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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...

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: Mechanism of Action

Local Anesthetics: Mechanism of Action

Local anesthetics (LAs) block sensory and motor impulses by inhibiting the sodium channels on the nerve cell membranes. This induces temporary loss of sensation, relieving pain in a specific body area.
Local anesthetics are amphiphilic molecules consisting of a hydrophobic aromatic part linked to a hydrophilic group by an ester or amide linkage. They are weak bases and are usually available as salts, which increases their solubility and stability. Once administered, LAs exist in the body either...

Local Anesthetics: Pharmacokinetics

Local Anesthetics: Pharmacokinetics

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...

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...

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Optogenetic Activation of Afferent Pathways in Brain Slices and Modulation of Responses by Volatile Anesthetics

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[Local anaesthetics].

Shems Al-Hayder¹, Sofie Marie Hody, Lene Birk-Sørensen

¹shemsalder@hotmail.com.

Ugeskrift for Laeger

|October 17, 2019

Summary

This summary is machine-generated.

Local anaesthetics block sodium channels to reduce pain during medical procedures. This review covers their pharmacology, use, adjuvants, and adverse effects for safe clinical application.

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Area of Science:

Pharmacology
Neuroscience
Anesthesiology

Background:

Local anaesthetics are essential in clinical practice for pain management.
They function by selectively blocking sodium channels in nerve cell membranes.
This mechanism impedes nerve depolarization and nociception transmission.

Purpose of the Study:

To provide an updated review of local anaesthetic pharmacology.
To discuss the clinical utilization of local anaesthetics.
To overview related aspects including adjuvants, allergies, and adverse effects.

Main Methods:

Literature review of pharmacology and clinical utilization.
Synthesis of information on adjuvants, allergies, and adverse effects.

Main Results:

Local anaesthetics are weak organic bases effective in pain reduction.
They are generally safe and widely used in procedures like biopsies and surgery.
The review details their mechanism of action and practical applications.

Conclusions:

Local anaesthetics are crucial for effective pain control in various medical settings.
Understanding their pharmacology and potential adverse effects is vital for safe use.
This review serves as a comprehensive resource for clinicians.