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Acute Toxicity of Ropivacaine Compared with That of Bupivacaine
Abstract
The acute central nervous and cardiovascular effects of the local anesthetics ropivacaine and bupivacaine were compared in 12 volunteers in a randomized double-blind manner with use of intravenous infusions at a rate of 10 mg/min up to a maximal dose of 150 mg. The volunteers were all healthy men. They were familiarized with the central nervous system (CNS) toxic effects of local anesthetics by receiving a preliminary intravenous injection of lidocaine. The infusions of ropivacaine and bupivacaine were given not less than 7 days apart. CNS toxicity was identified by the CNS symptoms and the volunteers were told to request that the infusion be stopped when they felt definite but not severe symptoms of toxicity such as numbness of the mouth, lightheadedness, and tinnitus. In the absence of definite symptoms, the infusion was stopped after 150 mg had been given. Cardiovascular system (CVS) changes in conductivity and myocardial contractility were monitored using an interpretive electrocardiograph (which measured PR interval, QRS duration, and QT interval corrected for heart rate) and echocardiography (which measured left ventricular dimensions from which stroke volume and ejection fraction were calculated). Ropivacaine caused less CNS symptoms and was at least 25% less toxic than bupivacaine in regard to the dose tolerated. Both drugs increased heart rate and arterial pressure. Stroke volume and ejection fraction were reduced. There was no change in cardiac output. Although both drugs caused evidence of depression of conductivity and contractility, these appeared at lower dosage and lower plasma concentrations with bupivacaine than with ropivacaine.(ABSTRACT TRUNCATED AT 250 WORDS)
... Por exemplo, a lidocaína é rapidamente absorvida e eliminada, enquanto a bupivacaína é absorvida e eliminada mais lentamente. 58 Efeitos colaterais e toxicidade são outra consideração importante. ALs têm risco de toxicidade sistêmica, que pode ser mitigada pela administração de dose adequada e pela monitoração cuidadosa do paciente. ...
Introdução: Avaliar as diferenças cicatriciais entre áreas previamente anestesiadas com diferentes anestésicos locais é interessante para verificar se a escolha do anestésico auxilia na cicatrização cirúrgica em relação à inflamação, neovascularização e deposição de colágeno. Objetivos: Revisar a literatura existente com foco de análise sobre o papel dos anestésicos locais no auxílio da cicatrização de feridas cirúrgicas. Método: Revisão narrativa da literatura selecionada das plataformas SciELO – Scientific Electronic Library Online, Google Scholar, Pubmed e Scopus. Inicialmente a revisão realizou a busca por palavras-chave no foco da pesquisa, com base no MESH/DeCS com os seguintes termos: “anestésicos locais, cicatrização, neovascularização, colágeno” com busca AND ou OR, considerando o título e/ou resumo. A seguir, foram incluídos somente os que tinham maior relação ao tema, e realizada a leitura dos textos para inclusão. Resultados: Foram incluídos, lidos e interpretados 73 artigos enfocando o papel dos anestésicos na cicatrização, dor, efeitos colaterais e os melhores que despontam na atualidade na analgesia e potencial cicatricial. Conclusões: Não se observou diferenças entre anestésicos pesquisados quanto à cicatrização, inflamação e neovascularização. Contudo, verificou-se diferença significativa na produção de colágenos com intensidade de 6 a 12 vezes maior de colágenos tipos I, II e III com o uso da levobupivacaína.
... To ensure both safety and efficacy, and to use the same amount of LA in both groups, we administered 10 mL of 0.2% ropivacaine to each TAP block, and 5 mL of 0.2% ropivacaine to each side of the rectus abdominis muscle for the RS block, so that the total dose of ropivacaine was 60 mg for each group. This was within the safe range of LAST, which was lower than 150 mg of ropivacaine, suggested as an acceptable threshold for acute central nervous system toxicity in the literature [22,24]. Nonetheless, the dose may not have been sufficient to provide effective analgesia, and this may have influenced the results of our study. ...
Background
Ultrasound-guided transversus abdominis plane (TAP) block is commonly used for pain control in laparoscopic cholecystectomy. However, significant pain persists, affecting patient recovery and sleep quality on the day of surgery. We compared the analgesic effect of ultrasound-guided TAP block with or without rectus sheath (RS) block in patients undergoing laparoscopic cholecystectomy using the visual analog scale (VAS) scores.
Methods
The study was registered before patient enrollment at the Clinical Research Information Service (registration number: KCT0006468, 19/08/2021). 88 American Society of Anesthesiologist physical status I-III patients undergoing laparoscopic cholecystectomy were divided into two groups. RS-TAP group received right lateral and right subcostal TAP block, and RS block with 0.2% ropivacaine (30 mL); Bi-TAP group received bilateral and right subcostal TAP block with same amount of ropivacaine. The primary outcome was visual analogue scale (VAS) for 48 h postoperatively. Secondary outcomes included the use of rescue analgesics, cumulative intravenous patient-controlled analgesia (IV-PCA) consumption, patient satisfaction, sleep quality, and incidence of adverse events.
Results
There was no significant difference in VAS score between two groups for 48 h postoperatively. We found no difference between the groups in any of the secondary outcomes: the use of rescue analgesics, consumption of IV-PCA, patient satisfaction with postoperative pain control, sleep quality, and the incidence of postoperative adverse events.
Conclusion
Both RS-TAP and Bi-TAP blocks provided clinically acceptable pain control in patients undergoing laparoscopic cholecystectomy, although there was no significant difference between two combination blocks in postoperative analgesia or sleep quality.
... It has a pro le similar to bupivacaine but with less neuro and carditoxic effect. 6 Opioids are the most widely used class of adjuvant to epidural local anaesthetic in labour analgesia practice. Fentanyl and remifentanyl are the two most commonly used opioid for this purpose. ...
Background: Pain relief in labour has always been surrounded with myths and controversies. Hence providing effective and safe analgesia during labour has remain an ongoing challenge. This study was undertaken to compare fentanyl and clonidine with ropivacaine in epidural labour analgesia. Methods: A total of 60 term parturients with uncomplicated pregnancy, vertex presentation, posted for on-demand epidural labour analgesia were divided into two groups. Group RF (n=30) patients received 10ml solution comprising 0.1% ropivacaine with fentanyl 20mcg. Group RC (n=30) patients received 10ml of 0.1% ropivacaine with clonidine 60mcg. Characteristics of the block, onset and duration of analgesia and total analgesic requirements were noted. Pain and overall satisfaction scores were assessed with a 10-point visual analogue scale. Mode of delivery and neonatal APGAR scores were recorded. Result: At baseline, groups were matched demographically, haemodynamically as well as for intensity of pain. A significant difference among groups in VAS was observed from 120min intervals and lowest values were in group RC. No significant difference was observed in haemodynamic parameters, mode of delivery and expulsive efforts. Total analgesic dose and top up dose requirement was more in group RF. Six percent of patients in group RF and 10 percent of patients in group RC developed nausea. Conclusion: Ropivacaine 0.1% was effective in decreasing labour pain without any motor blockade. Clonidine was superior to fentanyl as an adjuvant in labour without any significant feto-maternal adverse effects.
... Por exemplo, a lidocaína é rapidamente absorvida e eliminada, enquanto a bupivacaína é absorvida e eliminada mais lentamente. 58 Efeitos colaterais e toxicidade são outra consideração importante. ALs têm risco de toxicidade sistêmica, que pode ser mitigada pela administração de dose adequada e pela monitoração cuidadosa do paciente. ...
Introdução: Avaliar as diferenças cicatriciais entre áreas previamente anestesiadas com diferentes anestésicos locais é interessante para verificar se a escolha do anestésico auxilia na cicatrização cirúrgica em relação à inflamação, neovascularização e deposição de colágeno. Objetivos: Revisar a literatura existente com foco de análise sobre o papel dos anestésicos locais no auxílio da cicatrização de feridas cirúrgicas. Método: Revisão narrativa da literatura selecionada das plataformas SciELO – Scientific Electronic Library Online, Google Scholar, Pubmed e Scopus. Inicialmente a revisão realizou a busca por palavras-chave no foco da pesquisa, com base no MESH/DeCS com os seguintes termos: “anestésicos locais, cicatrização, neovascularização, colágeno” com busca AND ou OR, considerando o título e/ou resumo. A seguir, foram incluídos somente os que tinham maior relação ao tema, e realizada a leitura dos textos para inclusão. Resultados: Foram incluídos, lidos e interpretados 73 artigos enfocando o papel dos anestésicos na cicatrização, dor, efeitos colaterais e os melhores que despontam na atualidade na analgesia e potencial cicatricial. Conclusões: Não se observou diferenças entre anestésicos pesquisados quanto à cicatrização, inflamação e neovascularização. Contudo, verificou-se diferença significativa na produção de colágenos com intensidade de 6 a 12 vezes maior de colágenos tipos I, II e III com o uso da levobupivacaína.
... Por exemplo, a lidocaína é rapidamente absorvida e eliminada, enquanto a bupivacaína é absorvida e eliminada mais lentamente. 58 Efeitos colaterais e toxicidade são outra consideração importante. ALs têm risco de toxicidade sistêmica, que pode ser mitigada pela administração de dose adequada e pela monitoração cuidadosa do paciente. ...
