Rowland and Tozer's Clinical Pharmacokinetics and Pharmacodynamics: Concepts and Applications
Höfundar:
Hartmut Derendorf; Stephan Schmidt (Útgáfa: 5)
Kaup valmöguleikar
Updated with the latest clinical advances, Rowland and Tozer’s Clinical Pharmacokinetics and Pharmacodynamics, Fifth Edition , explains the relationship between drug administration and drug response, taking a conceptual approach that emphasizes clinical application rather than science and mathematics. Bringing a real-life perspective to the topic, the book simplifies concepts and gives readers the knowledge they need to better evaluate drug applications.
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- Wolters Kluwer Health
- 9781496385901
- 9781496385048
- ePub
- 5
- Hartmut Derendorf; Stephan Schmidt
- English
- 2019-07-11
- 10
- 2
- 2
Kaflar
- About the Authors
- Preface
- Nonproprietary and Brand Names of Drugs in Text and Illustrations
- Definition of Symbols
- SECTION 1 BASIC CONSIDERATIONS
- CHAPTER 1 Therapeutic Relevance
- CLINICAL SETTING
- Input–Response Phases
- Variability in Drug Response
- Adherence
- THE INDUSTRIAL PERSPECTIVE
- ORGANIZATION OF THE BOOK
- CHAPTER 2 Fundamental Concepts and Terminology
- PHARMACOKINETICS
- Systemic Exposure
- Sites of Measurement
- Unbound Drug Concentration
- Exposure–Time Profile
- Period of Observation
- Chemical Purity and Analytic Specificity
- Active Metabolites and Prodrugs
- Anatomic and Physiologic Considerations
- Sites of Administration
- Events after Entering Systemically
- Models for Drug Absorption and Disposition
- Definitions of Pharmacokinetic Terms
- Systemic Absorption
- Disposition
- Distribution
- Elimination
- Biliary Secretion and Fecal Excretion
- PHARMACODYNAMICS
- Classification of Response
- Assessment of Drug Response
- Relating Response to Exposure
- Graded Response
- Quantal Response
- Desirable Characteristics
- DOSE–TIME–RESPONSE RELATIONSHIPS
- Turnover Concepts in Drug Response
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- SECTION 2 EXPOSURE AND RESPONSE AFTERA SINGLE DOSE
- CHAPTER 3 Kinetics Following an Intravenous Bolus Dose
- APPRECIATION OF KINETIC CONCEPTS
- Volume of Distribution and Clearance
- First-order Elimination
- Half-life
- Fraction of Dose Remaining
- Clearance, Area, and Volume of Distribution
- Mean Residence Time
- A CASE STUDY
- Distribution Phase
- Terminal Phase
- Elimination Half-life
- Clearance
- Volume of Distribution
- Clearance and Elimination
- Distribution and Elimination: Competing Processes
- PATHWAYS OF ELIMINATION
- Renal Clearance
- Renal Excretion as a Fraction of Total Elimination
- ESTIMATION OF PHARMACOKINETIC PARAMETERS
- Plasma Data Alone
- Plasma and Urine Data
- A Question of Precision
- Measurement Fluid
- Use of Computers
- CHANGE IN DOSE
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 4 Membranes and Distribution
- MEMBRANES
- TRANSPORT PROCESSES
- Protein Binding
- Diffusion
- Drug Properties Determining Permeability
- Membrane Characteristics
- Carrier-Mediated Transport
- REVERSIBLE NATURE OF TRANSPORT
- RATE OF DISTRIBUTION TO TISSUES
