BOOK
Lehne's Pharmacotherapeutics for Advanced Practice Providers - E-Book
Laura Rosenthal | Jacqueline Burchum
(2017)
Additional Information
Book Details
Abstract
Awarded second place in the 2017 AJN Book of the Year Awards in the Adult Primary Care Category and a 2019 PROSE Award finalist. Get all of the pharmacotherapeutics principles and content you need to become a safe and effective prescriber with Lehne's Pharmacotherapeutics for Advanced Practice Providers. This new text is built on the same solid foundation of clearly explained, up-to-date, and clinically current content as the undergraduate-level Lehne’s Pharmacology for Nursing Care, yet carefully focuses on the specific principles and drug content needed by primary and acute care nurse practitioners, physician assistants, and clinical nurse specialists. Three introductory chapters provide foundational content in the areas of prescriptive authority, rational drug selection, prescription writing, and promoting positive outcomes of drug therapy. Core chapter content centers on the drugs that advanced practitioner prescribers will see most commonly in clinical practice. You’ll also notice a sharp focus on pharmacotherapeutic decision-making along with a number of prescriber-focused pedagogical aids — including Black Box Warnings — to reinforce the most important information and help you make optimal pharmacotherapeutic decisions.
- Introductory chapters tailored to the specific needs of advanced practice prescribers cover topics such as prescriptive authority, rational drug selection and prescription writing, and promoting positive outcomes of drug therapy.
- Carefully focused pharmacotherapeutic content reflects the drugs most commonly seen and used by advanced practice prescribers, with emphasis not on the first drug discovered or developed in each class but on the agents most often used today. Primary care drugs are addressed first in each chapter as appropriate, followed by and acute care drugs.
- UNIQUE! Prescriber-focused pedagogical aids further reinforce the most important information for advanced practice prescribers. Black Box Warnings alert you to special warnings and precautions related to particular drugs.
- Integrated coverage of Canadian trade names appears throughout the text and is highlighted with a familiar maple-leaf icon.
- Integrated coverage of interprofessional collaboration addresses the growing global interest in interprofessional collaboration and incorporates opportunities for interprofessional collaborative practice throughout.
Table of Contents
Section Title | Page | Action | Price |
---|---|---|---|
Front Cover | cover | ||
Inside Front Cover | ifc1 | ||
page 2 of simple TOC | i | ||
Evolve page | ii | ||
Lehne's Pharmacotherapeutics for Advanced Practice Providers | iii | ||
Copyright Page | iv | ||
Dedications | v | ||
Acknowledgments | vii | ||
About the Authors | viii | ||
Contributor and Reviewers | ix | ||
Preface | xi | ||
Laying Foundations in Basic Principles | xi | ||
Reviewing Physiology and Pathophysiology | xi | ||
Teaching Through Prototypes | xi | ||
Large Print and Small Print: A Way to Focus on Essentials | xi | ||
Using Clinical Reality to Prioritize Content | xii | ||
Special Features | xii | ||
Teaching Supplements for Instructors | xii | ||
Ways to Use This Textbook | xii | ||
Table Of Contents | xiii | ||
Unit I Introduction | 1 | ||
1 Prescriptive Authority | 1 | ||
What Is Prescriptive Authority? | 1 | ||
Prescriptive Authority Regulations | 1 | ||
The Case for Full Prescriptive Authority | 2 | ||
Prescriptive Authority and Responsibility | 2 | ||
2 Rational Drug Selection and Prescription Writing | 5 | ||
The Responsibility of Prescribing | 5 | ||
Drug Selection | 5 | ||
Cost | 5 | ||
Guidelines | 5 | ||
Availability | 5 | ||
Interactions | 5 | ||
Side Effects | 6 | ||
Allergies | 6 | ||
Liver and Renal Function | 6 | ||
Need for Monitoring | 6 | ||
Special Populations | 6 | ||
Prescriptions | 6 | ||
Necessities | 6 | ||
Types of Prescriptions | 7 | ||
Telephone | 7 | ||
Written | 7 | ||
E-Prescribing | 7 | ||
Refills | 8 | ||
Assistance | 8 | ||
Applications for Tablets and Phones | 8 | ||
Collaboration | 9 | ||
3 Promoting Positive Outcomes of Drug Therapy | 11 | ||
Medication Education | 11 | ||
Medication Education Components | 11 | ||
Medication Name | 11 | ||
Purpose | 11 | ||
Dosing | 11 | ||
Administration | 11 | ||
Adverse Effects | 11 | ||
Storage | 12 | ||
Laboratory Testing | 12 | ||
Food or Drug Interactions | 12 | ||
Duration of Therapy | 12 | ||
Written Instructions | 12 | ||
Monitoring | 12 | ||
Determining Therapeutic Dosage | 13 | ||
Evaluating Medication Adequacy | 13 | ||
Identifying Adverse Effects | 13 | ||
Adherence | 13 | ||
Forgetfulness | 14 | ||
Lack of Planning | 15 | ||
Cost | 15 | ||
Dissatisfaction | 15 | ||
Altered Dosing | 15 | ||
Managing Medication Therapy | 16 | ||
Summary | 16 | ||
Unit II Basic Principles of Pharmacology | 17 | ||
4 Pharmacokinetics, Pharmacodynamics, and Drug Interactions | 17 | ||
Pharmacokinetics | 17 | ||
Application of Pharmacokinetics in Pharmacotherapeutics | 17 | ||
Passage of Drugs Across Membranes | 17 | ||
Three Ways to Cross a Cell Membrane | 17 | ||
Channels and Pores | 17 | ||
Transport Systems | 18 | ||
Direct Penetration of the Membrane | 18 | ||
Polar Molecules | 18 | ||
Ions | 18 | ||
Ion Trapping (pH Partitioning) | 19 | ||
Absorption | 19 | ||
Factors Affecting Drug Absorption | 19 | ||
Rate of Dissolution | 19 | ||
Surface Area | 19 | ||
Blood Flow | 19 | ||
Lipid Solubility | 19 | ||
pH Partitioning | 19 | ||
Characteristics of Commonly Used Routes of Administration | 19 | ||
Distribution | 19 | ||
Blood Flow to Tissues | 19 | ||
Exiting the Vascular System | 20 | ||
Typical Capillary Beds | 20 | ||
The Blood-Brain Barrier | 20 | ||
Placental Drug Transfer | 20 | ||
Protein Binding | 21 | ||
Entering Cells | 21 | ||
Metabolism | 22 | ||
Hepatic Drug-Metabolizing Enzymes | 22 | ||
Therapeutic Consequences of Drug Metabolism | 22 | ||
Accelerated Renal Drug Excretion | 22 | ||
Drug Inactivation | 22 | ||
Increased Therapeutic Action | 22 | ||
Activation of Prodrugs | 22 | ||
Increased or Decreased Toxicity | 22 | ||
Special Considerations in Drug Metabolism | 22 | ||
Age | 22 | ||
Induction and Inhibition of Drug-Metabolizing Enzymes | 22 | ||
First-Pass Effect | 22 | ||
Nutritional Status | 23 | ||
Competition Between Drugs | 23 | ||
Enterohepatic Recirculation | 23 | ||
Excretion | 23 | ||
Renal Drug Excretion | 23 | ||
Steps in Renal Drug Excretion | 23 | ||
Glomerular Filtration | 23 | ||
Passive Tubular Reabsorption | 23 | ||
Active Tubular Secretion | 23 | ||
Factors That Modify Renal Drug Excretion | 24 | ||
pH-Dependent Ionization | 24 | ||
Competition for Active Tubular Transport | 24 | ||
Age | 24 | ||
Nonrenal Routes of Drug Excretion | 24 | ||
Breast Milk | 24 | ||
Other Nonrenal Routes of Excretion | 24 | ||
Time Course of Drug Responses | 24 | ||
Plasma Drug Levels | 25 | ||
Clinical Significance of Plasma Drug Levels | 25 | ||
Two Plasma Drug Levels Defined | 25 | ||
Minimum Effective Concentration | 25 | ||
Toxic Concentration | 25 | ||
Therapeutic Range | 25 | ||
Single-Dose Time Course | 25 | ||
Drug Half-Life | 25 | ||
Drug Levels Produced With Repeated Doses | 26 | ||
The Process by Which Plateau Drug Levels Are Achieved | 26 | ||
Time to Plateau | 26 | ||
Techniques for Reducing Fluctuations in Drug Levels | 26 | ||
Loading Doses Versus Maintenance Doses | 27 | ||
Decline From Plateau | 27 | ||
Pharmacodynamics | 27 | ||
Dose-Response Relationships | 27 | ||
Basic Features of the Dose-Response Relationship | 27 | ||
Maximal Efficacy and Relative Potency | 27 | ||
Maximal Efficacy | 27 | ||
Relative Potency | 28 | ||
Drug-Receptor Interactions | 29 | ||
Introduction to Drug Receptors | 29 | ||
Receptors and Selectivity of Drug Action | 29 | ||
Theories of Drug-Receptor Interaction | 29 | ||
Simple Occupancy Theory | 29 | ||
Modified Occupancy Theory | 30 | ||
Affinity | 30 | ||
Intrinsic Activity | 31 | ||
Agonists, Antagonists, and Partial Agonists | 31 | ||
Agonists | 31 | ||
Antagonists | 31 | ||
Noncompetitive (Insurmountable) Antagonists | 31 | ||
Competitive (Surmountable) Antagonists | 32 | ||
Partial Agonists | 32 | ||
Regulation of Receptor Sensitivity | 32 | ||
Drug Responses That Do Not Involve Receptors | 33 | ||
Interpatient Variability in Drug Responses | 33 | ||
The ED50 | 33 | ||
Clinical Implications of Interpatient Variability | 34 | ||
The Therapeutic Index | 34 | ||
Drug Interaction | 34 | ||
