Pharmacokinetics : basics to applications / / Biswajit Mukherjee

• Record Nr.: UNINA9910743212503321
• Autore: Mukherjee Biswajit
• Pubbl/distr/stampa: Singapore : , : Springer Nature Singapore Pte Ltd., , [2022]; ©2022
• ISBN: 981-16-8949-0; 981-16-8950-4
• Descrizione fisica: 1 online resource (354 pages)
• Disciplina: 570.151
• Soggetti: Internal medicine; Biomathematics; Pharmaceutical chemistry
• Lingua di pubblicazione: Inglese
• Formato: Materiale a stampa
• Livello bibliografico: Monografia
• Nota di contenuto: Intro -- Preface -- Acknowledgment -- Contents -- About the Author -- List of Figures -- List of Tables -- 1: Fundamentals of Pharmacokinetics -- 1.1 Fundamentals of Pharmacokinetics -- 1.1.1 Pharmacokinetic Parameters and Blood Drug Profile -- 1.1.2 Multiple-Dose Regimen -- 1.1.3 Apparent Volume of Distribution or Volume of Distribution (vd) -- 1.1.4 Steady-State Plasma Concentration of Drug -- 1.1.5 Drug Accumulation Factor -- 1.1.6 Krüger-Thiemer´s ``Pharmacokinetic Factor´´ -- 1.1.7 Krüger-Thiemer Dose Ratio -- 1.1.8 Concept of a Loading Dose -- 1.1.9 Relationship Between Elimination Rate Constant (KE) and Steady-State Drug Plasma Concentration (css) from Krüger-Thiemer... -- References -- 2: Drug Absorption -- 2.1 Drug Absorption and Determination of Drug Absorption Rate Constant ``Ka´´ -- 2.1.1 Dominguez Equation and Its Importance -- 2.1.2 Wagner-Nelson Equation and Method of Determination of Drug Absorption Rate Constant -- 2.1.3 Determination of Absorption Rate Constant (Ka) from Urinary Excretion Data -- 2.1.4 Nelson Equation -- 2.1.5 Wagner and Nelson Equation -- 2.1.6 Loo-Riegelman Method for Determination of Drug Absorption Rate (Ka) -- 2.1.7 Method of Residual for Determination of Drug Absorption Rate -- 2.1.8 Flip-Flop Phenomenon -- References -- 3: ; Extent of Drug Absorption: Bioavailability, Clearance, Bioequivalence, and Protein Binding -- 3.1 Extent of Drug Absorption: Bioavailability -- 3.1.1 Renal Clearance -- 3.1.2 Determination of Absolute Bioavailability -- 3.1.3 Determination of Absolute Bioavailability by Urinary Excretion Data -- 3.1.4 Bioequivalence -- 3.1.4.1 Chemical Equivalents -- 3.1.4.2 Pharmaceutical Equivalents -- 3.1.4.3 Bioequivalents -- 3.1.4.4 Therapeutic Equivalence -- 3.1.4.5 Experimental Study Design in Bioequivalence -- 3.1.5 Drug-Protein Binding -- 3.1.6 Reciprocal Plot or Klotz Reciprocal Plot.; 3.1.7 Scatchard Plot -- 3.1.8 Sandberg Plot -- References -- 4: Pharmacokinetic Models and Drug Distribution -- 4.1 Various Pharmacokinetic Models and Drug Distribution -- 4.1.1 Physiological Pharmacokinetic Model (Flow Model) -- 4.1.2 Blood Flow-Limited Physiological Pharmacokinetic Model or Perfusion Model -- 4.1.3 Physiological Pharmacokinetic Model with Drug-Protein Binding -- 4.1.4 Membrane-Limited Model or Diffusion-Limited Model -- 4.1.5 Statistical Moment Theory -- 4.1.6 Compartment Models -- 4.1.6.1 One-Compartment Closed Model -- 4.1.6.2 One-Compartment Open Model -- 4.1.6.3 Catenary Model -- 4.1.6.4 Cyclic Model -- 4.1.6.5 Mammillary Model -- 4.1.7 Some Mathematical Approaches for Easy Computation of Compartmental Equations and Their Applications -- 4.1.7.1 Matrix and Determinant -- 4.1.7.1.1 Cramer´s Rule -- 4.1.7.2 Laplace Transform -- 4.1.7.3 Use of Logarithm and Antilogarithm