Local Anaesthetics. VII. Local Anaesthetic Potency and Inhibition of Acetylcholinesterase.

2009 ◽  
Vol 12 (1) ◽  
pp. 109-114 ◽  
Author(s):  
Jens Chr. Skou.
Author(s):  
Giorgio Capogna

In this chapter, the rationale for the choice of commonly used local anaesthetics—racemic bupivacaine, ropivacaine, and levobupivacaine—is reviewed, particularly with respect to their potency and differential block. Epidural and spinal dosing for labour analgesia and the role of ‘up–down’ studies to determine the minimum local anaesthetic concentration (MLAC) for labour analgesia is explained. Applying the MLAC model has enabled clinical comparisons at equipotent concentrations and doses. It has also quantified what contribution opioids have on the overall effectiveness of the analgesic mixture, provided a means of optimizing combinations of local anaesthetic–opioid solutions, examined the effect of inter-individual and obstetric variables on local anaesthetic potency, and provided a pharmacological-based rationale for analgesia solutions used for labour analgesia.


1975 ◽  
Vol 148 (3) ◽  
pp. 527-531 ◽  
Author(s):  
D R Fayle ◽  
G J Barritt ◽  
F L Bygrave

The effect of the local anaesthetic, butacaine, on adenine nucleotide binding and translocation in rat liver mitochondria partially depleted of their adenine nucleotide content was investigated. The range of butacaine concentrations that inhibit adenine nucleotide translocation and the extent of the inhibition are similar to the values obtained for native mitochondria. Butacaine does not alter either the total number of atractyloside-sensitive binding sites of depleted mitochondria, or the affinity of these sites for ADP or ATP under conditions where a partial inhibition of the rate of adenine nucleotide translocation is observed. The data are consistent with an effect of butacaine on the process by which adenine nucleotides are transported across the mitochondrial inner membrane rather than on the binding of adenine nucleotides to sites on the adenine nucleotide carrier. The results are briefly discussed in relation to the use of local anaesthetics in investigations of the mechanism of adenine nucleotide translocation.


Author(s):  
Gareth Allen ◽  
Rebecca Butler

Local anaesthetics are frequently used in both primary and secondary care. These agents transiently reduce the nervous conduction of nociceptive signals, reducing sensations of pain. In primary care, local anaesthetics are often used for minor surgical procedures. However, there are other uses for these agents. It is important to understand the issues encountered when using local anaesthetics in primary care. This review will cover clinical use, relevant pharmacology and adverse effects of the different local anaesthetic preparations.


2002 ◽  
Vol 27 (5) ◽  
pp. 462-464 ◽  
Author(s):  
T. M. LAWRENCE ◽  
V. V. DESAI

This randomized, double-blinded study assessed the effectiveness of a topical anaesthetic, eutectic mixture of local anaesthetics (EMLA), in reducing pain associated with carpal tunnel release performed under local anaesthetic. Fifty-six patients undergoing carpal tunnel release under local anaesthetic were randomized into either EMLA ( n=29) or placebo ( n=27) groups. Visual analogue pain scores were obtained for needle insertion, injection of anaesthetic and surgery itself. Pain scores were significantly less for needle insertion ( P=0.001) and injection of anaesthetic ( P=0.0005). Scores related to surgery were also lower in the EMLA group, but this did not reach statistical significance.


1990 ◽  
Vol 271 (1) ◽  
pp. 269-272 ◽  
Author(s):  
M Grouselle ◽  
O Tueux ◽  
P Dabadie ◽  
D Georgescaud ◽  
J P Mazat

Using the laser dye rhodamine 123, we demonstrated that local anaesthetics can reach mitochondria in cell culture and reversibly decrease, or even collapse, their transmembrane potential. This effect is highly dependent on the lipid-solubility of the local anaesthetic and can be facilitated by the presence of a lipophilic anion.


1988 ◽  
Vol 102 (7) ◽  
pp. 628-629 ◽  
Author(s):  
D. A. Jonathan ◽  
N. S. Violaris

AbstractThe relative efficacy of Cocaine and Lignocaine as local anaesthetic agents in the nose were compared. Twenty-five patients undergoing bilateral intra-nasal antroscopy under local anaesthetic were used as their own controls when one nasal cavity was anaesthetised with Cocaine and the other with Lignocaine. On 56 per cent of occasions the patients experienced no difference in the level of discomfort. However, on 36 per cent of occasions Cocaine was noted to give better subjective anaesthesia as compared with 8 per cent of occasions when Lignocaine was superior.


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