Drug-Drug Interactions | 34 | ||
Consequences of Drug-Drug Interactions | 35 | ||
Intensification of Effects | 35 | ||
Increased Therapeutic Effects | 35 | ||
Increased Adverse Effects | 35 | ||
Reduction of Effects | 35 | ||
Reduced Therapeutic Effects | 35 | ||
Reduced Adverse Effects | 35 | ||
Creation of a Unique Response | 35 | ||
Basic Mechanisms of Drug-Drug Interactions | 35 | ||
Direct Chemical or Physical Interactions | 35 | ||
Pharmacokinetic Interactions | 35 | ||
Altered Absorption | 35 | ||
Altered Distribution | 36 | ||
Competition for Protein Binding. | 36 | ||
Alteration of Extracellular pH. | 36 | ||
Altered Metabolism | 36 | ||
Induction of CYP Enzymes | 36 | ||
Inhibition of CYP Enzymes | 36 | ||
Altered Renal Excretion | 36 | ||
Interactions That Involve P-Glycoprotein | 36 | ||
Pharmacodynamic Interactions | 36 | ||
Interactions at the Same Receptor | 38 | ||
Interactions Resulting From Actions at Separate Sites | 38 | ||
Combined Toxicity | 38 | ||
Clinical Significance of Drug-Drug Interactions | 38 | ||
Minimizing Adverse Drug-Drug Interactions | 38 | ||
Drug-Food Interactions | 38 | ||
Effects of Food on Drug Absorption | 38 | ||
Decreased Absorption | 38 | ||
Increased Absorption | 38 | ||
Effects of Food on Drug Metabolism: The Grapefruit Juice Effect | 39 | ||
Effects of Food on Drug Toxicity | 39 | ||
Effects of Food on Drug Action | 40 | ||
Timing of Drug Administration With Respect to Meals | 40 | ||
Drug-Supplement Interactions | 40 | ||
5 Adverse Drug Reactions and Medication Errors | 41 | ||
Adverse Drug Reactions | 41 | ||
Scope of the Problem | 41 | ||
Definitions | 41 | ||
Side Effect | 41 | ||
Toxicity | 41 | ||
Allergic Reaction | 41 | ||
Idiosyncratic Effect | 41 | ||
Paradoxical Effect | 42 | ||
Iatrogenic Disease | 42 | ||
Physical Dependence | 42 | ||
Carcinogenic Effect | 42 | ||
Teratogenic Effect | 42 | ||
Organ-Specific Toxicity | 42 | ||
Hepatotoxic Drugs | 42 | ||
QT Interval Drugs | 42 | ||
Identifying Adverse Drug Reactions | 42 | ||
Adverse Reactions to New Drugs | 43 | ||
Ways to Minimize Adverse Drug Reactions | 43 | ||
Special Alerts and Management Guidelines | 45 | ||
Medication Guides | 45 | ||
Boxed Warnings | 45 | ||
Risk Evaluation and Mitigation Strategies | 45 | ||
Medication Errors | 45 | ||
What Is a Medication Error? | 45 | ||
Prescribing Practices | 45 | ||
Oversight | 45 | ||
Communication | 46 | ||
Ways to Reduce Medication Errors | 46 | ||
How to Report a Medication Error | 47 | ||
6 Individual Variation in Drug Responses | 51 | ||
Body Weight and Composition | 51 | ||
Age | 51 | ||
Pathophysiology | 51 | ||
Kidney Disease | 51 | ||
Liver Disease | 51 | ||
Acid-Base Imbalance | 51 | ||
Altered Electrolyte Status | 51 | ||
Tolerance | 52 | ||
Pharmacodynamic Tolerance | 52 | ||
Metabolic Tolerance | 52 | ||
Tachyphylaxis | 52 | ||
Placebo Effect | 52 | ||
Variability in Absorption | 52 | ||
Bioavailability | 52 | ||
Individual Causes of Variable Absorption | 52 | ||
Genetics and Pharmacogenomics | 52 | ||
Genetic Variants That Alter Drug Metabolism | 53 | ||
Genetic Variants That Alter Drug Targets | 54 | ||
Genetic Variants That Alter Immune Responses to Drugs | 55 | ||
Gender- and Race-Related Variations | 55 | ||
Gender | 55 | ||
Race | 56 | ||
Comorbidities and Drug Interactions | 56 | ||
Unit III Drug Therapy Across the Life Span | 57 | ||
7 Drug Therapy During Pregnancy and Breastfeeding | 57 | ||
Drug Therapy During Pregnancy: Basic Considerations | 57 | ||
Physiologic Changes During Pregnancy and Their Effects on Drug Disposition and Dosing | 57 | ||
Placental Drug Transfer | 58 | ||
Adverse Reactions During Pregnancy | 58 | ||
Drug Therapy During Pregnancy: Teratogenesis | 58 | ||
Incidence and Causes of Congenital Anomalies | 58 | ||
Teratogenesis and Stage of Development | 58 | ||
Identification of Teratogens | 58 | ||
FDA Pregnancy Risk Categories | 61 | ||
FDA Pregnancy and Lactation Labeling Rule | 61 | ||
Minimizing the Drug Risk During Pregnancy | 61 | ||
Responding to Teratogen Exposure | 62 | ||
Drug Therapy During Breastfeeding | 62 | ||
8 Drug Therapy in Pediatric Patients | 65 | ||
Pharmacokinetics: Neonates and Infants | 65 | ||
Absorption | 65 | ||
Oral Administration | 65 | ||
Intramuscular Administration | 65 | ||
Transdermal Absorption | 66 | ||
Distribution | 66 | ||
Protein Binding | 66 | ||
Blood-Brain Barrier | 66 | ||
Hepatic Metabolism | 66 | ||
Renal Excretion | 66 | ||
Pharmacokinetics: Children 1 Year and Older | 66 | ||
Adverse Drug Reactions | 66 | ||
Dosage Determination | 67 | ||
Promoting Adherence | 67 | ||
9 Drug Therapy in Geriatric Patients | 69 | ||
Pharmacokinetic Changes in Older Adults | 69 | ||
Absorption | 69 | ||
Distribution | 69 | ||
Metabolism | 69 | ||
Excretion | 69 | ||
Pharmacodynamic Changes in Older Adults | 70 | ||
Adverse Drug Reactions and Drug Interactions | 70 | ||
Promoting Adherence | 70 | ||
Unit IV Peripheral Nervous System Drugs | 73 | ||
10 Basic Principles of Neuropharmacology | 73 | ||
How Neurons Regulate Physiologic Processes | 73 | ||
Basic Mechanisms by Which Neuropharmacologic Agents Act | 73 | ||
Sites of Action: Axons Versus Synapses | 73 | ||
Axonal Conduction | 74 | ||
Synaptic Transmission | 74 | ||
Receptors | 74 | ||
Steps in Synaptic Transmission | 74 | ||
Step 1: Transmitter Synthesis | 74 | ||
Step 2: Transmitter Storage | 74 | ||
Step 3: Transmitter Release | 75 | ||
Step 4: Receptor Binding | 75 | ||
Step 5: Termination of Transmission | 75 | ||
Effects of Drugs on the Steps of Synaptic Transmission | 75 | ||
Transmitter Synthesis | 75 | ||
Transmitter Storage | 76 | ||
Transmitter Release | 76 | ||
Receptor Binding | 76 | ||
Termination of Transmitter Action | 76 | ||
Multiple Receptor Types and Selectivity of Drug Action | 76 | ||
An Approach to Learning About Peripheral Nervous System Drugs | 77 | ||
11 Physiology of the Peripheral Nervous System | 79 | ||
Divisions of the Nervous System | 79 | ||
Overview of Autonomic Nervous System Functions | 79 | ||
Functions of the Parasympathetic Nervous System | 79 | ||
Functions of the Sympathetic Nervous System | 79 | ||
Basic Mechanisms by Which the Autonomic Nervous System Regulates Physiologic Processes | 80 | ||
Patterns of Innervation and Control | 80 | ||
Feedback Regulation | 80 | ||
Baroreceptor Reflex | 80 | ||
Autonomic Tone | 81 | ||
Anatomic Considerations | 81 | ||
Parasympathetic Nervous System | 81 | ||
Sympathetic Nervous System | 81 | ||
Somatic Motor System | 82 | ||
Introduction to Transmitters of the Peripheral Nervous System | 82 | ||
Introduction to Receptors of the Peripheral Nervous System | 83 | ||
Primary Receptor Types: Cholinergic Receptors and Adrenergic Receptors | 83 | ||
Subtypes of Cholinergic and Adrenergic Receptors | 83 | ||
Exploring the Concept of Receptor Subtypes | 83 | ||
What Do We Mean by “Receptor Subtype”? | 83 | ||
How Do We Know That Receptor Subtypes Exist? | 83 | ||
How Can Drugs Be More Selective Than Natural Transmitters at Receptor Subtypes? | 84 | ||
Why Do Receptor Subtypes Exist, and Why Do They Matter? | 84 | ||
Locations of Receptor Subtypes | 85 | ||
Functions of Cholinergic and Adrenergic Receptor Subtypes | 85 | ||
Functions of Cholinergic Receptor Subtypes | 86 | ||
Functions of Adrenergic Receptor Subtypes | 87 | ||
Alpha1 Receptors | 87 | ||
Alpha2 Receptors | 87 | ||
Beta1 Receptors | 88 | ||
Beta2 Receptors | 88 | ||
Dopamine Receptors | 88 | ||
Receptor Specificity of the Adrenergic Transmitters | 88 | ||
Transmitter Life Cycles | 88 | ||
Life Cycle of Acetylcholine | 88 | ||
Life Cycle of Norepinephrine | 89 | ||
Life Cycle of Epinephrine | 90 | ||
12 Muscarinic Agonists and Antagonists | 91 | ||
Introduction to Cholinergic Drugs | 91 | ||
Muscarinic Agonists, Cholinesterase Inhibitors, and Muscarinic Antagonists | 91 | ||
Muscarinic Agonists | 91 | ||
Bethanechol | 92 | ||
Mechanism of Action | 92 | ||
Pharmacologic Effects | 92 | ||
Pharmacokinetics | 92 | ||
Preparations, Dosage, and Administration | 92 | ||
Therapeutic Uses | 93 | ||
Urinary Retention. | 93 | ||
GI Uses. | 93 | ||
Adverse Effects | 93 | ||
Cardiovascular System. | 93 | ||
GI System. | 93 | ||
Urinary Tract. | 94 | ||
Exacerbation of Asthma. | 94 | ||
Dysrhythmias in Hyperthyroid Patients. | 94 | ||
Other Muscarinic Agonists | 94 | ||
Cevimeline | 94 | ||
Actions and Uses | 94 | ||
Adverse Effects | 94 | ||
Drug Interactions | 94 | ||
Pilocarpine | 94 | ||
Cholinesterase Inhibitors | 94 | ||
Reversible Cholinesterase Inhibitors | 95 | ||
Neostigmine | 95 | ||
