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The authors have provided an overview of the relationships between hormones that are physiologic constituents of the body as well as their pharmacologic use in replacement therapies and related endocrine dys- function. Principles of Endocrine Pharmacology concerns itself with the ther- apeutic use of hormones, and hormone like substances, or drugs that can act either by suppressing or enhancing the metabolism of certain glands of internal secretion. Other drugs used for nonendocrine ther- apies can likewise affect the endocrine system. Endocrine pharmacology emerged in the early 1900s with the use of crude pituitary extracts. By the mid-1900s several investigators had isolated and begun to synthesize hormones or hormonelike substances. Recognizing the limited supply of hormones that could be obtained both from animal sources and human autopsy material, the search for so- called hormone substitutes also began early in the 1900s. Recently, re- combinant DNA technologies have been used to provide alternative therapeutic sources of human insulin and human growth hormone. Aside from insulin, perhaps no other use of hormonally-active sub- stance is better exemplified by those drugs which affect fertility. The synthesis of an orally-effective steroid represented one of the first major breakthroughs in the chemical suppression of ovulation. Since the orally- active 19-norsteroids were introduced in the 1950s, several oral contra- ceptive steroid preparations have been marketed. Indeed, the advent of oral contraceptives for birth control has led to a renewed interest in endocrine pharmacology.
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Table of Contents

1. Introduction and General Mechanisms of Hormonal Actions.- 1.1. History and Scope of Endocrine Pharmacology.- 1.2. General Concepts of Hormone Actions.- 1.2.1. Hormone Receptor/Acceptors.- 1.2.2. Hormone Substitutes.- 1.2.3. Hormone Antagonists.- 1.2.4. Hormone Synthesis Inhibitors.- 1.3. Hormonal Feedback Systems.- Recommended Readings.- 2. Pharmacology of Adenohypophyseal Hormones.- 2.1. Factors Modifying Adenohypophyseal Secretion: Hypophysiotrophic Hormones.- 2.1.1. CRH.- 2.1.2. TRH.- 2.1.3. LH/FSH-RH (GnRH).- 2.1.4. GH-RF and GH-IF (SRIF).- 2.1.5. PRF and PIF.- 2.1.6. MRF and MIF.- 2.2. Pharmacology of Anterior Pituitary Hormones.- 2.2.1. TSH.- 2.2.2. STH or GH.- 2.2.3. ACTH.- 2.2.4. FSH/LH.- 2.2.5. PRL.- Recommended Readings.- 3. Posterior Pituitary Hormones, Oxytocics, and Prostaglandins.- 3.1. Posterior Pituitary Hormones.- 3.1.1. History.- 3.1.2. Synthesis, Transport, and Release.- 3.1.3. Antidiuretic Hormone.- 3.1.4. Oxytocin.- 3.2. Ergot Alkaloids.- 3.2.1. Chemistry.- 3.2.2. Mechanism of Action and Biochemical Effects.- 3.2.3. Therapeutic Uses and Preparations.- 3.2.4. Adverse Effects.- 3.3. Prostaglandins: Reproductive Actions.- 3.3.1. Chemistry.- 3.3.2. Mechanism of Action and Biochemical Effects.- 3.3.3. Therapeutic Uses and Preparations.- 3.3.4. Adverse Effects.- 3.3.5. Prostaglandin Inhibitors.- 3.3.6. Uterine Relaxants.- Recommended Readings.- 4. Thyroid and Antithyroidal Drugs.- 4.1. Thyroid.- 4.1.1. History.- 4.1.2. Central Regulation of the Thyroid.- 4.1.3. Chemistry, Biosynthesis, Secretion, and Metabolism.- 4.1.4. Thyroid Hormone Receptors.- 4.1.5. Biochemical Actions.- 4.1.6. Management of Hypothyroidal States.- 4.1.7. Therapeutic Uses and Preparations.- 4.1.8. Adverse Effects.- 4.2. Antithyroidal Agents.