Contents. 1. General Principles of Pharmacology Drugs Acting on Autonomic Nervous System Drugs Acting on Central Nervous System 62

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1 Contents 1. General Principles of Pharmacology 1 Drug 1; History of Pharmacology 1; Route of Administration 3; Pharmacodynamics (Mode of Action of Drugs) 6; Drug Combinations 7; Factors Modifying Drug Action 8; True Tolerance 9; Apparent or Pseudotolerance 9; Drug Receptors 10; Ion Channels 12; Pharmacokinetics 13; Absorption 14; Distribution of Drugs 16; Half-Life of Drugs 19; Drug Concentration 19; Biotransformation (Drug Metabolism) 20; Excretion of Drugs 23; Drug Interactions 25; Drug Toxicity 26; Apoptosis Drugs Acting on Autonomic Nervous System 28 Autonomic Nervous System 28; Central Autonomic Connections 30; Sympathetic System 30; Parasympathetic System 30; Neurohumoral Transmission 32; Adrenergic Neurohumoral Transmission 33; Cholinergic Neurotransmission 35; Adrenergic Agonists (Sympathomimetics) 37; Catecholamines 37; Epinephrine, Norepinephrine and Isoproterenol 37; Non-catecholamines 40; Amphetamine 41; Phenylephrine 41; Methoxamine and Metaraminol 41; Mephentermine 41; Antiadrenergic Drugs 42; Ergot Alkaloids 42; Phenoxybenzamine 43; Tolazoline 43; Phentolamine 44; Prazosin 44; Yohimbine 45; b-adrenergic Blocking Drugs 45; Adrenergic Neuron Blocking Drugs 49; Cholinergic Drugs 50; Parasympathomimetic Agents 50; Acetylcholine 51; Methacholine, Carbachol and Bethanechol 51; Naturally Occurring Cholinomimetic Alkaloids 52; Cholinesterase Inhibitors 53; Organophosphorus Compounds 56; Anticholinergic Drugs (Parasympatholytic Agents) 57; Atropine, Scopolamine and Related Belladonna Alkaloids 58; Synthetic Muscarinic Blocking Agents 59; Selective Muscarinic Receptor Antagonists Drugs Acting on Central Nervous System 62 Central Nervous System 62; Neurotransmitters 63; General Anesthetics 63; Stages of Anesthesia 65; Preanesthetic Medication 66; Administration of General Anesthetics 67; Inhalation Anesthetics 67; Pharmacokinetics of General Anesthetics Inhalation Anesthetics 68; Injectable Anesthetics 69; Inhalation Anesthetics 70; Parenteral Anesthetics 74; Dissociative Anesthetics 81; Sedatives Hypnotics 83; Hypnotics Sedatives 83; Benzodiazepine Antagonist 89; Anticonvulsants (Antiepileptic Drugs) 90; Antiepileptic Drugs 91; Barbiturates 91; Deoxybarbiturates 92; Hydantoins 93; Benzodiazepines 94; Iminostilbene 95; Aliphatic Carboxylic Acid 95; Succinides 96; Phenyltriazine 97; Cyclic Gaba

2 x Veterinary Pharmacology Analog 97; Newer Drugs 97; Miscellaneous Drugs 98; Drugs Controlling Muscle Rigidity and Tremors 99; Antipsychotic and Antianxiety Drugs 102; Antipsychotic Drugs 102; Phenothiazine Derivatives 102; Butyrophenones 105; Thioxanthenes 106; Other Heterocyclics 107; Tardive Dyskinesia 108; Benzodiazepines 108; Azapirones 110; Sedative Antihistaminic 110; b-blocker 111; Drugs for Behavioral Disorders (Antidepressant and Antimanic Drugs) 111; Antidepressants 111; Monoamine Oxidase Inhibitors 112; Reversible Inhibitors of MAO-A 112; Tricyclic Antidepressants 113; Selective Serotonin Reuptake Inhibitors 115; Atypical Antidepressants 116; Antimanic Drugs (Mood Stabilizers) 117; Hallucinogens (Psychedelics, Psychotomimetics, Psychodysleptics, Psychotogens) 117; Opioid Analgesics and Antagonists 119; Opioid Analgesics 119; Other Opium Alkaloids 129; Complex Action Opioids and Antagonists 129; Antipyretics, Analgesics and NSAIDs 132; Non-Selective Cox Inhibitors Salicylates 134; Preferential COX-2 Inhibitors 146; Selective COX-2 Inhibitors 147; Analgesic- Antipyretic with Poor Anti-Inflammatory Action 148; CNS Stimulants and Cerebroactive Drugs Drugs Acting on Peripheral (Somatic) Nervous System 154 Local Anesthetics 154; Miscellaneous Local Anesthetics 160 Skeletal Muscle Relaxants 160 Neuromuscular Blocking Drugs 160 Peripherally Acting Muscle Relaxants 164 Neuromuscular Blocking Drugs 164; Non-Depolarizing Neuromuscular Blocking Drugs 164; Depolarizing Neuromuscular Blocking Drugs 167; Directly Acting Muscle Relaxants 168; Centrally Acting Muscle Relaxants 169; Muscle Relaxant Antagonists Drugs Acting on Respiratory System 172 Classifications 172; Pharyngeal Demulcents 172; Expectorants (Mucokinetics) 173; Mucolytics 175; Antitussives 176; Bronchodilators 178; Drugs for Allergic and Inflammatory Disorders of Respiratory Tract 183; Leukotriene Antagonists 183; Mast Cell Stabilizers 183; Corticosteroids Drugs Acting on Cardiovascular System 186 Cardiovascular Drugs 186; Antihypertensives 191; Ganglionic Blocking Agents 193; Mixed Adrenergic Antagonists 194; b-adrenergic Blockers 194; Antiarrhythmic Agents 200; Antiarrhythmic Drugs 201; Vasodilators Drugs Affecting Blood and Blood Formation 211 Hematinics 211 Iron 211; Cobalt 214; Copper (Blue Vitriol, Roman Vitriol) 214; Vitamin B 12 (Cyanocobalamin, Erythrocyte Maturing Factor, Antipernicious Anemia Factor) 215; Folic Acid 215

