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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...

Local Anesthetics: Chemistry and Structure-Activity Relationship

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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: 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...

Local Anesthetics: Clinical Application as Spinal Anesthesia

Local Anesthetics: Clinical Application as Spinal Anesthesia

Spinal anesthetics are given during lower abdomen and limb surgeries to block sensory and motor neurons. They are administered in the mid to low lumbar regions, primarily acting on the cauda equina's nerve roots. The blockade level depends on the local anesthetic (LA) concentration. Usually, low LA concentrations are sufficient to block sensory fibers, while only high LA concentrations block motor fibers. Other factors like injection volume and speed, the patient's posture, and the drug...

Local Anesthetics: Clinical Application as Surface, Infiltration, and Conduction Block Anesthesia

Local Anesthetics: Clinical Application as Surface, Infiltration, and Conduction Block Anesthesia

Depending on the target organ, local anesthetics (LAs) can be administered via various routes. In surface anesthesia, LAs are applied directly to the surface of the skin or mucous membranes. It is widely used for topical skin numbing before venipuncture or minor surgical procedures. Commonly used surface local anesthetics are lidocaine or benzocaine sprays or creams. Surface anesthesia occurs within 5 minutes and lasts for about 60 minutes. One of the main disadvantages of topical anesthesia is...

Local Anesthetics: Pharmacokinetics

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The potency and duration of action of local anesthetics (LAs) are determined by their pharmacokinetics. Pharmacokinetics describes how LAs are absorbed, distributed, metabolized, and eliminated from the body. When administered to the vascular tissues, LAs are quickly absorbed and enter the systemic circulation, reducing their localized effects. Adding vasoconstrictors such as epinephrine to LAs reduces their absorption into the systemic circulation, making them clinically effective. The...

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Local anesthetics and their adjuncts.

Jean-Xavier Mazoit¹

¹Département d'Anesthésie-Réanimation, Hôpitaux Universitaires Paris-Sud, AP-HP, Le Kremlin-Bicětre, France. jean-xavier.mazoit@u-psud.fr

Paediatric Anaesthesia

|September 20, 2011

Summary

This summary is machine-generated.

Local anesthetics (LA) block nerve impulses by inactivating sodium channels. This article focuses on amide-type LAs, which are metabolized by the liver.

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Area of Science:

Pharmacology
Neuroscience
Medicinal Chemistry

Background:

Local anesthetics (LA) are crucial for nerve impulse blocking.
They function by inactivating voltage-gated sodium channels, preventing action potentials.
Two main classes exist: amino esters and amino amides.

Purpose of the Study:

To review the properties and metabolism of amide-type local anesthetics.
To differentiate amide LAs from amino esters based on metabolic pathways.

Main Methods:

Literature review focusing on amide local anesthetics.
Analysis of metabolic pathways for amino esters versus amino amides.

Main Results:

Amide local anesthetics are metabolized exclusively by the liver.
Amino esters are hydrolyzed by plasma pseudocholinesterases.
This distinction is critical for understanding LA pharmacokinetics.

Conclusions:

The liver is the primary site for amide LA metabolism.
Understanding metabolic differences is key for safe and effective clinical use of local anesthetics.