Chemistry. | 95 | ||
Mechanism of Action. | 95 | ||
Pharmacologic Effects. | 95 | ||
Muscarinic Responses. | 95 | ||
Neuromuscular Effects. | 95 | ||
Central Nervous System. | 95 | ||
Pharmacokinetics. | 95 | ||
Preparation, Dosage, and Administration. | 95 | ||
Therapeutic Uses | 95 | ||
Myasthenia Gravis. | 95 | ||
Adverse Effects | 95 | ||
Excessive Muscarinic Stimulation. | 95 | ||
Neuromuscular Blockade. | 96 | ||
Precautions and Contraindications. | 96 | ||
Drug Interactions | 96 | ||
Muscarinic Antagonists. | 96 | ||
Other Reversible Cholinesterase Inhibitors | 96 | ||
Physostigmine. | 96 | ||
Edrophonium and Pyridostigmine. | 96 | ||
Drugs for Alzheimer Disease. | 96 | ||
Irreversible Cholinesterase Inhibitors | 96 | ||
Basic Pharmacology | 96 | ||
Chemistry. | 96 | ||
Mechanism of Action. | 97 | ||
Pharmacologic Effects. | 97 | ||
Therapeutic Uses. | 97 | ||
Toxicology of Cholinesterase Inhibitors | 97 | ||
Sources of Poisoning | 97 | ||
Symptoms | 97 | ||
Treatment | 97 | ||
Pralidoxime. | 97 | ||
Myasthenia Gravis | 97 | ||
Pathophysiology | 97 | ||
Treatment With Cholinesterase Inhibitors | 97 | ||
Beneficial Effects. | 97 | ||
Side Effects. | 98 | ||
Dosage Adjustment. | 98 | ||
Myasthenic Crisis and Cholinergic Crisis | 98 | ||
Myasthenic Crisis. | 98 | ||
Cholinergic Crisis. | 98 | ||
Distinguishing Myasthenic Crisis From Cholinergic Crisis. | 98 | ||
Use of Identification by the Patient. | 98 | ||
Toxicology of Muscarinic Agonists | 98 | ||
Sources of Muscarinic Poisoning | 98 | ||
Symptoms | 98 | ||
Treatment | 98 | ||
Muscarinic Antagonists (Anticholinergic Drugs) | 99 | ||
Atropine | 99 | ||
Mechanism of Action | 99 | ||
Pharmacologic Effects | 99 | ||
Heart. | 99 | ||
Exocrine Glands. | 99 | ||
Smooth Muscle. | 99 | ||
Eyes. | 99 | ||
Central Nervous System. | 99 | ||
Dose Dependency of Muscarinic Blockade. | 99 | ||
Pharmacokinetics | 100 | ||
Therapeutic Uses | 100 | ||
Preanesthetic Medication. | 100 | ||
Disorders of the Eyes. | 100 | ||
Bradycardia. | 100 | ||
Intestinal Hypertonicity and Hypermotility. | 100 | ||
Muscarinic Agonist Poisoning. | 100 | ||
Peptic Ulcer Disease. | 100 | ||
Asthma. | 100 | ||
Biliary Colic. | 100 | ||
Adverse Effects | 100 | ||
Xerostomia (Dry Mouth). | 100 | ||
Blurred Vision and Photophobia. | 100 | ||
Elevation of Intraocular Pressure. | 101 | ||
Urinary Retention. | 101 | ||
Constipation. | 101 | ||
Anhidrosis. | 101 | ||
Tachycardia. | 101 | ||
Asthma. | 101 | ||
Drug Interactions. | 101 | ||
Preparations, Dosage, and Administration | 101 | ||
General Systemic Therapy. | 101 | ||
Muscarinic Antagonists for Overactive Bladder | 101 | ||
Overactive Bladder: Characteristics and Overview of Treatment | 101 | ||
Introduction to Anticholinergic Therapy of OAB | 101 | ||
Specific Anticholinergic Drugs for Overactive Bladder | 102 | ||
Oxybutynin | 103 | ||
Extended-Release Tablets. | 104 | ||
Transdermal Patch. | 104 | ||
Topical Gel. | 104 | ||
Darifenacin | 104 | ||
Solifenacin | 104 | ||
Tolterodine | 104 | ||
Immediate-Release Tablets. | 104 | ||
Fesoterodine | 104 | ||
Trospium | 105 | ||
Immediate-Release Tablets. | 105 | ||
Extended-Release Capsules. | 105 | ||
Other Muscarinic Antagonists | 105 | ||
Scopolamine | 105 | ||
Ipratropium Bromide | 105 | ||
Antisecretory Anticholinergics | 105 | ||
Dicyclomine | 105 | ||
Mydriatic Cycloplegics | 105 | ||
Centrally Acting Anticholinergics | 105 | ||
Toxicology of Muscarinic Antagonists | 105 | ||
Sources of Antimuscarinic Poisoning | 105 | ||
Symptoms | 105 | ||
Treatment | 106 | ||
Warning | 106 | ||
Prescribing and Monitoring Considerations | 106 | ||
Bethanechol | 106 | ||
Unit V Central Nervous System Drugs | 139 | ||
16 Introduction to Central Nervous System Pharmacology | 139 | ||
Transmitters of the Central Nervous System | 139 | ||
The Blood-Brain Barrier | 139 | ||
How Do Central Nervous System Drugs Produce Therapeutic Effects? | 139 | ||
Adaptation of the Central Nervous System to Prolonged Drug Exposure | 140 | ||
Increased Therapeutic Effects | 140 | ||
Decreased Side Effects | 140 | ||
Tolerance and Physical Dependence | 140 | ||
Development of New Psychotherapeutic Drugs | 140 | ||
Approaching the Study of Central Nervous System Drugs | 140 | ||
17 Drugs for Parkinson Disease | 143 | ||
Pathophysiology That Underlies Motor Symptoms | 143 | ||
Overview of Motor Symptom Management | 143 | ||
Therapeutic Goal | 143 | ||
Drugs Employed | 144 | ||
Clinical Guidelines | 144 | ||
Drug Selection | 144 | ||
Initial Treatment | 144 | ||
Management of Motor Fluctuations | 145 | ||
Neuroprotection | 145 | ||
Pharmacology of the Drugs Used for Motor Symptoms | 146 | ||
Levodopa | 146 | ||
Use in Parkinson Disease | 146 | ||
Beneficial Effects | 146 | ||
Acute Loss of Effect | 146 | ||
Mechanism of Action | 146 | ||
Pharmacokinetics | 146 | ||
Adverse Effects | 147 | ||
Nausea and Vomiting | 147 | ||
Dyskinesias | 148 | ||
Cardiovascular Effects | 148 | ||
Psychosis | 148 | ||
Central Nervous System Effects | 148 | ||
Other Adverse Effects | 148 | ||
Drug Interactions | 148 | ||
First-Generation Antipsychotic Drugs | 148 | ||
Monoamine Oxidase Inhibitors | 148 | ||
Anticholinergic Drugs | 149 | ||
Pyridoxine | 149 | ||
Food Interactions | 149 | ||
Preparations | 149 | ||
Levodopa/Carbidopa | 149 | ||
Mechanism of Action | 149 | ||
Advantages of Carbidopa | 149 | ||
Disadvantages of Carbidopa | 149 | ||
Preparations, Dosage, and Administration | 150 | ||
Carbidopa Alone | 150 | ||
Dopamine Agonists | 150 | ||
Nonergot Derivatives: Pramipexole, Ropinirole, Rotigotine, and Apomorphine | 153 | ||
Pramipexole | 153 | ||
Unit VI Drugs for Pain | 197 | ||
21 Local Anesthetics | 197 | ||
Basic Pharmacology of the Local Anesthetics | 197 | ||
Classification | 197 | ||
Mechanism of Action | 197 | ||
Selectivity of Anesthetic Effects | 197 | ||
Time Course of Local Anesthesia | 197 | ||
Use With Vasoconstrictors | 198 | ||
Pharmacokinetics | 198 | ||
Absorption and Distribution | 198 | ||
Metabolism | 199 | ||
Adverse Effects | 199 | ||
Central Nervous System | 199 | ||
Cardiovascular System | 199 | ||
Allergic Reactions | 199 | ||
Methemoglobinemia | 199 | ||
Properties of Individual Local Anesthetics | 199 | ||
Chloroprocaine | 199 | ||
Lidocaine | 199 | ||
Cocaine | 200 | ||
Anesthetic Use | 200 | ||
CNS Effects | 200 | ||
Cardiovascular Effects | 200 | ||
Other Local Anesthetics | 200 | ||
Clinical Use of Local Anesthetics | 200 | ||
Topical Administration | 200 | ||
Therapeutic Uses | 200 | ||
Systemic Toxicity | 200 | ||
Administration by Injection | 200 | ||
Infiltration Anesthesia | 201 | ||
Nerve Block Anesthesia | 201 | ||
22 Opioid Analgesics, Opioid Antagonists, and Nonopioid Centrally Acting Analgesics | 203 | ||
Opioid Analgesics | 203 | ||
Introduction to the Opioids | 203 | ||
Terminology | 203 | ||
Endogenous Opioid Peptides | 203 | ||
Opioid Receptors | 203 | ||
Mu Receptors | 203 | ||
Kappa Receptors | 203 | ||
Classification of Drugs That Act at Opioid Receptors | 203 | ||
Pure Opioid Agonists | 203 | ||
Agonist-Antagonist Opioids | 203 | ||
Pure Opioid Antagonists | 204 | ||
Basic Pharmacology of the Opioids | 204 | ||
Morphine | 204 | ||
Overview of Pharmacologic Actions | 204 | ||
Therapeutic Use: Relief of Pain | 204 | ||
Adverse Effects | 204 | ||
Respiratory Depression | 204 | ||
Constipation | 205 | ||
Orthostatic Hypotension | 205 | ||
Urinary Retention | 205 | ||
Emesis | 205 | ||
Euphoria and Dysphoria | 205 | ||
Sedation | 206 | ||
Neurotoxicity | 206 | ||
Pharmacokinetics | 206 | ||
Tolerance and Physical Dependence | 206 | ||
Tolerance | 206 | ||
Physical Dependence | 206 | ||
Abuse Liability | 207 | ||
Precautions | 207 | ||
Decreased Respiratory Reserve | 207 | ||
Other Precautions | 207 | ||
Drug Interactions | 207 | ||
Toxicity | 207 | ||
Clinical Manifestations | 207 | ||
Treatment | 207 | ||
Preparations | 207 | ||
Morphine Alone | 207 | ||
Morphine and Naltrexone [Embeda] | 208 | ||
Dosage and Administration | 208 | ||
General Guidelines | 208 | ||
Routes and Dosages | 208 | ||
Oral | 208 | ||
Other Strong Opioid Agonists | 208 | ||
Fentanyl | 208 | ||
Transdermal System | 208 | ||
Transmucosal | 209 | ||
Lozenge on a Stick | 210 | ||
Buccal Tablets | 210 | ||
Sublingual Spray | 210 | ||
Sublingual Tablets | 210 | ||
Intranasal | 210 | ||
Meperidine | 210 | ||
Methadone | 210 | ||
Hydromorphone, Oxymorphone, and Levorphanol | 211 | ||
Basic Pharmacology | 211 | ||
Unit VII Psychotherapeutic Drugs | 231 | ||
24 Antipsychotic Agents and Their Use in Schizophrenia | 231 | ||