Introdução: Avaliar as diferenças cicatriciais entre áreas previamente anestesiadas com diferentes anestésicos locais é interessante para verificar se a escolha do anestésico auxilia na cicatrização cirúrgica em relação à inflamação, neovascularização e deposição de colágeno. Objetivos: Revisar a literatura existente com foco de análise sobre o papel dos anestésicos locais no auxílio da cicatrização de feridas cirúrgicas. Método: Revisão narrativa da literatura selecionada das plataformas SciELO – Scientific Electronic Library Online, Google Scholar, Pubmed e Scopus. Inicialmente a revisão realizou a busca por palavras-chave no foco da pesquisa, com base no MESH/DeCS com os seguintes termos: “anestésicos locais, cicatrização, neovascularização, colágeno” com busca AND ou OR, considerando o título e/ou resumo. A seguir, foram incluídos somente os que tinham maior relação ao tema, e realizada a leitura dos textos para inclusão. Resultados: Foram incluídos, lidos e interpretados 73 artigos enfocando o papel dos anestésicos na cicatrização, dor, efeitos colaterais e os melhores que despontam na atualidade na analgesia e potencial cicatricial. Conclusões: Não se observou diferenças entre anestésicos pesquisados quanto à cicatrização, inflamação e neovascularização. Contudo, verificou-se diferença significativa na produção de colágenos com intensidade de 6 a 12 vezes maior de colágenos tipos I, II e III com o uso da levobupivacaína.
... To ensure both safety and e cacy, and to use the same amount of local anesthetics in both groups, we administered 10 mL of 0.2% ropivacaine to each TAP block, and 5 mL of 0.2% ropivacaine to each sides of the rectus abdominis muscle for the RS block, so that the total dose of ropivacaine was 60 mg for each group. This was within the safe range of LAST, which was lower than 150 mg of ropivacaine, suggested as an acceptable threshold for acute central nervous system toxicity in the literature [22,24]. Nonetheless, the dose may not have been su cient to provide effective analgesia, and this may have in uenced the results of our study. ...
Background
Ultrasound-guided transversus abdominis plane (TAP) block is commonly used for pain control in laparoscopic cholecystectomy. However, significant pain persists, affecting patient recovery and sleep quality on the day of surgery. We compared the analgesic effect of ultrasound-guided TAP block with or without rectus sheath (RS) block in patients undergoing laparoscopic cholecystectomy using the visual analog scale (VAS) scores.
Methods
88 American Society of Anesthesiologist physical status I-III patients undergoing laparoscopic cholecystectomy were divided into two groups. RS-TAP group received right lateral and right subcostal TAP block, and RS block with 0.2% ropivacaine (30 mL); Bi-TAP group received bilateral and right subcostal TAP block with same amount of ropivacaine. The primary outcome was visual analogue scale (VAS) for 48 h postoperatively. Secondary outcomes included the use of rescue analgesics, cumulative intravenous patient-controlled analgesia (IV-PCA) consumption, patient satisfaction, sleep quality, and incidence of adverse events.
Results
There was no significant difference in VAS score between two groups for 48 h postoperatively. We found no difference between the groups in any of the secondary outcomes: the use of rescue analgesics, consumption of IV-PCA, patient satisfaction with postoperative pain control, sleep quality, and the incidence of postoperative adverse events.
Conclusion
Both RS-TAP and Bi-TAP blocks provided clinically acceptable pain control in patients undergoing laparoscopic cholecystectomy, although there was no significant difference between two combination blocks in postoperative analgesia or sleep quality.
... [8] In humans, ropivacaine also causes less central nervous system (CNS) and cardiovascular system (CVS) toxicity than bupivacaine. [9] Ropivacaine has been reported to have an approximately 70 to 75 percent greater margin of safety than bupivacaine. [10] Our study is comparative evaluation of efficacy of 0.2% ropivacaine and 0.25% bupivacaine as local anesthetic agents for cases of surgical removal of impacted mandibular third molar. ...
Background: Ropivacaine is a long-acting amide local anesthetic agent and firstproduced as a pure enantiomer. It produces effects similar to other local anesthetics via reversible inhibition of sodium ion influx in nerve fibers. Ropivacaine is lesslipophilic than bupivacaine and is less likely to penetrate large myelinated motorfibers, resulting in a relatively reduced motor blockade. Thus, ropivacaine has agreater degree of motor sensory differentiation, which could be useful when motorblockade is undesirable. The reduced lipophilicity is also associated with decreasedpotential for central nervous system toxicity and cardiotoxicity. The drug displayslinear and dose proportional pharmacokinetics (up to 80 mg administeredintravenously). It is metabolized extensively in the liver and excreted in urine. Thepresent article details the clinical applications of ropivacaine and its current place asa local anesthetic in the group. Materials and methods: The research was undertaken following approval from the institutional ethics committee and spanned a duration of two years, during which a comprehensive evaluation was performed on 52 participants. Results: A bigger sample size should beconsidered for more specific comparison. Bupivacaine has a very long duration ofaction which is not required for minor surgical procedure whereas Ropivacaine alsois long acting but less than Bupivacaine which is perfect for more time requiredprocedures and post-operative analgesia. Ropivacaine has vasoconstrictive natureand the difference was seen bleeding was more when Bupivacaine was used. In ourstudy no adverse effects were encountered when we used both the drugs butBupivacaine is cardiotoxic in nature and changes in blood pressure and heart ratewere seen when Bupivacaine was used so Ropivacaine can be considered to be usedin Oral and Maxillofacial surgery Conclusion: So, to conclude, my opinion when 0.2% Ropivacaine and 0.25%Bupivacaine was compared in sample size 52, 0.2% Ropivacaine was better in termsof early onset and duration than 0.25% Bupivacaine.
... It usually has an onset of action in 1-15 min with a duration of 2-6 h [82]. It is reported to have significantly less cardiotoxicity and neurotoxicity [81,83,84]. It is generally well tolerated with few side effects [85]. ...
Periarticular infiltration following total knee and hip arthroplasty has been demonstrated to be equivalent to peripheral nerve blocks for postoperative pain management. The ideal cocktail has not been established yet. We have conducted a literature search on PubMed and Embase. Our search criteria included randomized controlled trials (RCTs) and systematic reviews (SRs). We tried to only include the most recent studies to keep the information current. The included research focused at Dexmedetomidine, Liposomal Bupivacaine, Ropivacaine, Epinephrine, Ketorolac, Morphine, Ketamine and Glucocorticosteroids. Each medication’s mode of action, duration, ideal dosage, contraindications, side effects and effectiveness have been summarized in the review article. This article will help the clinician to make an informed evidence-based decision about which medications to include in their ideal cocktail.
... The mean reported C max was 0.71 µg/mL (SD ± 0.11 µg/mL). It is worth noting that the generally accepted threshold for neurological toxicity associated with ropivacaine is commonly cited as being around 2.2 µg/mL [7]. Intriguingly, several investigations have documented instances where C max levels reached up to 3 µg/mL yet failed to induce any discernible toxicity. ...
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... 29,3,16 Diversos anestésicos locales pueden ser usados para este fin, de los cuales la ropivacaína tiene el mejor perfil farmacocinético y de efectos adversos. 37,44 Sin embargo la principal desventaja es su duración limitada en el tiempo. Este problema intenta ser superado mediante la adición de adyuvantes a los anestésicos locales, potenciando y prolongando sus efectos. ...
Objetivos: Evaluar la efectividad de la infiltración del sitio quirúrgico, con ropivacaína, dexmedetomidina y ketorolac, en pacientes sometidos a instrumentación transpedicular dorsolumbar con técnica mini invasiva, en cuanto al consumo de opioides durante la internación.Materiales y métodos: Se recolectaron en forma retrospectiva los datos prospectivos de las historias clínicas de pacientes con una instrumentación con tornillos transpediculares percutáneos operados entre Junio del 2016 y Diciembre del 2018. 32 pacientes cumplieron con los criterios de selección. Se infiltró en el momento del cierre quirúrgico con una solución preparada con 150 mg de ropivacaína, 0,7 mcg/kg de dexmedetomidina y 60 mg de ketorolac, disuelto en solución fisiológica estéril para completar 40ml (Grupo M) y se la comparó con pacientes en los cuales solo se infiltró con 150mg de ropivacaína (Grupo E).Resultados: El consumo de equivalentes de morfina durante las primeras 72hs postoperatorias presentó en el grupo M una mediana de 0mg, y el grupo E, una mediana de 9,5mg (RIQ de 13,35), con una p<0,000. Por el contrario el consumo de morfina en la sala de recuperación presentó una mediana de 0mg (RIQ de 2) para el grupo M, y de 2mg (RIQ de 5) para el grupo E, sin encontrarse una diferencia significativa, p=0,132.Conclusión: Los resultados obtenidos en la comparación del consumo de opioides durante las primeras 72hs de la internación permite inferir que esta combinación de fármacos es superior respecto a la infiltración estándar con ropivacaína, independientemente de la estrategia analgésica utilizada durante el tiempo quirúrgico.
... Ropivacaine is a local anesthetic with greater degree of motor sensory differentiation with decreased potential for central nervous system toxicity and cardiotoxicity. 7 Tramadol is mixed opioid analgesic commonly used for postoperative pain management through intravenous or intramuscular injections and wound infiltration. It is also used as an adjuvant to local anaesthetics for peripheral nerve blocks. ...
... Apart from this Ropivacaine also has an improved safety profile when contrasted with Bupivacaine in terms of cardiac depression and neurological toxicity. [14,15] Limitations-1. We are unable to comment on just how much these pulmonary variables may actually decline after 15 minutes as it was not possible to gather measurements intraoperatively. ...
Background: Interscalene brachial plexus block (ISB) is a gold standard regional block for surgical procedures on the shoulder girdle and humerus shaft. Hemidiaphragmatic paralysis following ISB is almost inevitable. Its reduction would benefit patients with borderline respiratory function. To the best of our knowledge no study has compared the reduction in spirometric values by equipotent doses of Ropivacaine and Bupivacaine for ISB. Aims: to compare the degree of phrenic nerve blockade through measurement of reduction in FEV1 and PEF caused by equipotent doses of Bupivacaine and Ropivacaine for ISB (group B and group R) using bedside spirometry. Methods: Patients were randomly assigned to two groups: the Bupivacaine group [Group B (n=25): 20ml of 0.25% Bupivacaine for ISB] or the Ropivacaine group [Group R(n=25): 20ml of 0.375% Ropivacaine for ISB]. Before performing the ISB, bedside spirometry was performed using best of the three readings for FEV1 and PEF as baseline values. Readings were again taken at time points five minutes after performing the block, ten minutes, fifteen minutes and final readings were taken at the end of surgery. Results: FEV1 and PEFR values dropped in both groups. At the end of fifteen minutes, the PEFR in Group R was more than that in Group B (p=0.038) and the FEV1 in Group R was more than Group B (p=0.044). Conclusions: At fifteen minutes the Group R showed a smaller drop in PEFR and FEV1. Thus Ropivacaine 0.375% may be used preferentially over Bupivacaine 0.25% for ISB in patients with borderline respiratory function.
