Pharmacotherapeutics of the thyroid gland: [with 29 tables]
Saved in:
| Format: | Book |
|---|---|
| Language: | English |
| Published: |
Berlin [u.a.]
Springer
1997
|
| Series: | Handbook of experimental pharmacology
128 |
| Subjects: | |
| Online Access: | Inhaltsverzeichnis |
| Physical Description: | XVIII, 370 S. Ill., graph. Darst. |
| ISBN: | 3540624996 |
Staff View
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| 245 | 1 | 0 | |a Pharmacotherapeutics of the thyroid gland |b [with 29 tables] |c contributors J. W. Barlow ... Ed. A. P. Weetman ... |
| 264 | 1 | |a Berlin [u.a.] |b Springer |c 1997 | |
| 300 | |a XVIII, 370 S. |b Ill., graph. Darst. | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 490 | 1 | |a Handbook of experimental pharmacology |v 128 | |
| 650 | 7 | |a Thyroid Gland |2 cabt | |
| 650 | 7 | |a Drug Therapy |2 cabt | |
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| 650 | 7 | |a Schildklierhormonen |2 gtt | |
| 650 | 4 | |a Antithyroid Agents |x pharmacology | |
| 650 | 4 | |a Thyroid Gland |x drug effects | |
| 650 | 4 | |a Thyroid Hormones |x physiology | |
| 650 | 4 | |a Thyroid antagonists |x Physiological effect | |
| 650 | 4 | |a Thyroid gland |x Effect of drugs on | |
| 650 | 4 | |a Thyroid hormones |x Physiological effect | |
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| adam_text | Contents
CHAPTER 1
Introduction: Clinical Aspects of Thyroid Treatment
A.D. Toft 1
A. Introduction 1
B. Choices of Treatment for the Hyperthyroidism of
Graves Disease 2
I. Iodine 131 Therapy 2
1. Acceptability of Irradiation 2
2. Gastric Carcinoma 3
3. Ophthalmopathy 3
4. Calcitonin Deficiency 4
II. Thyroid Surgery 4
III. Antithyroid Drug Therapy 5
C. Subclinical Hyperthyroidism 6
D. Correct Dose of Thyroxine in Primary Hypothyroidism 6
E. Subclinical Hypothyroidism: Treatment or Not? 7
References 8
CHAPTER 2
Control of TRH and TSH Secretion
M.F. Scanlon. With 2 Figures 11
A. Introduction 11
B. Negative Feedback Action of Thyroid Hormones 11
C. Structure and Actions of TRH 13
D. Structure and Actions of Somatostatin 14
E. Actions of Neurotransmitters 16
F. Actions of Cytokines and Inflammatory Mediators 20
G. Physiological and Secondary TSH Changes 20
References 24
CHAPTER 3
The TSH Receptor
M. Misrahi and E. Milgrom. With 7 Figures 33
A. Introduction 33
B. TSH Receptor Cloning 34
C. Structure of the TSHR in the Human Thyroid Gland 35
D. Structure of the TSHR in Transfected Cells 37
E. Controversies on Receptor Structure 38
F. Expression of the TSH Receptor in the Baculovirus System 39
G. Shedding of TSH Receptor Ectodomain in Thyroid and
Transfected Cells 40
H. Cellular Expression of the TSH Receptor 42
I. Polarised Expression in the Thyroid 42
II. Expression in Other Cell Types 43
I. Intracellular Trafficking of the Receptor 43
I. Polarized Expression in MDCK Cells 43
II. Receptor Downregulation 46
J. Structure Function Relationships 47
I. Transduction Pathways of the TSH Receptor 47
II. Mutagenesis of Transmembrane and Intracellular Domains
of the TSH Receptor 48
III. Mutagenesis of the Extracellular Domain of the TSH
Receptor 50
K. Gene Structure and Regulation 52
I. Gene Organisation 52
II. Chromosomal Localisation and Genetic Mapping 53
1. Structure and Function of TSHR Promoter and
5 Flanking Region 53
L. The TSH Receptor and Pathology 55
I. Autoimmunity 55
1. The TSHR and the Genetics of Graves Disease 55
2. Epitopes of the TSH Receptor Recognised by
the Auto antibodies 56
II. Mutations of the TSH Receptor in Pathology 57
1. TSH Receptor and Tumorigenesis 57 .
2. TSHR and Non immune Hyperthyroidism 58