3 Contents xi Coagulants 216 Coagulation of Blood 216; Coagulants (Hemostatics) 217 Anticoagulants 222 In vitro Anticoagulants 222 Hypolipoproteinemic Drugs 228 Physiology of Lipoproteins 228 Plasma Volume Expanders 234 Blood Drugs Acting on Gastrointestinal System 236 Drugs Acting on Mouth 236 Sialics (Sialogogues) 236; Antisialogogues 236 Drugs Acting on Stomach 237 Drugs Stimulating Gastric Secretions 237; Drugs Inhibiting Gastric Secretions 237; H 2 Receptor Antagonists 238; Proton Pump Inhibitors 239; Muscarinic Receptor Antagonists 241; Prostaglandin Analogs 241 Antacids 241 Systemic Antacids 242; Non-Systemic Antacids 242; Antacid Combinations 244; Ulcer Protectives 244; Ulcer Healing Drugs 245 Emetics, Antiemetics and Prokinetic Drugs 245 Emetics 245; Locally Acting Emetics 245; Centrally Acting Emetics 246; Antiemetics 247; Locally Acting Antiemetics 248; Centrally Acting Antiemetics 248 Stomachic/Digestants 253 Digestants 253; Stomachics 255; Aromatic Bitters 256; Alkaloidal Bitters 256; Antistomachics 257; Carminatives 257; Antizymotics 260; Ruminotorics 261; Drugs for Closure of Esophageal Groove 262 Drugs Acting on Intestine 263 Antispasmodics 263 Purgatives 264 Bulk Purgatives 264; Stimulant Purgatives 266; Direct Stimulant Purgatives Diphenylmethanes 266; Resinous Cathartics 267; Fixed Oils 268; Indirect Irritant Purgatives 268; Osmotic Purgatives 270; Fecal Softeners 272; Docusates 272; Neuromuscular Purgatives 272 Antidiarrheal Drugs (Intestinal Astringents) 273