Tables -- 4.1.7.4 Relationship Between Common and Natural Logarithms -- 4.1.8 Details About Compartment Models -- 4.1.9 Drug Distribution Study Through Compartmental Models -- 4.1.9.1 One-Compartment Open Model -- 4.1.9.1.1 Intravenously Bolus Dose -- 4.1.9.1.2 Intravenous Infusion -- 4.1.9.1.3 Following One-Compartment Model, Determination of Overall Elimination Rate During the Time t′ Elapsed After the Stop... -- 4.1.9.1.4 Following One-Compartment Model, Determination of the Overall Elimination Rate While an Infusion of a Drug to a Pati... -- 4.1.9.2 Two-Compartment Open Model -- 4.1.9.2.1 Method 1 (Simple Algebraic Method, Simultaneous Quadratic Equation) -- 4.1.9.2.2 By Matrix and Determinant Method -- 4.1.9.2.3 Drug Level in the Peripheral (Tissue) Compartment -- 4.1.9.3 Three-Compartment Open Model -- References -- 5: Drug Metabolism -- 5.1 Drug Metabolism -- 5.1.1 Hepatic Drug Metabolism -- 5.1.1.1 Phase I -- 5.1.1.2 Phase II Reaction.; 5.1.2 Pharmacokinetic Compartmental Models and Equations for Assessing Hepatic ``First-Pass´´ Effect of a Drug -- 5.1.2.1 Model I -- 5.1.2.2 Model II -- 5.1.2.3 Model III -- 5.1.2.4 Model IV -- 5.1.3 Hepatic First-Pass Effect Invariably Reduces Total Bioavailability of a Drug More When Administered Orally than By Its I... -- 5.1.4 Determination of Drug Metabolite Levels in Plasma Using Compartmental Model -- References -- 6: Drug Elimination and Nonlinear Kinetics -- 6.1 Drug Elimination -- 6.1.1 Nonlinear Kinetics and Capacity-Limited Process -- 6.1.2 Michaelis-Menten Equation -- 6.1.3 Capacity-Limited Process/Nonlinear Kinetics -- 6.1.4 Dose-Plasma Drug Concentration Relationship with Michaelis-Menten Constant Km for Drugs That Undergo Elimination Followi... -- 6.1.5 Drug Elimination by More Than One Capacity-Limited Process -- 6.1.6 Sigma-Minus Method to Determine Elimination Rate Constant -- 6.1.7 Bi-Exponential Absorption-Elimination Equation for Orally Administered Drugs Excreted Unchanged Through Urine -- 6.1.8 Excretion Rate Method -- References -- 7: Pharmacokinetic Drug-Drug Interactions -- 7.1 Pharmacokinetic Drug-Drug Interactions -- 7.1.1 Importance of Drug-Drug Interactions -- 7.1.1.1 Alteration of Plasma ; Drug Level -- 7.1.1.2 Drug-Related Side Effects or Toxic Effects -- 7.1.1.3 Deteriorative Existing Medical Conditions -- 7.1.2 Categories -- 7.1.3 Drug-Drug Interactions: Pharmacokinetic Type -- 7.1.3.1 Absorption -- 7.1.3.2 Distribution -- 7.1.3.3 Metabolism -- 7.1.3.4 Elimination -- 7.1.4 Drug-Drug Interactions: Pharmacodynamic Type -- 7.1.4.1 Involving Receptor Activities -- 7.1.4.2 Modulating Biological or Physiological Regulatory Function -- 7.1.4.3 Pharmacological Agonistic/Antagonistic Action -- 7.1.5 Data Collection -- References -- 8: Pharmacokinetic Applications -- 8.1 Therapeutic Drug Monitoring and Dose Formula.; 8.1.1 Therapeutic Drug Monitoring -- 8.1.1.1 Plasma -- 8.1.1.2 Serum -- 8.1.1.3 Required Sectors of Therapeutic Drug Monitoring -- 8.1.2 Physiological Effects on the Pharmacokinetic Drug Parameters and Available Dose Formula in Neonates, Infants, Children, ... -- 8.1.2.1 Pediatric Patients -- 8.1.2.2 Absorption -- 8.1.2.3 Distribution -- 8.1.2.4 Metabolism -- 8.1.2.5 Elimination -- 8.1.2.6 Mosteller´s Equation -- 8.1.2.7 Clark´s Formula -- 8.1.2.8 Fried´s Rule for Infants -- 8.1.2.9 Cowling´s Formula -- 8.1.3 Physiological Effects on the Pharmacokinetic Parameters of Drugs and Available Dose Formula in Elderly or Geriatric Pati... -- 8.1.3.1 Absorption -- 8.1.3.2 Distribution -- 8.1.3.3 Metabolism -- 8.1.3.4 Elimination -- 8.1.3.5 Dose Calculation of Elderly Patients -- 8.1.4 Physiological Effects on the Pharmacokinetic Parameters of Drugs in Obese Patients -- 8.1.5 Physiological Effects on the Pharmacokinetic Parameters of Drugs and Available Dose Formula in Patients with Renal Insuf... -- 8.1.6 Chronological Pharmacokinetic Guidance for Preclinical and Clinical Studies and Research -- 8.1.6.1 Study Design -- 8.1.6.1.1 Group Design -- For Preclinical Investigation -- For Clinical Investigation -- Controlled TrialControlled Trial -- RandomizationRandomization -- Blinding (Masking) ProcessBlinding (Masking) Process -- Cohort StudyCohort Study -- 8.1.6.1.2 Sample Type -- 8.1.6.1.3 Sample Size -- 8.1.6.1.4 Route of Administration -- 8.1.6.1.5 Mode of Drug Administration -- 8.1.6.1.6 Scheduling of Drug Administration -- 8.1.6.1.7 Time Points of Sampling -- 8.1.6.1.8 Endpoints -- 8.1.6.1.9 Parameters to Be Analyzed -- 8.1.6.1.10 Method of Analysis -- 8.1.6.1.11 Statistical Analysis -- 8.1.7 Analysis of Pharmacokinetic Data -- 8.1.7.1 Data Handling -- 8.1.7.2 Data Editing -- 8.1.7.3 Outliers -- 8.1.7.4 Analysis of Pharmacokinetic Data.; 8.1.7.4.1 Noncompartmental Data Analysis -- Compartmental Data Analysis -- Model Selection -- Initial Estimates -- Selection of Minimizing Algorithm -- Choice of Weight -- Assessing Goodness of Fit -- Distinction Between the Models -- 8.1.7.4.2 Physiological Pharmacokinetic Model -- 8.1.7.4.3 Pharmacokinetic/Pharmacodynamic Model -- 8.1.7.4.4 Population-Based Pharmacokinetic Data Analysis -- 8.1.7.4.5 Nonlinear Mixed Effect Modeling Approach -- 8.1.7.5 Pharmacokinetic Report -- References -- 9: Pharmacokinetic Sample Collection and Processing -- 9.1 Pharmacokinetic Sample Collection and Processing for Preclinical and Clinical Experiments -- 9.1.1 Pharmacokinetic Sampling -- 9.1.2 Blood Sampling and Right Practices in Phlebotomy -- 9.1.2.1 Processing of Blood Samples -- 9.1.2.2 Blood Collections from Small Animals -- 9.1.3 Urine Specimen -- 9.1.4 Other Tissue Samples -- 9.1.5 Other Tissue Fluids -- 9.1.6 Processing of Fecal Samples -- 9.1.7 Extraction of Drug/Drug Metabolite from Biological Samples -- References -- 10: Important Bioanalytical Instrumental Techniques in Pharmacokinetics -- 10.1 Important Bioanalytical Instrumental Techniques -- 10.1.1 Liquid Chromatography with Tandem Mass Spectroscopy (LC-MS/MS) -- 10.1.1.1 Working Principle -- 10.1.1.2 ; Components and Their Applications -- 10.1.1.2.1 Liquid Chromatography Part -- 10.1.1.2.2 Sample Injector -- 10.1.1.2.3 Pump Device -- Direct Gas-Pressure System -- Syringe Pump -- Pneumatic Intensifier -- Reciprocating Pump -- 10.1.1.2.4 Interface -- 10.1.1.2.5 Atmospheric Pressure Ionization Technique -- 10.1.1.2.6 Electrospray Ionization Collision-Induced Dissociation -- 10.1.1.2.7 MS/MS System -- Quadrupole Assembly -- Mass Spectra Detectors -- 10.1.1.3 LC-MS/MS Method Optimization -- 10.1.1.3.1 Standard Solution -- 10.1.1.3.2 Optimization of MS/MS Operation and Parameters.; 10.1.1.3.3 Energy Optimization for Parent Ion Ionization.