III. Constitutive Mutations and Model of Receptor
Activation 59
IV. Loss of Function Mutations 60 (
1. Animal Model 60
2. Thyroid Resistance to TSH Due to TSHR
Mutations 61 j
M. Conclusions 62
References 62
CHAPTER 4
Thyroid Hormone Synthesis, Plasma Membrane Transport and
Metabolism
G. Hennemann and TJ. Visser. With 12 Figures 75
A. Thyroid Hormone Synthesis 75
I. Iodide Transport 75
II. Biosynthesis of T4 and T3 77
III. Thyroid Peroxidase 77
IV. H2O2 Generation 78
V. Iodination of Tyrosyl Residues in Thyroglobulin 78
VI. Coupling of Iodotyrosines 79
VII. Endocytosis of Iodinated Thyroglobulin 80
VIII. Release of T3 and T4 81
B. Thyroid Hormone Plasma Membrane Transport 82
I. Studies of Plasma Membrane Thyroid Hormone
Transport in Isolated Cells 82
II. Liver Perfusion Studies 84
III. (Patho)physiological Significance of Thyroid Hormone
Plasma Membrane Transport: Its Role in the Generation
of Low Serum T3 in Non thyroidal Illness in Man 86
C. Thyroid Hormone Metabolism 89
D. Deiodination 90
E. Characterization of Iodothyronine Deiodinases 94
F. Sulphation 98
I. Thyroid Hormone Sulphotransferases 98
II. Deiodination of Iodothyronine Sulphates 99
III. Occurrence of Iodothyronine Sulphates 100
IV. Possible Role of Iodothyronine Sulphation 102
G. Glucuronidation 103
I. Thyroid Hormone UDP Glucuronyltransferases 104
II. Role of Thyroid Hormone Glucuronidation in
Humans 105
III. Glucuronidation of Iodothyroacetic Acid Analogues 106
References 107
CHAPTER 5
Thyroid Hormone Transport
J.R. Stockigt, C F. Lim, J.W. Barlow, and D.J. Topliss.
With 7 Figures 119
A. Introduction 119
B. Serum Binding in Humans 120
I. Thyroxine Binding Globulin 122
1. Normal Structure 122
2. Inherited Variants 123
3. Acquired Variants 123
II. Transthyretin 124
1. Normal Structure 124
2. Inherited Variants 125
III. Albumin 126
1. Normal Structure 126
2. Inherited Variants 126
IV. Thyroxine Binding in Other Vertebrates 127
V. Role of Binding Proteins 128
C. Binding Kinetics 128
I. Binding Kinetics, Capacity and Affinity 128
II. Characterisation of High Capacity, Low Affinity
Binding 131
III. Specific Characterisation of TBG Binding 132
IV. Assay of TBG 132
D. Free Hormone Measurement 133
I. Factors Influencing Validity 135
1. Radiochemical Purity 135
2. Protein Tracer Interactions 135
3. Dilution Effects 135
4. Other Factors 136
II. Non isotopic Free T4 Methods 136
III. Thyroid Hormone Binding Ratio 136
E. Interactions with Competitors 137
I. Pre dilution and Co dilution 138
II. Estimation of In Vivo Competitor Potency 139
III. In Vivo Kinetics of Competitors 140
IV. Interaction Between Competitors 141
V. Spurious Competition 141
VI. Drug Competition at Other Sites 142
References 144
CHAPTER 6
Molecular Biology of Thyroid Hormone Action
J.A. Franklyn and V.K.K. Chatterjee. With 4 Figures 151
A. Introduction 151
B. Extranuclear Mechanisms of Thyroid Hormone Action 151
I. Plasma Membrane and Intracellular Transport of
Thyroid Hormones 151
II. Extranuclear Sites of Thyroid Hormone Action 152
C. Identification of High Affinity Nuclear Binding Sites for
Thyroid Hormones 152
D. Cloning of cDNAs Encoding Nuclear Receptors for T3 153
E. Recognition of Two Genes Encoding Two Major Classes of
TR 154
F. Thyroid Hormone Response Elements 155
G. Structural Characteristics of TRs and Identification of
Functional Domains 157
I. DNA Binding Domain 158
II. Hormone Binding Domain 159
III. Nuclear Localisation 159
IV. Dimerisation 159
V. Silencing of Basal Gene Transcription by Unliganded
TR 161
VI. Transcription Activation 162
1. Hormone Dependent Activation of Transcription
(AF 2) 162
