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经皮给药后的局部麻醉。I

[Local anesthesia after percutaneous administration. I].

作者信息

Ziegenmeyer J, Meyer F

出版信息

Arch Int Pharmacodyn Ther. 1976 Nov;224(1):164-76.

PMID:1037079
Abstract

Local anesthesia of the intact skin is difficult because of the skin barrier to epicutaneous penetration. Using solutions of local anesthetics in organic agents, which have the ability of penetrating the skin without causing irreversible damage and enhancing the percutaneous absorption of all materials dissolved therein, topical anesthesia seems to be attainable. A satisfactory method for determining pain threshold in uninjured skin of animals has been set up. Measurments of the pricking pain threshold have been made by exposing the skin of guinea-pigs to defined mechanical and electrical stimuli. A nociceptive muscle reflex (twitch) has been taken as the index of pain sensation. The suppression of this twitch has been used as an indicator of anesthetic potency. Two methods have been applied with varying parameters: stimulation at a fixed intensity until the pain threshold was reached (duration of anesthetic effect) and stimulation with increasing stimulus strenght until the cutaneous reflex was elicited (intensity or "depth" of anesthesia). The local anesthetic effects of lidocaine, fomocaine and procaine bases were studied, after dissolving them in dimethyl sulfoxide (DMSO), a wellknown carrier for transmembranal application. The duration of local anesthesia measured by electrical stimuli was longer than that obtained with mechanical ones. Differences are discussed. All results indicate that fomocaine (5%) has a greater local anesthetic potency than procaine (5%) but both are less active than lidocaine (5%). No effect could be seen after application of DMSO alone.

摘要

由于完整皮肤存在屏障,阻碍表面穿透,因此对其进行局部麻醉很困难。使用局部麻醉剂的有机溶液,这些溶液能够穿透皮肤而不造成不可逆损伤,并能增强溶解在其中的所有物质的经皮吸收,似乎可以实现局部麻醉。已经建立了一种测定动物未受伤皮肤疼痛阈值的令人满意的方法。通过将豚鼠的皮肤暴露于特定的机械和电刺激来测量刺痛疼痛阈值。伤害性肌肉反射(抽搐)被用作疼痛感觉的指标。这种抽搐的抑制被用作麻醉效力的指标。已经应用了两种方法,参数不同:以固定强度刺激直至达到疼痛阈值(麻醉效果持续时间),以及以增加的刺激强度刺激直至引发皮肤反射(麻醉强度或“深度”)。将利多卡因、甲哌卡因和普鲁卡因碱溶解在二甲基亚砜(DMSO)中后,研究了它们的局部麻醉效果,DMSO是一种众所周知的用于跨膜应用的载体。通过电刺激测量的局部麻醉持续时间比机械刺激获得的更长。对差异进行了讨论。所有结果表明,甲哌卡因(5%)的局部麻醉效力比普鲁卡因(5%)更强,但两者的活性均低于利多卡因(5%)。单独应用DMSO后未见效果。

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