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Related Concept Videos

Local Anesthetics: Common Agents and Their Applications01:23

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 Relationship01:30

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: Pharmacokinetics01:13

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 Anesthesia01:30

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: Clinical Application as Epidural Anesthesia01:29

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: Mechanism of Action01:23

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...

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Related Experiment Video

Updated: May 22, 2026

An Injectable and Drug-loaded Supramolecular Hydrogel for Local Catheter Injection into the Pig Heart
10:28

An Injectable and Drug-loaded Supramolecular Hydrogel for Local Catheter Injection into the Pig Heart

Published on: June 7, 2015

Extended release formulations for local anaesthetic agents.

C F Weiniger1, L Golovanevski, A J Domb

  • 1Department of Anesthesiology and Critical Care Medicine, Hadassah Hebrew University Medical Centre, Jerusalem, Israel. carolynfweiniger@gmail.com

Anaesthesia
|May 22, 2012
PubMed
Summary

Encapsulating local anesthetics in biodegradable carriers extends their action and improves safety by slowing release. This review covers various extended-duration formulations, including liposomes and polymer microspheres.

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Area of Science:

  • Pharmacology
  • Materials Science
  • Drug Delivery

Background:

  • Systemic toxicity from local anesthetic overdose is a significant clinical concern.
  • Biodegradable carriers offer a strategy to prolong anesthetic action and enhance safety profiles.
  • Naturally occurring local anesthetics show potential for reducing systemic and neurotoxicity.

Purpose of the Study:

  • To review extended-duration local anesthetic formulations currently in development or clinical use.
  • To analyze the duration of action, rationale, and limitations of various encapsulation strategies.
  • To highlight the potential of biodegradable carriers in improving local anesthetic safety and efficacy.

Main Methods:

  • Review of current literature on extended-duration local anesthetic formulations.
  • Analysis of encapsulation techniques including liposomes, Poly(lactic-co-glycolic acid) microspheres, and polymer systems.
  • Examination of both synthetic and natural local anesthetics in advanced formulations.

Main Results:

  • Various formulations like liposomes, PLGA microspheres, and polymer systems demonstrate prolonged anesthetic action.
  • Encapsulation strategies aim to reduce systemic toxicity by controlling drug release rates.
  • Natural local anesthetics show promise in mitigating neurotoxicity.

Conclusions:

  • Biodegradable carriers significantly enhance the safety and duration of local anesthetics.
  • Different formulations (liposomes, polymers) offer distinct advantages and limitations.
  • Further direct comparisons are needed to fully elucidate the comparative efficacy and safety of these advanced drug delivery systems.