Pharmacokinetics of drugs: [with 51 tables]
Gespeichert in:
| Format: | Buch |
|---|---|
| Sprache: | English |
| Veröffentlicht: |
Berlin [u.a.]
Springer
1994
|
| Schriftenreihe: | Handbook of experimental pharmacology
110 |
| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | Literaturangaben |
| Beschreibung: | XXVI, 537 S. Ill., graph. Darst. |
| ISBN: | 3540575065 0387575065 |
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| 245 | 1 | 0 | |a Pharmacokinetics of drugs |b [with 51 tables] |c contributors G. L. Amidon ... Ed. Peter G. Welling ... |
| 264 | 1 | |a Berlin [u.a.] |b Springer |c 1994 | |
| 300 | |a XXVI, 537 S. |b Ill., graph. Darst. | ||
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| 490 | 1 | |a Handbook of experimental pharmacology |v 110 | |
| 500 | |a Literaturangaben | ||
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| 650 | 7 | |a Farmacokinetica |2 gtt | |
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Datensatz im Suchindex
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| adam_text | CS X . PHARMACOKINETICS OF DRUGS CONTRIBUTORS G.L. AMIDON, J.P.F. BAI,
L.P. BALANT, CM. BARKSDALE, I.A. BLAIR D.D. BREIMER, M. CHIBA, J.
DELFORGE, M. EICHELBAUM B.L. FERRAIOLO, A.J. FISCHMAN, M. GEX-FABRY, N.
HOLFORD J. KANTROWITZ, H.K. KROEMER, T.M. LUDDEN, J.M. MAYER B. MAZIERE,
C. MCMARTIN, G. MIKUS, M.A. MOHLER G.D. NORDBLOM, R. O NEILL, K.S. PANG,
O. PELKONEN A. RACINE-POON, R.H. RUBIN, J.-L. STEIMER, B.H. STEWART H.W.
STRAUSS, B. TESTA, S. VOZEH, P.G. WELLING, R.J. WILLS A. YACOBI EDITORS
PETER G. WELLING AND LUC P. BALANT WITH A FOREWORD BY J.G. WAGNER (52
SPRINGER-VERLAG BERLIN HEIDELBERG NEW YORK LONDON PARIS TOKYO HONG KONG
BARCELONA BUDAPEST 2.T. CONTENTS A. INTRODUCTION CHAPTER 1 OF
PHARMACOKINETICS IN DRUG DISCOVERY AND DEVELOPMENT P.G. WELLING. WITH 3
FIGURES 3 A. HISTORICAL BACKGROUND 3 B. REGULATORY SUBMISSIONS 4 C. THE
PROCESS 4 D. DISCOVERY 5 E. PRECLINICAL DEVELOPMENT 6 I. TOXICOLOGY AND
TOXICOKINETICS 8 II. PHARMACOKINETIC-PHARMACODYNAMIC RELATIONSHIPS 10
III. INTERACTIONS 11 F. CLINICAL DEVELOPMENT 11 I. PHASE 1 : 11 II.
PHASE 2 13 III. PHASE 3 15 IV. INTERACTIONS 16 V. REGULATORY SUBMISSIONS
16 G. POSTSUBMISSION AND POSTMARKETING STUDIES 17 H. SUMMARY 18
REFERENCES 18 B. ANALYTICAL METHODS CHAPTER 2 CONTEMPORARY ASPECTS OF
RADIOIMMUNOASSAY DEVELOPMENT FOR DRUG ANALYSIS G.D. NORDBLOM AND CM.