Schizophrenia: Clinical Presentation and Etiology | 231 | ||
Clinical Presentation | 231 | ||
Three Types of Symptoms | 231 | ||
Positive Symptoms and Negative Symptoms | 231 | ||
Cognitive Symptoms | 231 | ||
Acute Episodes | 232 | ||
Residual Symptoms | 232 | ||
Long-Term Course | 232 | ||
Etiology | 232 | ||
First-Generation (Conventional) Antipsychotics | 232 | ||
Group Properties | 232 | ||
Classification | 232 | ||
Classification by Potency | 232 | ||
Chemical Classification | 232 | ||
Mechanism of Action | 234 | ||
Therapeutic Use: Schizophrenia | 234 | ||
Adverse Effects | 235 | ||
Extrapyramidal Symptoms | 235 | ||
Acute Dystonia | 235 | ||
Parkinsonism | 235 | ||
Akathisia | 235 | ||
Tardive Dyskinesia | 236 | ||
Other Adverse Effects | 236 | ||
Neuroleptic Malignant Syndrome. | 236 | ||
Anticholinergic Effects. | 236 | ||
Orthostatic Hypotension. | 236 | ||
Sedation. | 236 | ||
Neuroendocrine Effects. | 237 | ||
Seizures. | 237 | ||
Sexual Dysfunction. | 237 | ||
Agranulocytosis. | 237 | ||
Severe Dysrhythmias. | 237 | ||
Signs of Withdrawal and Extrapyramidal Symptoms in Neonates. | 237 | ||
Dermatologic Effects. | 237 | ||
Physical and Psychological Dependence | 237 | ||
Drug Interactions | 237 | ||
Anticholinergic Drugs | 237 | ||
Central Nervous System Depressants | 237 | ||
Levodopa and Direct Dopamine Receptor Agonists | 237 | ||
Toxicity | 238 | ||
Properties of Individual Agents | 238 | ||
High-Potency Agents | 238 | ||
Haloperidol | 238 | ||
Actions and Uses. | 238 | ||
Unit VIII Drug Abuse | 301 | ||
30 Drug Abuse I | 301 | ||
Definitions | 301 | ||
Drug Abuse | 301 | ||
Addiction | 301 | ||
Other Definitions | 302 | ||
Diagnostic Criteria Regarding Drugs of Abuse | 302 | ||
Factors That Contribute to Drug Abuse | 302 | ||
Reinforcing Properties of Drugs | 302 | ||
Physical Dependence | 302 | ||
Psychological Dependence | 303 | ||
Social Factors | 303 | ||
Drug Availability | 303 | ||
Vulnerability of the Individual | 303 | ||
Neurobiology of Addiction | 303 | ||
Principles of Addiction Treatment | 304 | ||
The Controlled Substances Act | 305 | ||
Record Keeping | 305 | ||
Drug Enforcement Agency Schedules | 305 | ||
Prescriptions | 305 | ||
Schedule II | 305 | ||
Schedules III and IV | 305 | ||
Schedule V | 305 | ||
Labeling | 305 | ||
State Laws | 305 | ||
31 Drug Abuse II | 307 | ||
Basic Pharmacology of Alcohol | 307 | ||
Central Nervous System Effects | 307 | ||
Acute Effects | 307 | ||
Chronic Effects | 307 | ||
Impact on Cognitive Function | 307 | ||
Effect on Sleep | 307 | ||
Other Pharmacologic Effects | 307 | ||
Cardiovascular System | 307 | ||
Glucose Metabolism | 308 | ||
Bone Health | 308 | ||
Respiration | 308 | ||
Liver | 308 | ||
Stomach | 308 | ||
Kidney | 308 | ||
Pancreas | 308 | ||
Sexual Function | 308 | ||
Cancer | 308 | ||
Pregnancy | 309 | ||
Lactation | 309 | ||
Impact on Longevity | 309 | ||
Pharmacokinetics | 309 | ||
Absorption | 309 | ||
Distribution | 309 | ||
Metabolism | 309 | ||
Tolerance | 310 | ||
Physical Dependence | 310 | ||
Drug Interactions | 310 | ||
Central Nervous System Depressants | 310 | ||
Nonsteroidal Antiinflammatory Drugs | 310 | ||
Acetaminophen | 310 | ||
Disulfiram | 310 | ||
Antihypertensive Drugs | 310 | ||
Acute Overdose | 310 | ||
Precautions and Contraindications | 310 | ||
Therapeutic Uses | 311 | ||
Topical | 311 | ||
Local Injection | 311 | ||
Alcohol Use Disorder | 311 | ||
Drugs for Alcohol Use Disorder | 312 | ||
Drugs Used to Treat the Symptoms of Withdrawal | 312 | ||
Benzodiazepines | 312 | ||
Adjuncts to Benzodiazepines | 312 | ||
Drugs Used to Maintain Abstinence | 313 | ||
Disulfiram Aversion Therapy | 313 | ||
Therapeutic Effects | 313 | ||
Mechanism of Action | 313 | ||
Pharmacologic Effects | 313 | ||
Patient Selection | 313 | ||
Preparations, Dosage, and Administration | 314 | ||
Naltrexone | 314 | ||
Acamprosate | 314 | ||
Therapeutic Use | 314 | ||
Mechanism of Action | 314 | ||
Pharmacokinetics | 314 | ||
Adverse Effects | 314 | ||
32 Drug Abuse III | 315 | ||
Basic Pharmacology of Nicotine | 315 | ||
Mechanism of Action | 315 | ||
Pharmacokinetics | 315 | ||
Pharmacologic Effects | 315 | ||
Cardiovascular Effects | 315 | ||
Gastrointestinal Effects | 315 | ||
Central Nervous System Effects | 316 | ||
Effects During Pregnancy and Lactation | 316 | ||
Tolerance and Dependence | 316 | ||
Tolerance | 316 | ||
Dependence | 316 | ||
Acute Poisoning | 316 | ||
Symptoms | 316 | ||
Treatment | 316 | ||
Chronic Toxicity From Smoking | 316 | ||
Pharmacologic Aids to Smoking Cessation | 316 | ||
Nicotine Replacement Therapy | 317 | ||
Nicotine Chewing Gum (Nicotine Polacrilex) | 317 | ||
Nicotine Lozenges (Nicotine Polacrilex) | 317 | ||
Nicotine Transdermal Systems (Patches) | 319 | ||
Nicotine Inhaler | 319 | ||
Nicotine Nasal Spray | 319 | ||
Bupropion SR | 319 | ||
Varenicline | 320 | ||
Mechanism of Action | 320 | ||
Pharmacokinetics | 320 | ||
Adverse Effects | 320 | ||
Preparations, Dosage, and Administration | 320 | ||
Products That Are Not Recommended | 320 | ||
33 Drug Abuse IV | 321 | ||
Heroin, Oxycodone, and Other Opioids | 321 | ||
Patterns of Use | 321 | ||
Subjective and Behavioral Effects | 321 | ||
Preferred Drugs and Routes of Administration | 321 | ||
Heroin | 322 | ||
Oxycodone | 322 | ||
Tolerance and Physical Dependence | 322 | ||
Tolerance | 322 | ||
Physical Dependence | 322 | ||
Treatment of Acute Toxicity | 322 | ||
Detoxification | 322 | ||
Methadone Substitution | 322 | ||
Buprenorphine | 323 | ||
Clonidine-Assisted Withdrawal | 323 | ||
Drugs for Long-Term Management of Opioid Addiction | 323 | ||
Methadone | 323 | ||
Buprenorphine | 324 | ||
Naltrexone | 324 | ||
General Central Nervous System Depressants | 324 | ||
Barbiturates | 324 | ||
Tolerance | 324 | ||
Physical Dependence and Withdrawal Techniques | 325 | ||
Acute Toxicity | 325 | ||
Benzodiazepines | 325 | ||
Psychostimulants | 325 | ||
Cocaine | 325 | ||
Forms | 325 | ||
Routes of Administration | 325 | ||
Subjective Effects and Addiction | 325 | ||
Acute Toxicity: Symptoms and Treatment | 325 | ||
Chronic Toxicity | 326 | ||
Tolerance, Dependence, and Withdrawal | 326 | ||
Treatment of Cocaine Addiction | 326 | ||
Methamphetamine | 326 | ||
Description and Routes | 326 | ||
Patterns of Use | 326 | ||
Subjective and Behavioral Effects | 326 | ||
Adverse Psychological Effects | 326 | ||
Adverse Cardiovascular Effects | 326 | ||
Other Adverse Effects | 326 | ||
Tolerance, Dependence, and Withdrawal | 327 | ||
Treatment | 327 | ||
Marijuana and Related Preparations | 327 | ||
Cannabis sativa, the Source of Marijuana | 327 | ||
Psychoactive Component | 327 | ||
Mechanism of Action | 327 | ||
Pharmacokinetics | 327 | ||
Administration by Smoking | 327 | ||
Oral Administration | 327 | ||
Behavioral and Subjective Effects | 327 | ||
Effects of Low to Moderate Doses | 327 | ||
High-Dose Effects | 328 | ||
Effects of Chronic Use | 328 | ||
Role in Schizophrenia | 328 | ||
Physiologic Effects | 328 | ||
Cardiovascular Effects | 328 | ||
Respiratory Effects | 328 | ||
Effects on Reproduction | 328 | ||
Altered Brain Structure | 328 | ||
Tolerance and Dependence | 328 | ||
Therapeutic Use | 328 | ||
Approved Uses for Cannabinoids | 328 | ||
Suppression of Emesis | 328 | ||
Appetite Stimulation | 329 | ||
Relief of Neuropathic Pain | 329 | ||
Unapproved Uses for Cannabinoids | 329 | ||
Glaucoma | 329 | ||
Multiple Sclerosis | 329 | ||
Medical Research on Marijuana | 329 | ||
Legal Status of Medical Marijuana | 329 | ||
United States | 329 | ||
Canada | 329 | ||
Comparison of Marijuana With Alcohol | 329 | ||
Synthetic Marijuana | 330 | ||
Psychedelics | 330 | ||
d-Lysergic Acid Diethylamide | 330 | ||
History | 330 | ||
Mechanism of Action | 330 | ||
Time Course | 330 | ||
Subjective and Behavioral Effects | 330 | ||
Physiologic Effects | 330 | ||
Tolerance and Dependence | 330 | ||
Toxicity | 331 | ||
Potential Therapeutic Uses | 331 | ||
Salvia | 331 | ||
Mescaline, Psilocin, Psilocybin, and Dimethyltryptamine | 331 | ||
Dextromethorphan | 331 | ||
3,4-Methylenedioxymethamphetamine (MDMA, Ecstasy) | 332 | ||
Time Course and Dosage | 332 | ||
Who Uses MDMA and Why? | 332 | ||
Adverse Effects | 332 | ||
Potential Medical Use | 332 | ||
Inhalants | 332 | ||
Anesthetics | 332 | ||
Organic Solvents | 333 | ||
Administration | 333 | ||
Acute Pharmacologic Effects | 333 | ||
Chronic Toxicity | 333 | ||
Management | 333 | ||
Anabolic Steroids | 333 | ||
Unit IX Drugs that Affect the Heart, Blood Vessels, Blood, and Blood Volume | 335 | ||
34 Review of Hemodynamics | 335 | ||
