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Related Concept Videos

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: Adverse Effects01:12

Local Anesthetics: Adverse Effects

While local anesthetics are generally safe and well-tolerated, they can occasionally cause adverse effects that vary in severity. Local anesthetics can induce toxicity at two distinct levels. They can either produce local effects through direct contact with the neural elements or be absorbed into the bloodstream from the injection site, leading to systemic effects.
Once absorbed into the systemic circulation, local anesthetics can affect the organs that depend on the functioning of sodium...
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: Clinical Application as Spinal Anesthesia01:11

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: 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...

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Topical Airway Anesthesia for Awake-endoscopic Intubation Using the Spray-as-you-go Technique with High Oxygen Flow
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Prolonged duration local anesthesia with minimal toxicity.

Hila Epstein-Barash1, Iris Shichor, Albert H Kwon

  • 1Laboratory for Biomaterials and Drug Delivery, Department of Anesthesiology, Division of Critical Care Medicine, Children's Hospital, Harvard Medical School, 300 Longwood Avenue, Boston, MA 02115, USA.

Proceedings of the National Academy of Sciences of the United States of America
|April 15, 2009
PubMed
Summary

New liposomal formulations of saxitoxin (STX) provide prolonged local anesthesia for up to 7.5 days. These novel drug delivery systems minimize local tissue toxicity and systemic side effects, improving pain management.

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Area of Science:

  • Pharmacology
  • Drug Delivery
  • Pain Management

Background:

  • Injectable local anesthetics are limited by short duration and potential toxicity.
  • Developing long-acting anesthetic formulations is crucial for improved periprocedural care.
  • Existing anesthetics can cause systemic toxicity, local tissue damage, and inflammation.

Purpose of the Study:

  • To develop and evaluate liposomal formulations of saxitoxin (STX) for prolonged local anesthesia.
  • To assess the toxicity and efficacy of these novel formulations in preclinical models.
  • To investigate the potential of controlled saxitoxin release for extended nerve blockade.

Main Methods:

  • Liposomal formulations of saxitoxin (STX), bupivacaine, and dexamethasone were created.
  • In vitro release kinetics and cytotoxicity (myotoxicity and neurotoxicity) were evaluated.
  • Sciatic nerve blockade duration and local/systemic toxicity were assessed in Sprague-Dawley rats.

Main Results:

  • Liposomal STX and dexamethasone achieved nerve blockade lasting up to 7.5 days.
  • Bupivacaine exhibited concentration- and time-dependent myotoxicity and neurotoxicity in vitro.
  • Minimal local toxicity and no nerve injury were observed with STX-based liposomes; systemic toxicity linked to high dexamethasone loading.

Conclusions:

  • Controlled release of saxitoxin via liposomal formulations offers a promising strategy for very prolonged nerve blocks.
  • These formulations demonstrate potential for safe and effective long-term pain management with reduced local and systemic toxicity.
  • The developed liposomal STX delivery system overcomes limitations of conventional local anesthetics.