BARKSDALE. WITH 2 FIGURES 23 A. INTRODUCTION 23 B. SYNTHESIS OF DRUG
DERIVATIVES FOR IMMUNOGEN PREPARATION 24 XIV CONTENTS I. COUPLING OF
HAPTEN CARBOXYL GROUP TO CARRIER PROTEIN 24 II. ADDITION OF CARBOXYL TO
EXISTING FUNCTIONAL GROUP 24 III. ADDITION OF A FUNCTIONAL GROUP FOR
BRIDGE TO CARBOXYLIC ACID 25 IV. ALTERING THE BASIC STRUCTURE OF THE
HAPTEN 26 C. IMMUNOGEN PREPARATION 26 I. HAPTEN-CARRIER PROTEIN RATIOS
26 II. CARRIER PROTEIN CHARACTERISTICS 28 D. IMMUNIZATION CONSIDERATIONS
29 I. SPECIES EFFECTS 29 II. USE OF ADJUVANTS 29 III. IMMUNIZATION SITES
AND SCHEDULES 30 E. MATRIX EFFECTS OF BIOLOGICAL FLUIDS 31 I. METHODS
FOR SAMPLE MATRIX EFFECT ELIMINATION 32 1. FILTRATION/PRECIPITATION OF
PROTEIN 32 2. SOLVENT EXTRACTION 32 3. SOLID PHASE CHROMATOGRAPHIC
EXTRACTION 33 4. HIGH-PERFORMANCE LIQUID CHROMATOGRAPHIC SAMPLE
PREPARATION 33 II. ELIMINATION OF SAMPLE MATRIX EFFECT BY SAMPLE SIZE 34
F. THE SUITABILITY OF RADIOIMMUNOASSAY FOR DRUG ANALYSIS 35 REFERENCES
37 CHAPTER 3 MASS SPECTROMETRY IN DRUG DISPOSITION AND PHARMACOKINETICS
LA. BLAIR 41 A. INTRODUCTION 41 B. IONIZATION TECHNIQUES 42 I. ELECTRON
IONIZATION 42 II. POSITIVE CHEMICAL IONIZATION 43 III. ELECTRON CAPTURE
NEGATIVE CHEMICAL IONIZATION 43 IV. LIQUID SECONDARY ION/FAST ATOM
BOMBARDMENT 44 V. THERMOSPRAY 46 VI. ATMOSPHERIC PRESSURE IONIZATION 47
VII. COLLISION-INDUCED DISSOCIATION 49 C. CHROMATOGRAPHIC TECHNIQUES 51
I. GAS CHROMATOGRAPHY/MASS SPECTROMETRY 51 II. LIQUID
CHROMATOGRAPHY/MASS SPECTROMETRY 54 D. METABOLISM STUDIES 57 I. IN VITRO
STUDIES 57 II. IN VIVO STUDIES IN ANIMAL MODELS 59 III. IN VIVO STUDIES
IN HUMANS 62 E. PHARMACOKINETIC STUDIES 64 CONTENTS XV I. INTRODUCTION
64 II. ANIMAL MODELS 65 III. HUMANS 65 F. SUMMARY 68 REFERENCES 69
CHAPTER 4 ANALYTICAL METHODS FOR BIOTECHNOLOGY PRODUCTS B.L. FERRAIOLO
AND M.A. MOHLER 85. A. INTRODUCTION 85 B. METHODS 85 I. RADIOLABELS 85
1. SELECTION OF RADIOLABEL 85 2. WHOLE-BODY AUTORADIOGRAPHY 86 3.
RADIOLABEL REALITIES 86 II. IMMUNOASSAYS 88 1. ENZYME IMMUNOASSAYS 89 2.
RADIOLABEL-BASED IMMUNOASSAYS 89 3. IMMUNOASSAY LIMITATIONS 89 4.
IMMUNOASSAY INTERFERENCES 90 III. BIOASSAYS 91 IV. OTHER IMMUNOLOGICAL
TECHNIQUES 92 V. CHROMATOGRAPHY 92 VI. ELECTROPHORETIC TECHNIQUES 93
VII. MASS SPECTROMETRY 93 C. CONCLUSIONS 94 REFERENCES 94 C. IN VITRO
METHODS-PROTEIN AND TISSUE BINDING CHAPTER 5 METABOLISM: SCALING-UP FROM
IN VITRO TO ORGAN AND WHOLE BODY K.S. PANG AND M. CHIBA. WITH 15 FIGURES
101 A. INTRODUCTION 101 B. CORRELATION OF IN VITRO AND IN VIVO DATA 102
I. CONCEPT OF ORGAN CLEARANCE 102 1. HEPATIC CLEARANCE MODELS 104 2. IN
VITRO-ORGAN CORRELATIONS 110 II. CONCEPT OF TOTAL BODY CLEARANCE ILL 1.
FROM IN VITRO TO IN VIVO: COMPARTMENTAL MODELING 124 2. FROM IN VITRO TO
IN VIVO: PHYSIOLOGICAL MODELING 125 3. FROM PERFUSED ORGANS TO IN VIVO
128 XVI CONTENTS C. POOR CORRELATIONS BETWEEN IN VITRO AND PERFUSED
ORGANS 132 I. INADEQUACY OF IN VITRO ESTIMATES 132 1. ESTIMATION OF
ENZYMATIC PARAMETERS 132 2. MULTIPLICITY OF ENZYMES 136 3.