- Perfusion Rate Limitation
- Permeability Rate Limitation
- EXTENT OF DISTRIBUTION
- Apparent Volume of Distribution
- Binding within Blood
- Plasma Protein Binding
- Tissue Distribution
- Tissue Binding
- Transporters
- SMALL VOLUME OF DISTRIBUTION
- Model
- Location in Body
- Altered Binding and Loading Dose
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 5 Elimination
- PROCESSES OF ELIMINATION
- CLEARANCE IN GENERAL
- Description of Clearance by Organ, Process, or Site of Measurement
- Plasma or Serum versus Blood Clearance
- Additivity of Clearance
- HEPATIC CLEARANCE
- Perfusion, Protein Binding, and Hepatocellular Activity
- Intrinsic Clearance
- Perfusion
- Plasma Protein Binding
- Hepatocellular Eliminating Activity
- A Memory Aid
- Some Complexities
- Permeability
- Location of Transporters
- Biliary Excretion and Enterohepatic Cycling
- RENAL CLEARANCE
- The Nephron: Anatomy and Function
- Glomerular Filtration
- Active Secretion
- Protein Binding and Perfusion
- Tubular Reabsorption
- Renal Metabolism
- DEPENDENCE OF ELIMINATION KINETICS ON CLEARANCE AND DISTRIBUTION
- Half-life in Plasma
- Half-life in Blood and Plasma Water
- INTEGRATION OF KINETIC AND PHYSIOLOGIC CONCEPTS
- Interrelationships among Pharmacokinetic Parameters and Physiologic Variables
- Primary Parameters and Physiologic Variables
- Secondary Pharmacokinetic Parameters and Derived Values
- Induction of Metabolism
- Metabolic Inhibition
- Altered Blood Flow
- Altered Active Tubular Secretion
- Altered Plasma Protein Binding
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 6 Kinetics Following an Extravascular Dose
- ROUTES OF EXTRAVASCULAR ADMINISTRATION
- KINETICS OF ABSORPTION
- EXPOSURE–TIME AND EXPOSURE–DOSE RELATIONSHIPS
- Comparison with Intravenous Administration
- CHANGES IN DOSE OR ABSORPTION KINETICS
- Changing Dose
- Changing Absorption Kinetics
- Disposition Is Rate-Limiting
- Absorption Is Rate-Limiting
- Distinguishing between Absorption and Disposition Rate Limitations
- Changing Disposition Kinetics
- Predicting Changes in Peak Concentration and Peak Time
- ASSESSMENT OF PRODUCT PERFORMANCE
- Formulation
- Bioequivalence Testing
- ASSESSMENT OF PHARMACOKINETIC PARAMETERS
- Plasma Data Alone
- Bioavailability
- Relative Bioavailability
- Fraction Eliminated
- Other Pharmacokinetic Parameters
- Urine Data Alone
- Plasma and Urine Data
- Virtual Bioequivalence
- Local Bioequivalence
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 7 Absorption
- ABSORPTION FROM SOLUTION
- Gastrointestinal Absorption
- Gastric Emptying
- Intestinal Absorption and Permeability
- Causes of Loss in Oral Bioavailability
- Competing Intestinal Reactions
- First-Pass Loss
- Separating Gut Wall from Hepatic First-Pass Loss
- Hepatic First-Pass Predictions
- Saturable First-Pass Metabolism
- Absorption from Intramuscular and Subcutaneous Sites
- ABSORPTION FROM SOLID DOSAGE FORMS
- Dissolution
- Gastric Emptying and Intestinal Transit
- Gastric Emptying
- Rapid Dissolution in Stomach
- Rapid Dissolution in Intestine
- Intestinal Absorption Windows