Overview of the Circulatory System | 335 | ||
Components of the Circulatory System | 335 | ||
Distribution of Blood | 335 | ||
What Makes Blood Flow? | 335 | ||
How Does Blood Get Back to the Heart? | 335 | ||
Regulation of Cardiac Output | 336 | ||
Determinants of Cardiac Output | 336 | ||
Heart Rate | 336 | ||
Stroke Volume | 337 | ||
Preload | 337 | ||
Afterload | 337 | ||
Starling’s Law of the Heart | 337 | ||
Factors That Determine Venous Return | 338 | ||
Starling’s Law and Maintenance of Systemic-Pulmonary Balance | 338 | ||
Regulation of Arterial Pressure | 339 | ||
Overview of Control Systems | 339 | ||
Steady-State Control by the Autonomic Nervous System | 339 | ||
Rapid Control by the Autonomic Nervous System: the Baroreceptor Reflex | 339 | ||
The Renin-Angiotensin-Aldosterone System | 339 | ||
Renal Retention of Water | 339 | ||
Postural Hypotension | 339 | ||
Natriuretic Peptides | 340 | ||
35 Diuretics | 341 | ||
Review of Renal Anatomy and Physiology | 341 | ||
Anatomy | 341 | ||
Physiology | 341 | ||
Overview of Kidney Functions | 341 | ||
The Three Basic Renal Processes | 341 | ||
Filtration | 341 | ||
Reabsorption | 341 | ||
Active Tubular Secretion | 341 | ||
Processes of Reabsorption That Occur at Specific Sites Along the Nephron | 341 | ||
Proximal Convoluted Tubule | 342 | ||
Loop of Henle | 342 | ||
Distal Convoluted Tubule (Early Segment) | 342 | ||
Distal Nephron: Late Distal Convoluted Tubule and Collecting Duct | 342 | ||
Sodium-Potassium Exchange | 343 | ||
Introduction to Diuretics | 343 | ||
How Diuretics Work | 343 | ||
Adverse Impact on Extracellular Fluid | 344 | ||
Classification of Diuretics | 344 | ||
Loop Diuretics | 344 | ||
Furosemide | 344 | ||
Mechanism of Action | 344 | ||
Pharmacokinetics | 344 | ||
Therapeutic Uses | 344 | ||
Adverse Effects | 344 | ||
Hyponatremia, Hypochloremia, and Dehydration | 344 | ||
Hypotension | 344 | ||
Hypokalemia | 345 | ||
Ototoxicity | 345 | ||
Hyperglycemia | 345 | ||
Hyperuricemia | 345 | ||
Use in Pregnancy | 345 | ||
Impact on Lipids, Magnesium, and Calcium | 345 | ||
Drug Interactions | 345 | ||
Digoxin | 345 | ||
Ototoxic Drugs | 345 | ||
Potassium-Sparing Diuretics | 345 | ||
Lithium | 345 | ||
Antihypertensive Agents | 345 | ||
Nonsteroidal Antiinflammatory Drugs (NSAIDs) | 345 | ||
Other Loop Diuretics | 346 | ||
Thiazides and Related Diuretics | 346 | ||
Hydrochlorothiazide | 346 | ||
Mechanism of Action | 346 | ||
Pharmacokinetics | 346 | ||
Therapeutic Uses | 347 | ||
Essential Hypertension | 347 | ||
Edema | 347 | ||
Protection Against Postmenopausal Osteoporosis | 347 | ||
Adverse Effects | 347 | ||
Hyponatremia, Hypochloremia, and Dehydration | 347 | ||
Hypokalemia | 347 | ||
Hyperglycemia | 347 | ||
Hyperuricemia | 347 | ||
Impact on Lipids and Magnesium | 347 | ||
Drug Interactions | 347 | ||
Potassium-Sparing Diuretics | 347 | ||
Spironolactone | 347 | ||
Mechanism of Action | 347 | ||
Unit X Drugs for Endocrine Disorders | 485 | ||
46 Drugs for Diabetes Mellitus | 485 | ||
Diabetes Mellitus: Basic Considerations | 485 | ||
Types of Diabetes Mellitus | 485 | ||
Type 1 Diabetes | 485 | ||
Type 2 Diabetes | 485 | ||
Diabetes and Pregnancy | 486 | ||
Diagnosis | 486 | ||
Tests Based on Blood Levels of Glucose | 487 | ||
Fasting Plasma Glucose Test | 487 | ||
Casual Plasma Glucose Test | 487 | ||
Oral Glucose Tolerance Test | 487 | ||
Hemoglobin A1c | 487 | ||
Increased Risk for Diabetes (Prediabetes) | 487 | ||
Overview of Treatment | 487 | ||
Type 1 Diabetes | 487 | ||
Dietary Measures | 488 | ||
Physical Activity | 488 | ||
Insulin Replacement | 488 | ||
Managing Hypertension and Dyslipidemia | 488 | ||
Type 2 Diabetes | 488 | ||
Determining Appropriate Glycemic Goals | 489 | ||
Type 1 Diabetes | 489 | ||
Benefits | 489 | ||
Drawbacks | 489 | ||
Type 2 Diabetes | 489 | ||
Monitoring Treatment | 490 | ||
Self-Monitoring of Blood Glucose | 490 | ||
Monitoring of Hemoglobin A1c | 490 | ||
Insulin | 491 | ||
Physiology | 491 | ||
Structure | 491 | ||
Biosynthesis | 491 | ||
Secretion | 491 | ||
Metabolic Actions | 491 | ||
Metabolic Consequences of Insulin Deficiency | 492 | ||
Preparations and Administration | 492 | ||
Sources of Insulin | 492 | ||
Types of Insulin | 492 | ||
Short Duration: Rapid Acting | 492 | ||
Insulin Lispro. | 492 | ||
Insulin Aspart. | 492 | ||
Insulin Glulisine. | 493 | ||
Short Duration: Slower Acting | 493 | ||
Regular Insulin Injection. | 493 | ||
Intermediate Duration | 494 | ||
Neutral Protamine Hagedorn (NPH) Insulin Suspension. | 494 | ||
Long Duration | 495 | ||
Insulin Glargine. | 495 | ||
Insulin Detemir. | 495 | ||
Ultralong Duration | 495 | ||
Insulin Degludec. | 495 | ||
Concentration | 495 | ||
Subcutaneous Infusion | 495 | ||
Portable Insulin Pumps. | 495 | ||
Implantable Insulin Pumps. | 495 | ||
Inhalation | 496 | ||
Storage | 496 | ||
Therapeutic Use | 496 | ||
Indications | 496 | ||
Insulin Therapy of Diabetes | 496 | ||
Dosage | 496 | ||
Dosing Schedules | 497 | ||
Twice-Daily Premixed Regimen. | 497 | ||
Intensive Basal/Bolus Strategy. | 497 | ||
Continuous Subcutaneous Insulin Infusion. | 497 | ||
Achieving Optimal Glucose Control | 497 | ||
Complications of Insulin Treatment | 497 | ||
Hypoglycemia | 497 | ||
Other Complications | 498 | ||
Hypokalemia. | 498 | ||
Lipohypertrophy. | 498 | ||
Allergic Reactions. | 498 | ||
Drug Interactions | 498 | ||
Hypoglycemic Agents | 498 | ||
Hyperglycemic Agents | 498 | ||
Beta-Adrenergic Blocking Agents | 498 | ||
Noninsulin Medications for the Treatment of Diabetes | 498 | ||
Oral Drugs | 498 | ||
Biguanides: Metformin | 500 | ||
Mechanism of Action | 500 | ||
Pharmacokinetics | 500 | ||
Therapeutic Uses | 500 | ||
Glycemic Control. | 500 | ||
Prevention of Type 2 Diabetes. | 500 | ||
Gestational Diabetes. | 500 | ||
Polycystic Ovary Syndrome (PCOS). | 500 | ||
Side Effects | 500 | ||
Drug Interactions | 501 | ||
Alcohol. | 501 | ||
Cimetidine. | 501 | ||
Iodinated Radiocontrast Media. | 501 | ||
Preparations, Dosage, and Administration | 501 | ||
Sulfonylureas | 501 | ||
Mechanism of Action | 501 | ||
Therapeutic Use | 501 | ||
Adverse Effects | 501 | ||
Hypoglycemia. | 501 | ||
Cardiovascular Toxicity. | 502 | ||
Use in Pregnancy and Lactation. | 502 | ||
Drug Interactions | 502 | ||
Alcohol. | 502 | ||
Drugs that Can Intensify Hypoglycemia | 502 | ||
Beta-Adrenergic Blocking Agents. | 502 | ||
Preparations, Dosage, and Administration | 503 | ||
Meglitinides (Glinides) | 503 | ||
Repaglinide | 503 | ||
Actions and Uses. | 503 | ||
Unit XI Women's Health | 521 | ||
48 Estrogens and Progestins | 521 | ||
The Menstrual Cycle | 521 | ||
Ovarian and Uterine Events | 521 | ||
The Roles of Estrogens and Progesterone | 521 | ||
The Role of Pituitary Hormones | 521 | ||
Estrogens | 522 | ||
Biosynthesis and Elimination | 522 | ||
Females | 522 | ||
Males | 522 | ||
Mechanism of Action | 522 | ||
Physiologic and Pharmacologic Effects | 523 | ||
Effects on Primary and Secondary Sex Characteristics of Females | 523 | ||
Metabolic Actions | 523 | ||
Bone | 523 | ||
Cardiovascular Effects | 523 | ||
Blood Coagulation | 523 | ||
Central Nervous System | 523 | ||
Glucose Homeostasis | 523 | ||
Physiologic Alterations Accompanying Menopause | 523 | ||
Vasomotor Symptoms | 524 | ||
Urogenital Atrophy | 524 | ||
Mental Changes | 524 | ||
Bone Loss | 524 | ||
Altered Lipid Metabolism | 524 | ||
Clinical Pharmacology | 524 | ||
Therapeutic Uses | 524 | ||
Menopausal Hormone Therapy | 524 | ||
Female Hypogonadism | 524 | ||
Acne | 524 | ||
Cancer Palliation | 524 | ||
Adverse Effects | 524 | ||
Contraindications | 524 | ||
Interactions | 525 | ||
Preparations and Routes of Administration | 525 | ||
Oral | 525 | ||
Transdermal | 525 | ||
Intravaginal | 525 | ||
Parenteral | 525 | ||
Selective Estrogen Receptor Modulators | 525 | ||
Progestins | 526 | ||
Biosynthesis | 526 | ||
Mechanism of Action | 526 | ||
Physiologic Effects | 526 | ||
Effects During the Menstrual Cycle | 526 | ||
Effects During Pregnancy | 526 | ||
Clinical Pharmacology | 526 | ||
Therapeutic Uses | 526 | ||
Menopausal Hormone Therapy | 526 | ||
Dysfunctional Uterine Bleeding | 526 | ||
Amenorrhea | 527 | ||
Endometrial Carcinoma and Hyperplasia | 527 | ||
Other Uses | 527 | ||
Adverse Effects | 527 | ||
Preparations and Routes of Administration | 527 | ||
Menopausal Hormone Therapy | 527 | ||
Benefits and Risks of Hormone Therapy | 528 | ||
Recommendations on Hormone Therapy Use | 528 | ||
General Recommendations | 528 | ||
Use for Approved Indications | 528 | ||
