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Sequence of events occurring during the propagation of the action potential. Source: http://www.vce.bioninja. com.au/aos‐2‐detecting‐and‐respond/coordination‐‐regulation/nervous‐system.html. Used with permission 05/11/2016.
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Local anaesthetics are commonly used drugs in clinical anaesthesia. The knowledge of their pharmacology is paramount for safe and optimal use of this group of drugs. This chapter consists of two sections. The first section will address the chemical and physical properties, pharmacokinetics and pharmacodynamics of the local anaesthetics. In the seco...
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... travel in one direction as the axonal membrane that has just under- gone depolarisation remains in the refractory state until the resting potential is restored by the Sodium/Potassium ATPass pumps on [2]. Figure 3 illustrates the sequence of events occurring during the propagation of the action potential. ...
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We extend the nonstandard finite difference method of solution to the study of pharmacokinetic–pharmacodynamic models. Pharmacokinetic (PK) models are commonly used to predict drug concentrations that drive controlled intravenous (I.V.) transfers (or infusion and oral transfers) while pharmacokinetic and pharmacodynamic (PD) interaction models are...
Citations
... Для этого препарат должен преодолеть липидный двуслой клеточной стенки, проникнуть в аксоплазму и блокировать канал внутриклеточно. Длительность и интенсивность блокады достигаются объемом и концентрацией используемых препаратов [22,23]. ...
Acute otitis media (AOM), one of the most common infectious and inflammatory diseases in infants, toddlers and young children, is defined as an infectious inflammation of the middle ear, usually bacterial, often with earache, fever, and possibly otorrhea. Almost all children suffer from otitis media, 80–90% – at preschool age. The frequency of acute otitis media in children in a megapolis is more than 4 000 cases per 100 000 population, however, given the large proportion of asymptomatic variants against the background of acute respiratory infections, insufficient equipment of pediatricians with otoscopes, registration of acute otitis media almost exclusively by ENT doctors, the frequency of acute otitis media may be significantly higher. The clinical picture may be nonspecific. Ear pain and otoscopy are decisive for the diagnosis. The severity of inflammation correlates well with the scale of visual assessment of pain according to the child’s facial expressions. The aims of treatment are to relieve pain using topical or systemic analgesics, decide together with an ENT specialist on the need for antibiotic therapy, avoid not indicated antibiotic therapy, prevent complications (tympanic membrane perforation, acute mastoiditis, meningitis). With unexpressed otitis media, it is advisable to use symptomatic therapy and drops. A complex of compounds (lidocaine, phenazone) provides a quick therapeutic effect. Topical anaesthetics block the transmission of the pain signal from the receptor to the central nervous system through the inhibition of voltage-gated sodium channels. The symptomatic treatment (analgesics, antipyretics, topical therapy) results in improvement in 60% of patients within the next 24 hours, and in 80% within the next 3 days.
For prophylaxis of otitis, it is necessary to prevent acute respiratory infections, do vaccination against influenza and pneumococcal infections, avoid exposure to tobacco smoke, and keep babies breastfeeding.
... Anestésico amida, aprovado em 1960, produz uma pequena vasodilatação, possui pH de 7,6, baixo índice de toxicidade, recomenda-se 4,4 mg/kg (Mumba et al, 2017). ...
... Atuam diretamente no coração, interferem nas atividades sódio e cálcio, o anestésico bupivacaína apresenta alta toxicidade cardiovascular; eles afetam indiretamente o átrio e o ventrículo e causam arritmia, bradicardia e subsequente parada sinusal (Mumba, 2017). ...
A hipertensão arterial é altamente prevalente, estima-se que no Brasil apenas 23% dos hipertensos controlam a doença corretamente, 36% não a controlam e 41% abandonam o tratamento após uma melhora inicial. Objetivo: enfatizar a importância a respeito do uso correto de soluções anestésicas e para o cuidado seguro desses paciente. Metodologia: realizou-se uma revisão bibliográfica com busca em bases de pesquisa online como PubMed, Lilacs e Scielo entre o período de 2010 a 2021. Conclusão: Em sintese o emprego de soluções anestésicas em pacientes portadores de hipertensão arterial é uma prática que deve ser realizada com cautela. É necessário, antes de decidir qual anestésico usar, realizar uma anamnese detalhada e exame físico, incluindo a medição da pressão arterial, que permitirá a prevenção de possíveis reações indesejadas.
