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Related Concept Videos

Local Anesthetics: Common Agents and Their Applications01:23

Local Anesthetics: Common Agents and Their Applications

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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...
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Local Anesthetics: Pharmacokinetics01:13

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: Chemistry and Structure-Activity Relationship01:30

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...
6.9K
Local Anesthetics: Clinical Application as Surface, Infiltration, and Conduction Block Anesthesia01:30

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

2.3K
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...
2.3K
Local Anesthetics: Mechanism of Action01:23

Local Anesthetics: Mechanism of Action

3.7K
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...
3.7K
Local Anesthetics: Clinical Application as Intravenous Regional Anesthesia01:16

Local Anesthetics: Clinical Application as Intravenous Regional Anesthesia

1.6K
Intravenous regional anesthesia or the Bier block technique is used to anesthetize a specific limb or extremity. It uses exsanguinated or blood-drained vessels to transport local anesthetics or LAs to the peripheral nerve trunks. Lidocaine without vasoconstrictors like epinephrine is most commonly used for this technique. Other drugs used are prilocaine, ropivacaine, and chloroprocaine. Bupivacaine is not recommended for this technique due to its high cardiac toxicity.
One of the advantages of...
1.6K

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Related Experiment Video

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Subcutaneous Trigeminal Nerve Field Stimulation for Refractory Facial Pain
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Extended local anesthesia enabled by flavonoid permeation enhancers.

Yiyuan Han1, Matthew Torre2, Xiaojing Ma1

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

Proceedings of the National Academy of Sciences of the United States of America
|March 2, 2026
PubMed
Summary

Selected flavonoids, like puerarin, significantly extend the nerve-blocking effects of local anesthetics. These natural compounds enhance drug delivery and offer a safer, long-lasting, nonopioid pain relief alternative.

Keywords:
biological barrierchemical permeation enhancerdrug deliveryflavonoidlocal anesthesia

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Area of Science:

  • Pharmacology
  • Biomedical Science
  • Pain Management

Background:

  • Site 1 sodium channel blockers (S1SCBs) are potent local anesthetics but have short durations of action.
  • High doses of S1SCBs can lead to systemic toxicity, limiting their clinical use.
  • There is a need for safe and effective methods to prolong the action of local anesthetics.

Purpose of the Study:

  • To investigate the potential of flavonoids as chemical permeation enhancers (CPEs) for S1SCBs.
  • To evaluate the ability of flavonoids to prolong the nerve block duration of S1SCBs.
  • To assess the safety profile of flavonoids as CPEs compared to conventional agents.

Main Methods:

  • Tested puerarin (PUE), naringenin, and kaempferol for their effects on S1SCB duration.
  • Utilized tympanic membrane (TM) permeation and sciatic nerve fluorescence models to assess drug penetration.
  • Coencapsulated tetrodotoxin (TTX) and PUE into liposomes for sustained release studies.

Main Results:

  • Flavonoids prolonged S1SCB nerve block duration by 4- to 25-fold.
  • Flavonoids demonstrated increased drug penetration across biological barriers (TM, nerve).
  • Liposomal coencapsulation of TTX and PUE resulted in anesthesia lasting over 25 days.

Conclusions:

  • Flavonoids act as safe and effective chemical permeation enhancers for S1SCBs.
  • Flavonoid compounds offer a promising platform for developing long-acting, nonopioid pain therapies.
  • Flavonoids represent attractive alternatives to conventional CPEs in various biomedical applications.