MEMBRANE-BOUND ENZYMES 137 4. TIME-DEPENDENT KINETICS 138 II. STRUCTURAL
CONSIDERATIONS AND PHYSIOLOGICAL VARIABLES 140 1. FLOW 144 2. PROTEIN
BINDING 145 3. TRANSMEMBRANE LIMITATION 150 4. COSUBSTRATE 151 5. ACINAR
HETEROGENEITY 153 D. REASONS FOR POOR CORRELATIONS BETWEEN IN VITRO,
PERFUSED ORGANS, AND IN VIVO 160 E. CONCLUSIONS 161 REFERENCES 162
CHAPTER 6 GASTROINTESTINAL TRANSPORT OF PEPTIDE AND PROTEIN DRUGS AND
PRODRUGS J.P.F. BAI, B.H. STEWART, AND G.L. AMIDON. WITH 7 FIGURES 189
A. INTRODUCTION 189 B. MUCOSAL CELL ABSORPTION 190 I. PARACELLULAR
ABSORPTION 190 II. TRANSCELLULAR ABSORPTION 190 1. SIMPLE DIFFUSION 190
2. CARRIER-MEDIATED PROCESS 191 3. ENDOCYTOSIS 191 C. MUCOSAL CELL
TRANSPORT OF PEPTIDE DRUGS 192 I. CHARACTERISTICS OF SMALL PEPTIDE
TRANSPORT 192 1. SUBSTRATE STRUCTURAL REQUIREMENTS 192 II.
CARRIER-MEDIATED TRANSPORT OF PEPTIDE DRUGS 193 1. Y5-LACTAM ANTIBIOTICS
193 2. ACE INHIBITORS 195 D. ESTIMATING EXTENT OF DRUG ABSORPTION 195 I.
FRACTION OF DOSE ABSORBED-PERMEABILITY CORRELATION 195 II. COMPARISON OF
PASSIVE AND CARRIER-MEDIATED TRANSPORT 196 E. PEPTIDE PRODRUG APPROACHES
TO IMPROVING INTESTINAL ABSORPTION 198 I. PEPTIDE PRODRUGS OF
A-METHYLDOPA 198 II. PEPTIDE PRODRUG APPROACHES FOR ACIDIC DRUGS 199
III. OTHER PEPTIDE PRODRUGS 202 F. SUMMARY 203 REFERENCES 203 CONTENTS
XVII D. CLASSICAL PROBLEMS CHAPTER 7 V STEREOSELECTIVITY IN METABOLIC
REACTIONS OF TOXICATION AND DETOXICATION J.M. MAYER AND B. TESTA. WITH 8
FIGURES 209 A. INTRODUCTION 209 B. PRINCIPLES OF STEREOSELECTIVE
XENOBIOTIC METABOLISM 210 I. CHIRAL RECOGNITION AND STEREOSELECTIVE
PROCESSES IN XENOBIOTIC METABOLISM AND DISPOSITION 210 II. SUBSTRATE
STEREOSELECTIVITY AND PRODUCT STEREOSELECTIVITY .... 211 III.
SUBSTRATE-PRODUCT STEREOSELECTIVITY 212 IV. RELEVANCE TO MOLECULAR
TOXICOLOGY 212 C. TOXICOLOGICALLY RELEVANT EXAMPLES OF STEREOSELECTIVE
METABOLISM 213 I. INTRODUCTION 213 II. SUBSTRATE STEREOSELECTIVITY IN
DRUG OXIDATION: DISOPYRAMIDE AND MIANSERIN 213 III. PRODUCT
STEREOSELECTIVITY IN DRUG OXIDATION AND REDUCTION: PHENYTOIN AND
NABILONE 219 IV. SUBSTRATE STEREOSELECTIVITY IN XENOBIOTIC CONJUGATION:
FENVALERATE 220 D. THE CASE OF PROFENS 220 I. METABOLIC CHIRAL
INVERSION: IN VIVO AND IN VITRO STUDIES.... 220 II. MECHANISM OF
INVERSION 224 III. TOXICOLOGICAL CONSEQUENCES OF CHIRAL INVERSION 226 E.
CONCLUSION 227 REFERENCES 228 CHAPTER 8 Y INTERETHNIC DIFFERENCES IN
DRUG DISPOSITION AND RESPONSE: RELEVANCE FOR DRUG DEVELOPMENT,
LICENSING, AND REGISTRATION L.P. BALANT AND P.G. WELLING 233 A.