4 xii Veterinary Pharmacology Non-Specific Antidiarrheal Drugs 273 Gastrointestinal Protectants and Adsorbents 273; Antisecretory Drugs 274; Antimotility Drugs 275; Miscellaneous Drugs 276; Intestinal Astringents 276 Specific Antidiarrheal Drugs 277 Drugs Acting on Liver Drugs Acting on Urinary System 279 Renal Functions and Urine Formation 279; Diuretics 282; High Ceiling (Loop) Diuretics 282 Medium Efficacy Diuretics 284 Thiazide and Related Diuretics 284; Carbonic Anhydrase Inhibitors 286; Potassium Sparing Diuretics 287; Aldosterone Antagonists 287; Osmotic Diuretics 288; Xanthines 289; Antidiuretics 289; Synthetic Analogs 291; Thiazides 292; Miscellaneous Drugs 292 Drugs Acting on Fluid, Electrolyte and Acid-Base Balance 292 Acidosis 296; Alkalosis 296; Edema 297; Urinary Acidifiers and Alkalinizers 297; Urinary Acidifiers 298; Urinary Alkalinizers (Alkalizers) 298; Urinary Antiseptics Drugs Acting on Endocrine System 301 Hormones 301; Hormone Therapy 302; Hormone Antagonists 303; Antihormones 303; Hormone Synthesis Inhibitors 303; Pituitary Hormones 304; Anterior Pituitary Hormones 304; Posterior Pituitary Hormones 311; Antidiuretic Hormone (Vasopressin) 311; Male Sex Hormones 314; Female Sex Hormones 319; Antiestrogens 322; Estrogen Receptor Inhibitors 322; Progestins 323; Synthetic Progestogens 325; Antiprogestins 326; Corticosteroids 327; Glucocorticoids 328; Preparations and Dose 331; Adrenal Cortex Inhibitors 333; Insulin and Oral Hypoglycemic Drugs 333; Oral Hypoglycemic Drugs 337; Sulfonylureas 337; Meglitinide/D-Phenylalanine Analogs 339; a-glucosidase Inhibitors 340; Glucagon 340; Thyroid and Parathyroid Hormones 341; Antithyroid Drugs 346; Calcitonin 348; Parathyroid Hormone (Parathormone) 348; Melatonin 349; Drugs Acting on Uterus 350; Ecbolics 350; Posterior Pituitary Hormones and Analogs 350; Ergot Alkaloids 351; Prostaglandins and Analogs 352; Miscellaneous Drugs 352; Tocolytics Autacoids and Related Drugs 355 Autacoids and Related Drugs 355; Histamine 355 Antihistamines (Antihistaminics) 358 H 1 Antagonists 359; Piperazine Group 360; 5-Hydroxytryptamine (Serotonin) 362; Pharmacological Actions 363; Modulators of Serotonergic System 364; Selective 5HT Receptor Antagonists 364; Lipid Derived Autacoids 365; Physiological Pharmacological Effects 367

5 Inhibitors of Eicosanoids 370 Inhibitors of Eicosanoid Synthesis 370; Platelet Activating Factor 370; Pharmacological Properties 372; Angiotensins 372; Angiotensin Converting Enzyme Inhibitors 374; Angiotensin-II Receptor Antagonists 375; Kinins 375; Kinin and Kininase Inhibitors 377 Drugs for Rheumatoid Arthritis and Gout 377 Antirheumatoid Drugs 377; Immunosuppressants 380; Adjuvant Drugs 380; Drugs for Gout 380; Drugs for Acute Gout 381; Drugs for Chronic Gout/Hyperuricemia 381; Uric Acid Synthesis Inhibitor 381; Uricosuric Drugs 382; Chondroprotective Drugs 382 Contents xiii 12. Antimicrobial Drugs 385 General Considerations 385; Mechanism of Bacterial Resistance 385; Importance of Extra-Chromosomal Resistance Factors 386; Antibiotics 387; Sulfonamides, Trimethoprim and Sulfones 388; Trimethoprim 392; Sulfonamide and Trimethoprim 392; Sulfones 393; b-lactam Antibiotics 393; Penicillins 394; Semisynthetic Penicillins 397; Penicillinase Resistant Penicillins 397; Acid Resistant Penicillins 398; Broad Spectrum Penicillins (Extended Spectrum Penicillins) 398; Aminopenicillins 399; Carboxypenicillins 400; Mecillinam (Amdinocillin) 401; Ureidopenicillins 401; β-lactamase Inhibitors 401; Cephalosporins 402; Cephamycins 408; Monobactams 408; Carbapenems 409 Broad-Spectrum Antibiotics 409 Tetracyclines 409; Amphenicols 411; Chloramphenicol 411; Aminoglycoside Antibiotics 413; Macrolides 419; Semisynthetic Macrolides 421; Miscellaneous Antibiotics 423; Polypeptide Antibiotics 424; Oxazolidinone 426; Quinolones 426; Fluoroquinolones 427; Nitrofurans 433 Antifungal Drugs 435 Characteristics of an Ideal Antifungal Agent 435; Fungal Nucleic Acid Inhibitors 436; Inhibitor of Fungal Mitosis 437; Inhibitors of the Ergosterol Synthesis Pathway 437; Inhibitors of Fungal Membrane Stability 440; Inhibitors of Fungal Cell Wall Synthesis 442; Iodides 442; Miscellaneous Drugs 443; Antitubercular Drugs 444; First Line Drugs 445; Second Line Drugs 446 Antiviral Drugs 448 Inhibitors of Viral Genome Replication 449; Antiherpes Virus Nucleoside and Nucleotide Analogs 449; Anti-HIV and HBV Nucleoside and Nucleotide Analogs 451; Non-Nucleoside DNA Polymerase Inhibitors 452; Non-Nucleoside Reverse Transcriptase Inhibitors 452; Inhibition of Viral Mutation 452; Inhibition of Viral Release 452; Anti-Influenza Virus Drugs 453; Antiviral Drugs with Unknown Mechanism of Action 453; Drugs that Modulate the Immune System 453 Anthelmintics 454 Classification of Anthelmintics 455; Piperazine Compounds 455; Benzimidazoles 456; Benzimidazole Prodrugs 460; Imidazothiazoles 461; Tetrahydropyrimidines 462; Pyrazinoisoquinolines and Benzazepins 463; Macrolides 464; Milbemycins 465; Sulfonamides 466; Salicylamides 466;