2. Constitutive Transcription Activation (AF 1) 163
H. Role of the TR Splice Variant TRa2 164
I. TRs and Human Disease 164
References 165
CHAPTER 7
Iodine: Metabolism and Pharmacology
S. Nagataki and N. Yokoyama. With 4 Figures 171
A. Introduction 171
B. Iodide Transport and Organification 172
C. Thyroid Autoregulation 173
I. Autoregulation in Animals 173
i 1. Wolff Chaikoff Effect and Escape 173
2. Effects of Graded Doses of Iodide 174
II. Autoregulation in Humans 175
1. Effects of Moderate Doses of Iodide 176
2. Effects of Excess Iodide in Normal Subjects 178
III. Intracellular Effects of Excess Iodide in Relation to
Other Regulators 180
1. Signal Transduction 180
2. Expression of HLA Molecules and Other Thyroidal
, Proteins 180
! 3. Protein Synthesis 181
| 4. Organic Iodinated Lipids 181
{ 5. Growth Factors 181
j IV. Mechanism of Autoregulation 182
1. Acute Inhibitory Effect (Wolff Chaikoff Effect) 182
2. Mechanism of Adaptation 183
3. Species Differences in Autoregulation 184
4. Role of TSH in Autoregulation 184
References 184
CHAPTER 8
Antithyroid Drugs: Their Mechanism of Action and Clinical Use
M. El Sheikh and A.M. McGregor. With 1 Figure 189
A. Introduction 189
B. Hyperthyroidism 189
C. Pharmacokinetics 190
D. Mechanism of Action 191
I. Inhibition of TPO 191
1. Thyroid Hormone Synthesis 191
2. Drug Action 192
II. Immunological Effects 192
1. Graves Disease 192
2. Drug Action 193
E. Clinical Use 194
I. Indications 194
II. Adverse Effects 195
III. Administration and Use 196
1. Graves Disease 196
2. Drug Usage with Radioiodine 202
3. Drug Usage in Pregnancy 202
4. Thyroid Storm 203
F. Conclusions 203
References 204
CHAPTER 9
Effect of Lithium on the Thyroid Gland
J.H. Lazarus. With 2 Figures 207
A. Introduction 207
B. Effect on Thyroid Physiology 207
I. Iodine Concentration 207
II. Intrathyroidal Effects 208
III. Effect on Thyroid Hormone Secretion 208
IV. Effect on Peripheral Thyroid Hormone Metabolism 209
C. Effect on the Hypothalamic Pituitary Axis 209
D. Lithium and Cell Function 211
E. Immunological Effects on Thyroid Function 212
F. Effect on Thyroid Hormone Action 213
G. Clinical Effects on the Thyroid 214
I. Goitre 214
II. Hypothyroidism 215
III. Hyperthyroidism 216
H. Clinical Use in Thyroid Disease 217
References 218
CHAPTER 10
Amiodarone and the Thyroid
W.M. Wiersinga. With 12 Figures 225
A. Pharmacology of Amiodarone 225
I. Physicochemical Properties 225
II. Pharmacokinetics 225
i 1. Absorption and Bioavailability 226
| 2. Plasma Kinetics 226
3. Tissue Distribution 227
4. Metabolism 228
5. Elimination 230
III. Pharmacology 231
1. Electrophysiological Effects 231
2. Haemodynamic Effects 231
IV. Pharmacotherapy 231
1. Indications for Use 231
2. Dosing Schedules 232
V. Toxicology 233
1. Nature of Side Effects 233
2. Pathogenesis of Side Effects 234
3. Prevention of Side Effects 235
B. Effects of Amiodarone on Thyroid Hormone Secretion and
Metabolism 235
i I. Changes in Plasma Thyroid Hormone Concentrations 235
1. Human Studies 235
2. Animal Studies 237
II. Changes in Thyroid and Extrathyroidal Tissues 238
1. Peripheral Tissues 238
2. Thyroid 239
3. Pituitary 242
III. Changes in Thyroid Hormone Kinetics 243
1. Human Studies 243
2. Animal Studies 243
IV. Summary 244
C. Amiodarone Induced Thyrotoxicosis and Amiodarone Induced
Hypothyroidism 246
I. Diagnosis 246
II. Incidence 248
III. Pathogenesis 250
1. Amiodarone Induced Hypothyroidism 250
2. Amiodarone Induced Thyrotoxicosis 253
IV. Treatment 257
1. Amiodarone Induced Hypothyroidism 257
2. Amiodarone Induced Thyrotoxicosis 258
3. Amiodarone Treatment in Pregnancy 260
4. Amiodarone Treatment of Hyperthyroidism 261