- Poor Dissolution
- Biopharmaceutics Classification System
- Modified-Release Products
- Changing Rate Control
- Precipitation and Redissolution
- Absorption from Other Sites
- INTEGRATION OF KINETIC AND PHYSIOLOGIC CONCEPTS
- Change in the Speed of Absorption
- Change in Extent of Absorption
- Change in Drug Disposition
- Induction, Low Extraction Ratio
- Induction, High Extraction Ratio
- Impaired Renal Function
- Increase in Urine pH
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 8 Response
- TIME DELAYS BETWEEN CONCENTRATION AND RESPONSE
- Detecting Time Delays
- Causes of Time Delay
- Tissue Distribution
- Pharmacodynamics
- Direct and Indirect Link
- Indirect Response Models
- Systems in Flux
- Revealing the Concentration–Response Relationship
- Effect Compartment
- Systems in Flux
- DECLINE OF RESPONSE WITH TIME
- When Pharmacokinetics Rate-Limits Decline
- When Pharmacodynamics Rate-Limits Decline
- ONSET AND DURATION OF RESPONSE
- Onset of Effect
- Duration of Effect
- Impact of Transporter Polymorphism on Exposure–Response Relationships
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- SECTION 3 THERAPEUTIC REGIMENS
- CHAPTER 9 Therapeutic Window
- DOSAGE REGIMENS
- THERAPEUTIC EXPOSURE
- THERAPEUTIC INDEX
- ADDITIONAL CONSIDERATIONS
- Multiple Active Species
- Single-Dose Therapy
- Duration versus Intensity of Exposure
- Time Delays
- ACHIEVING THERAPEUTIC GOALS
- STUDY PROBLEMS
- CHAPTER 10 Constant-Rate Input
- EXPOSURE–TIME RELATIONSHIPS
- The Plateau Value
- Mean Residence Time
- Time to Reach Plateau
- Postinfusion
- Changing Infusion Rates
- Bolus Plus Infusion
- SHORT-TERM INFUSIONS
- CONSEQUENCE OF SLOW TISSUE DISTRIBUTION
- Rapid Induction of Anesthesia
- Decrease in Infusion Rate on Chronic Administration
- Recovery from Anesthesia
- PHARMACODYNAMIC CONSIDERATIONS
- The Drug Itself
- Onset of Response
- Response on Stopping an Infusion
- Response Infusion versus Single Dose
- Turnover of Affected Systems
- Altered Turnover
- Establishment of a New Steady State
- Interpretation of Non–Steady-State Observations
- TOLERANCE
- INTEGRATION OF KINETIC AND PHYSIOLOGIC CONCEPTS
- Drug A. Inhibition of Hepatic Metabolism, Low Hepatic Extraction Ratio
- Drug B. Inhibition of Hepatic Metabolism, High Hepatic Extraction Ratio
- Drug C. Induction of Hepatic Metabolism, Low Hepatic Extraction Ratio
- Drug D Induction of Hepatic Metabolism, High Hepatic Extraction Ratio
- TRANSLATIONAL JUSTIFICATION FOR USING CONTINUOUS INFUSIONS
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 11 Multiple-Dose Regimens
- PRINCIPLES OF DRUG ACCUMULATION
- Maxima and Minima on Accumulation to the Plateau
- Average Level at Plateau
- Rate of Accumulation to Plateau
- Accumulation Index
- Change in Regimen
- RELATIONSHIP BETWEEN INITIAL AND MAINTENANCE DOSES
- MAINTENANCE OF DRUG IN THE THERAPEUTIC RANGE
- Half-lives Less than 30 Minutes
- Half-Lives between 30 min and 8 hr
- Half-Lives between 8 and 24 hr
- Half-Lives Greater than 24 hr
- Reinforcing the Principles
- ADDITIONAL CONSIDERATIONS
- Extravascular Administration