... Fentanyl 100mcg iv and patient was induced with inj. propofol 2 mg/kg, follwed by muscle relaxant inj.succinylcholine 2 mg/kg and intubated with appropriate size ET tube and prompt volatile anaesthetic, N2O, O2 will be given for maintenance of anaesthesia [7]. Monitoring of vital signs was instituted, that include Pulse oximetry, automated non-invasive blood pressure, ECG, Respiratory rate, ETCO2, and Heart rate throughout the procedure. ...
Erector spinae plane (ESP) block and serratus anterior plane (SAP) block promise effective thoracic analgesia compared with systemically administered opioids, but have never been compared in terms of terms of quality of recovery and overall morbidity after breast surgeries. Hence the present study designed to compare the efficacy and safety of the erector spinae plane block and serratus anterior plane block in the post-operative pain management in terms of duration of analgesia, time to 1st rescue analgesic, and incidence of PONV and patients satisfaction. The results proposed strongly that these are an alternative to other regional anaesthetic techniques with comparatively low or nil side effects. There is no incidence of post-operative nausea, vomiting and also not reported any pneumothorax.
... Lidocaine is a weak alkaline with pKa of 8, protein binding of 64%, and fat solubility of 1%. Lidocaine remains the drug of choice for a variety of medical procedures due to its strong anesthetic potential, fast onset of action, and wide safety limits [24,25]. Moreover, lidocaine can be administered via many routes, including topical (i.e., skin and airway), subcutaneous, intravenous, perineural, epidural, and intrathecal [22,26,27]. ...
Lidocaine is an amide-class local anesthetic used clinically to inhibit pain sensations. Systemic administration of lidocaine has antinociceptive, antiarrhythmic, anti-inflammatory, and antithrombotic effects. Lidocaine exerts these effects under both acute and chronic pain conditions and acute respiratory distress syndrome through mechanisms that can be independent of its primary mechanism of action, sodium channel inhibition. Here we review the pathophysiological underpinnings of lidocaine's role as an anti-nociceptive, anti-inflammatory mediated by toll-like receptor (TLR) and nuclear factor kappa-β (NF-kβ) signalling pathways and downstream cytokine effectors high mobility group box 1 (HMGB1) and tumour necrosis factor-α (TNF-α).
... The recommended dose for intrathecal administration is 50-300 μg, while as 2-5 mg of epidural loading dose is considered adequate. The risk of side effects increases exponentially with the increase in the dose [16,17]. ...
... Fentanyl as adjuvant does not prolong motor block, so it allows early ambulation, thereby reducing the morbidity. The duration of action is 2-4 h, and the risk of respiratory depression is very low and of short duration [17]. ...
... Its use in clinical practice is limited by its short duration of action and high side effect profile. The recommended intrathecal dose is 2.5-10 μg, and epidural loading dose is 10-50 μg [17]. ...
O consumo de cocaína pela população adulta é uma realidade mundial. A fim de aumentar o lucro da droga de rua, seus componentes são comumente adulterados com substâncias químicas capazes de mimetizar ou potencializar seus efeitos. Com o objetivo de descrever os adulterantes mais comuns identificados em amostras de cocaína apreendidas na cidade de São Paulo no primeiro semestre de 2021, foi realizado um estudo retrospectivo por meio da coleta de dados de amostras de cocaína analisadas pelo Núcleo de Exames de Entorpecentes do Instituto de Criminalística da Superintendência da Polícia Técnico-Científica de São Paulo. Os resultados das 1.809 amostras analisadas por Cromatografia Gasosa acoplada à Espectrometria de Massas revelaram que apenas 5,03% continham cocaína como única substância ativa. Foram identificados, em ordem decrescente de prevalência, os adulterantes: cafeína, lidocaína, tetracaína, fenacetina, levamisol, procaína, aminopirina, cetamina, benzocaína, acetaminofeno e teofilina.
