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Related Concept Videos

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: 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: 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...
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: 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...

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Local anaesthetics.

J French1, L M Sharp

  • 1Nottingham University Hospitals NHS Trust, City Hospital Campus, UK. james.french@nuh.nhs.uk

Annals of the Royal College of Surgeons of England
|March 7, 2012
PubMed
Summary
This summary is machine-generated.

Local anesthetics (LAs) have varying properties influencing their clinical use. Understanding LA pharmacology and physicochemical properties is key for effective pain management and treating toxicity with lipid rescue therapy.

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Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Anesthesiology

Background:

  • Local anesthetics (LAs) are crucial for regional anesthesia.
  • Amide-type LAs are currently more prevalent than ester types.
  • Knowledge of LA properties guides clinical application and safety.

Purpose of the Study:

  • To elucidate the pharmacological and physicochemical properties of local anesthetics.
  • To emphasize the importance of these properties in predicting anesthetic behavior.
  • To highlight the role of lipid rescue in managing local anesthetic toxicity.

Main Methods:

  • Review of pharmacological principles governing local anesthetics.
  • Analysis of physicochemical properties influencing onset and duration.
  • Discussion of concentration expression and its clinical relevance.
  • Examination of lipid rescue therapy as a treatment for local anesthetic systemic toxicity (LAST).

Main Results:

  • Amide LAs are favored in current clinical practice.
  • Pharmacology and physicochemical characteristics predict onset, duration, and suitability of LAs.
  • Standardized concentration expression (e.g., 1% = 10 mg/ml) aids clinical dosing.
  • Lipid rescue therapy is a proven effective treatment for LA toxicity.

Conclusions:

  • Understanding local anesthetic properties is essential for optimal clinical outcomes.
  • Amide LAs dominate current use due to their favorable profiles.
  • Accurate prediction of LA behavior and effective management of toxicity are critical for patient safety.