... Examples of some intraperitoneally used local analgesics are lignocaine [19,20], bupivacaine [21] meperidine [22], and recently, ropivacaine [23][24][25][26][27]. The latter has demonstrated a superior cardioprotective effect compared to bupivacaine [28][29][30], while providing longer pain relief and reducing opioid usage [31][32][33]. ...
... 7 It exhibits less cardiovascular or CNS toxicity when compared with bupivacaine in healthy volunteers. 8,9 While the contribution of ropivacaine in management of post-tonsillectomy pain reduction has been assessed, the reports anesthetic, ropivacaine, in the management of post-tonsillectomy pain relief. ...
... Для проведення епідурального знеболення був використаний 0,2 % розчин ропівакаїну виробництва «Astra Zeneca», оскільки ропівакаїн характеризується меншою токсичністю порівняно з бупівакаїном, також ропівакаїн забезпечує ефективне знеболення з мінімальним пригніченням моторної функції, та не потребує додаткового введення наркотичних анальгетиків для подовження знеболення в післяопераційному періоді. [20,21,22,23] Середня вартість добового забезпечення ропівакаїном 0,2% виробництва «Astra Zeneca» з розрахунку на середньою швидкістю епідурального введення 10 мл/годину (від 6-14 мл/годину) складає 424 грн. ...
Introduction. According to the 2020 database of the World Health Organization, unfortunately lung cancer ranks the second place among the new cases of cancer. One of the main causes of the lung cancer is tobacco smoking. More than 20% of the adult population are daily smokers, and the tobacco epidemic tends to grow steadily. Increasing number of patients who undergoing thoracotomy contributes to the constant search for perioperative anesthesia and it’s improvement. Objective: to compare different methods of perioperative analgesia in thoracic surgery and to determine the most effective and cost-effective method. Materials and methods. There were analyzed 80 lung cancer patients who underwent open access surgery. Patients were randomized into 4 groups. Group A: according to the concept of pre-emptive analgesia, 1 hour before incision - patients received 1000 mg of paracetamol intravenous, as well as dexketoprofen 50 mg intravenous, in the postoperative period dexketoprofen and paracetamol were administered every 8 hours, + epidural anesthesia: administration of 40 mg of 2% lidocaine solution during catheter placement, in the postoperative period - ropivacaine 2 mg/ml (3-14 ml/h). Group B: epidural anesthesia: administration of 40 mg of 2% lidocaine solution during catheter placement, in the postoperative - ropivacaine 2 mg/ml (3-14 ml/h). Group C: according to the concept of preemptive analgesia, 1 hour before incision - patients received 1000 mg of paracetamol intravenous, as well as dexketoprofen 50 mg intravenous, in the postoperative period dexketoprofen and paracetamol were administered every 8 hours. Group D: No pre-emptive analgesia and no epidural analgesia, morphine analgesia intravenous as needed. The severity of the pain syndrome was assessed by the numerological rating scale (NRS) after 3, 6, 12, 24, 32 hours. Results and discussion. There were not observed any statistically significant differences in the subgroups by age, body weight, duration of surgery and blood loss (p> 0.05). Patients of the Group A had the lowest level of pain, and only one patient required additional analgesia. There were no statistically significant differences in the severity of the pain syndrome between patients of the group B and the group C at all stages of the study (p <0.05). Using of the pre-emptive analgesia method with the use of the multimodal analgesia, but without the use of epidural anesthesia has the benefit in the amount of 728 hryvnias prevails.
... A recent study of Ivani and colleagues compared levobupivacaine with ropivacaine and bupivacaine by the caudal route in children undergoing minor surgery. 20 Levobupivacaine and bupivacaine were used in a concentration of 0.25% and ropivacaine in a concentration of 0.2%, but the same volume was administered for the three local anaesthetics. ...
Aim: The purpose of the present research was to assess and compare the efficacy of Ropivacaine, Levobupivacaine and Bupivacaine in paediatric patients as an anaesthetic in caudal block undergoing various lower abdominal surgeries. Methodology: This was a prospective randomized controlled study including 50 consecutive patients in the age group of 1‑10 years, who underwent urogenital surgeries under general anesthesia. Study was performed at Dr. Moopen's Medical College, Wayanad, Kerala. India and duration was from January 2022 to September 2022. Caudal block was given with either bupivacaine (0.25%) 1 ml/kg (Group I) or ropivacaine (0.25%) 1 ml/kg (Group II) or levobupivacaine 0.25% 1 mL /kg (Group III). Heart rate (HR) and systolic blood pressure (SBP) were recorded as a baseline, before the anesthesia induction and then at 30, 60 and 90 min after incision. Pain scores were assessed post‑operatively by a single observer at 30 min and then at 2, 4, 8 and 12 hour with a 5‑point observer pain score (OPS). Patients and observer were blinded to the medication given. The duration of absolute analgesia was defined as the time from caudal injection until the pain score was >2. Motor block was assessed by modified Bromage scale.
... Ropivacaine, one of the newer long-acting amide local anaesthetic, is the stereoisomer of bupivacaine and has been shown into be less toxic than bupivacaine. 4 The addition of an adjuvant to ropivacaine can further have advantage in prolonging the duration of block and postoperative analgesia. 5 In this regard alfa-2 agonists, previously used as antihypertensive agents, have been utilized for the role of adjuvants to local anaesthetics in nerve blocks. ...
Background: Transversus abdominis plane block is an important regional anaesthesia technique for postoperative analgesia after caesarean section. Addition of adjuvants to local anaesthetic in TAP block helps in improving the duration of analgesia. Objective of current study was to compare clonidine and dexmedetomidine as adjuvants to 0.2% ropivacaine in USG guided TAP block for duration of postoperative analgesia in caesarean section under spinal anaesthesia.Methods: A total of 75 pregnant patients belonging to ASA I-II scheduled for caesarean section were included and divided into three groups; Group I-0.2% Ropivacaine plus normal saline, Group II-0.2% Ropivacaine plus 50 mcg clonidine and Group III-0.2% ropivacaine plus 50 mcg dexmedetomidine. The patients were compared for duration of analgesia, total number and amount of rescue analgesia utilized in 24 hours.Results: The mean duration of analgesia was found to be more (statistically significant p<0.05) and number as well as amount of rescue analgesic doses were reduced in group III as compared to group I and group II.Conclusions: Dexmedetomidine is a better alternative to clonidine as adjuvant for 0.2% ropivacaine in USG guided TAP block to extend the duration of postoperative analgesia and decreased 24-hour analgesic requirement in caesarean section.
... The primary aim of epidural analgesia is to provide complete pain relief without neonatal compromise which is easily possible with the use of local anaesthetics with adjuvants, Ropivacaine has better cardioprotective and less neurotoxic effect, 10,11 Clonidine is an alpha 2adrenergic receptors in dorsal horn to reduce afferent pain transmission in nuleus tractus solitarii(NTS), exciting a pathway that inhibit excitatory cardiovascular neurons. It also has alpha antagonist effect in posterior hypothalamus and medulla resulting in reduced sympathetic outflow from central nervous system thereby reducing arterial blood pressure. ...
Epidural labour analgesia is considered as the gold standard of pain relief for paturients inspite of the hesitancy that is prevalent in our country in providing pain-free labour. There are several other pharmacological and non pharmacological methods available for providing labour analgesia. Local anaesthetic is an indispensable drug for administering epidural labour analgesia Ropivacaine is the most widely used local anaesthetic for labour analgesia because of its safety profile proven by various studies.
It is less potent and onset of action is slightly prolonged when compared to bupivacaine or levobupivacaine. Use of adjuvants along with local anaesthetic reduces the total dose of local anaesthetic that is required for providing effective labour analgesia. Clonidine is a centrally acting partial alpha 2 adrenergic agonist that reduces the anaesthetic and analgesic requirement of local anaesthetic. This study is aimed to study the effect of ropivacaine with clonidine as an adjuvant for labour analgesia.
To compare the time of onset of analgesia, total dose of local anaesthetic required, total duration of analgesia and neonatal outcome between the two groups, Group I with ropivacaine and Group II ropivacaine with clonidine.
: A prospective randomised controlled study was conducted in a government peripheral medical College after getting ethical committee clearance 100 patrurients randomised into two groups, Group I received 2% ropivacaine and Group II received 2% ropivacaine with 40 micrograms of clonidine.
: The results were analysed with SPSSVersion 13 using student t - test and chi square test
The mean age was 23.4 ±1.7 years. The mean onset time of Group A and Group B were 12.9±1.3 minutes and 17.7±1.3 minutes with p<0.001 which was significant. Total mean dose of Ropivacaine for both groups were 44.0±8.8 and 54.0±8.9 respectively with P <0.05. Neonatal outcome as measured using APGAR score were 8.5±0.5 and 8.4±0.5 being statistically insignificant.
Addition of 40 micrograms of clonidine with Ropivacaine epidurally resulted in rapid onset of analgesia with required dose of Ropivacaine. Use of Clonidine as adjuvant didn't produce any undesirable motor blockade or neonatal depression.
