General and molecular pharmacology : principles of drug action /
General and molecular pharmacology : principles of drug action /
Francesco Clementi, Guido Fumagalli, editors ; Christian Chiamulera, Emilio Clementi, Dino Fesce, Diego Fornasari, Cecilia Gotti, co-editors.
- xlviii, 732 pages : illustrations (black and white) ; 28 cm
pharmacy bookfair2016
Includes bibliographical references and index.
Title Page -- Copyright Page -- Contents -- List of Contributors -- Preface -- SECTION 1 INTRODUCTION TO PHARMACOLOGY -- CHAPTER 1 ESSENTIAL LEXICON OF PHARMACOLOGY -- THE SOCIAL IMPACT OF PHARMACOLOGY -- ESSENTIAL LEXICON -- Active Substances -- Pharmacological Disciplines -- Drug-Receptor Interactions -- Measure of the Clinical Response -- TAKE-HOME MESSAGE -- CHAPTER 2 A SHORT HISTORY OF PHARMACOLOGY -- BIRTH AND HISTORICAL DEVELOPMENTS OF PHARMACOLOGY -- From Magical and Natural Remedies of Ancient Medicine to Arabic Alchemy -- From Monastic Medicine to Botanical Gardens -- From Anatomical Renaissance to the "Experienz": Paracelsus' Spagyric -- From Iatrochemistry to the Age of Enlightenment -- From the Search of the Active Principle to the Discovery of Alkaloids and Glucosides -- The Drug Synthesis Revolution: From Handmade to Industrial Production -- MODERN PHARMACOLOGY -- Ehrlich and Chemotherapy: The Concept of Receptor -- The Birth of Modern Pharmacology -- THE BIOTECHNOLOGY ERA AND THE PHARMACOLOGY IN THE THIRD MILLENNIUM -- The Impact of New Biotechnologies: Molecular Biology, Bioinformatics, and Combinatorial Chemistry -- Biological Drugs and Pharmacology Perspectives -- Personalized Therapies and New Sceneries in Pharmaceutical Industry -- TAKE-HOME MESSAGE -- FURTHER READING -- SECTION 2 GETTING THE DRUG TO ITS SITE OF ACTION -- CHAPTER 3 CELLULAR BASIS OF PHARMACOKINETICS -- A QUICK JOURNEY WITH THE DRUG IN THE BODY -- Absorption -- Distribution -- Drug Elimination -- CROSSING CELL MEMBRANES -- Passive Diffusion across Cell Membranes -- Drug Transport across Cell Membranes -- Endocytosis -- DRUG DIFFUSION TO ORGANS AND TISSUES -- Properties of the Most Important Cell Barriers -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 4 DRUG ABSORPTION AND ADMINISTRATION ROUTES -- GENERAL RULES ABOUT DRUG ABSORPTION RATE.
Partition Coefficient -- Drug Dispersion -- Extension of the Absorbing Surface -- Permeability of the Absorbing Surface -- Vascularization -- ENTERAL ROUTES OF ADMINISTRATION -- Oral Route -- Sublingual and Rectal Routes -- SYSTEMIC PARENTERAL ROUTES OF ADMINISTRATION -- The Intravascular Route -- i.m. Injection -- Subcutaneous and Intradermal Injections -- OTHER ROUTES OF DRUG ADMINISTRATION -- Inhalation Route -- Topical/Regional Routes -- Intracavity Routes -- Dermal or Transcutaneous Route -- Mucosal Routes -- ABSORPTION KINETICS -- General Rules -- Interrelation between Gene Therapy and Drug Delivery Techniques -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 5 DRUG DISTRIBUTION AND ELIMINATION -- DISTRIBUTION -- Tissues and Avidity for Drugs -- The Apparent Distribution Volume -- Drug Binding to Plasma Proteins -- Factors That Determine the Distribution Rate of Drugs to the Various Compartments -- ELIMINATION -- The Concept of Half-Life -- The Concept of Clearance -- RENAL EXCRETION OF DRUGS -- Glomerular Filtration -- Tubular Functions and Pharmacokinetics -- Active Transport of Organic Anions and Cations -- Factors Determining Renal Clearance of Drugs -- HEPATIC EXCRETION AND ENTEROHEPATIC CYCLE -- Perfusion, Binding to Plasma Proteins, Enzymatic Activity, and Hepatic Clearance -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 6 DRUG METABOLISM -- METABOLIC MODIFICATION OF DRUG ACTIVITY -- TWO PHASES OF DRUG METABOLISM -- Phase I Reactions -- Phase II Enzymatic Reactions -- EXTRAHEPATIC BIOTRANSFORMATIONS -- Biotransformation by the Intestinal Flora -- PHARMACOMETABOLIC INDUCTION AND INHIBITION -- Induction of Drug Metabolism -- Inhibition of Drug Metabolism -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 7 CONTROL OF DRUG PLASMA CONCENTRATION -- TIME COURSE OF DRUG PLASMA CONCENTRATION FOLLOWING A SINGLE ADMINISTRATION.