- Plasma Concentration versus Amount in Body
- DESIGN OF DOSAGE REGIMENS USING PLASMA CONCENTRATION
- When Bioavailability and Volume Are Unknown
- MODIFIED-RELEASE PRODUCTS
- EVALUATION OF A MULTIPLE-DOSE REGIMEN
- Clearance/Bioavailability
- Half-life
- Degree of Accumulation
- Degree of Fluctuation at Plateau
- Other Parameters
- PHARMACODYNAMIC CONSIDERATIONS
- Time to Achieve Therapeutic Effect
- Intermittent Administration
- Onset, Duration, and Intensity
- Development of Tolerance
- Modality of Administration
- WHEN ABSORPTION OR DISPOSITION IS ALTERED
- Sketch of Concentration–Time Profiles
- Model of Multiple Intravenous Doses
- Extravascular Administration
- Inhibition of Hepatic Metabolism (Condition A)
- Induction of Metabolism (Condition B)
- TRANSLATIONAL JUSTIFICATION FOR USING SINGLE DAILY DOSING OVER MORE FREQUENT ADMINISTRATION
- Other Situations
- STUDY PROBLEMS
- SECTION 4 INDIVIDUALIZATION
- CHAPTER 12 Variability
- EXPRESSIONS OF INDIVIDUAL DIFFERENCES
- Quantifying Variability
- Describing Variability
- POPULATION ANALYSIS
- MAXIMUM LIKELIHOOD APPROACH
- WHY PEOPLE DIFFER
- DEFINING THE DOSE–RESPONSE RELATIONSHIP
- THERAPEUTIC EXPOSURE
- KINETIC MANIFESTATIONS
- DYNAMIC MANIFESTATIONS
- DOSE STRENGTHS
- STUDY PROBLEMS
- CHAPTER 13 Genetics
- INHERITED VARIATION IN PHARMACOKINETICS
- Oxidation
- S-Methylation
- Conjugation
- Acetylation
- Hydrolysis
- Additional Clinical Considerations
- INHERITED VARIABILITY IN PHARMACODYNAMICS
- METABOLIC PHENOTYPING
- PHARMACOGENETICS-BASED THERAPEUTIC RECOMMENDATIONS
- STUDY PROBLEMS
- CHAPTER 14 Age, Weight, and Gender
- THE TYPICAL PATIENT AND USUAL DOSAGE REGIMEN
- Who Is the “Typical Patient”?
- What Is the “Usual Dosage Regimen”?
- PHARMACODYNAMICS
- PHARMACOKINETICS
- Absorption
- Disposition
- Body Weight and Composition
- Loading Dose
- Maintenance Dosing Rate
- CHANGE IN PHYSIOLOGIC FUNCTIONS AND DRUG DISPOSITION WITH AGE
- Creatinine Clearance and Renal Function
- Neonates and Infants
- Children
- Adults and the Elderly
- Metabolism
- Neonates and Infants
- Children
- Adults and the Elderly
- Entire Lifespan
- GENDER DIFFERENCES
- Pharmacokinetics
- Pharmacodynamics
- ADJUSTMENT OF DOSAGE FOR AGE
- Neonates and Infants
- Children
- Adults
- The Elderly
- DOSAGES EXPRESSED PER KILOGRAM BODY WEIGHT OR PER 1.73 SQUARE METERS
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 15 Disease
- IMPACT OF DISEASE ON PHARMACOKINETICS
- Hepatic Diseases
- Cardiovascular Diseases
- Renal Diseases
- The Pharmacotherapeutic Problem
- Decrease in Unbound Clearance
- Decrease in Binding to Plasma Proteins
- Estimation of Renal Function
- Adjustment of Dosage Regimens
- General Guidelines and Additional Considerations
- HEMODIALYSIS
- Dialysis Clearance
- Extraction from Blood
- Rate of Recovery in Dialysate
- Amount Recovered in Dialysate
- Extraction Coefficient
- Drug Elimination
- Effectiveness of Procedure
- DRUG ADMINISTRATION TO DIALYSIS PATIENTS
- PERITONEAL DIALYSIS
- Dialysis Clearance
- Route of Administration
- DIALYSIS IN DRUG OVERDOSE
- Toxic Metabolites
- Other Considerations