INTRODUCTION 233 B. CASE REPORTS 234 I. UNEXPECTED BEHAVIOR 234 II. A
BIOPHARMACEUTICAL DILEMMA 234 III. THE DRUG WHICH DID NOT BECOME A CASE
235 IV. THE DRUG WHICH IS NOT A CASE 237 C. BASIC CONCEPTS AND
DEFINITIONS 237 D. INTEGRATION OF PHARMACOKINETIC, PHARMACODYNAMIC, AND
TOXICOKINETIC PRINCIPLES IN DRUG DEVELOPMENT 240 XVIII CONTENTS I. THE
CONCEPTUAL FRAMEWORK 240 II. PRECLINICAL STUDIES 241 III. PHASE 1
STUDIES 241 IV. PHASE 2 STUDIES 242 V. PHASE 3 CLINICAL STUDIES 242 VI.
REGULATORY CONSIDERATIONS 244 VII. INTERETHNIC DIFFERENCES IN DRUG
BEHAVIOR AND ACTION AND PK/PD INTEGRATION 244 E. PRECLINICAL STUDIES 245
F. PHASE 1 STUDIES AND INTERETHNIC DIFFERENCES 246 I. INVESTIGATIONAL
PHARMACOKINETICS 246 II. INVESTIGATIONAL PHARMACODYNAMICS 248 III.
BIOAVAILABILITY INVESTIGATIONS 249 IV. BIOEQUIVALENCE STUDIES 250 G.
PHASE 2 STUDIES 250 H. PHASE 3 STUDIES 251 I. PHASE 4 STUDIES IN THE
CONTEXT OF DRUG PRODUCT LICENSING 251 I. PHARMACOANTHROPOLOGICAL
CONSIDERATIONS 252 II. STUDIES IN HEALTHY VOLUNTEERS 253 III. STUDIES IN
PATIENTS 253 J. CONCLUSIONS 254 REFERENCES 255 APPENDIX. SELECTED
REFERENCES ON INTERETHNIC DIFFERENCES IN DRUG KINETICS . .* 257 CHAPTER
9 CLINICAL RELEVANCE OF PHARMACOGENETICS H.K. KROEMER, G. MIKUS, AND M.
EICHELBAUM 265 A. INTRODUCTION 265 B. THE GENETIC POLYMORPHISM OF THE
SPARTEINE/DEBRISOQUINE OXIDATION 269 I. MOLECULAR MECHANISMS OF THE
SPARTEINE/DEBRISOQUINE POLYMORPHISM 270 II. CLINICAL CONSEQUENCES OF THE
SPARTEINE/DEBRISOQUINE POLYMORPHISM AND ASSIGNMENT OF GENOTYPE OR
PHENOTYPE .. . 271 C. THE GENETIC POLYMORPHISM OF MEPHENYTOIN OXIDATION
273 I. MOLECULAR MECHANISMS OF THE MEPHENYTOIN POLYMORPHISM ... 274 II.
CLINICAL CONSEQUENCES OF POLYMORPHIC MEPHENYTOIN OXIDATION AND
ASSIGNMENT OF GENOTYPE OR PHENOTYPE 275 D. THE GENETIC POLYMORPHISM OF
N-ACETYLATION 277 I. MOLECULAR MECHANISMS OF POLYMORPHIC N-ACETYLATION
277 II. CLINICAL CONSEQUENCES OF POLYMORPHIC ACETYLATION AND ASSIGNMENT
OF GENOTYPE OR PHENOTYPE 278 CONTENTS XIX E. GENETIC POLYMORPHISMS AND
DRUG DEVELOPMENT 279 F. GENETIC POLYMORPHISMS AND DRUG INTERACTIONS 280
G. CONCLUSIONS 281 REFERENCES 281 CHAPTER 10 ROLE OF ENVIRONMENTAL
FACTORS IN THE PHARMACOKINETICS OF DRUGS: CONSIDERATIONS WITH RESPECT TO
ANIMAL MODELS, P-450 ENZYMES, AND PROBE DRUGS O. PELKONEN AND D.D.
BREIMER. WITH 2 FIGURES 289 A. INTRODUCTION 289 B. RELEVANT
ENVIRONMENTAL FACTORS 290 I. WHAT ARE RELEVANT ENVIRONMENTAL FACTORS?
290 II. EXAMPLES 293 1. CIGARETTE SMOKING 293 2. ALCOHOL DRINKING 294 3.
DRUGS 294 4. OCCUPATIONAL CHEMICALS 294 5. OTHER FACTORS 295 C. ANIMAL
MODELS 295 I. ENVIRONMENTAL REGULATION OF P-450 ISOFORMS IN THE RAT 298
II. SIMILARITIES AND DIFFERENCES BETWEEN SPECIES 298 III. REASONS FOR
INTERSPECIES DIFFERENCES 299 IV. MODEL EXPERIMENTS IN ANIMALS 300 D.
