1st Edition

Basic Pharmacology Understanding Drug Actions and Reactions

    388 Pages 277 B/W Illustrations
    by Routledge

    Intended for use in an introductory pharmacology course, Basic Pharmacology: Understanding Drug Actions and Reactions provides an in-depth discussion of how to apply the chemical and molecular pharmacology concepts, a discussion students need for more advanced study. The textbook introduces the principles of chemistry and biology necessary to understand drug interactions at the cellular level. The authors highlight chemical and physical properties of drugs, drug absorption and distribution, drug interactions with cellular receptors, and drug metabolism and elimination.

    The book begins with a review of chemical principles as they apply to drug molecules, focusing mainly on those for commonly prescribed drugs. The authors use drug structures to illustrate the chemical concepts learned in general and organic chemistry courses. They cover the dynamics of receptors in mediating the pharmacological effects of drugs. They clarify theories, drawn from the scientific literature, which explain drug-receptor interactions and the  quantitative relationship between drug binding and its effects at the cellular level.

    The authors’ extensive use of drug structures for teaching chemical and molecular pharmacology principles, and their emphasis on the relevance of these principles in future professional life makes this book unique. It provides the framework for better understanding of advanced pharmacology and therapeutics topics. Blending medicinal chemistry and  pharmacodynamics aspects, this textbook clearly elucidates the essential concepts that form the cornerstone for further work in pharmacology.


    Basic Chemical Properties of Drugs

    The Periodic Table and Properties of Drugs
    The Periodic Table and Chemical Reactivity
    Chemical Bonds
    Magnitude of Ionic Charge
    Polyatomic Ions
    Covalent Bonds
    Coordinate Covalent Bonds
    Resonance Structures
    Shapes of Drug Molecules
    Polarity of Chemical Bonds
    Molecular Polarity
    Further Reading

    Acid–Base Properties of Drugs

    Hydrolysis of Salts
    Conjugate Acids and Conjugate Bases
    Strength of Acids and Bases
    Resonance and Inductive Effects
    Inductive Effects
    Resonance Effects
    The Henderson–Hasselbach Equation
    Further Reading

    Structural Determinants of Drug Action

    Structurally Nonspecific Drugs
    Volatile Anesthetics
    Structurally Specific Drugs
    Isosterism and Isosteres
    Structural Changes in Drug Molecules
    Further Reading
    Chemical Approaches to the Treatment of Cancer
    Normal vs. Malignant Cells
    Cell Cycle and Chemotherapy
    From Chemical Warfare to Chemotherapy
    Anticancer Drugs
    Further Reading


    Administration and Absorption of Drugs

    Drug Administration
    Drug Absorption
    Physiological and Physicochemical Factors in Drug Absorption
    Drug Absorption, Bioavailability, and First-Pass Metabolism
    Further Reading

    Distribution and Excretion of Drugs

    Factors in Drug Distribution
    Patterns of Distribution
    Determination of the Volume of Distribution
    Clearance and Elimination Rate
    Clearance and the Maintenance Dose Rate
    Half-Life and the Steady State
    Drug Elimination
    Further Reading

    Metabolic Changes of Drugs

    Cytochromes P450
    Redox Reactions and the CYP450 Enzyme Complex
    NAD + /NADH System
    FAD/FADH System
    The Cytochrome P450 Cycle
    Phase I and Phase II Reactions of Drug Metabolism
    Dose-Dependent Toxicity of Acetaminophen
    Further Reading

    Drug Receptors and Pharmacodynamics

    Mechanisms of Drug Action
    Chemical Signaling and Receptor Function
    Models of Drug–Receptor Interaction
    Affinity and Intrinsic Activity
    Agonists, Antagonists, and Partial Agonists
    Differential Effects of Agonists
    Cholinergic Neurotransmission

    Drug-Induced Enzyme Inhibition

    Drug Effects Mediated through Enzyme Inhibition
    Competitive, Uncompetitive, and Noncompetitive Inhibition
    Examples of Drug–Enzyme Interactions
    Pharmacological Effects Produced by Transpeptidase-Penicillinase Inhibition 
    Suicide Inhibition of Enzymes

    Drug–Receptor Dynamics and Theories

    Occupation Theory (Clark)
    Modified Occupancy Theory (Ariën)
    Rate Theory (Paton)
    Relationship between Concentration and Response
    Concentration–Effect Curves
    Drug Antagonism
    Schild’s Equation
    What Is the Importance of This Mathematical Relationship?
    Irreversible Antagonism
    Noncompetitive Antagonism
    Partial Agonists
    Various Factors That Can Regulate a Drug’s Effect
    Efficacy and Potency
    Therapeutic Index
    Time–Action Curves
    Practice Problems
    Answers for the Problems

    Receptor Regulation and Signaling Mechanisms

    Spare Receptors
    Down Regulation
    Other Factors That Can Affect Drug Response
    Receptor Signaling and Second Messenger Systems
    Hormones Acting through Intracellular Receptors
    Receptor-Coupled (Membrane-Bound) Guanylate Cyclase (GC)
    Soluble Guanylate Cyclase
    Receptors Linked to G-Proteins and Second Messenger Production
    Activation of Adenylate Cyclase and G-Protein Function
    Downstream cAMP Second Messenger Pathway
    Ca++ /Phosphoinositide/PKC Signaling Pathway
    What Is the Purpose of G-Proteins or Any Other Second Messenger System?
    Ligand-Gated Ion Channels
    Signaling through Voltage-Dependent Ion Channels
    Ligand-Gated Sodium Channel
    Calcium Channels
    Location(s) of the voltage-sensitive Ca2+ channels (VSCC):
    How Does Calcium Contract the Skeletal Muscles and the Vascular Smooth Muscles?
    Chloride Channel
    References Index


    Maria A. Hernandez Ph.D., Ph.D. Rathinavelu