Treatment of Vasomotor Symptoms | 529 | ||
Treatment of Symptoms of Vulvar and Vaginal Atrophy | 529 | ||
Prevention of Osteoporosis | 530 | ||
Inappropriate Uses: Attempted Prevention of Heart Disease and Dementia | 530 | ||
Heart Disease | 530 | ||
Alzheimer Disease | 530 | ||
Discontinuing Hormone Therapy | 530 | ||
Drug Products for Hormone Therapy | 530 | ||
Preparations | 530 | ||
Dosing Schedules | 531 | ||
Prescribing and Monitoring Considerations | 531 | ||
Estrogens | 531 | ||
Preadministration Assessment | 531 | ||
Therapeutic Goal | 531 | ||
Baseline Data | 531 | ||
Identifying High-Risk Patients | 531 | ||
Dosing Schedules for Hormone Therapy | 531 | ||
Ongoing Monitoring and Interventions | 532 | ||
Monitoring Summary | 532 | ||
Minimizing Adverse Effects | 532 | ||
Nausea. | 532 | ||
Endometrial Hyperplasia and Cancer. | 532 | ||
Breast Cancer. | 532 | ||
Cardiovascular Events. | 532 | ||
Effects Resembling Those Caused by Oral Contraceptives. | 532 | ||
Minimizing Adverse Interactions | 532 | ||
Progestins | 533 | ||
Preadministration Assessment | 533 | ||
Therapeutic Goal | 533 | ||
Baseline Data | 533 | ||
Identifying High-Risk Patients | 533 | ||
Ongoing Monitoring and Interventions | 533 | ||
Gynecologic Effects | 533 | ||
49 Birth Control | 535 | ||
Effectiveness of Birth Control Methods | 535 | ||
Selecting a Birth Control Method | 535 | ||
Oral Contraceptives | 536 | ||
Combination Oral Contraceptives | 536 | ||
Mechanism of Action | 536 | ||
Components | 536 | ||
Estrogens | 536 | ||
Progestins | 536 | ||
Effectiveness | 537 | ||
Overall Safety | 537 | ||
Adverse Effects | 537 | ||
Thromboembolic Disorders | 537 | ||
Cancer | 538 | ||
Hypertension | 538 | ||
Abnormal Uterine Bleeding | 538 | ||
Use in Pregnancy and Lactation | 538 | ||
Stroke in Women With Migraine | 539 | ||
Benign Hepatic Adenoma | 539 | ||
Effects Related to Estrogen or Progestin Imbalance | 539 | ||
Hyperkalemia | 539 | ||
Glucose Intolerance | 539 | ||
Other Adverse Effects | 539 | ||
Noncontraceptive Benefits of Oral Contraceptives | 540 | ||
Drug Interactions | 540 | ||
Drugs and Herbs that Reduce the Effects of OCs | 540 | ||
Drugs Whose Effects Are Reduced by OCs | 540 | ||
Drugs Whose Effects Are Increased by OCs | 540 | ||
Preparations | 540 | ||
Beyaz and Safyral | 540 | ||
Natazia | 540 | ||
Dosing Schedules | 540 | ||
28-Day-Cycle Schedules | 540 | ||
Extended-Cycle and Continuous Schedules | 540 | ||
What to Do if Doses Are Missed | 543 | ||
Progestin-Only Oral Contraceptives | 543 | ||
Combination Contraceptives With Novel Delivery Systems | 543 | ||
Transdermal Contraceptive Patch | 543 | ||
Vaginal Contraceptive Ring | 544 | ||
Long-Acting Contraceptives | 544 | ||
Subdermal Etonogestrel Implants | 544 | ||
Description | 544 | ||
Mechanism of Action | 544 | ||
Pharmacokinetics | 544 | ||
Drug Interactions | 544 | ||
Adverse Effect: Irregular Bleeding | 544 | ||
Use During Breastfeeding | 544 | ||
Depot Medroxyprogesterone Acetate | 544 | ||
Intrauterine Devices | 545 | ||
Spermicides | 545 | ||
Emergency Contraception | 545 | ||
Progestin-Only Emergency Contraception Pills | 546 | ||
Plan B One-Step and Next Choice One Dose | 546 | ||
Next Choice | 546 | ||
Ulipristal Acetate Emergency Contraception Pill | 546 | ||
Estrogen/Progestin Emergency Contraception Pills (Yuzpe Regimen) | 546 | ||
Mifepristone as an Emergency Contraception Pill | 547 | ||
The Copper Intrauterine Device | 547 | ||
Drugs for Medical Abortion | 547 | ||
Mifepristone (RU 486) With Misoprostol | 547 | ||
Mechanism of Action | 547 | ||
Clinical Trials | 547 | ||
Adverse Effects | 547 | ||
Contraindications | 547 | ||
Preparations, Dosage, and Administration | 547 | ||
Unit XII Men's Health | 549 | ||
50 Androgens | 549 | ||
Testosterone | 549 | ||
Biosynthesis and Secretion | 549 | ||
Males | 549 | ||
Females | 549 | ||
Mechanism of Action | 549 | ||
Physiologic and Pharmacologic Effects | 549 | ||
Effects on Sex Characteristics in Males | 549 | ||
Pubertal Transformation | 549 | ||
Spermatogenesis | 550 | ||
Effects on Sex Characteristics in Females | 550 | ||
Anabolic Effects | 550 | ||
Erythropoietic Effects | 550 | ||
Clinical Pharmacology of the Androgens | 550 | ||
Classification | 550 | ||
Therapeutic Uses | 550 | ||
Male Hypogonadism | 550 | ||
Replacement Therapy | 551 | ||
Delayed Puberty | 551 | ||
Replacement Therapy in Menopausal Women | 551 | ||
Treatment of Transsexualism | 552 | ||
Cachexia | 552 | ||
Anemias | 552 | ||
Adverse Effects | 552 | ||
Virilization in Women, Girls, and Boys | 552 | ||
Premature Epiphyseal Closure | 552 | ||
Hepatotoxicity | 552 | ||
Effects on Cholesterol Levels | 552 | ||
Prostate Cancer | 552 | ||
Edema | 553 | ||
Abuse Potential | 553 | ||
Risk for Thromboembolic Events | 553 | ||
Androgen Preparations for Male Hypogonadism | 553 | ||
Oral Androgens | 553 | ||
Transdermal Testosterone | 553 | ||
Patches | 553 | ||
Gels | 553 | ||
Topical Solution | 553 | ||
Nasal Gel | 554 | ||
Implantable Testosterone Pellets | 554 | ||
Testosterone Buccal Tablets | 554 | ||
Intramuscular Testosterone Esters | 554 | ||
Androgen (Anabolic Steroid) Abuse by Athletes | 554 | ||
Prescribing and Monitoring Considerations | 555 | ||
Preadministration Assessment | 555 | ||
Therapeutic Goals | 555 | ||
Males | 555 | ||
Identifying High-Risk Patients | 555 | ||
Administration Considerations | 555 | ||
Transdermal Gel and Solution | 555 | ||
Buccal | 555 | ||
Implantable Pellets | 555 | ||
Nasal | 555 | ||
Ongoing Monitoring and Interventions | 555 | ||
Minimizing Adverse Effects | 555 | ||
Virilization | 555 | ||
Premature Epiphyseal Closure | 555 | ||
Hepatotoxicity | 555 | ||
Edema | 555 | ||
Teratogenesis | 555 | ||
Prostate Cancer | 555 | ||
Injury From Skin-to-Skin Transfer of Topical Testosterone | 555 | ||
51 Drugs for Erectile Dysfunction and Benign Prostatic Hyperplasia | 557 | ||
Erectile Dysfunction | 557 | ||
Physiology of Erection | 557 | ||
Oral Drugs for Erectile Dysfunction: PDE-5 Inhibitors | 557 | ||
Sildenafil | 557 | ||
Mechanism of Action | 557 | ||
Pharmacokinetics | 558 | ||
Sexual Benefits | 558 | ||
In Men With ED. | 558 | ||
In Men Without ED. | 558 | ||
In Women. | 558 | ||
Adverse Effects | 558 | ||
Hypotension. | 558 | ||
Priapism. | 561 | ||
Nonarteritic Ischemic Optic Neuropathy (NAION). | 561 | ||
Sudden Hearing Loss. | 561 | ||
Other Adverse Effects. | 561 | ||
Drug Interactions | 561 | ||
Nitrates. | 561 | ||
Alpha Blockers. | 561 | ||
Inhibitors of CYP3A4. | 561 | ||
Is Sildenafil Safe for Men With Coronary Heart Disease? | 561 | ||
Vardenafil, Tadalafil, and Avanafil | 562 | ||
Vardenafil | 562 | ||
Unit XIII Antiinflammatory, Antiallergic, and Immunologic Drugs | 571 | ||
52 Review of the Immune System | 571 | ||
Introduction to the Immune System | 571 | ||
Natural Immunity Versus Specific Acquired Immunity | 571 | ||
Cell-Mediated Immunity Versus Antibody-Mediated (Humoral) Immunity | 571 | ||
Introduction to Cells of the Immune System | 571 | ||
B Lymphocytes (B Cells) | 571 | ||
Cytolytic T Lymphocytes (Cytolytic T Cells, CD8 Cells) | 572 | ||
Helper T Lymphocytes (Helper T Cells, CD4 Cells) | 572 | ||
Macrophages | 572 | ||
Dendritic Cells | 573 | ||
Mast Cells and Basophils | 573 | ||
Neutrophils | 573 | ||
Eosinophils | 573 | ||
Antibodies | 573 | ||
Antigens | 574 | ||
Characteristic Features of Immune Responses | 575 | ||
Specificity | 575 | ||
Diversity | 575 | ||
Memory | 575 | ||
Time Limitation | 575 | ||
Selectivity for Antigens of Nonself Origin | 575 | ||
Phases of the Immune Response | 575 | ||
Recognition Phase | 575 | ||
Activation Phase | 575 | ||
Effector Phase | 575 | ||
Major Histocompatibility Complex Molecules | 575 | ||
Cytokines, Lymphokines, and Monokines | 576 | ||
Antibody-Mediated (Humoral) Immunity | 576 | ||
Production of Antibodies | 576 | ||
Overview of Antibody Production | 576 | ||
Specific Cellular Events in Antibody Production | 576 | ||
B Cells | 576 | ||
Antigen-Presenting Cells | 577 | ||
Helper T Cells (CD4 Cells) | 577 | ||
Antibody Effector Mechanisms | 578 | ||
Opsonization of Bacteria | 578 | ||
Activation of the Complement System | 578 | ||
Neutralization of Viruses and Bacterial Toxins | 578 | ||
Cell-Mediated Immunity | 578 | ||
Delayed-Type Hypersensitivity (Type IV Hypersensitivity) | 578 | ||
Activation of Helper T Cells | 578 | ||
Activation of Macrophages | 578 | ||
Cytolytic T Lymphocytes | 579 | ||
Activation of Cytolytic T Cells | 579 | ||
Recognition of Virally Infected Target Cells | 579 | ||
Mechanisms of Cell Kill | 580 | ||