IMPORTANT (ISO)ENZYMES IN MAN 300 I. P-450 ENZYMES 300 1. P-450 1A1 303
2. P-450 1A2 304 3. P-450 2A6 305 4. P-450 2B6 305 5. P-450 2C 305 6.
P-450 2D6 306 7. P-450 2E1 306 8. P-450 3A 307 II. CONJUGATIVE ENZYMES
308 III. HETEROLOGOUS EXPRESSION SYSTEMS 308 E. PROBE DRUGS 309 I. THE
PROBE DRUG CONCEPT 309 1. THE IDEAL PROBE DRUG 309 2. GENERAL VS
SPECIFIC PROBE DRUGS :... 310 II. IMPORTANCE OF ENZYME SPECIFICITY 310
III. SELECTED PROBE DRUGS 311 1. ANTIPYRINE 311 XX CONTENTS 2.
AMINOPYRINE 312 3. CAFFEINE 312 4. THEOPHYLLINE 313 5. NIFEDIPINE 314 6.
BARBITURATES 314 7. TOLBUTAMIDE 315 8. WARFARIN 315 9. OTHER POTENTIAL
PROBES 316 10. ENDOGENOUS PROBES 317 IV. COCKTAIL APPROACH 317 F.
PRACTICAL CONSIDERATIONS FOR HUMAN STUDIES 318 G. FINAL CONSIDERATIONS
319 REFERENCES 320 CHAPTER 11 TIME COURSE OF DRUG EFFECT N.H.G. HOLFORD
AND T.M. LUDDEN 333 A. INTRODUCTION 333 I. WHY PREDICTION OF EFFECT OVER
TIME IS IMPORTANT 334 1. DRUG DEVELOPMENT 334 2. DOSAGE
INDIVIDUALIZATION 335 B. METHODOLOGICAL CONSIDERATIONS RELEVANT TO
MEASURING EFFECTS ... 336 I. STANDARDIZATION 336 II. CONTINUOUS SCALE
VERSUS DISCRETE RESPONSE 337 III. BASELINE AND PLACEBO EFFECT 338 C.
PHARMACOKINETIC-PHARMACODYNAMIC MODELS 338 I. PHARMACOKINETICS 338 II.
KIETICS OF RECEPTOR BINDING 338 III. STEADY-STATE PHARMACODYNAMIC MODELS
339 IV. NON-STEADY-STATE PHARMACODYNAMIC MODELS 340 1. EFFECT
COMPARTMENT 340 2. PHYSIOLOGICAL MEDIATOR 341 V. PLACEBO EFFECT 343 1.
PHARMACOKINETICS 343 2. PLACEBO EFFECT MODEL 343 3. PLACEBO EFFICACY 344
VI. DISEASE TIME COURSE AND DRUG EFFECTS 344 1. DISEASE TIME COURSE 344
2. MODELS OF DRUG EFFECT ON DISEASE PROGRESSION 345 VII. TOLERANCE 346
1. PHARMACOKINETICS 346 2. PHARMACODYNAMICS 348 D. CONCLUSION 349
REFERENCES 350 CONTENTS XXI E. FUTURE TRENDS IN PHARMACOKINETICS CHAPTER
12 BIOTECHNOLOGY PRODUCTS B.L. FERRAIOLO, R.J. WILLS, AND M.A. MOHLER
355 A. INTRODUCTION 355 B. PHARMACOKINETIC/PHARMACODYNAMIC STUDIES 355
I. OLIGONUCLEOTIDES 355 II. PROTEINS 357 1. INSULIN 358 2. RELAXIN 358
3. INTERFERON-A-2A 358 C. REGIMEN-DEPENDENT EFFECTS 359 I. GROWTH
HORMONE 359 II. PARATHYROID HORMONE 359 III. TISSUE PLASMINOGEN
ACTIVATOR 359 D. BINDING PROTEINS/INHIBITORS 360 I. GROWTH HORMONE 360
II. TISSUE PLASMINOGEN ACTIVATOR 361 III. INSULIN-LIKE GROWTH FACTOR-I
361 IV. DEOXYRIBONUCLEASE 361 E. CATABOLISM OF BIOTECHNOLOGY PRODUCTS
362 I. CATABOLISM AT EXTRAVASCULAR SITES OF ADMINISTRATION 362 F. DRUG
INTERACTIONS 363 REFERENCES 364 CHAPTER 13 PEPTIDE AND PROTEIN DRUGS C.