Mepivacaine, an amide-type local anesthetic drug widely used in regional anesthesia, was studied by some aspects such as electrochemical behavior, mechanism illumination, and analytical applications by cyclic voltammetry (CV) and different pulse voltammetry (DPV) methods. In this study, a novel, fast, simple, portable, and the inexpensive electrochemical sensor was developed for the determination of mepivacaine. This study was carried out by mepivacaine anodic direction detection for the first time. The modified sensor was fabricated with silver nanoparticles (AgNP) and multiwalled carbon nanotubes paste electrode (MWCNTPE) by using the drop-dry method. Different experimental parameters, such as pulse amplitude, step potential, and scanning rate in the DPV application module, were optimized. Under optimal operation conditions, the limit of detection (LOD) as low as 31 μg L-1 was found over the dynamic range (0.1–8.0 mg L-1). In contrast to its high response towards mepivacaine, the DPV exhibits negligible responses on modified AgNP/MWCNTPE when exposed to interfering species such as dopamine, uric acid, glucose, ascorbic acid, and some heavy metals. Exceptionally, the proposed DPV method on modified AgNP/MWCNTPE was successfully applied to pharmaceutical dosage form and synthetic human serum with a low relative standard deviation (RSD) of 1.35% and 2.02%, respectively.
Background
In this study, a novel, fast, simple, portable, and inexpensive electrochemical sensor was developed for the determination of mepivacaine.
Objective
This study was carried out by mepivacaine anodic direction detection for the first time. The modified sensor was fabricated with silver nanoparticles (AgNP) and multiwalled carbon nanotubes paste electrode (MWCNTPE) by using drop-dry method.
Result
Under optimal operation conditions, the limit of detection (LOD) as low as 31 μg L-1 was found over the dynamic range (0.1–8.0 mg L-1).
Objective
To compare a 2% lidocaine solution containing 5 μg/ml (1:200 000) epinephrine with 2% mepivacaine for reducing lameness in horses after use in proximal nerve blocks.
Study design
Experimental randomized crossover.
Animals
Six adult horses with naturally occurring forelimb lameness.
Methods
Horses were evaluated using an inertial gait sensor system. Lameness was measured as a vector sum (VS). Following baseline lameness examination, median and ulnar nerve blocks were performed with lidocaine/epinephrine (0.5 mg epinephrine added to 50 ml of 2% lidocaine immediately prior to administration) or an equal volume of 2% mepivacaine. Horses were trotted at 5 min and then at 30 min intervals for 150 min. After 24 h, nerve blocks were repeated using the other local anesthetic. Data were evaluated using linear models.
Results
The reduction in the VS did not differ after nerve blocks with lidocaine/epinephrine or mepivacaine (P = .791). Mean time to VS <8.5 mm (n = 5) was 5 and 9.6 min for lidocaine/epinephrine and mepivacaine, respectively. For one horse, VS was not reduced to <8.5 mm with either treatment (this horse had the highest VS before treatments were administered). The decrease in VS to <8.5 mm lasted for 150 min in both treatment groups.
Conclusion
The outcomes of the median and ulnar nerve blocks performed with 2% lidocaine with epinephrine did not differ from blocks performed with 2% mepivacaine.
Clinical relevance
Two percent lidocaine with epinephrine may serve as an adequate replacement for proximal nerve blocks when mepivacaine is unavailable.
Objectives The study aimed to evaluate and compare various commercially available local anesthetic solutions.
Materials and Methods A total of 150 commercially available local anesthetic cartridges of similar composition (2% lidocaine with epinephrine 1:100,000) were randomly collected and divided into 3 groups. The designations of groups were selected from their product names such that each group consisted of 60 cartridges. Group S (Septodont, France) Group M (Medicaine, Korea) and Group H (HD-Caine, Pakistan). The samples were divided into five sub-groups, each consisting of 10 cartridges from each group to investigate each parameter.
Results The acquired data was statistically analyzed and compared (using SPSS version 12). Compositional analysis revealed a non-significant (P>0.05) difference when the three Groups were compared with standard lidocaine and epinephrine solutions. The mean pH values of samples from group S, M and H respectively fell within the range of pH values of commercially available solutions. Non-significant difference in EPT values of Group S and H was found when efficacy was compared (p = 0.3), however a significant difference (p < 0.01) was observed in contrast to Group M. Anti-bacterial activity was observed in all the group and a non-significant difference in cell viability values of Group S and M was found (p = 0.6), while the difference was significant in comparison to Group H.
Conclusion Within the limitations of these investigations, it appears that the properties of different manufacturers fall within the recommended ranges as mentioned in literature and do not appear to be statistically different in the variables we have tested.
