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Ester combination local anesthetic

A technology of local anesthesia and anesthesia, applied in the direction of anesthesia, drug combination, prosthesis, etc., can solve discomfort, pain and other problems

Inactive Publication Date: 2006-02-01
THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, currently used local anesthetics such as lidocaine can cause pain and discomfort (eg, stinging) when administered

Method used

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  • Ester combination local anesthetic
  • Ester combination local anesthetic
  • Ester combination local anesthetic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Example 1: Formulation

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Embodiment 2

[0103] Example 2: Comparison of Local Anesthetics Administered Alone or in Combination

[0104] In a study in rats, the initiation and discontinuation of sciatic nerve blocks by lidocaine, bupivacaine, tetracaine and 2-chloroprocaine were examined. Three different modalities were tested: (1) pain (eg, squeezing and retracting); (2) proprioception (eg, ability to square the paw on a table); and (3) motor intensity (eg, the paw could be placed on a scale apply downward pressure). In each case, the same volume of local anesthetic was tested. The property of interest is withdrawal from pinch pain. Each local anesthetic was tested on 5 rats of approximately the same size and age. The result is as figure 1 shown.

[0105] figure 1 The upper panel shows the time course of sciatic nerve blockade of 2.0%, the strongest concentration of commercially available lidocaine. At this concentration, lidocaine started to block almost immediately (ie 100% at the first time point tested, w...

Embodiment 3

[0108] Example 3: Demonstration of synergistic effect of combination administration of local anesthetics

[0109] figure 2 Shows the onset and duration of sciatic nerve blockade in rats following administration of 2% 2-chloroprocaine. Without administration of tetracaine, the duration of hypoblockia was significantly shorter, with complete sensory blockade lasting only about 30 minutes. In addition, the block onset of 2-chloroprocaine administration was slower than that of tetracaine administration, indicating that tetracaine played a synergistic effect in enhancing the onset of anesthesia with 2-chloroprocaine.

[0110] image 3 Onset and duration of sciatic nerve block following administration of 0.22% tetracaine (upper panel) or 0.5% tetracaine (lower panel) are shown. Surprisingly, neither concentration of tetracaine produced sufficient sensory blockade (eg, less than 60% sensory blockade). Complete sensory blockade was achieved at lower concentrations of tetracaine c...

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Abstract

The present invention provides compositions and methods for improved local anesthesia and / or analgesia, in which onset of action is rapid, the risk of toxicity is low, and the effect is sustained. More particularly, the present invention provides a combination of at least two ester anesthetics for administration to a subject, where at least one ester anesthetic provides a rapid onset of action and at least one ester anesthetic provides sustained activity. The compositions of the present invention are useful for the production of analgesia and / or anesthesia and are particularly useful for the prophylaxis and / or treatment of pain.

Description

Background of the invention [0001] Local anesthetics are drugs that produce a reversible loss of sensation in a specific part of the body. Most clinically useful local anesthetics consist of an aromatic ring with a carbonyl-containing moiety attached to a substituted amino group through a carbon chain. There are two main classes, determined by the nature of the carbonyl-containing linking group. Anesthetics with ester linkages include cocaine, procaine, tetracaine, benzocaine, amethocaine, and chloroprocaine. Anesthetics with an amide linkage include lidocaine, prilocaine, mepivacaine, ropivacaine, etidocaine, and levobupivacaine and bupivacaine. There are important practical differences between these two classes of local anesthetics. Esters are less stable than amides chemically and are rapidly hydrolyzed in humans by plasma cholinesterase and other esterases. This metabolism generally prevents the ester from accumulating in the body to toxic levels, even with repeated or ...

Claims

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Application Information

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IPC IPC(8): A61K31/625A61K31/135A61F2/00A61KA61K9/00A61K31/215A61K31/245A61MA61M37/00
CPCA61K9/0014A61K31/245A61K9/0019A61P23/02A61P25/02A61K2300/00A61K31/135A61K31/215A61K31/625A61M37/00
Inventor S·L·谢弗
Owner THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
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