... Ropivacaine is thought to be safer in regard to toxicity than racemic bupivacaine. When ropivacaine was administered systemically to healthy volunteers, the tolerated maximum dose before cardiovascular or neurological effects occurred was about twice as high as when racemic bupivacaine was used [106,107]. However, ropivacaine is about 30-50% less potent than racemic bupivacaine and levobupivacaine [108,109] and it is also approximately two and a half times less lipophilic [110]. ...
Neuraxial drug administration, i.e., the injection of drugs into the epidural or intrathecal space to produce anesthesia or analgesia, is a technique developed more than 120 years ago. Today, it still is widely used in daily practice in anesthesiology and in acute and chronic pain therapy. A multitude of different drugs have been introduced for neuraxial injection, only a part of which have obtained official approval for that indication. A broad understanding of the pharmacology of those agents is essential to the clinician to utilize them in a safe and efficient manner. In the present narrative review, we summarize current knowledge on neuraxial anatomy relevant to clinical practice, including pediatric anatomy. Then, we delineate the general pharmacology of neuraxial drug administration, with particular attention to specific aspects of epidural and intrathecal pharmacokinetics and pharmacodynamics. Furthermore, we describe the most common clinical indications for neuraxial drug administration, including the perioperative setting, obstetrics, and chronic pain. Then, we discuss possible neurotoxic effects of neuraxial drugs, and moreover, we detail the specific properties of the most commonly used neuraxial drugs that are relevant to clinicians who employ epidural or intrathecal drug administration, in order to ensure adequate treatment and patient safety in these techniques. Finally, we give a brief overview on new developments in neuraxial drug therapy.
... Considering that the duration of the analgesic effect of liposomal bupivacaine is generally 24 h, it may be assumed that PF-72 overcomes the limitations of liposomal bupivacaine in terms of analgesic duration. Additionally, ropivacaine is a long-acting amide local anesthetic with a potentially better safety profile compared with bupivacaine [21,22]. These facts collectively suggest that PF-72 may be a viable alternative for the conventionally used liposomal bupivacaine. ...
Background
A temperature-responsive hydrogel (PF-72; TGel Bio, Inc., Ltd, Seoul, Korea), developed as a sustained drug delivery device, can be mixed with ropivacaine to reduce pain in the incision area. The hydrogel is soluble at low temperatures (2–8 °C) and is converted into a gel at high temperatures (> 30 °C). We aimed to evaluate whether the administration of ropivacaine using PF-72 at incision sites reduces pain until 72 h postoperatively in patients undergoing laparoscopic stomach or colorectal surgery.
Methods
Patients were randomly assigned to the control group (0.75% ropivacaine) or PF-72 group (PF-72 mixed with 0.75% ropivacaine). Before surgical incision closure, 0.75% ropivacaine or PF-72 mixed with 0.75% ropivacaine was injected into the subcutaneous fat and muscle of all incisions. Postoperative pain was evaluated by the Numerical Rating Scale (NRS, 0 = no pain, 10 = most severe pain) for wound pain at 3, 6, 24, 48, and 72 h after the end of surgery.
Results
Ninety-nine patients (control, n = 51; PF-72, n = 48) were included in the analysis. The areas under the curve of NRS for wound pain until 72 h in the control group and the PF-72 group were 188.7 ± 46.1 and 135.3 ± 49.9 h, respectively (P < 0.001). The frequency of the administration of rescue analgesics in the general ward was similar between the two groups.
Conclusion
PF-72 mixed with 0.75% ropivacaine reduced postoperative pain until 72 h in patients undergoing laparoscopic surgery. Although the study population was not large enough for safety evaluation, no adverse events associated with PF-72 were observed.
... The effects of intravenous infusion of bupivacaine and ropivacaine both at the rate of 10 mg/min were assessed by Scott et al [16]. They found that there was evidence of depression of conductivity and contractility was displayed by both the groups at lower doses and lower plasma concentrations with ropivacaine and bupivacaine. ...
Background: Generally, to perform the Peribulbar anaesthesia, different mixtures of local anaesthetics are used, the most common of which are lidocaine and bupivacaine. It was observed that overdose of bupivacaine proves to be serious because of its cardiotoxic effects. Even more it responded poorly to the traditional resuscitation methods. This study evaluated the efficacy of bupivacaine and ropivacaine. To assess the efficacy hyaluronidase and lidocaine were used to combine the two. Here, for the patients of cataract surgery, two-point injection technique was used for peribulbar anaesthesia. Aim: To assess bupivacaine's and ropivacaine's efficacy each of which were combined with hyaluronidase and lidocaine.
... Bupivacaine and ropivacaine also differ in their toxicity profiles. Human and animal studies have demonstrated that large intravascular doses of bupivacaine and ropivacaine can induce central nervous system (CNS) symptoms, including seizure, but the dose required for bupivacaine is likely lower than for ropivacaine [5,10,11]. This should be interpreted with caution, however, because of the differences in potency: equianalgesic doses may be a more apt comparison than raw milligrams administered. ...
Since the advent of neuraxial analgesia for labor, approaches to maintaining intrapartum pain relief have seen significant advancement. Through pharmacologic innovations and improved drug delivery mechanisms, current neuraxial labor analgesia maintenance techniques have been shaped by efforts to maximize patient comfort during the birthing process, while minimizing undesirable side effects and promoting the unimpeded progress of labor. To these ends, a modern anesthesiologist may avail themselves of several techniques, including programmed intermittent epidural bolus (PIEB), patient controlled epidural analgesia (PCEA) and dilute concentration local anesthetic + opioid epidural solutions. We explore the historical development and the evidential underpinnings of these techniques, in addition to several contemporary neuraxial labor analgesia practices. We also summarize current understanding of the effects these interventions have on maternal/fetal health and the labor course, as well as several important aspects of analgesic safety and monitoring.
... Ropivacaine was selected for administering peribulbar block on account of its favorable cardiac and neurologic profile as compared with bupivacaine. [3,4,11,12] Combination of 2% lignocaine in an equimixture of 1:1 was used in the present study on account of achieving an earlier onset with lignocaine and a possible prolonged duration of post-operative pain relief with ropivacaine. [10] Similar observations to our study regarding block characteristics were recorded by few earlier studies while using 0.75% ropivacaine, 0.5% bupivacaine or 2% mepivacaine for different peripheral nerve blocks. ...
... administration than racemic bupivacaine [35]. The same properties apply to another local anesthetic, ropivacaine (propyl homologue of bupivacaine) [36]. ...
Chirality of pharmaceutical substances is an important aspect in drug research because it determines how enantiomers will interact with chiral biological targets. Enantiomers of a chiral drug can have different pharmacokinetic and pharmacological profiles; consequently, using a single pure enantiomer instead of a racemate can enhance the effectiveness and/or safety of the treatment. The tendencies of modern pharmaceutical industry regarding the current market of chiral drugs are divided between the chiral switch of previously used racemates and the development of new enantiopure drugs. The term chiral switch refers to the replacement on the market of a previously approved racemate with its single enantiomer version. The potential advantages of chiral switch can be related to a higher therapeutic index due to better potency, selectivity and fewer adverse effects, faster onset of action and exposure of the patient to lower drug dosages. However, chiral switch is also a strategy that permits manufacturers to keep market exclusivity for chiral pharmaceuticals that have lost their patent protection, even if the pure enantiomers have not demonstrated higher effectiveness or safety profile compared with the racemates.
... Ropivacaine is a long-acting local anesthetic structurally related to bupivacaine with all the assets of bupivacaine and without cardiotoxicity. [16] Hence, ropivacaine has been selected as the regional anesthetic of choice in our study for its improved quality of block and reduced potential toxicity wide margin of safety. [17] Yasuda et al. [18] used a nerve stimulator and an insulated needle for supraclavicular brachial plexus block with a success rate of 98% of patients. ...
Abstract
Background: Brachial plexus block is one of the most common regional anesthetic techniques used for upper limb surgeries. Various adjuvants have been tried for prolonging the duration of post-operative analgesia and also to enhance the quality of block. We aimed to study the effects of the addition of potassium chloride to ropivacaine in supraclavicular brachial plexus block compared to plain ropivacaine.
Materials and Methods: This prospective, randomized, double-blind, and controlled study includes 80 adult patients aged between 20 and 60 years with ASA Grade I and II scheduled for upper limb surgeries. These patients were randomly allocated into two groups of 40 each. The patients in the group I/non-KCL group received 30 ml of 0.5 % ropivacaine along with 1 ml normal saline (control group). Group II/KCL group received 30 ml of 0.5% ropivacaine along with 0.2 mmol (0.1 ml) of potassium chloride (prepared by adding 0.1 ml of potassium chloride diluted with normal saline to make a volume of 1 ml) (study group). The onset, duration of sensory and motor blockade, quality of sensory and motor blockade, and the duration of post-operative analgesia were compared between both the groups.
Results: The onset of sensory and motor blockade was earlier in Group II/ study group when compared to plain ropivacaine group/Group I and was statistically significant with a P < 0.05. The mean duration of sensory and motor blockade was prolonged in Group II with enhanced quality of analgesia compared to Group I.
Conclusion: In our study, it concludes that the addition of potassium chloride as an adjuvant to ropivacaine had a significant clinical advantage over plain ropivacaine on the onset, duration, quality of sensory and motor blockade, and post-operative analgesia in supraclavicular brachial plexus block.
Key words: Adjuvants, Potassium chloride, Ropivacaine, Supraclavicular brachial plexus block
... Ropivacaine, a new aminoamide LA, shows longer analgesic duration (up to 12 h) and less cardiovascular or central nervous system toxicities compared with bupivacaine (Scott et al., 1989;Yang et al., 2019). Ropivacaine hydrochloride injection (Naropin) has been approved for local or regional anesthesia of surgery and for acute pain management, with a plasma clearance rate of 8 L/min, a renal clearance rate of 1 mL/min, and a final half-life of 1.8 h (Peskin, 2005). ...