6 xiv Veterinary Pharmacology Substituted Phenols 467; Arsenicals 468; Bromsalans 469; Halogenated Hydrocarbons 469; Organophosphate Anthelmintics 469; Miscellaneous Anthelmintics 471 Antiprotozoal Drugs 472 Anticoccidial Drugs 472; Sulfonamides 472; Pyrimidines (Diaminopyrimidines) 473; Thiamine Antagonists 473; Symmetrical Triazinones 474; Benzene Acetonitriles 474; Carbanilides 475; Benzylpurines 475; Dinitrobenzamide 475; Guanides 476; Pyridinoles 476; Polyether Antibiotics 476; Quinazolines 478; Nitrofurans 478; Miscellaneous Drugs 478 Antihistomonial Drugs 479 Nitrothiazole Compounds 479; Nitroimidazoles 479 Antitrypanosomal and Antipyroplasmic Drugs 480 Classification 480; Aminophenanthridium Compounds 480; Quinapyramine Compounds 481; Carbamide Derivative 482; Dyes 482; Naphthoquinones 483; Miscellaneous Drugs 483; Drugs for Intestinal Protozoa 484; Benzimidazoles 486 Antimalarial Drugs 487 Mode of Action Antineoplastic Drugs 493 Classification of Anticancer Drugs 493; Alkylating Agents and Related Compounds 494; Antimetabolites 496; Cytotoxic Antibiotics 497; Plant Derivatives 499; Hormones 500; Hormone Antagonists 500; Miscellaneous Drugs 501; Monoclonal Antibodies 502; Biological Response Modifiers Miscellaneous Drugs 503 Drugs Acting on Skin and Mucous Membranes 503 Demulcents 503; Emollients 504; Adsorbents and Protectives 504; Astringents 505; Irritants and Counter-Irritants 506; Caustics and Escharotics 508; Keratolytics and Keratoplastics 508; Antiseborrheics 509; Melanizing Agents 510; Demelanizing Agents 511; Antiseptics and Disinfectants 511 Properties of an Ideal Antiseptic 511; Factors which Modify Antisepsis or Disinfection 512; Phenolic Compounds 513; Oxidizing Agents 514; Reducing Agents 515; Halogens 515 Surface Acting Agents 517 Anionic Surfactants 517; Cationic Compounds 517 Biguanides (Bisguanides) 518 Chlorhexidine 518

7 Alcohols 518 Ethanol (Ethyl Alcohol) 518; Isopropanol 518; Acids 518; Alkalies 519 Metallic Salts 519 Silver Compounds 519; Mercury Compounds 520; Zinc Compounds 520 Dyes 520 Acridine Dyes 520; Rosaniline Dyes 521; Azo Dyes 522; Miscellaneous Agents 522; EDTA 522; Ectoparasiticides 522 Insecticides 523 Organophosphorus Compounds 523; Carbamates 524; Organochlorine Insecticides 525; Formamidine Compounds 526; Chloronicotinyl Compounds 527; Phenylpyrazole Insecticides 527; Herbal Insecticides 527; Pyrethrins and Pyrethroid Insecticides 528; Natural Compounds 528; Synthetic Pyrethroids 528 Avermectins and Milbemycins/Macrocyclic Lactons (For Details See Anthelmintics) 530 Insect Growth Regulators 530; Juvenile Hormone Analogs/ Juvenoids 530; Chitin Synthesis Inhibitors 531; Miscellaneous Agents 531 Repellents and Synergists 532 Repellents 532; Synergists 532; Chelating Agents and Antidotes 532; Chelating Agents 533; Monodentate and Bidentate Chelators 533 Polydentate Agents 535 EDTA and its Salts 535; DTPA and its Salts 536; Other Polydentate Chelators 536 Agents Act through Enzyme Associated Reactions 537 Enzyme Reactivators 537; Enzyme Inhibitors 538; Antidotes 538; Functional Antidotes 539; Pharmacological Antidotes 540; Immunomodulators 541; Immunostimulants 541; Immunosuppressants 544 Agents Inhibit IL-2 Production or Action 544 Cyclosporine (Cyclosporin-A) 544; Agents Inhibiting Cytokine Gene Expression 546; Cytostatics 546; Alkylating Agents 546; Antimetabolites 546; Cytotoxic Antibiotics 547; Antibodies 548; Polyclonal Antibodies 548; Monoclonal Antibodies 548; Synthetic Androgens 548; Gene Therapy 549; Methods of Gene Therapy 549 Contents xv Bibliography 551 Index 553