Local Anesthetics

Softcover Nachdruck of the original 1. Auflage 1987
ISBN: 978-3-642-71112-1
Verlag: Springer

Buch, Englisch, Band 81, 294 Seiten, Format (B × H): 170 mm x 244 mm, Gewicht: 542 g

Reihe: Handbook of Experimental Pharmacology

Local anesthetics are among the most widely used drugs. Their development over the past century ranges from a documented influence on Freud's Interpretation of Dreams 1 to the synthesis of the ubiquitously popular lidocaine, as described in Chapter 1. For surgical procedures the use of regional, epidural and intrathecal local anesthesia has increased continuously during the past decade. Local anesthetics are also applied by physicians to ameliorate unpleasant sensations and reactions to other procedures, such as tracheal intubation. The presence or the threat of cardiac arrhythmias is often countered by chronic administration oflocal anesthetic-like agents, such as lidocaine or procainamide. Relief of acute pain, accompanying dental manipulations, for example, and of chronic pain are also accomplished with traditional local anesthetics. And over-the-counter formula­ tions of topical local anesthetics provide practitioners of solar indiscretion welcome relief from their otherwise unaccommodating sunburn. In all these applications the final effect of the local anesthetic is an inhibition of electrical activity, accomplished as a reduction or total blockade of action potentials. The primary site of action is the sodium channel, a transmembrane protein which is essential for the influx of sodium ions that subserves impulse generation and propagation in nerves, skeletal muscle, and heart. The detailed mechanisms oflocal anesthetic action are still being investigated and Chapter 2 of this volume provides a current overview of that subject.

Zielgruppe

Research

Autoren/Hrsg.

Strichartz, Gary R.

Weitere Mitwirkende

Arthur, G.R.

Courtney, K.R.

Covino, B.G.

Garfield, J.M.

Gintant, G.A.

Gissen, A.J.

Gugino, L.

Hoffman, B.F.

Raymond, S.A.

Ritchie, J.M.

Strichartz, G.R.

Vandam, L.D.

Inhaltsverzeichnis

1 Some Aspects of the History of Local Anesthesia.- A. Introduction.- B. Freud, Koller and the Early History of Cocaine.- C. Structure and Synthesis of Local Anesthetics.- D. Epinephrine and Local Anesthesia.- E. Toxicity of Local Anesthetics.- F. The Nervous Impulse and the Action of Local Anesthetics.- G. Pharmacokinetics of Local Anesthetics.- H. Summary and Conclusions.- References.- 2 The Action of Local Anesthetics on Ion Channels of Excitable Tissues.- A. Introduction.- B. Physiological Basis of Generation of the Action Potential.- C. The Action of Local Anesthetics on Sodium Channels.- D. Current Questions in Local Anesthetic Action.- E. New Kinds of Local Anesthetic Agents.- F. Effects of Local Anesthetics on Potassium Channels.- G. Conclusion.- References.- 3 Structural Elements which Determine Local Anesthetic Activity.- A. Introduction.- B. Structure and Physico-Chemical Properties of Local Anesthetics.- C. Resolution of Structural Contributions to Potency.- D. Comparisons of Nerve Blocking Actions with Antiarrhythmic Actions of Local Anesthetics.- E. Models for Local Anesthetic Receptors.- References.- 4 Mechanisms of Differential Nerve Block.- A. Introduction.- B. Historical Discussion.- C. Confirmations, Extensions, Clarifications, and Contradictions.- D. Summary and Conclusion.- References.- 5 Pharmacokinetics of Local Anesthetics.- A. Introduction.- B. Factors Affecting the Interpretation of Local Anesthetic Blood Concentrations.- C. Metabolism.- D. Pharmacokinetics in Man.- E. Factors Affecting Pharmacokinetics of Local Anesthetics.- F. Pharmacokinetics in Experimental Animals.- References.- 6 Toxicity and Systemic Effects of Local Anesthetic Agents.- A. Effects on the Central Nervous System.- B. Effects on the Cardiovascular System.- C. Effects on theNeuromuscular Junction.- D. Miscellaneous Effects.- E. Other Toxicological Effects.- F. Treatment of Systemic Toxicity.- G. Local Tissue Toxicity.- H. Summary.- References.- 7 The Role of Local Anesthetic Effects in the Actions of Antiarrhythmic Drugs.- A. Introduction.- B. Electrophysiology of Cardiac Fibers.- C. The Effects of Local Anesthetics on Cardiac Fibers.- D. Antiarrhythmic Effects of Local Anesthetic Agents.- E. Conclusion.- References.- 8 Central Effects of Local Anesthetic Agents.- A. Introduction.- B. Routes of Entry of Local Anesthetic Agents into the CNS.- C. Behavioral Pharmacology of Local Anesthetic Agents.- D. Effects of Local Anesthetics on Electrical Activity of the Brain.- E. Anticonvulsant Properties of Local Anesthetics.- F. Temporal and Spatial Effects of Local Anesthetics at Regional CNS Sites.- G. The Mechanisms Underlying Local Anesthetic-Induced Seizures.- H. Central Nervous System Metabolic Effects of Local Anesthetics.- I. Summary.- References.