Combination therapy combining two drugs in one modified drug delivery system is used to achieve synergistic analgesic effect, and bring effective control of pain management, especially postoperative pain management. In the present study, a combination of drug delivery technologies was utilized. Transcriptional transactivator (TAT) peptide modified, transdermal nanocarriers were designed to co-deliver ropivacaine (RVC) and meloxicam (MLX) and anticipated to achieve longer analgesic effect and lower side effect. TAT modified nanostructured lipid carriers (TAT-NLCs) were used to co-deliver RVC and MLX. RVC and MLX co-loaded TAT-NLCs (TAT-NLCs-RVC/MLX) were evaluated through in vitro skin permeation and in vivo treatment studies. NLCs-RVC/MLX showed uniform and spherical morphology, with a size of 133.4 ± 4.6 nm and a zeta potential of 20.6 ± 1.8 mV. The results illustrated the anesthetic pain relief ability of the present constructed system was significantly improved by the TAT modification through the enhanced skin permeation efficiency and the co-delivery of MLX along with RVC that improved pain management by reducing inflammation at the injured area. This study provides an efficient and facile method for preparing TAT-NLCs-RVC/MLX as a promising system to achieve synergistic analgesic effect.
... Knudsen et al. [8] found that ropivacaine toxicity occurred at concentrations of 0.34-0.85 μg/ml (arterial blood, free form) and Scott et al. [9] found ropivacaine toxicity at concentrations of 1-2 μg/ml (venous blood). Therefore, it is possible ropivacaine induced LAST in our cases. ...
Background:
Local anesthetics systemic toxicity (LAST) is a grave complication of regional anesthesia that usually occurs immediately after local anesthetics injection. Here, we report on rare late-onset toxicity cases after supraclavicular brachial plexus blocks.
Case:
Two patients underwent surgery for radius fractures. We used lidocaine 100 mg and ropivacaine 150 mg for blocking and infused dexmedetomidine for intraoperative sedation. The 63-year-old male patient's blood pressure dropped to 87/60 mmHg after 3 h 15 min after blocking. Ventricular fibrillation occurred 10 min later. After five defibrillations, electrocardiography showed ventricular tachycardia that was normalized through one cardioversion. The 54-year-old female patient's heart rate decreased to 35 beats/min 2 h 30 min after blocking. Her vital signs returned to normal after administering atropine, ephedrine, epinephrine, and lipid emulsion.
Conclusions:
Physicians should remember that LAST may occur long after local anesthetic injection and be aware of factors that may adversely affect the course of LAST.
... Ropivacaine exists as an S-enantiomer and exhibits less central nervous system and cardiovascular toxicity than bupivacaine in healthy individuals [29][30][31][32]. It has been shown that combined use of ropivacaine and Bupivacaine yields lower postoperative pain scores [33]. ...
To systematically identify, evaluate and assess the efficacy of systemic analgesics with that of long acting local anaesthetic agents in management of post-operative pain in patients undergoing palatoplasty. Objective: To identify, appraise and assess the available evidence in literature on the use of long acting amide local anaesthetic agent as an alternative and/or adjuvant to systemic analgesics in management of post-operative pain in paediatric patients undergoing palatoplasty which in turn may lead to reduction in complications associated with opioid/ NSAIDs consumption. Methods: A comprehensive search was done using electronic databases of PubMed, Google Scholar and Cochrane central register of controlled trials were searched for related studies along with a complementary manual search of relevant journals using PICO terms. The title scan was done to identify relevant articles, which were further evaluated for inclusion by reading the abstract. Bibliography of all the identified studies was scanned to include studies published outside the electronic database. Results: Electronic database search identified 29 articles. Out of which, 19 were excluded after removing duplication and 15 were excluded after reading titles. 4 studies were evaluated in detail after reading the abstract and full text. A final of 2 studies were included based on the inclusion criteria to meet the research question. The studies analysed quantity and need for post-operative rescue analgesia in patients undergoing palatoplasty. Conclusion: Cleft palate repair is a painful procedure which needs a standardised approach to address post-operative pain in children. The available evidence based on the included studies show those loco-regional nerve blocks with long acting amide local anaesthetic agents are a safe, effective and simple measure for management of postoperative pain in a predictable manner after palatoplasty. Regional anaesthesia also reduces the total consumption of systemic analgesics in the first 48 hours post operatively. However, limited number of studies is available, hence we can only draw a guarded conclusion that postoperative complications associated with systemic analgesics can also be reduced in children.
... However, this pain relief is usually short-lived because of the relatively brief duration of action of currently available local anesthetics (LA) [3], resulting in resolution of block before the period of worst postoperative pain [4]. Increasing the volume (dose) of LAs prolongs the duration of analgesia [5], but also increases the risk of systemic LA toxicity [6]. Continuous catheter-based nerve blocks can extend postoperative analgesia, but their placement requires additional time, cost, and skill. ...
Background: The current study attempts to evaluate the effect of intravenous (IV) infusion of magnesium sulfate during spinal anesthesia on postoperative pain and postoperative analgesic requirements in lower limb surgeries.
Methods: In this double blind, randomized controlled study, 60 patients undergoing elective lower limb surgeries, were selected and randomly divided into two groups. Group I received isotonic saline and group II was administered magnesium sulfate 50 mg Kg-1 IV for 15 min and then 15 mg Kg-1 h-1 by continuous IV infusion till the end of surgery or 2 hours, whichever was earlier. Ramsay sedation scores, VAS scores for pain, time of first administration of rescue analgesic and total analgesic requirement were noted in both the groups.
Results: Statistically significant difference was observed in the VAS score between the two groups at 1st, 2nd, 3rd, 6th, 9th and 12th hour intervals; with VAS scores being lower in the magnesium group (p
... However, adverse reactions are often associated with the use of these agents. 5,6 Therefore, there is a growing demand for preventing and managing undesired pain without adverse effects using natural compounds. ...
Eugenol is a major phenolic component derived from clove oil with potential medical applications. Of particular interest, it has been used as a therapeutic agent in topical applications because of its analgesic and local anesthetic properties. However, topical formulations of eugenol produce skin irritation, which limits its clinical applications. One promising strategy to overcome this disadvantage is by using a biocompatible material that could be an appropriate topical vehicle for eugenol. Researchers have recently focused on the development of eugenol-embedded calcium citrate nanoparticles (Eu-CaCit NPs) without adverse effects. The Eu-CaCit NPs were developed as a topical delivery system and their biocompatibility and penetration ability were evaluated. Eu-CaCit NPs at 1.2 mg/mL did not show cytotoxicity effects in human cells. Moreover, the Eu-CaCit NPs presented the ability to penetrate the dermis layer of the human intact skin following 12 h exposure. All the results concluded that Eu-CaCit NPs have shown a potential as a carrier for topical delivery of eugenol. These novel nanoparticles represent a promising alternative for topical application of local anesthetic with natural pain relievers.
Background
Caudal epidural block is widely used in the pediatric age group. This study aims to determine that ropivacaine with fentanyl provides a shorter duration of motor blockade than the comparable sensory blockade, which can be used as an effective alternative to bupivacaine in caudal epidural anesthesia.
Objective
The objective of this study was to assess the efficacy of ropivacaine versus bupivacaine when combined with fentanyl in single-shot caudal epidural anesthesia in pediatric infraumbilical surgeries in terms of time taken for motor regression.
Subjects and Methods
This was a prospective randomized double blinded study done among the pediatric population of 1-12years, undergoing infraumbilical surgeries under general anaesthesia. Efficacy of caudal epidural anaesthesia assessed with fentanyl+bupivacaine 30 patients (50%) and fentanyl+ ropivocaine 30 patients (50%). Group 1 received 0.25% of 0.7 mL/kg bupivacaine + 1 mg/kg of fentanyl with normal saline in a caudal epidural. Group 2 received 0.25% of 0.7 mL/kg ropivacaine + 1 mg/kg of fentanyl with normal saline in a caudal epidural. The demographic details and anthropometry were compared. The hemodynamic parameters were compared both intraoperatively and postoperatively. Bromage scale and Face, Legs, Activity, Cry, and Consolability pain score were compared postoperatively between both the groups.
Results
The hemodynamic parameters, sedation, and pain were not statistically different between the groups. Among the bupivacaine group, there was a statistically significant, higher Bromage scale ( P = 0.001), decreased time to rescue analgesia ( P = 0.001), and higher duration of motor blockade ( P = 0.001).
Conclusion
We conclude that ropivacaine (0.25%) with fentanyl provides less intense motor nerve blockade with a shorter duration of analgesia, hence facilitating early ambulation.
Introduction:
Intercostal nerve block (ICNB) has long been used in thoracic surgery. Local anesthetic thoracoscopy (LAT) is performed under conscious sedation with local anesthesia at the port insertion site. This alone, however, does not anesthetize the parietal pleura from where biopsies are taken and patients can experience pain.
Objectives:
To compare LAT with multilevel ICNB versus standard care to determine whether it reduces pain during and post-LAT, its effect on analgesia use, the hospital length of stay (LOS), and related complications.
Methods:
Prospective analysis of patients undergoing LAT between January and June 2021. In the ICNB group, levobupivacaine/xylocaine is administered at the angle of the rib immediately before LAT (up to 5 rib spaces). Visual Analog Score for pain (0 to 100 mm) was measured at 1 and 2 hours post-LAT and daily including analgesia use.
Results:
Twenty patients (10 ICNB vs. 10 standard care group). The mean age is 68 years with 70% males. Visual Analog Score for pain in the ICNB group reduced by 55 mm at 1 and 2 hours post-LAT and 45 mm at day 1 (P<0.05) (minimal clinically important difference >16 mm]. Median LOS was reduced by 50% in the ICNB group (P<0.05). Paracetamol use reduced by 56% (P<0.05).
Conclusion:
ICNB not only significantly reduces postprocedure pain but also reduces LOS.