MCMARTIN. WITH 2 FIGURES 371 A. INTRODUCTION 371 I. DIFFERENCES BETWEEN
THE PHARMACOKINETICS OF PEPTIDES/ PROTEINS AND OTHER DRUGS 371 II. SCOPE
OF THIS REVIEW 374 B. PHARMACOKINETIC MECHANISMS 374 I. DISTRIBUTION IN
THE BODY 374 II. INACTIVATION AND ELIMINATION 375 1. GLOMERULAR
FILTRATION 375 2. PEPTIDOLYSIS 375 3. RECEPTOR-MEDIATED CLEARANCE 375
III. UPTAKE FROM SITE OF ADMINISTRATION 375 1. SUBCUTANEOUS OR
INTRAMUSCULAR INJECTION 376 2. INTRANASAL ADMINISTRATION 376 3. ORAL OR
RECTAL ADMINISTRATION 376 XXII CONTENTS IV. PHARMACOKINETIC BEHAVIOR
RESULTING FROM THE DISTRIBUTION AND ELIMINATION PROCESSES 376 C.
EXPERIMENTAL APPROACHES 376 I. ANALYTICAL METHODS 377 1. EX VIVO
BIOASSAY 377 2. RADIOIMMUNOASSAY 377 3. RADIOLABELING 377 4.
HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY 377 5. RADIOSEQUENCING 378 II.
PLASMA PHARMACOKINETICS 378 1. INTRAVENOUS BOLUS AND INFUSION STUDIES
378 2. METHODS OF ASSAYING SAMPLES 378 3. INFORMATION THAT CAN BE
DERIVED FROM PLASMA PHARMACOKINETIC STUDIES 378 4. USE OF ORGAN ABLATION
TO LOCATE CLEARANCE SITES 378 III. DISTRIBUTION, METABOLISM, AND
ELIMINATION 379 1. TYPICAL EXPERIMENTS AND RESULTS 379 2. DIFFICULTIES
IN INTERPRETING RESULTS 379 3. PROBLEMS IN CARRYING OUT DRUG ELIMINATION
STUDIES 379 IV. ORGAN CLEARANCE 380 V. RECEPTOR-MEDIATED CLEARANCE
KINETICS 380 VI. ABSORPTION (BIOAVAILABILITY) MEASUREMENT 380 1. ORAL
ROUTE 380 2. NASAL ROUTE 381 D. CONCLUSIONS 381 REFERENCES 381 CHAPTER
14 TOXICOKINETICS J. KANTROWITZ AND A. YACOBI. WITH 7 FIGURES 383 A.
INTRODUCTION 383 B. PRINCIPLES OF TOXICOKINETICS 383 C. BIOANALYTICAL
PROCEDURES TO SUPPORT TOXICOKINETIC STUDIES 385 D. DOSE-PLASMA
CONCENTRATION RELATIONSHIP (LINEAR-NONLINEAR KINETICS) 386 E. CHANGES IN
CONCENTRATIONS UPON MULTIPLE DOSING 392 F. DESIGNING TROUBLESHOOTING
STUDIES TO EXPLAIN ABERRANT DATA ... 395 I. ABSORPTION ISSUES 395 1.
DOSE PROPORTIONALITY 395 2. EFFECT OF DIET 396 3. EFFECT OF VEHICLES 396
II. METABOLISM ISSUES 396 1. ENZYME INDUCTION 396 CONTENTS XXIII 2.
EFFECT OF AGE 397 3. SEX DEPENDENCY 399 G. SPECIES COMPARISONS AND
INTERSPECIES (ALLOMETRIC) SCALING 399 H. UTILIZATION OF
PHARMACOKINETIC/TOXICOKINETIC DATA IN THE DESIGN OF EARLY CLINICAL
TRIALS 402 REFERENCES 403 CHAPTER 15 THE POPULATION APPROACH: RATIONALE,
METHODS, AND APPLICATIONS IN CLINICAL PHARMACOLOGY AND DRUG DEVELOPMENT
J.-L. STEIMER, S. VOZEH, A. RACINE-POON, N. HOLFORD, AND R. O NEILL.
WITH 8 FIGURES 405 A. INTRODUCTION 405 B. RATIONALE 406 I. POPULATION
STUDIES IN LARGE SAMPLES OF SUBJECTS 407 II. CONTROLLED EXPERIMENTAL
STUDIES IN SMALL GROUPS 409 III. THE POPULATION APPROACH 412 C. AN
OVERVIEW OF STATISTICAL METHODOLOGY FOR MODEL-BASED POPULATION ANALYSIS
414 I. POPULATION MODEL 414 II. POPULATION METHODS FOR DATA ANALYSIS 417
III. SYNTHESIS 418 D. CURRENT EXPERIENCE WITH THE POPULATION APPROACH
AND ITS APPLICATIONS TO DRUG THERAPY 419 I. INTRODUCTION 419 II.