- 4.2.1. Thyrotoxicosis (Hyperthyroidism).- 4.2.2. Drugs Used in the Management of Thyrotoxicosis.- 4.3. Drug Interactions and Thyroid Function Tests.- Recommended Readings.- 5. Parathyroid Hormone and Calcitonin.- 5.1. Introduction.- 5.2. History.- 5.3. Parathyroid Hormone.- 5.3.1. Chemistry.- 5.3.2. Biosynthesis, Secretion, and Metabolism.- 5.3.3. Mechanism of Action.- 5.3.4. Physiological and Pharmacological Actions.- 5.3.5. Preparations.- 5.3.6. Therapeutic Uses.- 5.3.7. Adverse Effects.- 5.4. Calcitonin.- 5.4.1. Chemistry.- 5.4.2. Biosynthesis, Secretion, and Metabolism.- 5.4.3. Mechanism of Action.- 5.4.4. Physiological and Pharmacological Actions.- 5.4.5. Preparations.- 5.4.6. Therapeutic Uses.- 5.4.7. Adverse Effects.- Recommended Readings.- 6. Androgenic and Anabolic Steroids.- 6.1. Introduction.- 6.2. History.- 6.3. Chemistry.- 6.4. Biosynthesis, Secretion, and Metabolism.- 6.5. Mechanism of Action.- 6.6. Physiological and Pharmacological Actions of Androgens.- 6.7. Preparations.- 6.8. Therapeutic Uses.- 6.9. Adverse Effects.- 6.10. Weak or Impeded Androgens.- 6.11. Androgen Antagonists.- Recommended Readings.- 7. Estrogens and Antiestrogenic Drugs.- 7.1. Estrogens.- 7.1.1. Introduction.- 7.1.2. History.- 7.1.3. Chemistry.- 7.1.4. Biosynthesis, Secretion, and Metabolism.- 7.1.5. Mechanism of Action.- 7.1.6. Physiological Actions.- 7.1.7. Therapeutic Uses.- 7.1.8. Preparations.- 7.1.9. Adverse Effects.- 7.2. Antiestrogens.- 7.2.1. Clomiphene.- 7.2.2. Tamoxifen.- Recommended Readings.- 8. Progestins and Oral Contraceptives.- 8.1. Progestins.- 8.1.1. Introduction.- 8.1.2. History.- 8.1.3. Chemistry.- 8.1.4. Biosynthesis, Secretion, and Metabolism.- 8.1.5. Mechanism of Action.- 8.1.6. Physiological Effects.- 8.1.7. Therapeutic Uses.- 8.1.8. Preparations.- 8.1.9. Adverse Effects.- 8.2. Oral Contraceptives.- 8.2.1. Preparations.- 8.2.2. Mechanism of Action.- 8.2.3. Adverse Effects.- Recommended Readings.- 9. Adrenocorticosteroid Drugs.- 9.1. Introduction.- 9.2. History.- 9.3. Chemistry.- 9.4. Biosynthesis, Secretion, and Metabolism.- 9.5. Mechanism of Action.- 9.6. Physiological and Pharmacological Actions.- 9.7. Preparations.- 9.8. Therapeutic Uses.- 9.9. Adverse Effects.- 9.10. Inhibitors of Adrenocortical Steroid Biosynthesis.- Recommended Readings.- 10. Insulin and Oral Hypoglycemic Agents.- 10.1. Insulin.- 10.1.1. History of Diabetes Mellitus.- 10.1.2. Chemistry of Insulin.- 10.1.3. Secretion and Metabolism.- 10.1.4. General Biochemical Events and Actions.- 10.1.5. Insulin Receptors.- 10.1.6. Receptor-Mediated Internalization.- 10.1.7. Factors Affecting Insulin and Insulin Resistance.- 10.1.8. Uses and Preparations.- 10.1.9. Adverse Effects.- 10.2. Oral Hypoglycemic Agents.- 10.2.1. Sulfonylureas.- 10.2.2. Biguanides.- 10.3. Glucagon.- 10.4. Somatostatin.- 10.5. Nonhormonal Hyperglycemic Agents.- Recommended Readings.- 11. Effects of Drugs on the Endocrine System.- 11.1. Introduction.- 11.2. Basic Mechanisms of Drug-Hormone Interactions.- 11.3. Effects of Drugs on Adenohypophyseal Function.- 11.4. Effects of Drugs on Neurohypophyseal Function.- 11.5. Effects of Drugs on Lactation and Their Presence in Milk.- 11.6. Effects of Drugs on Hormone Transport.- 11.7. Effects of Drugs on Steroidogenesis.- 11.8. Effects of Drugs on Gonadal Function.- 11.9. Effects of Drugs on Pancreatic Function.- 11.10. Effects of Drugs on Thyroid Function.- 11.11. Effects of Drugs on Laboratory Analyses.- Recommended Readings.

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