Advances in Pharmacology

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ISBN: 9780120329366 | 0120329360
Cover: Hardcover
Copyright: 4/3/1996

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Each volume of Advances in Pharmacology provides a rich collection of reviews on timely topics. Emphasis is placed on the molecular bases of drug action, both applied and experimental.Key Features* This volume includes reviews on some of the hottest topics in pharmacology, including: * Multidrug resistance and the MDR1 gene in gene therapy* Regulation of calcium channels in epithelial cells* Gene therapy and vascular disease* Potential therapeutic applications for Heparin * Calcium channel blockers* Antithrombotic agents* Regulation of potassium channels in epithelial cells

Contributors

xiii

Interactions between Drugs and Nutrients

C. Tschanz

W. Wayne Stargel

J. A. Thomas

Introduction

(2)

Factors Affecting Gastrointestinal Absorption

(5)

Bioavailability and Metabolism

(1)

Excretion and Elimination

(2)

Special Interactions/Conditions

(14)

Antimicrobials

(1)

Drug---Ethanol Interactions

(3)

Drug---Vitamins

(1)

Drug---Minerals

(2)

Genetic Differences

(3)

Geriatrics

(2)

Hypoglycemics

(1)

Parenteral Nutrition

(1)

Concluding Remarks

(3)

References

(3)

Induction of Cyclo-Oxygenase and Nitric Oxide Synthase in Inflammation

Ian Appleton

Annette Tomlinson

Derek A. Willoughby

General Introduction

(1)

Cyclo-Oxygenase

(2)

Isoforms of Cyclo-Oxygenase

(1)

Regulation of COX-1 and COX-2

(1)

Prostanoids

(7)

Prostanoids and Inflammation

(4)

Prostanoids and Chronic Inflammation

(1)

Prostaglandins and Pain

(2)

Nonsteroidal Anti-Inflammatory Drugs and Inflammatory Pain

(2)

COX-1 and COX-2 in Inflammation

(1)

Pharmacological Inhibition of COX-1 and COX-2

(3)

Conclusion

(1)

Nitric Oxide Synthase

(6)

Induction and Inhibition of Nitric Oxide Synthase

(1)

Cellular Production and Activity of NO at Inflammatory Sites

(1)

Arginine Metabolism at Inflammatory Sites

(2)

Nitric Oxide Production by Human Macrophages

(1)

Cell Types in Which Nitric Oxide Synthase Is Induced

(1)

Cytotoxicity and Tissue Damage

(1)

Nitric Oxide in Mechanisms of Acute Inflammation

(2)

Complement-Mediated and Cell-Mediated Inflammatory Models

(1)

Neurogenic Inflammation

(1)

Nitric Oxide in Mechanisms of Chronic Inflammation

(2)

Nitric Oxide in Angiogenesis

(1)

Nitric Oxide in Inflammatory Disease

(4)

Rheumatoid Arthritis

(1)

Multiple Sclerosis

(1)

Graft-Versus-Host Reaction

(1)

Renal Inflammation

(1)

Gastrointestinal Inflammation

(1)

Other Inflammatory Disease States

(1)

Involvement of Nitric Oxide in Inflammatory Pain

(1)

Conclusion

(1)

Interactions between the Nitric Oxide Synthase and Cyclo-Oxygenase Pathways

(20)

References

(18)

Current and Future Therapeutic Approaches to Hyperlipidemia

John A. Farmer

Antonio M. Gotto, Jr.