DRUGS DISTRIBUTE TO ORGANS AND TISSUES AND THEN ARE ELIMINATED -- Description of Drug Plasma Concentration Time Course Following a Single Administration -- Area under the Plasma Concentration Curve (AUC) -- The Plasma Concentration Peak -- DRUG PLASMA CONCENTRATION TIME COURSE DURING REPETITIVE ADMINISTRATIONS -- During Repetitive Administrations, the Drug Plasma Concentration Time Course Is Given by the Sum of the Time Courses of the Single Doses -- In a Chronic Therapy at Steady State, Each New Dose Replaces the Drug Amount that has been Eliminated Since the Last Administration -- The Time to Reach the Steady State Depends on the Drug Half-Life -- Plasma Concentration at Steady State -- The Single Dose to Administer is Computed as a Function of the Interval between Successive Administrations -- Fluctuations of Drug Plasma Concentration at Steady State -- Absorption Kinetics Influence the Amplitude of Oscillations in Plasma Concentration at Steady State -- Loading (Attack) Doses to Rapidly Attain Steady-State Concentration -- MULTICOMPARTMENTAL KINETICS -- Drug Binding to Plasma Proteins and Tissue Equilibration with Plasma -- The Particular Case of the Nephron -- Drugs Redistribution among Compartments -- CORRECTIONS OF THE THERAPEUTIC REGIMEN -- Normally Available Pharmacokinetic Data Are Average Values -- Varying Dosage as a Function of Body Weight and Physical Constitution -- Varying Dosage as a Function of Age -- Dosage Correction in the Presence of Hepatic Pathologies -- Dosage Correction in the Presence of Renal Pathologies -- TAKE-HOME MESSAGE -- FURTHER READING -- SECTION 3 RECEPTORS AND SIGNAL TRANSDUCTION -- CHAPTER 8 DRUG-RECEPTOR INTERACTIONS: QUANTITATIVE AND QUALITATIVE ASPECTS -- GENERAL PROPERTIES OF DRUG RECEPTORS -- Drug Receptors Are Molecules Relevant for Cellular Functions -- Not All Drugs Interact with a Receptor.