DETECTION OF PATIENT GROUPS WITH ALTERED KINETICS 419 III. DESIGN OF
OPTIMUM A PRIORI DOSAGE REGIMEN 424 IV. BAYESIAN ESTIMATION OF
INDIVIDUAL PHARMACOKINETIC PARAMETERS 426 V. RECENT NOVEL APPLICATIONS
OF NONLINEAR MIXED EFFECTS MODELS TO OTHER DRUG-RELATED AREAS 427 E.
PROBLEMS AND ISSUES? 431 I. MISCONCEPTIONS 431 II. SOME PRACTICAL
PROBLEMS 432 1. RELIABILITY OF DATA AND ANALYSIS 432 2. METHODOLOGICAL
ISSUES 433 III. VALIDATION OF THE RESULTS 435 F. INTEGRATION OF THE
POPULATION APPROACH INTO CLINICAL DRUG DEVELOPMENT 437 I. INTRODUCTION
437 II. EARLY HUMAN STUDIES (PHASE I) 438 III. EARLY CLINICAL STUDIES
(PHASE II) 438 IV. CLINICAL TRIALS (LATE PHASE II, PHASE III) 439 XXIV
CONTENTS V. LATE CLINICAL TRIALS (LATE PHASE III, PHASE IV) 441 G.
CONCLUDING REMARKS 441 REFERENCES 443 F. IMPACT OF NEW METHODS ON
PHARMACOKINETICS CHAPTER 16 CONTRIBUTION OF POSITRON EMISSION TOMOGRAPHY
TO PHARMACOKINETIC STUDIES B. MAZIERE AND J. DELFORGE. WITH 7 FIGURES
455 A. INTRODUCTION 455 B. POSITRON EMITTERS 456 C. DRUG LABELING -
RADIOCHEMISTRY 456 D. POSITRON EMISSION TOMOGRAPHY 457 E. DIRECT
RADIOLABELED DRUG STUDIES 459 I. DRUG DISTRIBUTION 459 II. DRUG-DRUG AND
DRUG-NUTRIENT INTERACTIONS 460 III. DRUG-RECEPTOR INTERACTIONS 461 1.
TRANQUILIZERS 464 2. NEUROLEPTICS 464 F. INDIRECT RADIOACTIVE
PHARMACOKINETIC STUDIES 465 G. KINETIC MODELING WITH PET 467 I. A
TWO-COMPARTMENT MODEL: THE [ 15 O] WATER MODEL 468 II. A
THREE-COMPARTMENT LINEAR MODEL: THE [ 18 F] FLUORO- DEOXYGLUCOSE MODEL
469 HI. A MULTICOMPARTMENT NONLINEAR MODEL: THE LIGAND- RECEPTOR MODEL
470 IV. MODELING USING SIMPLIFIED MODELS 472 V. MODELING USING THE
MULTI-INJECTION APPROACH 474 H. CONCLUSION 474 REFERENCES 475 CHAPTER 17
IN VIVO IMAGING IN DRUG DISCOVERY AND DESIGN A.J. FISCHMAN, R.H. RUBIN,
AND H.W. STRAUSS. WITH 8 FIGURES .... 481 A. INTRODUCTION 481 B.
PHARMACOKINETICS 482 I. ANTIMICROBIAL AGENTS 485 1. ERYTHROMYCIN 485 2.
FLUCONAZOLE 486 II. ANTINEOPLASTIC AGENTS 488 CONTENTS XXV 1. PLATINUM
COMPOUNDS 488 2. 5-FLUOROURACIL 489 III. NEUROLEPTICS 489 IV.
ANGIOTENSIN-CONVERTING ENZYME INHIBITORS 489 V. NUCLEAR MAGNETIC
RESONANCE 490 C. PHARMACODYNAMICS 491 I. CARDIOVASCULAR 491 1.
VENTRICULAR FUNCTION 491 2. BLOOD VOLUME 494 3. CARDIAC OUTPUT 495 II.
RENAL PERFUSION AND FUNCTION 495 III. ANTINEOPLASTIC AGENTS 496 IV.
LIVER FUNCTION 497 V. INTESTINAL FUNCTION 497 VI. ANTIMICROBIAL AGENTS
498 VII. NUCLEAR MAGNETIC RESONANCE 498 D. SUMMARY 499 REFERENCES 501 G.
APPENDIX CHAPTER 18 CONSIDERATIONS ON DATA ANALYSIS USING COMPUTER
METHODS AND CURRENTLY AVAILABLE SOFTWARE FOR PERSONAL COMPUTERS M.
