Local anaesthetic agents

2017 ◽  
Author(s):  
Malachy O. Columb
Keyword(s):  
Local Anaesthetic ◽  
Neuronal Damage ◽  
Scientific Evidence ◽  
Local Anaesthetics ◽  
Systemic Toxicity ◽  
Lipid Solubility ◽  
Blood Concentrations ◽  
Anaesthetic Agents ◽  
Weak Bases ◽  
Initiation And Propagation

Local anaesthetic agents cause a pharmacologically induced reversible neuropathy characterized by axonal conduction blockade. They act by blocking the sodium ionophore and exhibit membrane stabilizing activity by inhibiting initiation and propagation of action potentials. They are weak bases consisting of three components: a lipophilic aromatic ring, a link, and a hydrophilic amine. The chemical link classifies them as esters or amides. Local anaesthetics diffuse through the axolemma as unionized free-base and block the ionophore in the quaternary ammonium ionized form. The speed of onset of block is therefore dependent on the pKa of the agent and the ambient tissue pH. Esters undergo hydrolysis by plasma esterases and amides are metabolized by hepatic microsomal mixed-function oxidases. Local anaesthetics are bound in the blood to α‎1-acid glycoproteins. Pharmacological potency is dependent on the lipid solubility of the drug as is the potential for systemic toxicity. The blood concentrations required to cause cardiovascular system (CVS) collapse and early central nervous system (CNS) toxicity are used to quantify the CVS:CNS toxicity ratio. Local anaesthetics also have the potential to induce direct neuronal damage. Intravenous lipid emulsion is used for the treatment of systemic toxicity but the scientific evidence is inconsistent. With regard to the pipecoloxylidine local anaesthetics, early evidence indicated that the S- was less toxic than the R-enantiomer. However, clinical research using minimum local analgesic concentration designs suggests that reduced systemic toxicity and motor block sparing is mainly explained by potency rather than enantiomerism.

scholarly journals Effect of local anaesthetics on mitochondrial membrane potential in living cells

1990 ◽  
Vol 271 (1) ◽  
pp. 269-272 ◽  
Author(s):  
M Grouselle ◽  
O Tueux ◽  
P Dabadie ◽  
D Georgescaud ◽  
J P Mazat
Keyword(s):  
Cell Culture ◽  
Membrane Potential ◽  
Local Anaesthetic ◽  
Mitochondrial Membrane ◽  
Transmembrane Potential ◽  
Local Anaesthetics ◽  
Living Cells ◽  
Lipid Solubility ◽  
Laser Dye ◽  
Lipophilic Anion

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.

Comparison of cocaine and lignocaine as intranasal local anaesthetics

1988 ◽  
Vol 102 (7) ◽  
pp. 628-629 ◽  
Author(s):  
D. A. Jonathan ◽  
N. S. Violaris
Keyword(s):  
Nasal Cavity ◽  
Local Anaesthetic ◽  
Local Anaesthetics ◽  
The Other ◽  
Relative Efficacy ◽  
Anaesthetic Agents

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.

scholarly journals Private Practitioners Knowledge of Local Anaesthetic Systemic Toxicity (LAST)

2021 ◽  
Vol 10 (41) ◽  
pp. 3571-3576
Author(s):  
Neha Yadav ◽  
Reshu Madan Sanan ◽  
Shefali Phogat ◽  
Nisha Yadav ◽  
Nupur Dabas ◽  
...  
Keyword(s):  
Local Anaesthetic ◽  
Anaesthetic Agent ◽  
Nerve Impulse ◽  
Local Anaesthetics ◽  
Systemic Toxicity ◽  
Blood Levels ◽  
Private Practitioners ◽  
Adequate Knowledge ◽  
Online Mode ◽  
Administration Methods

BACKGROUND Local anaesthetics (LAs) by definition are drugs that reversibly block the transmission of a nerve impulse, causing reversible absence of pain sensations without affecting consciousness. As a complication of local anaesthetic administration, a condition called as local anaesthetic systemic toxicity (LAST) can occur which affects central nervous system (CNS) and cardiovascular system (CVS). Local anaesthetic systemic toxicity is a very serious condition that can cause death. In LAST, blood levels of anaesthetic agent exceed the maximum dose, usually as a result of multiple injections or an accidental injection into a vein. The main objective of this survey was to assess the knowledge of LAST among private practitioners and to spread awareness about this common but often neglected complication of local anaesthetic administration. METHODS A survey was conducted with a questionnaire comprising of 15 questions for 251 private practitioners (registered in Indian Dental Association, Gurugram). The survey was mailed to the participants and the response was collected through online mode only. Using Excel program, the results were organized in graphs and tables, and presented as descriptive statistics. RESULTS Of the 251 surveys sent online, 151 were completed, with a survey completion rate of 60 %. On an average, only 39.9 % of the participating dentists had adequate knowledge of local anaesthetic systemic toxicity. Based on the survey, only 3.3 % of participating dentists knew how to use lipid treatment and 55.6 % had no idea about lipid treatment. CONCLUSIONS If LAST occurs, the key is to recognize it immediately and institute appropriate management. Based on the survey, there is a need to create awareness about local anaesthetic systemic toxicity and its management among dentists. KEY WORDS Local Anaesthesia, Last, Complication, Toxicity, Overdose