Introduction

(1)

Agents That Predominantly Lower Cholesterol

(18)

Bile-Acid Sequestrants

(6)

3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase Inhibitors

(7)

Probucol

(2)

Estrogen-Replacement Therapy

(2)

Agents That Predominantly Lower Triglyceride

(7)

Nicotinic Acid

(2)

Fibric-Acid Derivatives

101

(3)

Fish Oil

104

(1)

Combination-Drug Therapy

105

(1)

Future Developments

105

(2)

Conclusion

107

(8)

References

107

(8)

In Vivo Pharmacological Effects of Ciclosporin and Some Analogues

Jean F. Borel

Gotz Baumann

Ian Chapman

Peter Donatsch

Alfred Fahr

Edgar A. Mueller

Jean-Marie Vigouret

Introduction and Summary

115

(9)

Molecular Mechanism of Immunosuppression

124

(4)

Suppressive Effects on Cell-Mediated Immunity

128

(26)

T Cell-Mediated Cytotoxicity

128

(5)

T-Cell Functions for Help, Memory, and Delayed-Type Hypersensitivity (DTH)

133

(4)

Cell-Mediated Suppressor Function

137

(6)

Induction of Antigen-Specific Hypo- or Unresponsiveness

143

(11)

Other Biological Effects Associated with the Immunosuppressive Activity

154

(11)

Chronic Inflammation

154

(1)

Prolactin Antagonism

154

(2)

Possible Interactions with the Central Nervous System

156

(2)

Major Side Effects

158

(7)

Biological Effects Possibly Correlated with the Immunosuppressive Activity

165

(15)

Development of Suppressor Cells

165

(1)

Interference in the Regulation of Tolerance to Self and Nonself

165

(7)

Therapeutic Effects in Psoriasis

172

(3)

Therapeutic Effects in Asthma?

175

(4)

Effects on Hair Follicles

179

(1)

Biological Effects Appearing Independently of Immunosuppressive Activity

180

(14)

Effects on Nonlymphoid Cells

180

(7)

Effects on Various Cellular Functions

187

(2)

Antibiotic Effects

189

(5)

Chronic Allograft Rejection

194

(10)

Clinical Situation

194

(1)

Experimental Approaches

195

(4)

Factors Involved in Chronic Allograft Rejection

199

(5)

Impact of Galenic Formulation on Pharmacokinetics

204

(43)

Clinical Pharmacokinetics of CS (SANDIMMUN)

204

(3)

New Galenical Formulation of CS (SANDIMMUN NEORAL)

207

(1)

References

208

(39)

Mono-ADP-ribosylation: A Reversible Posttranslational Modification of Proteins

Ian J. Okazaki

Joel Moss

Introduction

247

(3)

Mono-ADP-ribosyltransferases

250

(12)

Avian ADP-ribosyltransferases

250

(6)

Mammalian ADP-ribosyltransferases

256

(5)

Inhibitors of Mono-ADP-ribosyltransferase

261

(1)

Conserved Regions among ADP-ribosyltransferases

262

(6)

Region I

263

(2)

Region II

265

(1)

Region III

266

(2)

ADP-ribosylarginine Hydrolases

268

(3)

Turkey ADP-ribosylarginine Hydrolase

269

(1)

Mammalian ADP-ribosylarginine Hydrolases

270

(1)

Summary

271

(10)

References

272

(9)

Activation of Programmed (Apoptotic) Cell Death for the Treatment of Prostate Cancer

Samuel R. Denmeade

John T. Isaacs

Overview of the Problem

281

(1)

Androgen Sensitivity of Prostate Cancer

282

(1)

Cell Kinetics During Progression of Prostate Cancer

283

(2)

Proliferation-Independent Therapeutic Approach for Androgen-Independent Proliferate Cancer Cells

285

(2)

Summary of the Temporal Sequences Involved in the Programmed Death of Normal Prostatic Glandular Cells Following Androgen Ablation

287

(3)

Prostate Gene Expression during Programmed Cell Death Pathway Induced by Androgen Ablation

290

(1)

Role of Cell Proliferation in the Prostatic Death Process Induced by Castration

291

(2)

Androgen Ablation Induced Programmed Cell Death Does not Require Recruitment into a Perturbed Cell Cycle

293

(1)

p53 Expression Is not Required for Androgen Ablation-Induced Programmed Death of G0 Prostatic Glandular Cells

294

(1)

Redefining the Prostate ``Cell Cycle''

295

(1)

Therapeutic Implication of Programmed Cell Death for Prostatic Cancer

295

(2)