Drug Activity Follows to Drug-Receptor Complex Formation -- Drug-Receptor Interaction Is Mostly Mediated by Weak Chemical Bonds -- Reversible or Irreversible Drug-Receptor Interactions -- CHARACTERISTICS OF DRUG-RECEPTOR INTERACTION -- The Relationship between Drug Concentration and Drug-Receptor Complex Is Similar to the Michaelis-Menten Equation -- The Binding Isotherm and Its Linear Transformations Allow to Obtain the Parameters of the Drug-Receptor Interaction -- Receptors Can Be Heterogeneous -- Drug Competition for a Same Receptor Binding Site -- QUANTITATIVE ASPECTS OF DRUG EFFECTS: DOSE-RESPONSE CURVES -- Potency and Efficacy -- FROM DRUG-RECEPTOR INTERACTION TO DRUG RESPONSE -- Occupancy Theory -- Modifications to the Occupancy Assumption -- Efficacy Theory -- Nonlinear Function between Receptor Occupancy and Tissue Response: EC50 Different from Kd -- Constitutively Active Receptors and Inverse Agonists -- Two-State Receptor Model and Beyond: Multiple Receptor States and "Biased" Signaling -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 9 RECEPTORS AND MODULATION OF THEIR RESPONSE -- CLASSES OF RECEPTORS AND STRATEGIES OF SIGNAL TRANSDUCTION -- Intracellular/Intranuclear Receptors -- Membrane Receptors -- CONTROL OF RECEPTOR LOCALIZATION IN THE CELL MEMBRANE -- INTRACELLULAR TRAFFIC OF CELL RECEPTORS -- How Receptors Reach the Cell Membrane and how Their Number is Regulated -- MODULATION OF RECEPTOR RESPONSES -- RECEPTOR MODULATION BY DRUGS -- TAKE-HOME MESSAGE -- FURTHER READING -- General -- Intracellular Receptors -- Ligand-gated Ion Channels -- G Protein-Coupled Receptors -- Catalytic Receptors -- Chemokine Receptors -- Toll-Like Receptors -- Death Receptors -- CHAPTER 10 ADAPTATION TO DRUG RESPONSE AND DRUG DEPENDENCE -- MOLECULAR, CELLULAR, AND SYSTEMIC ADAPTATION -- Cellular Adaptation -- Effects of Repeated Drug Exposure. DRUG ADDICTION AS A PARADIGM OF ALLOSTATIC ADAPTATION -- Adaptation and Stages of Drug Addiction -- Research on Drug Addiction -- THERAPY FOR DRUG DEPENDENCE -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 11 PHARMACOLOGICAL MODULATION OF POSTTRANSLATIONAL MODIFICATIONS -- PROTEIN PHOSPHORYLATION -- Protein Kinases -- Protein Phosphatases -- SUMOylation -- UBIQUITINATION -- GLYCOSYLATION -- ACETYLATION -- HYDROXYLATION -- CARBOXYLATION -- METHYLATION -- S-NITROSYLATION -- DISULFIDE BONDS -- LIPID MODIFICATIONS -- Myristoylation -- Prenylation -- Palmitoylation -- Attachment of Glycosylphosphatidylinositols -- PHARMACOLOGICAL MODULATION OF POST TRANSLATIONAL MODIFICATIONS -- Deacetylase Inhibitors -- Glycosylation Inhibitors -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 12 CALCIUM HOMEOSTASIS WITHIN THE CELLS -- THE CYTOSOL: A CROSSROAD OF Ca2+ FLUXES -- Free Ca2+ in the Cytosol and Total Cell Calcium -- The High-Affinity Buffering of Cytosolic Proteins -- THE PLASMA MEMBRANE: CHANNELS, PUMPS, AND TRANSPORTERS -- Surface Channels Permeable to Ca2+ -- Surface Pumps and Transporters -- Ca2+ IN INTRACELLULAR ORGANELLES -- The ER: A Rapidly Exchanging Ca2+ Pool -- Mitochondria as Local Buffers of [Ca2+]i -- ER and Mitochondria Allow Rapid Changes of [Ca2+]i within Cells -- [Ca2+]i Control in Other Intracellular Structures -- Local Relevance of Organelle Calcium Pools -- Ca2+ IN CELL PATHOLOGY -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 13 PHARMACOLOGY OF MAP KINASES -- THE MAPK FAMILY AND THE ACTIVATION MECHANISM -- The ERK Family -- The JNK Family -- The p38 Family -- ERK5 -- MAPK SPECIFICITY -- Duration of Action -- Multiple Enzyme Isoforms -- Subcellular Localization and Interaction with Scaffold Proteins -- miRNAs -- PHARMACOLOGICAL INHIBITION OF MAPK -- Inhibition of the Ras/RAF/MEK/ERK Cascade -- MEK -- RAF -- JNKs -- p38.
