利多卡因 - 脂质体 - 一个有前途的跨皮疼痛管理前沿
Maria Magdalena Leon1, Alexandra Maștaleru1, Andra Oancea1
1Department of Medical Specialties I, "Grigore T. Popa" University of Medicine and Pharmacy, 700115 Iaşi, Romania.
Journal of clinical medicine
|January 11, 2024
概括
新的凝配方显示出通过皮肤缓解疼痛的前景. 带有脂质体的利多卡因 (L-LP) 在动物模型中表现出显著的麻醉作用,为急性和炎症性疼痛治疗提供了潜在的新选择.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
- 疼痛管理 疼痛管理
背景情况:
- 开发新的透皮药物递送系统 (TDDS) 对于有效的急性和炎症性疼痛治疗至关重要.
- 目前的疗法往往需要提高疗效和副作用的概况.
- 凝配方为通过皮肤给药提供了一个有前途的媒介.
研究的目的:
- 开发和评估用于通过皮肤递送药物的新型凝配方.
- 在急性炎症的动物模型中评估基于利多卡因的配方的止痛效果.
- 为了比较不同配方的疗效,包括脂质体和奇托,与商业麻醉剂.
主要方法:
- 在Wistar大鼠中使用兰巴卡拉基注射诱导了急性炎症.
- 八十只老鼠被分为八个组,接受安慰剂,EMLATM,利多卡因或利多卡因与环极素,脂质体,奇托桑或奇托桑化物结合.
- 在诱导后的不同时间点使用热板,冷板和藻度测试来评估镇痛效果,然后进行组织学评估.
主要成果:
- 与安慰剂和EMLATM (p ≤ 0.001) 相比,利多卡因-脂质体配方 (L-LP) 在冷板测试中表现出最显著的麻醉作用.
- 与安慰剂和EMLATM (p ≤ 0.001,p = 0.018) 相比,利多卡因-基托桑-脂质体配方 (L-CS-LP) 在冷板和热板测试中显示出显著的止痛作用.
- 在治疗后的头120分钟内,L-LP表现出显著的止痛作用.
结论:
- 利多卡因 - 脂酶体 (L-LP) 配方代表了一种具有显著的急性疼痛止痛潜力的新物质.
- 需要使用更大的样本大小进行进一步的研究,以优化剂量以获得最大的止痛效果和最小的副作用.
- 这些发现支持开发用于疼痛管理的先进的透皮系统.
相关概念视频
Local Anesthetics: Common Agents and Their Applications
448
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...
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...
448
Local Anesthetics: Clinical Application as Surface, Infiltration, and Conduction Block Anesthesia
1.1K
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...
1.1K
Local Anesthetics: Chemistry and Structure-Activity Relationship
4.4K
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...
4.4K
Local Anesthetics: Mechanism of Action
2.2K
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 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...
2.2K
Local Anesthetics: Pharmacokinetics
760
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...
760
Local Anesthetics: Clinical Application as Epidural Anesthesia
434
Epidural anesthetics are administered in the fat-filled epidural space, the outermost part of the spinal canal. This technique is commonly employed for pain management and anesthesia during lower abdomen and pelvis surgeries or labor and delivery.
Since epidural anesthetics can be infused through an epidural catheter, all types of drugs, including short-acting ones, can be administered. Chloroprocaine and lidocaine are examples of short and long-duration anesthetics, respectively. Bupivacaine...
Since epidural anesthetics can be infused through an epidural catheter, all types of drugs, including short-acting ones, can be administered. Chloroprocaine and lidocaine are examples of short and long-duration anesthetics, respectively. Bupivacaine...
434