Ability of Thapsigargin (TG) to Activate Programmed Cell Death

297

(3)

Thapsigargin as Therapy for Prostate Cancer

300

(7)

References

302

(5)

Reversal of Atherosclerosis with Therapy: Update of Coronary Angiographic Trials

Howard N. Hodis

Overview

307

(1)

Coronary Angiographic Trials Utilizing Pharmacological Intervention

308

(7)

The NHLBI Type II Coronary Intervention Study

308

(1)

The Cholesterol-Lowering Atherosclerosis Study (CLAS)

308

(1)

The Familial Atherosclerosis Treatment Study (FATS)

309

(1)

The University of California, San Francisco, Specialized Center of Research Intervention Trial (UCSF SCOR)

309

(1)

The Monitored Atherosclerosis Regression Study (MARS)

310

(1)

The Canadian Coronary Atherosclerosis Intervention Trial (CCAIT)

311

(3)

Multicentre Anti-Atheroma Study (MAAS)

314

(1)

The Stanford Coronary Risk Intervention Project (SCRIP)

314

(1)

The St. Thomas' Atherosclerosis Regression Study (STARS)

315

(1)

Coronary Angiographic Trials Utilizing Nonpharmacological Intervention

315

(2)

The Leiden Intervention Trial

315

(1)

The Lifestyle Heart Trial

316

(1)

Heidelberg Exercise-Diet Study

316

(1)

The Program on the Surgical Control of the Hyperlipidemias (POSCH)

317

(1)

Summary of the Coronary Angiographic Trials

317

(1)

Conclusions from Coronary Angiographic Trials

317

(4)

References

318

(3)

Unnatural Nucleotide Sequences in Biopharmaceutics

Lawrence A. Loeb

Introduction

321

(1)

Site-Specific Mutagenesis and Rational Drug Design

322

(1)

Molecular Evolution and Its Consequences

323

(1)

Random Molecular and Chemical Libraries

324

(4)

Random Genetic Selection for Biologically Active Proteins

324

(1)

Phage Display Libraries for Binding Proteins

324

(2)

Peptide Libraries for Modeling Peptide Hormones and Drugs

326

(1)

Nucleic Acid Libraries

326

(2)

Combinatorial Chemical Libraries

328

(1)

Random Sequence Selection

328

(5)

General Protocol

328

(1)

Choice of a Plasmid Vector and Host

329

(1)

``Dummy'' or Nonfunctional Inserts

330

(1)

Oligonucleotide Inserts Containing Random Nucleotide Sequences

330

(1)

Randomization of Oligonucleotides

331

(1)

Combinatorial Consideration

332

(1)

Applications of Random Sequence Selection

333

(1)

Regulatory DNA Sequences and Binding Proteins

333

(1)

Production of Mutant Enzymes

334

(2)

β-Lactamase

334

(1)

Related Studies

335

(1)

Gene Therapy for Human Cancer

336

(7)

Herpes Thymidine Kinase

336

(5)

Protection of Bone Marrow

341

(2)

Status, Summary, and Future Prospects

343

(6)

References

344

(5)

Pharmacology of the Neurotransmitter Release Enhancer Linopirdine (DuP 996), and Insights into Its Mechanism of Action

Simon P. Aiken

Robert Zaczek

Barry S. Brown

Introduction

349

(4)

The Unmet Medical Need of Alzheimer's Disease

349

(1)

The Cholinergic Hypothesis of Alzheimer's Disease

350

(1)

Rationale behind the Use of Linopirdine

351

(2)

Pharmacology of Linopirdine

353

(11)

Enhancement of Evoked Neurotransmitter Release by Linopirdine

353

(5)

Behavioral Effects of Linopirdine

358

(3)

Other Effects of Linopirdine

361

(3)

Mechanistic Studies on Linopirdine

364

(21)

Neurochemical Studies

364

(7)

Electrophysiological Studies

371

(9)

References

380

(5)

Index

385

(10)

Contents of Previous Volumes

395

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Advances in Pharmacology

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Table of Contents

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