- IMPACT OF DISEASE ON PHARMACODYNAMICS
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 16 Nonlinearities
- DEFINITION OF NONLINEAR KINETIC BEHAVIOR
- CAUSES OF NONLINEARITY
- SATURABLE PROCESSES
- Saturable Metabolism
- Saturable Transport
- Saturable Binding to Plasma Proteins
- Pharmacodynamics
- NONLINEAR ABSORPTION
- Solubility
- Saturable Active Transport
- SATURABLE FIRST-PASS METABOLISM
- CAPACITY-LIMITED METABOLISM
- Alcohol
- Phenytoin
- Plateau
- Time to Plateau
- Alterations in Metabolism
- CONCENTRATION-DEPENDENT RENAL EXCRETION
- SATURABLE TRANSPORT
- SATURABILITY OF PLASMA PROTEIN AND TISSUE BINDING
- Binding to Plasma Proteins
- Tissue Binding
- TIME-DEPENDENT DISPOSITION
- RECOGNITION OF NONLINEARITIES
- Urinary Recovery
- Analysis
- Concentration–Time Profile
- Analysis
- Protein-Binding Data
- Analysis
- KINETICS IN DRUG OVERDOSE
- THERAPEUTIC CONSEQUENCES OF NONLINEARITIES
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 17 Drug Interactions
- CLASSIFICATION
- ALTERED ABSORPTION
- ALTERED DISTRIBUTION
- Conditions Favoring Displacement
- Therapeutic Implications
- Acute Events
- Events at Plateau
- Kinetic Features
- ALTERED CLEARANCE
- Inhibition
- Competitive Inhibition
- Mechanism-Based Inhibition
- Induction
- Other Causes of Altered Clearance
- MULTIFACETED INTERACTIONS
- Warfarin–Phenylbutazone Interaction
- Digoxin–Quinidine Interaction
- Atorvastatin–Rifampicin Interaction
- PHARMACODYNAMIC INTERACTIONS
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 18 Initiating and Managing Therapy
- ANTICIPATING SOURCES OF VARIABILITY
- Pharmacodynamic Variability
- Pharmacokinetic Variability
- INITIATING THERAPY
- Choosing the Starting Dose
- When Is a Loading Dose Needed?
- What Should the Loading Dose Be?
- Dose Titration
- MANAGING THERAPY
- Low Therapeutic Index
- Use of Biomarkers, Surrogates, and Clinical Endpoints
- Tolerance
- Dose Strengths and Stratification of Patients
- Adherence and Persistence Issues
- Missed Dose(s)
- “Makeup” Dose(s)
- Doubling Up of Doses
- DISCONTINUING THERAPY
- TARGET CONCENTRATION STRATEGY
- Criteria for Monitoring Plasma Drug Concentrations
- Good Concentration–Response Relationship
- High Probability of Therapeutic Failure
- When a Problem Arises
- Population Pharmacokinetic Information Available
- Reliable Assay
- Concentration Monitoring
- When Is It Useful?
- The Target Concentration
- Frequency of Monitoring
- Pertinent Information Needed
- Evaluation Procedure
- Dosing Scenarios
- Missed Dose(s)
- 9-13-17-21 Regimen
- Dose and Interval Unequal
- Confidence in Estimates
- Changes in Therapy
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- SECTION 5 SUPPLEMENTAL TOPICS
- CHAPTER 19 Distribution Kinetics
- EVIDENCE OF DISTRIBUTION KINETICS
- INTRAVENOUS BOLUS DOSE
- Presentation of Data
- Sum of Exponential Terms
- A Compartmental Model
- Pharmacokinetic Parameters
- Clearance
- Volume of Distribution
- Distribution Kinetics and Elimination
- A Mathematical Aid
- AN EXTRAVASCULAR DOSE
- CONSTANT-RATE INFUSION
- Short-Term Infusion
- Long-Term Infusion
- Events at Plateau