The local analgesic efficacy and adverse effects of a new Long-acting Ropivacaine formulation were examined based on pharmacokinetic-pharmacodynamic (PK-PD) modelling in Bama minipigs. 24 Bama minipigs, 12 males and 12 females, were randomly and equally divided into the following treatment groups: normal saline injection, drug vehicle injection, Long-acting Ropivacaine Injection and Ropivacaine Hydrochloride Injection. After routine disinfection, a skin incision about 3 cm long and 3 cm deep was produced in the leg of each pig, and mechanical withdrawal threshold (MWT) measured at various times pre- and post-injection as an index of analgesia against incision pain. Plasma ropivacaine concentrations were also measured at the same times using a novel liquid chromatography-tandem mass spectroscopy (LC-MS/MS) method. Minipigs were sacrificed 24 h post-injection and hearts collected for drug concentration measurements by LC-MS/MS. The LC-MS/MS method demonstrated high sensitivity, linearity and precision. The Long-acting Ropivacaine formulation produced a longer analgesic effect (∼12 h) at a lower plasma concentration than Ropivacaine Hydrochloride (∼4h), suggesting a better side-effects profile. A PK-PD model revealed a direct relationship between plasma ropivacaine concentration and MWT, with peak analgesia at about 1000 ng/mL and behaved good prediction ability. Long-acting Ropivacaine Injection is a superior local anaesthetic-analgesic treatment due to longer-lasting efficacy at lower concentrations compared to Ropivacaine Hydrochloride, which will reduce the risk of side effects such as cardiotoxicity.
Considering the amount of local anesthetic administered on a daily basis, dental professionals must be familiar with the factors that influence the dose and type of local anesthetic that induces a toxic or allergic reaction. In addition to the route and rate of administration, the patient’s physical condition and health may also influence the dose of local anesthetic that could be safely administered. This article reviews the different causes of local anesthesia toxicity and allergy. With prevention and early recognition of the warning signs, poor prognosis can be avoided.
Introduction: Labour pain is of major concern since most parturients experience signicant pain of extremely severe intensity. Labour pain can have deleterious effects on the mother, on the foetus and on the labour outcome. Epidural anaesthesia is an effective means of providing analgesia during labour. To compare the efcacy of epidural analgesia using 0.125% bupivacaine and 0.0002% Aim: fentanyl versus an epidural using 0.25% bupivacaine alone for labour analgesia. It is a prospective comparative study c Methods: onducted at a Tertiary care hospital, Fifty parturients who were admitted to the antenatal ward and who requested pain relief during labor and who fullled the inclusion criteria were selected for the study after taking written informed consent. Analgesia provided by both techniques Conclusion: was found to be similar. Women in group FB retained motor power in their legs. Motor Block was minimized in Group FB. Both the intervention group had lesser impact on the hemodynamics. Complications were minor and were easily managed.
Targeted blockade of the nerves of the scalp have been found to be beneficial for many different types of surgeries of the head, as well as for some nonsurgical conditions. Craniotomy has been the most widely studied surgical procedure of the head, and it is associated with a high risk of severe acute and chronic pain. Several techniques to combat this pain include the use of multimodal analgesia, infiltration of local anesthetic, and the regional technique of scalp blocks. The common indications for scalp blocks include extracranial surgery, blunting of the hemodynamic response to intracranial surgery, and reducing acute and chronic pain following intracranial surgery. Its evolving role in decreasing acute and chronic pain parallels that of other types of neural blockade, and efforts to find efficacious combinations of procedure, patient, and technique are ongoing. However, the fact that extracranial blockade of the dura is not possible is one of the limits to the analgesia provided by scalp blockade (Papangelou et al., J Clin Anesth 25:150–159, 2013.
Objective:
To provide an overview of the current available literature on peripheral nerve blocks for the management of migraine and other headache disorders in adults.
Background:
Peripheral nerve blocks have been commonly performed in the headache practice for migraine, cluster headache, occipital neuralgia, and other headache disorders, despite a paucity of evidence supporting their use historically. In the past decade, there has been an effort to explore the efficacy and safety of peripheral nerve blocks for the management of headache, with the greatest interest centered around greater occipital blocks.
Design:
We performed a search in PubMed using key words including "occipital nerve blocks," "peripheral nerve blocks," "occipital nerve," "migraine," "cluster headache," and "neuralgia." We reviewed the randomized controlled trials (RCTs), observational studies, and case series, and summarized the anatomy, techniques, and the evidence for the use of peripheral nerve blocks in different headache disorders, with particular focus on available RCTs. Case reports were included for a detail review of adverse events.
Results:
Of 12 RCTs examining the use of greater occipital nerve blocks for migraine, all but one demonstrate efficacy with reduction in headache frequency, intensity, and/or duration compared to placebo. Studies have not demonstrated a difference in clinical outcomes with the use of corticosteroids for nerve blocks compared to blocks with local anesthetic in the treatment of migraine. There are two RCTs supporting the use of greater occipital blockade for cluster headache, both showing benefit of suboccipitally injected corticosteroid. One RCT suggests benefit of greater occipital nerve blocks for cervicogenic headache. Observational studies and case series/reports show that greater occipital nerve block may be effective in prolonged migraine aura, status migrainosus, post-dural puncture headache, and occipital neuralgia. Overall, peripheral nerve blocks are well tolerated. Serious side effects are rare but have been reported, including acute cerebellar syndrome and infection.
Conclusions:
Peripheral nerve blocks, especially occipital nerve blocks, are a viable treatment option for migraine and may be helpful in cluster headache as a transitional therapy or rescue therapy. Additional prospective studies are needed to investigate the efficacy and safety of occipital nerve blocks for long-term migraine prevention, as well as for other headache disorders, such as occipital neuralgia.
Hintergrund und Ziele: Intoxikationen mit Ionenkanalblockern wie Lokalanästhetika, beispielsweise durch akzidentielle intravenöse Applikation, können zu schwerwiegenden kardiovaskulären Nebenwirkungen bis hin zum Herz-Kreislauf-Stillstand führen. Lipophile Lokalanästhetika wie Bupivacain weisen eine besonders hohe Kardiotoxizität auf, was die Behandlung von Intoxikationen mit der Substanz erschwert. Es existieren erfolgsversprechende Berichte über den Einsatz von intravenöser Lipidemulsion bei Reanimationen nach Intoxikationen mit Lokalanästhetika, ein Therapieansatz, der in Fachkreisen als Lipid Rescue bezeichnet wird. Die Lipid Sink Theorie ist eine Hypothese, die eine Reduktion der freien Lokalanästhetikakonzentration als Mechanismus annimmt. Daneben werden unter anderem metabolische Effekte als Ursache diskutiert. Jedoch wird der zugrunde liegende Mechanismus bislang nicht vollständig verstanden. Das Ziel dieser Arbeit ist, den Mechanismus von Lipid Rescue auf Ionenkanalebene zu untersuchen. Methoden: Die vorliegende Arbeit untersucht die Effekte einer klinisch verwendeten Lipidemulsion (Lipovenös MCT 20%; Fresenius Kabi AG, Bad Homburg, Deutschland) auf Aktionspotentiale und auf den Block des schnellen Na+ Kanals (INa) durch das lipophile Lokalanästhetikum Bupivacain in Kardiomyozyten der Ratte mit Hilfe der whole-cell Patch-Clamp Technik. Analog werden die Effekte der Lipidemulsion auf Aktionspotentiale und den Block von INa durch das weniger lipophile Mepivacain untersucht. Da abhängig von der Lokalisation von Kardiomyozyten im linken Ventrikel bezüglich Aktionspotentialdauer große Unterschiede bestehen, erfolgte eine regionspezifische Isolation von Kardiomyozyten und die getrennte Betrachtung epi- und endokardialer Zellen. Um herauszufinden, ob der Wirkmechanismus auf eine Reduktion der freien Konzentration der Lokalanästhetika, einen sogenannten Lipid Sink Effekt, zurückzuführen ist, erfolgte in einem Teil der Experimente die Ultrazentrifugation der Lipidemulsionen. Die effektive Reduktion der freien Lokalanästhetikakonzentration durch die Lipidemulsion wurde durch die Klinik für Anästhesie des Universitätsklinikums Regensburg mittels Gaschromatographie mit Massenspektroskopie-Kopplung bestimmt. Ergebnisse und Beobachtungen: 10 μM Bupivacain verursachte in epikardialen Kardiomyozyten eine Reduktion der maximalen Aufstrichgeschwindigkeit von Aktionspotentialen (dV/dtmax) um 56% (P < 0.001). Der Overshoot wurde um 43% (P < 0.001) reduziert. Nach Applikation einer 10 μM Bupivacainlösung, die zusätzlich 10% einer klinisch verwendeten Lipidemulsion enthielt, nahmen dV/dtmax und der Overshoot jeweils um 31% zu (P < 0.001). In endokardialen Zellen fanden sich vergleichbare Effekte. Das hydrophile Lokalanästhetikum Mepivacain (40 μM) führte ebenfalls sowohl in epi- als auch endokardialen Zellen zu einer signifikanten Reduktion von dV/dtmax (P < 0.001) und Overshoot (P < 0.001). Applikation einer 40 μM Mepivacainlösung, die zusätzlich 10% Lipidemulsion enthielt, hatte keine Auswirkungen auf diese Effekte, im Gegensatz zu denen des lipophilen Bupivacains. Bei der Untersuchung des schnellen spannungsgesteuerten Na+ Stromes reduzierte 10 μM Bupivacain INa um 54% (-19.3 ± 1.9 pApF-1 gegen -42.3 ± 4.3 pApF-1; n = 17; P < 0.001; VPip = -40mV). Der Zusatz von 10% Lipidemulsion zusätzlich zu Bupivacain führte zu einer Zunahme von INa um 37% (-26.4 ± 2.8 pApF-1; n = 17; P < 0.001 gegen Bupivacain allein). Um zu testen, ob die Ergebnisse durch eine Reduktion der freien Bupivacainkonzentration bedingt wird (Lipid Sink Effekt), wurde die Lipidphase durch Ultrazentrifugation entfernt. Die übrigbleibende Wasserphase führte zu einer Zunahme von INa (+19%; n = 17; P < 0.001 gegen Bupivacain), was zeigt, dass ein Teil der Lipidwirkung durch eine Verminderung der Bupivacainkonzentration in der wässrigen Phase der Lösung zustande kommt. Vergleiche der Versuche mit zentrifugierter und unzentrifugierter Emulsion sowie Versuche mit Lipidemulsion ohne Lokalanästhetika zeigten, dass neben der Reduktion der freien Lokalanästhetikakonzentration ein spezifischer Lipid Effekt auftrat, der unabhängig von der Anwesenheit von Lokalanästhetika war. Bei der Untersuchung des weniger lipophilen Mepivacains zeigte sich durch 40 μM Mepivacain eine Reduktion von INa um 27% (n = 24; P <0.001). Zusatz von Lipidemulsion führte zu einer Zunahme von INa um 17% (n = 24; P <0.001). Nach Ultrazentrifugation fand sich nur ein kleiner Effekt mit einer Zunahme von INa um 8% (n = 23; P < 0.01). Schlussfolgerungen: Die Experimente dieser Arbeit zeigen auf zellulärer Ebene, dass die Effekte von Lokalanästhetika auf den Na+ Strom und auf Aktionspotentiale durch Lipidemulsion vermindert werden können. Das Ausmaß der Reduktion des Effekts war bei lipophilen im Vergleich zu hydrophilen Lokalanästhetika größer. Der Mechanismus hierfür besteht aus einer Reduktion der freien Lokalanästhetikakonzentration, dem Lipid Sink Effekt, sowie aus einem spezifischen Lipid Effekt, der unabhängig von der Anwesenheit von Lokalanästhetika auftritt. Die Ergebnisse legen außerdem nahe, dass Lipid Rescue auch zur Behandlung von Intoxikationen mit weiteren lipophilen Substanzen mit ionenkanalinhibitorischer Wirkung, wie zum Beispiel trizyklischen Antidepressiva, geeignet ist. Teilergebnisse dieser Arbeit wurden veröffentlicht (Wagner et al., 2014).
