary Hormones 307
Chapter 30 Gonadal Hormone and Contraceptives 308
Estrogen and Antiestrogens 308
Estrogen 308
Antiestrogens 308
Progestin and Antiprogestins 309
Androgens and Antiandrogens 309
Contraceptives 310
Chapter 31 Drugs that Affect Bone Mineral Homeostasis 312
Hormonal Regulators of Bone Mineral Homeostasis 312
Nonhormonal Regulators of Bone Mineral Homeostasis 313
Section 7 Drugs Affecting Other Systems 315
Chapter 32 Respiratory Pharmacology 315
Drugs Used in Asthma 315
Glucocorticoids 315
Bronchodilators 317
Anti-leukotrienes 323
Other Drugs 324
Antihistamines 324
Anti-IgE Monoclonal Antibodies 324
Antitussives 325
Centrally Active Antitussives 325
Peripherally Acting Antitussives 325
Expectorants 326
Chapter 33 Digestive Pharmacology 330
Drugs Used In Acid Peptic Diseases 330
Agents That Reduce Intragastric Acidity 330
Proton Pump Inhibitors （PPIs） 331
H2 Receptor Antagonists 332
Antacids 333
Mucosal Protective Agents 334
Antiemetic Agents 335
Pathophysiology 335
Serotonin 5-HT3 Antagonists 336
Neurokinin Receptor Antagonists 337
Substituted Benzamides 337
Drugs Stimulating Gastrointestinal Motility 337
Physiology of the Enteric Nervous System 337
Cholinomimetic Agents 338
Metoclopramide and Domperidone 338
Laxatives 338
Bulk-forming Laxatives 338
Stool Surfactant Agents 339
Osmotic Laxatives 339
Nonabsorbable Sugars or Salts 339
Balanced Polyethylene Glycol 339
Stimulant Laxatives 339
Anthraquinone Derivatives 339
Antidiarrheal Agents 340
Opioid Agonists 340
Pancreatic Enzyme Supplements 340
Bile Acid Therapy for Gallstone 340
Chapter 34 Drugs Affecting Hematologic System 343
Hemostasis and Drug Classification 343
Anticoagulant Agents 344
Heparin and Low-molecular-weight Heparin 344
Thrombolytic Drugs 347
Platelet Aggregation Inhibitors 347
Drugs Used to Treat Bleeding （Coagulants） 348
Chapter 35 Antianemic Drugs and Hematopoietic Growth Factors 351
Antianemic Drugs 351
Hematopoietic Growth Factors 353
Section 8 Chemotherapeutic Drugs 359
Chapter 36 General Principles of Antimicrobial Agents 359
General Concepts 359
Mechanisms for the Antimicrobial Action 360
Inhibition of Synthesis of Bacterial Cell Wall 361
Increased Permeability of Cell Membrane 361
Inhibition of Synthesis and Repair of Nucleic Acids 362
Inhibition of Protein Synthesis 362
Resistance to Antimicrobial Agents 362
Categories of Bacterial Resistance 363
Mechanisms for Bacterial Resistance 363
Transfer of Resistance Gene 365
Multidrug Resistance 365
Principles towards Rational Use of Antibiotics 367
General Principles for Therapeutic Application 367
General Principles for Prophylactic Use of Antibiotics 368
Combination Therapy of Antibiotic Agents 369
Chapter 37 β-lactam Antibiotics 372
Classification， Mechanisms of Action and Resistance 372
Classification 372
Mechanisms of Action 372
Mechanisms of Resistance 373
Penicillins 375
Narrow-spectrum Penicillins 375
Penicillinase-resistant Penicillins 378
Broad-spectrum Penicillins 379
Antipseudomonal Penicillins 380
Penicillins Mainly against Gram-negative Bacteria 380
Cephalosporins 380
First-generation Cephalosporins 380
Second-generation Cephalosporins 382