53 Childhood Immunization | 581 | ||
General Considerations | 581 | ||
Definitions | 581 | ||
Vaccine | 581 | ||
Killed Vaccines versus Live Vaccines | 581 | ||
Toxoid | 581 | ||
Vaccination | 581 | ||
Immunization: Active versus Passive | 581 | ||
Specific Immune Globulins | 581 | ||
Public Health Effects of Immunization | 581 | ||
Reporting Vaccine-Preventable Diseases | 582 | ||
Immunization Records | 582 | ||
Adverse Effects of Immunization | 582 | ||
Vaccine Information Statements | 583 | ||
Childhood Immunization Schedule | 583 | ||
Target Diseases | 583 | ||
Measles, Mumps, and Rubella | 583 | ||
Measles | 583 | ||
Mumps | 583 | ||
Rubella | 584 | ||
Diphtheria, Tetanus, and Pertussis | 584 | ||
Diphtheria | 584 | ||
Tetanus (Lockjaw) | 584 | ||
Pertussis (Whooping Cough) | 584 | ||
Poliomyelitis | 584 | ||
Haemophilus influenzae Type b | 584 | ||
Varicella (Chickenpox) | 584 | ||
Hepatitis B | 585 | ||
Hepatitis A | 585 | ||
Pneumococcal Infection | 585 | ||
Meningococcal Infection | 585 | ||
Influenza | 585 | ||
Rotavirus Gastroenteritis | 586 | ||
Genital Human Papillomavirus Infection | 586 | ||
Respiratory Syncytial Virus | 586 | ||
Specific Vaccines and Toxoids | 586 | ||
Measles, Mumps, and Rubella Virus Vaccine | 586 | ||
Description | 586 | ||
Efficacy | 586 | ||
Adverse Effects | 586 | ||
Mild | 586 | ||
Severe | 589 | ||
Precautions and Contraindications | 589 | ||
Diphtheria and Tetanus Toxoids and Acellular Pertussis Vaccine | 589 | ||
Preparations | 589 | ||
Efficacy | 589 | ||
Adverse Effects | 589 | ||
Mild | 589 | ||
Moderate | 589 | ||
Severe: Encephalopathy | 590 | ||
Precautions and Contraindications | 590 | ||
Poliovirus Vaccine | 590 | ||
Unit XIV Drugs for Bone and Joint Disorders | 629 | ||
57 Drug Therapy of Rheumatoid Arthritis | 629 | ||
Pathophysiology of Rheumatoid Arthritis | 629 | ||
Overview of Therapy | 629 | ||
Nondrug Measures | 629 | ||
Drug Therapy | 630 | ||
Classes of Antiarthritic Drugs | 630 | ||
Drug Selection | 630 | ||
Nonsteroidal Antiinflammatory Drugs | 630 | ||
Therapeutic Role | 632 | ||
Nonsteroidal Antiinflammatory Drug Classification | 632 | ||
Drug Selection | 632 | ||
Efficacy | 632 | ||
Safety and Cost | 632 | ||
Dosage | 632 | ||
Glucocorticoids | 632 | ||
Nonbiologic (Traditional) Disease-Antimodifying Rheumatic Drugs | 632 | ||
Methotrexate | 633 | ||
Sulfasalazine | 634 | ||
Leflunomide | 634 | ||
Actions and Uses | 634 | ||
Pharmacokinetics | 634 | ||
Adverse Effects | 634 | ||
Leflunomide and Pregnancy | 634 | ||
Drug Interactions | 634 | ||
Hydroxychloroquine | 634 | ||
Other Nonbiologic Disease-Modifying Antirheumatic Drugs | 634 | ||
Penicillamine | 634 | ||
Gold Salts | 634 | ||
Azathioprine | 634 | ||
Cyclosporine | 635 | ||
Minocycline | 635 | ||
Protein A Column [Prosorba] | 635 | ||
Biologic Disease-Modifying Antirheumatic Drugs | 635 | ||
Tumor Necrosis Factor Antagonists | 635 | ||
Etanercept | 635 | ||
Mechanism of Action | 635 | ||
Therapeutic Uses | 636 | ||
Pharmacokinetics | 636 | ||
Adverse Effects | 636 | ||
Mild Effects. | 636 | ||
Serious Infections. | 636 | ||
Severe Allergic Reactions. | 636 | ||
Heart Failure. | 636 | ||
Cancer. | 636 | ||
Hematologic Disorders. | 636 | ||
Liver Injury. | 636 | ||
CNS Demyelinating Disorders. | 637 | ||
Drug Interactions. | 637 | ||
Preparations, Dosage, and Administration. | 637 | ||
Infliximab | 637 | ||
Unit XV Respiratory Tract Drugs | 673 | ||
60 Drugs for Asthma and Chronic Obstructive Pulmonary Disease | 673 | ||
Basic Considerations | 673 | ||
Pathophysiology of Asthma | 673 | ||
Pathophysiology of Chronic Obstructive Pulmonary Disease | 673 | ||
Overview of Drugs for Asthma and Chronic Obstructive Pulmonary Disease | 674 | ||
Administering Drugs by Inhalation | 675 | ||
Metered-Dose Inhalers | 675 | ||
Dry-Powder Inhalers | 677 | ||
Nebulizers | 677 | ||
Antiinflammatory Drugs | 677 | ||
Glucocorticoids | 677 | ||
Mechanism of Antiasthma Action | 677 | ||
Use in Asthma | 677 | ||
Inhalation Use | 677 | ||
Oral Use | 678 | ||
Adverse Effects | 678 | ||
Inhaled Glucocorticoids | 678 | ||
Oral Glucocorticoids | 678 | ||
Compensating for Adrenal Insufficiency | 678 | ||
Preparations, Dosage, and Administration | 679 | ||
Inhaled Glucocorticoids | 679 | ||
Nebulized Budesonide | 679 | ||
Oral Glucocorticoids | 679 | ||
Leukotriene Modifiers | 679 | ||
Zileuton | 679 | ||
Mechanism of Action | 679 | ||
Pharmacokinetics | 679 | ||
Adverse Effects | 679 | ||
Unit XVI Gastrointestinal Drugs | 703 | ||
62 Drugs for Peptic Ulcer Disease | 703 | ||
Pathogenesis of Peptic Ulcers | 703 | ||
Defensive Factors | 703 | ||
Mucus | 703 | ||
Bicarbonate | 703 | ||
Blood Flow | 703 | ||
Prostaglandins | 703 | ||
Aggressive Factors | 703 | ||
Helicobacter pylori | 703 | ||
Nonsteroidal Antiinflammatory Drugs | 704 | ||
Gastric Acid | 704 | ||
Pepsin | 704 | ||
Smoking | 704 | ||
Summary | 704 | ||
Overview of Treatment | 704 | ||
Drug Therapy | 704 | ||
Classes of Antiulcer Drugs | 704 | ||
Drug Selection | 706 | ||
Helicobacter pylori–Associated Ulcers | 706 | ||
NSAID-Induced Ulcers | 706 | ||
Prophylaxis. | 706 | ||
Treatment. | 706 | ||
Evaluation | 706 | ||
A Note About the Effects of Drugs on Pepsin | 706 | ||
Nondrug Therapy | 706 | ||
Diet | 706 | ||
Other Nondrug Measures | 706 | ||
Antibacterial Drugs | 706 | ||
Antibiotics Employed | 706 | ||
Clarithromycin | 706 | ||
Amoxicillin | 706 | ||
Bismuth | 706 | ||
Tetracycline | 707 | ||
Metronidazole | 707 | ||
Tinidazole | 707 | ||
Antibiotic Regimens | 707 | ||
Histamine-2 Receptor Antagonists | 707 | ||
Cimetidine | 708 | ||
Mechanism of Action | 708 | ||
Pharmacokinetics | 708 | ||
Unit XVII Nutrition and Complementary Therapies | 737 | ||
65 Vitamins | 737 | ||
Basic Considerations | 737 | ||
Dietary Reference Intakes | 737 | ||
Recommended Dietary Allowance | 737 | ||
Adequate Intake | 737 | ||
Tolerable Upper Intake Level | 737 | ||
Estimated Average Requirement | 737 | ||
Acceptable Macronutrient Distribution Range | 737 | ||
Classification of Vitamins | 737 | ||
Should We Take Multivitamin Supplements? | 738 | ||
What About Protective Antioxidant Effects? | 738 | ||
Fat-Soluble Vitamins | 738 | ||
Vitamin A (Retinol) | 738 | ||
Actions | 738 | ||
Sources | 738 | ||
Units | 738 | ||
Requirements | 738 | ||
Pharmacokinetics | 738 | ||
Deficiency | 738 | ||
Toxicity | 740 | ||
Therapeutic Uses | 740 | ||
Preparations and Routes of Administration | 740 | ||
Vitamin D | 740 | ||
Vitamin E (Alpha-Tocopherol) | 740 | ||
Forms of Vitamin E | 740 | ||
Sources | 740 | ||
Requirements | 740 | ||
Deficiency | 740 | ||
Potential Benefits | 740 | ||
Potential Risks | 740 | ||
Vitamin K | 741 | ||
Action | 741 | ||
Forms and Sources of Vitamin K | 741 | ||
Requirements | 741 | ||
Pharmacokinetics | 741 | ||
Deficiency | 741 | ||
Adverse Effects | 741 | ||
Severe Hypersensitivity Reactions | 741 | ||
Hyperbilirubinemia | 741 | ||
Therapeutic Uses and Dosage | 741 | ||
Vitamin K Replacement | 741 | ||
Warfarin Antidote | 742 | ||
Unit XVIII Therapy of Infectious and Parasitic Diseases | 769 | ||
68 Basic Principles of Antimicrobial Therapy | 769 | ||
Selective Toxicity | 769 | ||
Achieving Selective Toxicity | 769 | ||
Disruption of the Bacterial Cell Wall | 769 | ||
Inhibition of an Enzyme Unique to Bacteria | 769 | ||
Disruption of Bacterial Protein Synthesis | 770 | ||
Classification of Antimicrobial Drugs | 770 | ||
Classification by Susceptible Organism | 770 | ||
Classification by Mechanism of Action | 770 | ||
Acquired Resistance to Antimicrobial Drugs | 771 | ||
Microbial Mechanisms of Drug Resistance | 771 | ||
Reduction of Drug Concentration at Its Site of Action | 771 | ||
Alteration of Drug Target Molecules | 771 | ||
Antagonist Production | 771 | ||
Drug Inactivation | 771 | ||
New Delhi Metallo-Beta-Lactamase 1 (NDM-1) Gene | 772 | ||
Mechanisms by Which Resistance Is Acquired | 772 | ||
Spontaneous Mutation | 773 | ||
Conjugation | 773 | ||
Relationships Between Antibiotic Use and Emergence of Drug-Resistant Microbes | 773 | ||
How Do Antibiotics Promote Resistance? | 773 | ||
Which Antibiotics Promote Resistance? | 773 | ||
Influence of Increased Antibiotic Use on the Emergence of Resistance | 773 | ||
Health Care−Associated Infections | 773 | ||
Superinfection | 773 | ||
Antimicrobial Stewardship | 773 | ||
Selection of Antibiotics | 774 | ||
Empiric Therapy Before Completion of Laboratory Tests | 774 | ||
Identifying the Infecting Organism | 774 | ||
Determining Drug Susceptibility | 777 | ||
Host Factors That Modify Drug Choice, Route of Administration, or Dosage | 777 | ||