9781118768570 (cloth : alk. paper)
2015008098
Chemistry, Pharmaceutical.
Molecular Biology.
Pharmacological Phenomena.
615.19 / G
pharmacy bookfair2016
Includes bibliographical references and index.
Title Page -- Copyright Page -- Contents -- List of Contributors -- Preface -- SECTION 1 INTRODUCTION TO PHARMACOLOGY -- CHAPTER 1 ESSENTIAL LEXICON OF PHARMACOLOGY -- THE SOCIAL IMPACT OF PHARMACOLOGY -- ESSENTIAL LEXICON -- Active Substances -- Pharmacological Disciplines -- Drug-Receptor Interactions -- Measure of the Clinical Response -- TAKE-HOME MESSAGE -- CHAPTER 2 A SHORT HISTORY OF PHARMACOLOGY -- BIRTH AND HISTORICAL DEVELOPMENTS OF PHARMACOLOGY -- From Magical and Natural Remedies of Ancient Medicine to Arabic Alchemy -- From Monastic Medicine to Botanical Gardens -- From Anatomical Renaissance to the "Experienz": Paracelsus' Spagyric -- From Iatrochemistry to the Age of Enlightenment -- From the Search of the Active Principle to the Discovery of Alkaloids and Glucosides -- The Drug Synthesis Revolution: From Handmade to Industrial Production -- MODERN PHARMACOLOGY -- Ehrlich and Chemotherapy: The Concept of Receptor -- The Birth of Modern Pharmacology -- THE BIOTECHNOLOGY ERA AND THE PHARMACOLOGY IN THE THIRD MILLENNIUM -- The Impact of New Biotechnologies: Molecular Biology, Bioinformatics, and Combinatorial Chemistry -- Biological Drugs and Pharmacology Perspectives -- Personalized Therapies and New Sceneries in Pharmaceutical Industry -- TAKE-HOME MESSAGE -- FURTHER READING -- SECTION 2 GETTING THE DRUG TO ITS SITE OF ACTION -- CHAPTER 3 CELLULAR BASIS OF PHARMACOKINETICS -- A QUICK JOURNEY WITH THE DRUG IN THE BODY -- Absorption -- Distribution -- Drug Elimination -- CROSSING CELL MEMBRANES -- Passive Diffusion across Cell Membranes -- Drug Transport across Cell Membranes -- Endocytosis -- DRUG DIFFUSION TO ORGANS AND TISSUES -- Properties of the Most Important Cell Barriers -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 4 DRUG ABSORPTION AND ADMINISTRATION ROUTES -- GENERAL RULES ABOUT DRUG ABSORPTION RATE.
Partition Coefficient -- Drug Dispersion -- Extension of the Absorbing Surface -- Permeability of the Absorbing Surface -- Vascularization -- ENTERAL ROUTES OF ADMINISTRATION -- Oral Route -- Sublingual and Rectal Routes -- SYSTEMIC PARENTERAL ROUTES OF ADMINISTRATION -- The Intravascular Route -- i.m. Injection -- Subcutaneous and Intradermal Injections -- OTHER ROUTES OF DRUG ADMINISTRATION -- Inhalation Route -- Topical/Regional Routes -- Intracavity Routes -- Dermal or Transcutaneous Route -- Mucosal Routes -- ABSORPTION KINETICS -- General Rules -- Interrelation between Gene Therapy and Drug Delivery Techniques -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 5 DRUG DISTRIBUTION AND ELIMINATION -- DISTRIBUTION -- Tissues and Avidity for Drugs -- The Apparent Distribution Volume -- Drug Binding to Plasma Proteins -- Factors That Determine the Distribution Rate of Drugs to the Various Compartments -- ELIMINATION -- The Concept of Half-Life -- The Concept of Clearance -- RENAL EXCRETION OF DRUGS -- Glomerular Filtration -- Tubular Functions and Pharmacokinetics -- Active Transport of Organic Anions and Cations -- Factors Determining Renal Clearance of Drugs -- HEPATIC EXCRETION AND ENTEROHEPATIC CYCLE -- Perfusion, Binding to Plasma Proteins, Enzymatic Activity, and Hepatic Clearance -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 6 DRUG METABOLISM -- METABOLIC MODIFICATION OF DRUG ACTIVITY -- TWO PHASES OF DRUG METABOLISM -- Phase I Reactions -- Phase II Enzymatic Reactions -- EXTRAHEPATIC BIOTRANSFORMATIONS -- Biotransformation by the Intestinal Flora -- PHARMACOMETABOLIC INDUCTION AND INHIBITION -- Induction of Drug Metabolism -- Inhibition of Drug Metabolism -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 7 CONTROL OF DRUG PLASMA CONCENTRATION -- TIME COURSE OF DRUG PLASMA CONCENTRATION FOLLOWING A SINGLE ADMINISTRATION.
