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Local Anesthetics: Chemistry and Structure-Activity Relationship

Local Anesthetics: Chemistry and Structure-Activity Relationship

Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...

Local Anesthetics: Common Agents and Their Applications

Local Anesthetics: Common Agents and Their Applications

Local anesthetics (LAs) are commonly used for various applications in medical and dental procedures. Some of the common agents used are cocaine, lidocaine, and bupivacaine.
Cocaine is an ester of benzoic acid and methylecgogine. It is used to anesthetize and vasoconstrict locally. Currently, it is used primarily for topical applications. It is beneficial for surgeries on the upper respiratory tract, providing anesthesia and shrinking the mucosa. Cocaine in the form of cocaine hydrochloride is...

Parenteral Anesthetics: Overview

Parenteral Anesthetics: Overview

Intravenous anesthetics are drugs administered parenterally to induce anesthesia or sedation. Propofol is a widely used agent formulated as a 1% emulsion in soybean oil, glycerol, and egg phosphatide. It induces rapid anesthesia primarily due to its rapid distribution from the bloodstream to target tissues and is metabolized in the liver. However, it can cause significant pain on injection and hypertriglyceridemia. Fospropofol, a water-based prodrug of propofol, lacks these adverse effects.

General Anesthesia: Overview

General Anesthesia: Overview

Anesthesia is a medical procedure that uses drugs for CNS suppression to enable painless surgeries and procedures. The selection of anesthetics is influenced by their pharmacokinetic properties, side effects, and patient characteristics. Various types of anesthesia include general, local, regional, spinal, and inhalational.
General anesthesia induces unconsciousness in the whole body, while the others target specific areas or sensations. It is administered to minimize adverse effects, maintain...

Local Anesthetics: Clinical Application as Epidural Anesthesia

Local Anesthetics: Clinical Application as Epidural Anesthesia

Epidural anesthetics are administered in the fat-filled epidural space, the outermost part of the spinal canal. This technique is commonly employed for pain management and anesthesia during lower abdomen and pelvis surgeries or labor and delivery.
Since epidural anesthetics can be infused through an epidural catheter, all types of drugs, including short-acting ones, can be administered. Chloroprocaine and lidocaine are examples of short and long-duration anesthetics, respectively. Bupivacaine...

Inhalational Anesthetics: Overview

Inhalational Anesthetics: Overview

Inhalation anesthetics are drugs that induce general anesthesia upon inhalation. They work by increasing the sensitivity of GABAA receptors or inhibiting NMDA receptors, leading to a decrease in central nervous system activity. The depth of anesthesia can be rapidly adjusted by changing the concentration of the inhaled gas. Some common examples of inhalational anesthetics include volatile liquids like isoflurane, desflurane, sevoflurane and gases like xenon and nitrous oxide. Isoflurane, a...

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Related Experiment Video

Updated: Jun 22, 2026

A Protocol for Measuring Cue Reactivity in a Rat Model of Cocaine Use Disorder

A Protocol for Measuring Cue Reactivity in a Rat Model of Cocaine Use Disorder

Published on: June 18, 2018

[Anesthesia in cocaine users.].

Ana Luft¹, Florentino Fernandes Mendes

¹Fundação Faculdade Federal de Ciências Médicas de Porto Alegre.

Revista Brasileira De Anestesiologia

|May 26, 2009

Summary

Anesthesiologists must understand cocaine

Area of Science:

Anesthesiology
Pharmacology
Toxicology

Context:

Cocaine is a significant cause of drug-related mortality.
Perioperative complications arise in patients with acute cocaine intoxication or chronic use.
Understanding cocaine's effects is crucial for managing surgical patients.

Purpose:

To review cocaine's neurophysiology, pharmacology, and physiopathological consequences.
To examine cocaine's interactions with anesthetic agents and techniques.

Summary:

Cocaine abuse presents unique challenges in perioperative care.
Anesthesiologists require comprehensive knowledge of cocaine's adverse effects.
Both regional and general anesthesia pose risks for cocaine users.

More Related Videos

Assessment of Cocaine-induced Behavioral Sensitization and Conditioned Place Preference in Mice

Assessment of Cocaine-induced Behavioral Sensitization and Conditioned Place Preference in Mice

Published on: February 18, 2016

Related Experiment Videos

Last Updated: Jun 22, 2026

A Protocol for Measuring Cue Reactivity in a Rat Model of Cocaine Use Disorder

A Protocol for Measuring Cue Reactivity in a Rat Model of Cocaine Use Disorder

Published on: June 18, 2018

Assessment of Cocaine-induced Behavioral Sensitization and Conditioned Place Preference in Mice

Assessment of Cocaine-induced Behavioral Sensitization and Conditioned Place Preference in Mice

Published on: February 18, 2016

Impact:

Early recognition and management of cocaine-associated complications improve patient outcomes.
Preparedness is essential for anesthesiologists managing patients with cocaine use history.
This review facilitates safer anesthetic practices for this patient population.