scholarly journals Antimicrobial Activity of Lidocaine, Bupivacaine, Mepivacaine and Ropivacaine on Staphylococcus epidermidis, Staphylococcus aureus and Bacillus subtilis

2017 ◽  
Vol 10 (1) ◽  
pp. 1-4 ◽  
Author(s):  
S. Neuwersch ◽  
M. Köstenberger ◽  
S. Sorschag ◽  
W. Ilias ◽  
R. Likar
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Local Anaesthetic ◽  
Staphylococcus Epidermidis ◽  
Diagnostic Procedures ◽  
Local Anaesthetics ◽  
Zone Of Inhibition ◽  
Anaesthetic Agents ◽  
Mueller Hinton Agar

Introduction: Various studies have shown a possible antimicrobial activity of different local anaesthetics, which may affect the results of microbial assessment of biopsies. The purpose of this study was to test the antimicrobial activity of different commonly used anaesthetic agents on Staphylococcus epidermidis, Staphylococcus aureus and Bacillus subtitles to reproduce data and to compare the findings. Methods: Local anaesthetics tested were commercially available solutions of lidocaine (Xyloneural®, Xylanaest pur.®), bupivacaine (Bucain®), mepivacaine (Mecain®) and ropivacaine (Naropin®, Ropinaest®).2%, 1%, 0.5%, 0.25% and 0.1% (20, 10, 5, 2.5, 1 mg/ml) dilutions of these local anaesthetics were prepared with sterile 0.9% saline. Bacteria used in this study were Staphylococcus epidermidis, Staphylococcus aureus and Bacillus subtilis. 10 μl of different local anaesthetic dilution placed on thin wafers were added to Mueller Hinton Agar and cultured. After 24 hours, a zone of inhibition around the wafers was evaluated. Results: Local anaesthetics in different concentrations did not show any zone of inhibition on Staphylococcus epidermidis, Staphylococcus aureus or Bacillus subtilis. Conclusion: In summary, neither lidocaine, bupivacaine, mepivacaine nor ropivacaine showed an antibacterial effect on Staphylococcus epidermidis, Staphylococcus aureus and Bacillus subtilis. Implications: Due to these findings this local anaesthetics can be used in daily clinical routine to perform pain free diagnostic procedures in which culture specimens are to be obtained. Due to inconsistent results in prior studies, we recommend to use the lowest concentration possible of the local anaesthetic, also to avoid other possible side effects of local agents.

A review of the human and veterinary literature on local anaesthetics and their intraarticular use

2010 ◽  
Vol 23 (04) ◽  
pp. 225-230 ◽  
Author(s):  
I. Polis ◽  
F. Verschooten ◽  
Van Ryssen ◽  
D. Van Vynckt
Keyword(s):  
Local Anaesthetic ◽  
Local Anaesthetics ◽  
Pain Tolerance ◽  
Pain Response ◽  
Diagnostic Challenge ◽  
Future Studies ◽  
Anaesthetic Agents

SummaryLameness in dogs is often a diagnostic challenge. In many cases it is difficult to determine the exact localisation of lameness because of the absence of palpable changes, or because of unreliable pain response due to high pain tolerance, stress or aggression of the dog. In horses and humans, intra-articular administration of local anaesthetics is commonly used for diagnostic purposes. In this review, information from human and veterinary studies on different local anaesthetic agents and their application for diagnostic intra-articular anaesthesia is given. Based on this information, a protocol for diagnostic intra-articular anaesthesia in the dog can be developed and evaluated in future studies.

scholarly journals New Delivery Systems for Local Anaesthetics—Part 2

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Edward A. Shipton
Keyword(s):  
Drug Delivery ◽  
Direct Current ◽  
Local Anaesthetic ◽  
Low Voltage ◽  
Eutectic Mixture ◽  
Local Anaesthetics ◽  
Delivery Systems ◽  
Active Transportation ◽  
Anaesthetic Agents ◽  
Extended Range