DRUGS DISTRIBUTE TO ORGANS AND TISSUES AND THEN ARE ELIMINATED -- Description of Drug Plasma Concentration Time Course Following a Single Administration -- Area under the Plasma Concentration Curve (AUC) -- The Plasma Concentration Peak -- DRUG PLASMA CONCENTRATION TIME COURSE DURING REPETITIVE ADMINISTRATIONS -- During Repetitive Administrations, the Drug Plasma Concentration Time Course Is Given by the Sum of the Time Courses of the Single Doses -- In a Chronic Therapy at Steady State, Each New Dose Replaces the Drug Amount that has been Eliminated Since the Last Administration -- The Time to Reach the Steady State Depends on the Drug Half-Life -- Plasma Concentration at Steady State -- The Single Dose to Administer is Computed as a Function of the Interval between Successive Administrations -- Fluctuations of Drug Plasma Concentration at Steady State -- Absorption Kinetics Influence the Amplitude of Oscillations in Plasma Concentration at Steady State -- Loading (Attack) Doses to Rapidly Attain Steady-State Concentration -- MULTICOMPARTMENTAL KINETICS -- Drug Binding to Plasma Proteins and Tissue Equilibration with Plasma -- The Particular Case of the Nephron -- Drugs Redistribution among Compartments -- CORRECTIONS OF THE THERAPEUTIC REGIMEN -- Normally Available Pharmacokinetic Data Are Average Values -- Varying Dosage as a Function of Body Weight and Physical Constitution -- Varying Dosage as a Function of Age -- Dosage Correction in the Presence of Hepatic Pathologies -- Dosage Correction in the Presence of Renal Pathologies -- TAKE-HOME MESSAGE -- FURTHER READING -- SECTION 3 RECEPTORS AND SIGNAL TRANSDUCTION -- CHAPTER 8 DRUG-RECEPTOR INTERACTIONS: QUANTITATIVE AND QUALITATIVE ASPECTS -- GENERAL PROPERTIES OF DRUG RECEPTORS -- Drug Receptors Are Molecules Relevant for Cellular Functions -- Not All Drugs Interact with a Receptor.