Host Defenses | 777 | ||
Site of Infection | 778 | ||
Other Host Factors | 778 | ||
Previous Allergic Reaction | 778 | ||
Genetic Factors | 778 | ||
Dosage and Duration of Treatment | 778 | ||
Therapy With Antibiotic Combinations | 778 | ||
Antimicrobial Effects of Antibiotic Combinations | 779 | ||
Indications for Antibiotic Combinations | 779 | ||
Initial Therapy of Severe Infection | 779 | ||
Mixed Infections | 779 | ||
Preventing Resistance | 779 | ||
Decreased Toxicity | 779 | ||
Enhanced Antibacterial Action | 779 | ||
Disadvantages of Antibiotic Combinations | 779 | ||
Prophylactic Use of Antimicrobial Drugs | 779 | ||
Surgery | 779 | ||
Bacterial Endocarditis | 780 | ||
Neutropenia | 780 | ||
Other Indications for Antimicrobial Prophylaxis | 780 | ||
Misuses of Antimicrobial Drugs | 780 | ||
Attempted Treatment of Viral Infection | 780 | ||
Treatment of Fever of Unknown Origin | 780 | ||
Improper Dosage | 780 | ||
Treatment in the Absence of Adequate Bacteriologic Information | 780 | ||
Omission of Surgical Drainage | 780 | ||
Monitoring Antimicrobial Therapy | 780 | ||
69 Drugs That Weaken the Bacterial Cell Wall I | 783 | ||
Introduction to the Penicillins | 783 | ||
Mechanism of Action | 783 | ||
Mechanisms of Bacterial Resistance | 783 | ||
The Gram-Negative Cell Envelope | 783 | ||
Penicillinases (Beta-Lactamases) | 783 | ||
Altered Penicillin-Binding Proteins | 784 | ||
Methicillin-Resistant Staphylococcus aureus | 784 | ||
Health Care−Associated MRSA | 785 | ||
Community-Associated MRSA | 785 | ||
Chemistry | 785 | ||
Classification | 786 | ||
Properties of Individual Penicillins | 786 | ||
Penicillin G | 786 | ||
Antimicrobial Spectrum | 786 | ||
Therapeutic Uses | 786 | ||
Pharmacokinetics | 786 | ||
Absorption | 786 | ||
Intramuscular. | 786 | ||
Distribution | 787 | ||
Metabolism and Excretion | 787 | ||
Side Effects and Toxicities | 787 | ||
Penicillin Allergy | 787 | ||
General Considerations | 787 | ||
Types of Allergic Reactions | 788 | ||
Development of Penicillin Allergy | 788 | ||
Skin Tests for Penicillin Allergy | 788 | ||
Management of Patients With a History of Penicillin Allergy | 788 | ||
Drug Interactions | 788 | ||
Bacteriostatic Antibiotics | 788 | ||
Penicillin V | 788 | ||
Penicillinase-Resistant Penicillins (Antistaphylococcal Penicillins) | 788 | ||
Nafcillin | 789 | ||
Oxacillin and Dicloxacillin | 789 | ||
Broad-Spectrum Penicillins (Aminopenicillins) | 789 | ||
Ampicillin | 789 | ||
Amoxicillin | 789 | ||
Extended-Spectrum Penicillins (Antipseudomonal Penicillins) | 789 | ||
Piperacillin | 790 | ||
Penicillins Combined With a Beta-Lactamase Inhibitor | 790 | ||
70 Drugs That Weaken the Bacterial Cell Wall II | 791 | ||
Cephalosporins | 791 | ||
Chemistry | 791 | ||
Mechanism of Action | 791 | ||
Resistance | 791 | ||
Classification and Antimicrobial Spectra | 791 | ||
First Generation | 791 | ||
Second Generation | 791 | ||
Third Generation | 791 | ||
Fourth Generation | 791 | ||
Fifth Generation | 792 | ||
Pharmacokinetics | 792 | ||
Absorption | 792 | ||
Distribution | 792 | ||
Elimination | 792 | ||
Adverse Effects | 793 | ||
Allergic Reactions | 793 | ||
Bleeding | 793 | ||
Thrombophlebitis | 793 | ||
Hemolytic Anemia | 793 | ||
Other Adverse Effects | 793 | ||
Drug Interactions | 793 | ||
Alcohol | 793 | ||
Drugs That Promote Bleeding | 793 | ||
Therapeutic Uses | 793 | ||
First-Generation Cephalosporins | 793 | ||
Second-Generation Cephalosporins | 794 | ||
Third-Generation Cephalosporins | 794 | ||
Fourth-Generation Cephalosporins | 794 | ||
Fifth-Generation Cephalosporins | 794 | ||
Drug Selection | 794 | ||
Antimicrobial Spectrum | 794 | ||
Adverse Effects | 794 | ||
Pharmacokinetics | 794 | ||
Route of Administration | 794 | ||
Duration of Action | 794 | ||
Distribution to Cerebrospinal Fluid | 794 | ||
Route of Elimination | 794 | ||
Dosage and Administration | 794 | ||
Routes | 794 | ||
Dosage | 794 | ||
Administration | 794 | ||
Oral | 794 | ||
Intramuscular | 794 | ||
Intravenous | 795 | ||
Carbapenems | 795 | ||
Imipenem | 795 | ||
Mechanism of Action | 795 | ||
Antimicrobial Spectrum | 795 | ||
Pharmacokinetics | 795 | ||
Adverse Effects | 796 | ||
Interaction With Valproate | 796 | ||
Therapeutic Use | 796 | ||
Other Carbapenems | 796 | ||
Meropenem | 796 | ||
Unit XIX Drug Therapy for Patients with Cancer | 917 | ||
82 Anti-Cancer Drugs for the Nonspecialist | 917 | ||
Basic Principals of Cancer Chemotherapy | 917 | ||
The Role of the Nonspecialist | 917 | ||
What Is Cancer? | 917 | ||
Characteristics of Neoplastic Cells | 917 | ||
Persistent Proliferation | 917 | ||
Invasive Growth | 917 | ||
Formation of Metastases | 917 | ||
Immortality | 917 | ||
Etiology of Cancer | 918 | ||
Epidemiology | 918 | ||
Treatment of Cancer | 918 | ||
Introduction to the Cytotoxic Anticancer Drugs | 918 | ||
Mechanisms of Cytotoxic Action | 918 | ||
Cell-Cycle Phase Specificity | 920 | ||
Cell-Cycle Phase–Specific Drugs | 921 | ||
Cell-Cycle Phase–Nonspecific Drugs | 922 | ||
Toxicity to Normal Cells | 922 | ||
Major Toxicities of Chemotherapeutic Drugs | 922 | ||
Bone Marrow Suppression | 922 | ||
Neutropenia | 922 | ||
Thrombocytopenia | 923 | ||
Anemia | 923 | ||
Digestive Tract Injury | 923 | ||
Stomatitis | 923 | ||
Diarrhea | 924 | ||
Nausea and Vomiting | 924 | ||
Other Important Toxicities | 924 | ||
Alopecia | 924 | ||
Reproductive Toxicity | 924 | ||
Hyperuricemia | 925 | ||
Local Injury From Extravasation of Vesicants | 925 | ||
Unique Toxicities | 925 | ||
Carcinogenesis | 925 | ||
Making the Decision to Treat | 925 | ||
Cytotoxic Agents | 926 | ||
Alkylating Agents | 926 | ||
Shared Properties | 926 | ||
Mechanism of Action | 926 | ||
Toxicities | 926 | ||
Nitrosoureas | 926 | ||
Platinum Compounds | 926 | ||
Antimetabolites | 926 | ||
Folic Acid Analogs | 927 | ||
Pyrimidine Analogs | 927 | ||
Purine Analogs | 927 | ||
Hypomethylating Agents | 928 | ||
Antitumor Antibiotics | 928 | ||
Anthracyclines | 928 | ||
Nonanthracyclines | 928 | ||
Mitotic Inhibitors | 928 | ||
Topoisomerase Inhibitors | 928 | ||
Miscellaneous Cytotoxic Drugs | 928 | ||
Asparaginase | 928 | ||
Hydroxyurea | 928 | ||
Mitotane | 928 | ||
Hormonal Agents, Targeted Drugs, and Other Noncytotoxic Anticancer Drugs | 928 | ||
Drugs for Breast Cancer | 928 | ||
Antiestrogens | 929 | ||
Tamoxifen | 929 | ||
Overview of Actions | 929 | ||
Mechanism of Action in Breast Cancer | 929 | ||
Use for Treatment of Breast Cancer | 929 | ||
Use for Prevention of Breast Cancer | 929 | ||
Pharmacokinetics | 929 | ||
Unit XX Drugs for Eyes, Ears, and Skin | 967 | ||
84 Drugs for the Eye | 967 | ||
Drugs for Glaucoma | 967 | ||
Pathophysiology and Treatment Overview | 967 | ||
Primary Open-Angle Glaucoma | 967 | ||
Characteristics | 967 | ||
Risk Factors | 967 | ||
Screening | 967 | ||
Management | 967 | ||
Angle-Closure Glaucoma | 969 | ||
Drugs Used to Treat Glaucoma | 969 | ||
Beta-Adrenergic Blocking Agents | 969 | ||
Actions and Use in Glaucoma | 969 | ||
Adverse Effects | 970 | ||
Local. | 970 | ||
Systemic. | 970 | ||
Prostaglandin Analogs | 970 | ||
Latanoprost | 970 | ||
Other Prostaglandin Analogs | 971 | ||
Alpha2-Adrenergic Agonists | 971 | ||
Brimonidine | 971 | ||
Apraclonidine | 971 | ||
Alpha2 Agonist/Beta Blocker Combination | 971 | ||
Pilocarpine, a Direct-Acting Muscarinic Agonist | 971 | ||
Effects on the Eye | 971 | ||
Therapeutic Uses | 971 | ||
Adverse Effects | 971 | ||
Echothiophate, a Cholinesterase Inhibitor | 972 | ||
Effects on the Eye | 972 | ||
Use in Glaucoma | 972 | ||
Unit XXI Drug Therapy in Acute Care | 1003 | ||
87 Agents Affecting the Volume and Ion Content of Body Fluids | 1003 | ||
Disorders of Fluid Volume and Osmolality | 1003 | ||
Volume Contraction | 1003 | ||
Isotonic Contraction | 1003 | ||
Appendix A Canadian Drug Information | 1033 | ||
Canadian Drug Legislation | 1033 | ||
Prescription Drugs (Schedule F) | 1033 | ||
Nonprescription Medications—National Drug Schedules | 1034 | ||
New-Drug Development in Canada | 1034 | ||
Patent Laws | 1034 | ||
Drug Advertising | 1035 | ||
International System of Units | 1035 | ||
Drug Serum Concentrations | 1035 | ||
References | 1036 | ||
Index | 1037 | ||
A | 1037 | ||
B | 1042 | ||
C | 1044 | ||
D | 1047 | ||
E | 1049 | ||
F | 1050 | ||
G | 1051 | ||
H | 1052 | ||
I | 1053 | ||
K | 1055 | ||
L | 1055 | ||
M | 1056 | ||
N | 1057 | ||
O | 1059 | ||
P | 1060 | ||
Q | 1063 | ||
R | 1064 | ||
S | 1064 | ||
T | 1066 | ||
U | 1068 | ||
V | 1068 | ||
W | 1069 | ||
X | 1069 | ||
Y | 1069 | ||
Z | 1069 |