Introduction
Liver resection patients may be at an increased risk of local anesthetic (LA) toxicity because the liver is essential for metabolizing LA and producing proteins (mainly α 1 -acid glycoprotein (AAG)) that bind to it and reduce the free (and pharmacologically active/toxic) levels in circulation. The liver resection itself, manipulation during surgery, and pre-existing liver disease may all interfere with normal hepatic protein synthesis and result in an attenuation of the increased AAG (a positive acute-phase protein) that normally occurs postoperatively. The purpose of this study was to determine whether the AAG response is attenuated postoperatively following liver resection and whether patients approach toxicity thresholds with continuous postoperative epidural infusion of bupivacaine.
Methods
Prospective, observational study with blood drawn preoperatively, in the postanesthetic care unit, on postoperative day (POD) 2, and prior to discontinuation of epidural analgesia on POD3/POD4. Plasma was analyzed for total and unbound bupivacaine via liquid chromatography–mass spectrometry and AAG via ELISA. Signs/symptoms of local anesthetic systemic toxicity (LAST), pain, and sedation scores were also recorded.
Results
For the 19 patients completed, total plasma bupivacaine was correlated with total administered, but unbound levels were not associated with the total administered. Unlike non-hepatectomy surgery where unbound LA plasma levels remain stable (or decrease) with continuous postoperative epidural administration, we observed an overall increase. Several patients approached toxicity thresholds and 47% reported at least one symptom of LAST, but no epidurals were discontinued because of LAST. In contrast to the AAG response reported following major non-liver surgery where AAG levels increase twofold, we observed a reduction until POD2 and the magnitude was proportional to resection weight.
Discussion
Our results are supported by the literature in suggesting that major liver resection patients may be at an increased vulnerability for LAST. Factors such as the extent of liver disease, resection and intraoperative blood loss should be considered when using continuous postoperative epidural infusion of bupivacaine and vigilance should be used in monitoring, for signs/symptoms of LAST, even for those subtle and non-specific. Future research will be required to verify these findings.
Trial registration number
NCT03145805 .
Background: Choice of an appropriate analgesic regimen is especially important in ESRD patients. Regional analgesia technique such as epidural with local anaesthetic drugs has been found suitable in such patients. This study was designed to compare a high-volume/low-concentration with low-volume/high concentration ropivacaine regimen in ESRD transplant patients. Materials And Methods: This prospective, open level randomized control study was conducted on 40 end stage renal disease (ESRD) patients, aged between 20- 60 years of either sex who underwent live-related renal transplant surgery.GROUP A Low volume/High concentration group received 6 ml of 0.75% ropivacaine and GROUP B High volume/Low concentration group received 12 ml of 0.375% ropivacaine.Total dose of ropivacaine needed for postoperative pain control and for achieving T6 to S5 sensory block, Level of motor blockade and Dose of vasopressors needed for haemodynamic stability was compared. Results: Total dose of ropivacaine required to achieve T6 to S5 sensory block and total dose of vasopressor used was higher in low volume high concentration group at initiation of block. Postoperative quality of analgesia as assessed by VAS score and top up requirements (total dose of postoperative ropivacaine used) was comparable in both the groups. Conclusion: We conclude no added advantage of using low volume high concentration ropivacaine drug regimen in renal transplant recipients in terms of quality of analgesia and haemodynamic stability.
Introduction
Emergency clinicians utilize local anesthetics for a variety of procedures in the emergency department (ED) setting. Local anesthetic systemic toxicity (LAST) is a potentially deadly complication.
Objective
This narrative review provides emergency clinicians with the most current evidence regarding the pathophysiology, evaluation, and management of patients with LAST.
Discussion
LAST is an uncommon but potentially life-threatening complication of local anesthetic use that may be encountered in the ED. Patients at extremes of age or with organ dysfunction are at higher risk. Inadvertent intra-arterial or intravenous injection, as well as repeated doses and higher doses of local anesthetics are associated with greater risk of developing LAST. Neurologic and cardiovascular manifestations can occur. Early recognition and intervention, including supportive care and intravenous lipid emulsion 20%, are the mainstays of treatment. Using ultrasound guidance, aspirating prior to injection, and utilizing the minimal local anesthetic dose needed are techniques that can reduce the risk of LAST.
Conclusions
This focused review provides an update for the emergency clinician to manage patients with LAST.
Purpose: To compare efficacies of bupivacaine-lidocaine and ropivacaine-lidocaine mixtures in terms of inducing retrobulbar anesthesia during vitrectomy.Methods: Sixty patients who underwent retrobulbar anesthesia during vitrectomy were divided into two groups. Patients in group 1 received a mixture of bupivacaine and lidocaine (n = 30); patients in group 2 received a mixture of ropivacaine and lidocaine (n = 30). The effects of the two combinations were retrospectively compared and analyzed. The onset times of analgesia and akinesia were measured. Two hours after surgery, sensory blockade was assessed by touching the corneas with cotton swabs and by communicating with patients. Ocular movement was evaluated in four gaze direction quadrants. A 10-point visual analog pain scale was used to assess pain during and 2 hours after surgery. Intra- and postoperative complications were recorded.Results: The mean analgesia onset times in groups 1 and 2 were 94.62 ± 28.87 and 92.32 ± 35.53 seconds, respectively (p = 0.071); the mean akinesia onset times were 147.89 ± 59.35 and 132.57 ± 76.38 seconds (p = 0.223), respectively. Patients in group 2 reported significantly less postoperative pain and exhibited less postoperative ocular movement, compared with patients in group 1 (both p = 0.002). One patient in group 1 experienced respiratory depression after retrobulbar blockade.Conclusions: When retrobulbar anesthesia is required during vitrectomy, a ropivacaine-lidocaine mixture and a bupivacaine-lidocaine mixture induce anesthesia with similar rapidity. However, the ropivacaine-lidocaine mixture is safer and affords better-quality intra- and postoperative anesthesia.
Local analgesics effectively allow patients to relieve postoperative pain and reduce the need for inhaled general anesthetics or opioids. Compared with other similar long-acting local anesthetics, ropivacaine (Rop) is widely used due to its potential to minimize cardiotoxicity. However, the relatively short duration of Rop efficacy, which lasts for several hours after injection, is considered insufficient for long-term acute and chronic pain treatment. At present, repeated injections or indwelling catheters are used to achieve long-term drug delivery, which can easily cause infection and inflammation. To achieve externally controllable analgesia for a prolonged time, we prepared near-infrared (NIR)-responsive Rop liposomes ([email protected]) containing photosensitizers PdPC(OBu)8 and unsaturated phospholipid DLPC. The particle size of the [email protected] was 234.73±5.21 nm, the PDI was 0.42±0.02, and the drug encapsulation rate was 94.62±1.1%. The release of Rop was highly NIR-dependent in vitro and in vivo. To ensure that the liposomes reside around the nerve for an extended period, we next designed an in situ gel with chitosan (CS) and β-sodium glycerophosphate (β-GP) to form a liposomal gel (Lip/Gel). This Lip/Gel composite drug delivery system could be retained in vivo for 10 d, reduce the side effects caused by drug overdose, and prolong the duration of efficacy. In summary, the NIR-responsive Rop composite drug delivery system generated in this paper can effectively solve the shortcomings of traditional local injections, reduce the toxicity and side effects of free Rop, and provide a basis for a light-responsive delivery system of analgesic drugs.