Third-generation Cephalosporins 382
Fourth-generation Cephalosporins 383
Fifth-generation Cephalosporins 384
Other β-Lactam Antibiotics 384
Carbapenems 384
Cephamycins 385
Oxacephems 386
Monobactams 386
β-Lactamase Inhibitors 386
Chapter 38 Aminoglycosides and Polypeptide Antibiotics 390
Aminoglycosides 390
Common Features of Aminoglycoside Families 390
Polypeptide Antibiotics 396
Glycopeptides Antibiotics 396
Polymyxins 397
Bacitracin 398
Chapter 39 Macrolides and Other Antibiotics 399
Macrolides 399
Clindamycin 401
Tetracyclines 402
Chloramphenicol 404
Oxazolidinones 405
Chapter 40 Quinolones， Sulfon-amides， and Other Synthetic Drugs 408
Quinolones 408
Sulfonamides 411
Other Synthetic Antibacterial Drugs 414
Chapter 41 Drugs for Tuberculosis and Leprosy 417
Antimycobacterial Drugs 417
First-line Drugs for Tuberculosis 417
Second-line Drugs for Tuberculosis 422
Basic Principles of Anti-tuberculosis Drug Administration 424
Anti-leprosy Drugs 425
Chapter 42 Antifungal Agents 429
Drugs for Subcutaneous and Systemic Mycotic Infections 429
Drugs for Cutaneous Mycotic Infections 434
Chapter 43 Antiviral Drugs 436
Nucleoside Reverse Transcriptase Inhibitors 438
Non-nucleoside Reverse Transcriptase Inhibitors 439
Protease Inhibitors 440
DNA and RNA Polymerase Inhibitors 441
Inhibitors of HIV Fusion with Host Cells 442
Neuraminidase Inhibitors and Inhibitors of Viral Coat Disassembly 442
Integrase Inhibitors 443
Chemokine Receptor Antagonists 444
Biologics and Immunomodulators 444
Chapter 44 Drugs Treating Parasitic Infections 447
Antiprotozoal Drugs 447
Chemotherapy for Malaria 447
Drug Classification for Malaria Treatment and Prophylaxis 448
Drugs that Disrupt Parasitic Membrane Structure 448
Artemisinin and Its Derivatives 448
Drugs that Inhibit Heme Polymerase 449
Drugs that Alter Mitochondrial Function 450
Inhibitor of Folate Synthesis 451
Chemotherapy for Amebiasis 451
Antihelminthic Drugs 452
Drugs for the Treatment of Schistosomiasis 452
Drugs for Intestinal Worm Infections 453
Drug for Leishmaniasis 453
Chapter 45 Anticancer Drugs 455
Role of Cell Cycle Kinetics 455
Mechanism of Antineoplastic Agents 456
Antimetabolites 457
Agents Interfering with Synthesis and Function of Protein 460
Agents Interfering with Process of Transcription and RNA Synthesis 461
Agents Directly Affecting Structure and Function of DNA 463
Alkylating Agents 463
Platinum Analogs 464
Antibiotics 466
Topoisomerase Inhibitors 468
Agents Affecting the Balance of Endogenous Hormone 469
Estrogens and Estrogen Antagonists 469
Androgens and Antiandrogens 470
Progestins 471
Antagonists of Adrenocortical Agents 471
GnRH Agents 472
Aromatase Inhibitors 472
Agents that Specifically Inhibit or Block Enzymes and Receptors 472
Topoisomerase Inhibitors 472
Protein Tyrosine Kinase Inhibitors and Growth Factor Receptor Inhibitors 473
Leucine Peptidase Inhibitors 474
Human Epidermal Growth Factor-receptor Protein 2 （HER2） Inhibitors 474
Adenosine Deaminase Inhibitors 475
Ribonucleotide Reductase Inhibitors 475
Agents Inducing Tumor Differentiation 475
Problems Associated with Chemotherapy 477
Index 480