Basic Pharmacology: Understanding Drug Actions and Reactions, 1st Edition (Hardback) book cover

Basic Pharmacology

Understanding Drug Actions and Reactions, 1st Edition

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

Routledge

388 pages | 277 B/W Illus.

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pub: 2006-02-14
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Description

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.

Table of Contents

Contents

PHYSICOCHEMICAL PROPERTIES OF DRUGS

Basic Chemical Properties of Drugs

Introduction

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

Electronegativity

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

PRINCIPLES OF BIOPHARMACEUTICS

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

Bioavailability

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

PRINCIPLES OF DRUG–RECEPTOR AND DRUG–ENZYME INTERACTIONS

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

References

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

References

Receptor Regulation and Signaling Mechanisms

Spare Receptors

Overshoot

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

About the Series

Pharmacy Education Series

Learn more…

Subject Categories

BISAC Subject Codes/Headings:
MED035000
MEDICAL / Health Care Delivery
MED071000
MEDICAL / Pharmacology
MED072000
MEDICAL / Pharmacy