V. Summary 262
D. Amiodarone as a Thyroid Hormone Antagonist 264
I. Hypothyroid Like Effects of Amiodarone 264
1. Heart 264
2. Liver 268
3. Pituitary 270
II. Amiodarone as a T3 Receptor Antagonist 271
1. Inhibition of T3 Binding to Nuclear T3 Receptors 271
2. Structure Function Relationship 273
III. Summary 274
References 276
CHAPTER 11
Effects of Other Pharmacological Agents on Thyroid Function
C.A. Meier and A.G. Burger. With 3 Figures 289
A. Introduction 289
B. Effects of Various Drugs on Thyroidal Hormonogenesis 289
C. Effects of Drugs on Thyroid Hormone Metabolism 293
I. Deiodination 293
II. Microsomal Oxidation 295
D. Drug Effects on Cellular and Intestinal Uptake of
Thyroid Hormone 296
I. Cellular Uptake 297
II. Intestinal Absorption 297
References 297
CHAPTER 12
Effects of Environmental Agents on Thyroid Function
E. Gaitan. With 1 Figure 301
A. Introduction 301
B. Chemical Categories, Sources, Pharmacokinetics, and
Mechanism of Action 303
I. Sulphurated Organics 303
1. Thiocyanate, Isothiocyanates, and Thio oxazolidone
(Goitrin) 303
2. Disulphides 306
II. Flavonoids 306
III. Polyhydroxyphenols and Phenol Derivatives 308
IV. Pyridines 310
V. Phthalate Esters and Metabolites 311
VI. Polychlorinated and Polybrominated Biphenyls 312
1 VII. Other Organochlorines 313
VIII. Polycyclic Aromatic Hydrocarbons 314
References 315
[• CHAPTER 13
Thyroid Hormone Antagonism
J.W. Barlow, T.C. Crowe, and D.J. Topliss. With 4 Figures 319
I A. Introduction 319
B. Inhibition of Uptake 320
I. Mechanisms of Cell Entry 320
II. Purification of Membrane Binding Sites 321
III. Inhibition of Uptake 322
f IV. Uptake Inhibition and Hormone Responsiveness 323
I C. Cytoplasmic Binding 324
I. Role of Cytoplasmic Binding 324
| II. Cytoplasmic Binding and Hormone Responsiveness 325
i III. Pharmacological Antagonism of Cytoplasmic Binding 327
D. Antagonism at the Receptor Level 328
I. Thyroid Hormone Receptors and the Receptor
Superfamily 328
, II. Heterogeneity Among Thyroid Hormone Receptors 329
i III. Tissue Distribution of Receptors 331
IV. Receptor Regulation of Tissue Responsiveness 331
V. Drug Interactions at the Ligand Binding Site 334
i References 336
; CHAPTER 14
| Immunomodulatory Agents in Autoimmune Thyroid Disease
S* A.P. Weetman. With 4 Figures 343
A. Introduction 343
B. Hormones and Autoimmune Thyroid Disease 343
I. Sex Hormones 343
II. Glucocorticoids 344
III. Thyroid Hormones 344
C. Toxins and Autoimmune Thyroid Disease 346
D. Trace Elements and Autoimmune Thyroiditis 346
E. Drugs and Autoimmune Thyroid Disease 347
F. Cytokines and Autoimmune Thyroid Disease 351
G. Immunomodulatory Agents in TAO 353
I. Glucocorticoids 353
II. Other Immunosuppressive Drugs 353
III. Other Treatments 354
References 355
Subject Index 361
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| genre | (DE-588)4143413-4 Aufsatzsammlung gnd-content |
| genre_facet | Aufsatzsammlung |
| id | DE-604.BV011425747 |
| illustrated | Illustrated |
| indexdate | 2024-07-09T18:09:32Z |
| institution | BVB |
| isbn | 3540624996 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-007682829 |
| oclc_num | 36188359 |
| open_access_boolean | |
| owner | DE-355 DE-BY-UBR DE-19 DE-BY-UBM DE-12 DE-20 DE-11 DE-188 DE-578 |
| owner_facet | DE-355 DE-BY-UBR DE-19 DE-BY-UBM DE-12 DE-20 DE-11 DE-188 DE-578 |
| physical | XVIII, 370 S. Ill., graph. Darst. |
| publishDate | 1997 |
| publishDateSearch | 1997 |
| publishDateSort | 1997 |
| publisher | Springer |
| record_format | marc |
| series | Handbook of experimental pharmacology |
| series2 | Handbook of experimental pharmacology |