- Turnover of Endogenous Substances
- Time to Reach Plateau
- Bolus plus Infusion
- MULTIPLE DOSING AND REGIMEN DESIGN
- Absorption Kinetics
- Frequency of Dosing
- Utility of Volume Terms
- ALTERED CLEARANCE
- Changes in Concentration and Half-life
- DRUG REDISTRIBUTION
- PHARMACODYNAMIC CONSIDERATIONS
- Single Bolus Dose
- Multiple Dosing
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 20 Metabolites and Drug Response
- CONTRIBUTION OF METABOLITES TO DRUG RESPONSE
- SINGLE DOSE OF DRUG
- Rate-Limiting Step
- Plasma Concentration
- Impact of Hepatic Extraction
- CONSTANT-RATE DRUG INFUSION
- The Plateau
- Time to Plateau
- Bolus plus Infusion
- Infusion Alone
- Postinfusion
- MULTIPLE-DOSE DRUG REGIMEN
- PREDICTION FROM SINGLE-DOSE DATA
- VARIABILITY
- NONLINEAR METABOLITE FORMATION OR ELIMINATION
- ADDITIONAL CONSIDERATIONS
- Response
- Interconversion
- Estimation of Metabolite Formation
- From Plasma Metabolite Concentration
- From Metabolite Excretion
- Detection of Changes in Pharmacokinetics
- KEY RELATIONSHIPS
- STUDY PROBLEMS
- CHAPTER 21 Protein Drugs
- PEPTIDE, POLYPEPTIDE, AND PROTEIN DRUGS
- COMPARISON OF THE PHARMACOKINETICS OF PROTEIN DRUGS WITH THAT OF CONVENTIONAL NONPROTEIN DRUGS
- Absorption
- Distribution
- Renal Excretion
- Metabolism
- Fcγ-Mediated Clearance
- FcRn-Mediated Clearance
- NONLINEARITIES
- Target-Mediated Drug Disposition
- Immunogenicity-Mediated Clearance
- PHARMACODYNAMICS
- Pharmacodynamics of Nonantibody Protein Drugs
- Pharmacodynamics of Antibody Drugs
- Immunotoxicotherapeutic Agents
- Agents that Destroy Target Cells
- Agents that Alter Cell Function
- Antibody-Directed Drug Delivery
- Pharmacokinetic and Pharmacodynamic Rate Limitations
- INTRAVENOUS ADMINISTRATION
- SUBCUTANEOUS AND INTRAMUSCULAR ADMINISTRATION
- Large Proteins and Lymphatic Transport
- Capillary Permeability
- Molecular Size
- Rate and Extent of Systemic Absorption
- CONCURRENT DISEASE STATES
- Renal Disease
- Hepatic Disease
- IMMUNOGENIC RESPONSES
- FUTURE OF THE AREA
- STUDY PROBLEMS
- CHAPTER 22 Prediction and Refinement of Human Kinetics from In Vitro, Preclinical, and Early Clinical Data
- ALLOMETRY AND DISPOSITION KINETICS
- Origin
- Application to Drugs
- Deviation from Expectation
- Correcting for Protein Binding
- MICRODOSING
- PREDICTION OF CLEARANCE
- PREDICTION OF DISTRIBUTION
- PREDICTION OF ABSORPTION
- PHYSIOLOGICALLY BASED PHARMACOKINETIC MODELS
- Development and Verification of Physiologically Based Pharmacokinetic Models
- PREDICTING PHARMACODYNAMICS
- MOVING TO VIRTUAL PATIENT POPULATIONS
- APPENDICES
- APPENDIX A Assessment of AUC
- APPENDIX B Ionization and the pH Partition Hypothesis
- APPENDIX C Distribution of Drugs Extensively Bound to Plasma Proteins
- APPENDIX D Plasma-to-Blood Concentration Ratio
- APPENDIX E Well-Stirred Model of Hepatic Clearance
- APPENDIX F Absorption Kinetics
- APPENDIX G Wagner-Nelson Method
- APPENDIX H Mean Residence Time
- APPENDIX I Amount of Drug in Body on Accumulation to Plateau
- APPENDIX J Introduction to MS Excel Simulations
- APPENDIX K Answers to Study Problems
- Index