GEX-FABRY AND L.P. BALANT 507 A. INTRODUCTION 507 B. PROGRAM FEATURES
AND REQUIREMENTS 508 I. DATA ENTRY 508 II. PHARMACOKINETIC MODEL
SPECIFICATION 509 1. COMPARTMENTAL MODELS 509 2. NONCOMPARTMENTAL
APPROACH 510 3. PHARMACODYNAMIC MODELS 510 4. ABSORPTION KINETICS AND
BIOAVAILABILITY STUDIES 511 5. URINARY DATA ANALYSIS 511 6. POPULATION
PHARMACOKINETICS 511 7. CALCULATION OF INDIVIDUAL DOSAGE REGIMEN 512
III. ERROR MODEL SPECIFICATION 512 IV. PARAMETER ESTIMATION 513 1.
LEAST-SQUARES AND MAXIMUM LIKELIHOOD ESTIMATORS ... 513 2. LINEAR
EQUATIONS 514 3. NONLINEAR EQUATIONS 514 V. CONFIDENCE LIMITS ON
ESTIMATED PARAMETERS 517 VI. STATISTICAL MEASURES OF GOODNESS OF FIT 517
XXVI CONTENTS VII. SOLVING SYSTEMS OF DIFFERENTIAL EQUATIONS 518 VIII.
GRAPHIC DISPLAY OF RESULTS 519 IX. PRINTING AND PLOTTING RESULTS 520 X.
USER INTERFACE AND DOCUMENTATION 520 XL HARDWARE AND SOFTWARE
REQUIREMENTS 521 C. DIRECTORY OF SURVEYED SOFTWARE 521 D. CONCLUSION 526
REFERENCES 526 SUBJECT INDEX 529
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| id | DE-604.BV008897322 |
| illustrated | Illustrated |
| indexdate | 2024-07-09T17:26:53Z |
| institution | BVB |
| isbn | 3540575065 0387575065 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-005887552 |
| oclc_num | 29356861 |
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| physical | XXVI, 537 S. Ill., graph. Darst. |
| publishDate | 1994 |
| publishDateSearch | 1994 |
| publishDateSort | 1994 |
| publisher | Springer |
| record_format | marc |
| series | Handbook of experimental pharmacology |
| series2 | Handbook of experimental pharmacology |
| spelling | Pharmacokinetics of drugs [with 51 tables] contributors G. L. Amidon ... Ed. Peter G. Welling ... Berlin [u.a.] Springer 1994 XXVI, 537 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier Handbook of experimental pharmacology 110 Literaturangaben Pharmacokinetics cabt Farmacokinetica gtt Geneesmiddelen gtt Pharmacokinetics Pharmakokinetik (DE-588)4115557-9 gnd rswk-swf Pharmakokinetik (DE-588)4115557-9 s DE-604 Welling, Peter G. Sonstige oth Amidon, Gordon L. Sonstige oth Handbook of experimental pharmacology 110 (DE-604)BV002390716 110 GBV Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=005887552&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Pharmacokinetics of drugs [with 51 tables] Handbook of experimental pharmacology Pharmacokinetics cabt Farmacokinetica gtt Geneesmiddelen gtt Pharmacokinetics Pharmakokinetik (DE-588)4115557-9 gnd |
| subject_GND | (DE-588)4115557-9 |
| title | Pharmacokinetics of drugs [with 51 tables] |
| title_auth | Pharmacokinetics of drugs [with 51 tables] |
| title_exact_search | Pharmacokinetics of drugs [with 51 tables] |
| title_full | Pharmacokinetics of drugs [with 51 tables] contributors G. L. Amidon ... Ed. Peter G. Welling ... |
| title_fullStr | Pharmacokinetics of drugs [with 51 tables] contributors G. L. Amidon ... Ed. Peter G. Welling ... |
| title_full_unstemmed | Pharmacokinetics of drugs [with 51 tables] contributors G. L. Amidon ... Ed. Peter G. Welling ... |
| title_short | Pharmacokinetics of drugs |
| title_sort | pharmacokinetics of drugs with 51 tables |
| title_sub | [with 51 tables] |
| topic | Pharmacokinetics cabt Farmacokinetica gtt Geneesmiddelen gtt Pharmacokinetics Pharmakokinetik (DE-588)4115557-9 gnd |
| topic_facet | Pharmacokinetics Farmacokinetica Geneesmiddelen Pharmakokinetik |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=005887552&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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