| spelling | Pharmacotherapeutics of the thyroid gland [with 29 tables] contributors J. W. Barlow ... Ed. A. P. Weetman ... Berlin [u.a.] Springer 1997 XVIII, 370 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier Handbook of experimental pharmacology 128 Thyroid Gland cabt Drug Therapy cabt Farmacotherapie gtt Schildklier gtt Schildklierhormonen gtt Antithyroid Agents pharmacology Thyroid Gland drug effects Thyroid Hormones physiology Thyroid antagonists Physiological effect Thyroid gland Effect of drugs on Thyroid hormones Physiological effect Schilddrüse (DE-588)4052461-9 gnd rswk-swf Pharmakotherapie (DE-588)4076066-2 gnd rswk-swf Schilddrüsenkrankheit (DE-588)4116387-4 gnd rswk-swf (DE-588)4143413-4 Aufsatzsammlung gnd-content Schilddrüse (DE-588)4052461-9 s Pharmakotherapie (DE-588)4076066-2 s DE-604 Schilddrüsenkrankheit (DE-588)4116387-4 s Weetman, Anthony P. Sonstige oth Barlow, John W. Sonstige oth Handbook of experimental pharmacology 128 (DE-604)BV002390716 128 HBZ Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=007682829&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Pharmacotherapeutics of the thyroid gland [with 29 tables] Handbook of experimental pharmacology Thyroid Gland cabt Drug Therapy cabt Farmacotherapie gtt Schildklier gtt Schildklierhormonen gtt Antithyroid Agents pharmacology Thyroid Gland drug effects Thyroid Hormones physiology Thyroid antagonists Physiological effect Thyroid gland Effect of drugs on Thyroid hormones Physiological effect Schilddrüse (DE-588)4052461-9 gnd Pharmakotherapie (DE-588)4076066-2 gnd Schilddrüsenkrankheit (DE-588)4116387-4 gnd |
| subject_GND | (DE-588)4052461-9 (DE-588)4076066-2 (DE-588)4116387-4 (DE-588)4143413-4 |
| title | Pharmacotherapeutics of the thyroid gland [with 29 tables] |
| title_auth | Pharmacotherapeutics of the thyroid gland [with 29 tables] |
| title_exact_search | Pharmacotherapeutics of the thyroid gland [with 29 tables] |
| title_full | Pharmacotherapeutics of the thyroid gland [with 29 tables] contributors J. W. Barlow ... Ed. A. P. Weetman ... |
| title_fullStr | Pharmacotherapeutics of the thyroid gland [with 29 tables] contributors J. W. Barlow ... Ed. A. P. Weetman ... |
| title_full_unstemmed | Pharmacotherapeutics of the thyroid gland [with 29 tables] contributors J. W. Barlow ... Ed. A. P. Weetman ... |
| title_short | Pharmacotherapeutics of the thyroid gland |
| title_sort | pharmacotherapeutics of the thyroid gland with 29 tables |
| title_sub | [with 29 tables] |
| topic | Thyroid Gland cabt Drug Therapy cabt Farmacotherapie gtt Schildklier gtt Schildklierhormonen gtt Antithyroid Agents pharmacology Thyroid Gland drug effects Thyroid Hormones physiology Thyroid antagonists Physiological effect Thyroid gland Effect of drugs on Thyroid hormones Physiological effect Schilddrüse (DE-588)4052461-9 gnd Pharmakotherapie (DE-588)4076066-2 gnd Schilddrüsenkrankheit (DE-588)4116387-4 gnd |
| topic_facet | Thyroid Gland Drug Therapy Farmacotherapie Schildklier Schildklierhormonen Antithyroid Agents pharmacology Thyroid Gland drug effects Thyroid Hormones physiology Thyroid antagonists Physiological effect Thyroid gland Effect of drugs on Thyroid hormones Physiological effect Schilddrüse Pharmakotherapie Schilddrüsenkrankheit Aufsatzsammlung |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=007682829&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| volume_link | (DE-604)BV002390716 |
| work_keys_str_mv | AT weetmananthonyp pharmacotherapeuticsofthethyroidglandwith29tables AT barlowjohnw pharmacotherapeuticsofthethyroidglandwith29tables |