Drug Activity Follows to Drug-Receptor Complex Formation -- Drug-Receptor Interaction Is Mostly Mediated by Weak Chemical Bonds -- Reversible or Irreversible Drug-Receptor Interactions -- CHARACTERISTICS OF DRUG-RECEPTOR INTERACTION -- The Relationship between Drug Concentration and Drug-Receptor Complex Is Similar to the Michaelis-Menten Equation -- The Binding Isotherm and Its Linear Transformations Allow to Obtain the Parameters of the Drug-Receptor Interaction -- Receptors Can Be Heterogeneous -- Drug Competition for a Same Receptor Binding Site -- QUANTITATIVE ASPECTS OF DRUG EFFECTS: DOSE-RESPONSE CURVES -- Potency and Efficacy -- FROM DRUG-RECEPTOR INTERACTION TO DRUG RESPONSE -- Occupancy Theory -- Modifications to the Occupancy Assumption -- Efficacy Theory -- Nonlinear Function between Receptor Occupancy and Tissue Response: EC50 Different from Kd -- Constitutively Active Receptors and Inverse Agonists -- Two-State Receptor Model and Beyond: Multiple Receptor States and "Biased" Signaling -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 9 RECEPTORS AND MODULATION OF THEIR RESPONSE -- CLASSES OF RECEPTORS AND STRATEGIES OF SIGNAL TRANSDUCTION -- Intracellular/Intranuclear Receptors -- Membrane Receptors -- CONTROL OF RECEPTOR LOCALIZATION IN THE CELL MEMBRANE -- INTRACELLULAR TRAFFIC OF CELL RECEPTORS -- How Receptors Reach the Cell Membrane and how Their Number is Regulated -- MODULATION OF RECEPTOR RESPONSES -- RECEPTOR MODULATION BY DRUGS -- TAKE-HOME MESSAGE -- FURTHER READING -- General -- Intracellular Receptors -- Ligand-gated Ion Channels -- G Protein-Coupled Receptors -- Catalytic Receptors -- Chemokine Receptors -- Toll-Like Receptors -- Death Receptors -- CHAPTER 10 ADAPTATION TO DRUG RESPONSE AND DRUG DEPENDENCE -- MOLECULAR, CELLULAR, AND SYSTEMIC ADAPTATION -- Cellular Adaptation -- Effects of Repeated Drug Exposure. DRUG ADDICTION AS A PARADIGM OF ALLOSTATIC ADAPTATION -- Adaptation and Stages of Drug Addiction -- Research on Drug Addiction -- THERAPY FOR DRUG DEPENDENCE -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 11 PHARMACOLOGICAL MODULATION OF POSTTRANSLATIONAL MODIFICATIONS -- PROTEIN PHOSPHORYLATION -- Protein Kinases -- Protein Phosphatases -- SUMOylation -- UBIQUITINATION -- GLYCOSYLATION -- ACETYLATION -- HYDROXYLATION -- CARBOXYLATION -- METHYLATION -- S-NITROSYLATION -- DISULFIDE BONDS -- LIPID MODIFICATIONS -- Myristoylation -- Prenylation -- Palmitoylation -- Attachment of Glycosylphosphatidylinositols -- PHARMACOLOGICAL MODULATION OF POST TRANSLATIONAL MODIFICATIONS -- Deacetylase Inhibitors -- Glycosylation Inhibitors -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 12 CALCIUM HOMEOSTASIS WITHIN THE CELLS -- THE CYTOSOL: A CROSSROAD OF Ca2+ FLUXES -- Free Ca2+ in the Cytosol and Total Cell Calcium -- The High-Affinity Buffering of Cytosolic Proteins -- THE PLASMA MEMBRANE: CHANNELS, PUMPS, AND TRANSPORTERS -- Surface Channels Permeable to Ca2+ -- Surface Pumps and Transporters -- Ca2+ IN INTRACELLULAR ORGANELLES -- The ER: A Rapidly Exchanging Ca2+ Pool -- Mitochondria as Local Buffers of [Ca2+]i -- ER and Mitochondria Allow Rapid Changes of [Ca2+]i within Cells -- [Ca2+]i Control in Other Intracellular Structures -- Local Relevance of Organelle Calcium Pools -- Ca2+ IN CELL PATHOLOGY -- TAKE-HOME MESSAGE -- FURTHER READING -- CHAPTER 13 PHARMACOLOGY OF MAP KINASES -- THE MAPK FAMILY AND THE ACTIVATION MECHANISM -- The ERK Family -- The JNK Family -- The p38 Family -- ERK5 -- MAPK SPECIFICITY -- Duration of Action -- Multiple Enzyme Isoforms -- Subcellular Localization and Interaction with Scaffold Proteins -- miRNAs -- PHARMACOLOGICAL INHIBITION OF MAPK -- Inhibition of the Ras/RAF/MEK/ERK Cascade -- MEK -- RAF -- JNKs -- p38.
9781118768570 (cloth : alk. paper)
2015008098
Chemistry, Pharmaceutical.
Molecular Biology.
Pharmacological Phenomena.
615.19 / G