Part 2 of this paper deals with the techniques for drug delivery of topical and injectable local anaesthetics. The various routes of local anaesthetic delivery (epidural, peripheral, wound catheters, intra-nasal, intra-vesical, intra-articular, intra-osseous) are explored. To enhance transdermal local anaesthetic permeation, additional methods to the use of an eutectic mixture of local anaesthetics and the use of controlled heat can be used. These methods include iontophoresis, electroporation, sonophoresis, and magnetophoresis. The potential clinical uses of topical local anaesthetics are elucidated. Iontophoresis, the active transportation of a drug into the skin using a constant low-voltage direct current is discussed. It is desirable to prolong local anaesthetic blockade by extending its sensory component only. The optimal release and safety of the encapsulated local anaesthetic agents still need to be determined. The use of different delivery systems should provide the clinician with both an extended range and choice in the degree of prolongation of action of each agent.

scholarly journals PERBEDAAN DAYA HAMBAT OBAT ANESTESI LOKAL LIDOCAINE 2% DAN ARTICAINE 4% TERHADAP PERTUMBUHAN BAKTERI Porphyromonas gingivalis SECARA IN VITRO

2016 ◽  
Vol 4 (2) ◽  
pp. 89-97
Author(s):  
Fairuza Muharammy ◽  
Rizanda Machmud ◽  
Surya Nelis
Keyword(s):  
Porphyromonas Gingivalis ◽  
Local Anaesthetic ◽  
Anaerobic Bacteria ◽  
Inhibition Zone ◽  
Local Anaesthetics ◽  
Control Group ◽  
Invasive Procedures ◽  
Control Group Design ◽  
Anaesthetic Agents

Porphyromonas gingivalis is a  gram-negative anaerobic bacteria which is an oral normal microflora located in subgingival area.This bacteria can cause inflamation and delayed wound healing after dental invasive procedures. Lidocaine 2% and articaine 4% are the most used anaesthetic agents in dentistry. Both of these agents have been studied for having antibacterial effect in certain concentrations. This will open the possibility of using local anaesthetic agents as antibacterial agent in dental invasive procedures to prevent infection after procedures. The purpose of this study is to analyze the difference inhibition of local anaesthetics drug lidocaine 2% and articaine 4% on the growth of Porphyromonas gingivalis bacteria in vitro. The study subject was pure culture of Porphyromonas gingivalis ATCC 33277 divided by two group, one group  with lidocaine 2% and other with  articaine 4%. This study was experimental laboratory with post test only control group design. The mean of inhibitions were obtained by measuring inhibition zone formed around paper discs with caliper in milimeter scale. The result showed Inhibition rate lidocaine 2% had greater rate than articaine 4% in inhibiting the growth of Porphyromonas gingivalis bacteria in vitro.The conclusion was lidocaine 2% was more effective than articaine 4% in inhibiting the growth of Porphyromonas gingivalis bacteria in vitro. Keywords: Antibacteria, Local anaesthetic,  Lidocaine 2%, Articaine 4%, Porphyromonas gingivalis

Combined Approach of QSAR and Docking Studies for the Design of Local Anaesthetic Agents

2017 ◽  
Vol 20 (3) ◽  
Author(s):  
Chunyan Zhang ◽  
Zhi Li ◽  
Jiahai Ma ◽  
Jing Zhang ◽  
Longming Zhang ◽  
...  
Keyword(s):  
Local Anaesthetic ◽  
Docking Studies ◽  
Combined Approach ◽  
Anaesthetic Agents

An Animal Protection Sponsor's View of MEIC

1997 ◽  
Vol 25 (3) ◽  
pp. 343-345
Author(s):  
Ethel Thurston
Keyword(s):  
Gold Standard ◽  
Animal Cell ◽  
Scientific Evidence ◽  
In Vitro Cytotoxicity ◽  
In Vitro Tests ◽  
Blood Concentrations ◽  
Animal Protection ◽  
Animal Tests ◽  
Lethal Blood

The Multicenter Evaluation of In Vitro Cytotoxicity programme is most important to animal protection, since it has validated 64 in vitro tests using advanced human data for 50 chemicals as the “gold standard”. Therefore, it has been able to compare animal cell tests, human cell tests and whole-animal tests fairly with unbiased scientific evidence. Added bonuses have included the identification and development of missing in vitro information (“missing tests”), publication of time-related lethal blood concentrations for all 50 chemicals, and some preliminary plans to resolve the 50,000 untested (or poorly tested) chemicals in the chemical mountain.

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