全国高等学校药学类专业教材 药理学 英文版PDF电子书下载

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