Local anesthetics provide analgesia and can be incorporated into multimodal anesthetic protocols. They work by blocking the voltage-dependent sodium ion channels along neurons that mediate nociception. Systemically, these drugs can be cardiotoxic in a dose-dependent manner. Lidocaine and bupivacaine are the most commonly used local anesthetics and their use has been reported in all classes of vertebrates. Despite anecdotal reports to the contrary, zoologic companion animals are unlikely to be more susceptible to the cardiotoxic effects of local anesthetics than domestic small animals. Local anesthetics can be clinically useful for analgesia and anesthesia in zoologic companion animal practice.
A 9‐year‐old male neutered domestic short hair cat was referred to our practice after a road traffic accident. On presentation, the cat was obtunded, with bilateral hindlimb fractures. The fractures were surgically repaired, and an epidural catheter was placed for perioperative pain management. Postoperative analgesia consisted of bupivacaine administered intermittently through the epidural catheter. In the days after surgery, the cat became duller and more obtunded, and marked bilateral mydriasis with absence of a pupillary reflex was noted. After ruling out different causes for mydriasis and weaning the cat from systemic opioids, local anaesthetic systemic toxicity (LAST) emerged the primary differential diagnosis. Bupivacaine plasma concentrations were measured and found a fourfold increase in concentration over that reported after a perineural block. Mydriasis and absent pupillary light reflex, among other clinical signs, could be early indicators of LAST secondary to accumulation of the local anaesthetic in patients with an epidural catheter.
Background:
Dexmedetomidine and magnesium sulfate (MgSO4) as an adjuvant to local anesthetics and ultrasound guidance improves the quality of peripheral nerve block.
Aim:
We aim to compare the efficacy of dexmedetomidine and MgSO4 as an adjuvant to ropivacaine in supraclavicular brachial plexus block.
Methodology:
Sixty patients undergoing upper extremity orthopedic surgery were randomly allocated into three groups of 20 each. Group A received 29 mL of 0.5% ropivacaine plus 1 mL of normal saline, Group B received 29 mL of 0.5% ropivacaine plus 1 mL dexmedetomidine (100 μg), and Group C received 29 mL of 0.5% ropivacaine plus 1 mL MgSO4 (250 mg). Onset and duration of sensory and motor block, duration of analgesia, quality of anesthesia, total 24 h analgesic consumption, sedation, and complications were recorded.
Statistical analysis:
Software SPSS-16 was used for statistical analysis.
Results:
The onset of sensory block and motor block was fastest for Group B, followed by Group C and slowest in Group A. The duration of sensory block and motor block was maximum for Group B, followed by Group C and minimum for Group A. The duration of analgesia was maximum for Group B, followed by Group C and minimum for Group A. Analgesic consumption was minimum for Group B. Quality of anesthesia was better in Group B than other groups. The visual analog scale was higher in Group A than other groups. Group B reported higher sedation score.
Conclusion:
Dexmedetomidine provides earlier onset of sensory and motor block as well as prolonged duration of sensory and motor blocks and duration of analgesia is longer and postoperative rescue analgesia is less as compared to patients receiving MgSO4. The incidence of hypotension and bradycardia and sedation score was higher with dexmedetomidine.
The validity of using echocardiography to measure the effects of cardiovascular drugs on the heart has been investigated. A standardised method of measuring left ventricular diameters is described and used to measure variability and therefore reproducibility in 20 subjects. Immediate variability was measured in 10 normal subjects. In 5 of these subjects varaiability was measured every few minutes, hourly, and weekly during control periods of drug studies and also after an interval of 1 year. Estimates were made of the minimum significant change in heart size which could be defined under these circumstances. Reproducibility decreased with increasing time interval between studies but overall was very good (coefficient of variation in diameters from 1 to 8%). Even with a time interval of 1 year the individual absolute difference in the mean of diameters was never greater than 0.3 cm. Reproducibility was similar in small groups of patients with hypertension or ischaemic heart disease (without dyskinesia). Estimated sensitvity could be increased for any time interval equally as much by increasing the number of measurements on each occasion and modifying statistical analysis accordingly as by doubling the number of subjects. There was a fourfold difference between minimum and maximum sensitivity. After 0.5 mg sublingual glyceryl trinitrate, diastolic and systolic diameters decreased significantly in all subects. Estimated ventricular and stroke volumes were reduced. Cardiac output was unchanged as heart rate increased from 67 to 80 beats per minute while blood pressure fell. The estimated ejection phase indices (ejection fraction, fractional shortening, and fibre shortening rate) all increased significantly. With rigid standardisation echocardiography could be a potentially useful non-invasive method of measuring the effects of cardiovascular drugs on the heart.
In planning a cardiac operation, the key objective should be to accomplish the best possible benefit for the myocardium with the least possible stress. The ultimate objective for most cardiac operations is to preserve and protect myocardial function through correction of the mechanical burden, such as a septal defect, malfunctioning valve, or obstructed coronary artery. In the preoperative evaluation of the cardiac patient, the anesthesiologist wishes to know the basis for the existing burden on the myocardium, its current state of compensation and, if possible, its margin of functional reserve. This information will influence all phases of surgical management: preoperative, intraoperative, and postoperative. There is no single examination or parameter that will provide the anesthesiologist with all that he needs to know.
The simplest and most cost-effective means of evaluating the cardiac patient is a careful review of the history and physical examination by the anesthesiologist who will be responsible for his management. Much can be learned about the state of the myocardium by observing such simple signs as the persistent, nonproductive cough, cold clammy skin, pulsus alternans, among many others. The chest roentgenogram and electrocardiogram should be systematically evaluated rather than the mere acceptance of the officially recorded interpretations.
A number of “noninvasive methods” are available, which may help supplement the simple clinical observations. The echocardiogram may demonstrate abnormal dilatation of one or more chambers, diminished wall motion, or paradoxical motion of the interventricular septum. The interpretation should be made with caution, however, for the M-mode echocardiogram provides only . . .
The introduction of the new long acting local anaesthetics, bupivacaine and etidocaine, has stimulated an expansion of interest in regional anaesthesia, particularly for obstetrical applications and pain therapy.
Systemic toxicity following injection of local anaesthetics occurs albeit infrequently, and tentative correlations have been made between the onset of CNS and cardiovascular effects and circulating drug concentrations in both adults and neonates. Amongst other factors, interpretation of these relationships depends upon blood distribution and plasma binding of the agents, sampling sites and acid-base balance.
The disposition kinetics and placental transfer of the amide type agents have been well characterised. In adults their clearance is almost entirely hepatic but in neonates an increase in the renal component is, in part, a reflection of the immaturity of some of the enzymes responsible for their metabolism. Ester type agents are rapidly hydrolysed by plasma pseudocholin-esterase and this has led to a preference for chloroprocaine in some obstetric procedures.
Major determinants of the systemic absorption of the agents after perineural administration include their physicochemical and vasoactive properties, perfusion and tissue binding at the site of injection and whether or not adrenaline has been added. In respect of blood drug concentrations achieved after various regional anaesthetic procedures, the margin of systemic safety appears to favour bupivacaine and etidocaine compared to shorter acting analogues such as lignocaine and mepivacaine. The time course of local anaesthetic remaining at the site of injection has been calculated following intravenous regional anaesthesia and peridural block. This has allowed prediction of the local and systemic accumulation of the drugs following continued dosage.
Blood concentrations of local anaesthetics after perineural injection are not closely related to age, weight or pregnancy but may be influenced by diseases associated with haemodynamic changes and by other drugs given at or around the time of regional blockade.
Originally intended to be a modest ancillary tool in diagnosing structural abnormalities of the heart and the pericardium, the noninvasive technique of echocardiography has greatly expanded its diagnostic orbit. It now competes successfully with invasive angiographic techniques for diagnosing and evaluating valvular and myocardial disorders, as well as those of ventricular function—the latter reflected in the measurements of left ventricular diameters and derived hemodynamic indices. Currently, two-dimensional cross-sectional echocardiography is proving even more informative than M-mode techniques in estimating left ventricular ejection fraction—a reliable index of left ventricular performance.
Can measuring left ventricular diameters be similarly helpful in studying the action of cardiovascular drugs? Gibson1 in 1973 and Burggraf and Parker2 in 1974 suggested this possibility, which has since been explored by a number of investigators with results that varied from endorsement to rejection.
Clearly, no satisfactory answer could be given to the value of echocardiography in the
A number of assumptions are inherent in the echocardiographic estimation of left ventricular volumes. Initial validation of the method compared echocardiographic and angiographic volume measurements. Reasonable correlation was shown between groups in these studies but with major differences in some individuals. Both methods assume an ellipsoid shape for the left ventricle but a standard echocardiographic volume formula (volume = D 3) also assumes a fixed 2:1 ratio between the major and minor axes of the left ventricle. This ratio is only valid in normal sized hearts, and at extremes of heart size it can vary from 3.2:1 to 1.2:1. This introduces a potential source of error into the echo method, but it has been suggested that a correction formula can compensate for the variable ratio at different cardiac sizes. The validity of this formula has been assessed by using it to recalculate the results in four studies comparing echocardiographic and angiographic volumes. The recalculated correlation coefficients and their associated errors were compared with the original results and no consistent improvement was evident. In addition it has previously been shown that the correction formula is unhelpful in the presence of dyskinesia and it is, therefore, suggested that the general use of this formula in correcting echo volume estimations is not helpful.
Four hundred M-mode echocardiographic surveys were distributed to determine interobserver variability in M-mode echocardiographic measurements. This was done with a view toward examining the need and determining the criteria for standardization of measurement. Each survey consisted of five M-mode echocardiograms with a calibration marker, measured by the survey participants anonymously. The echoes were judged of adequate quality for measurement of structures. Seventy-six of the 400 (19%) were returned, allowing comparison of interobserver variability as well as examination of the measurement criteria which were used. Mean measurements and percent uncertainty were derived for each structure for each criterion of measurement. For example, for the aorta, 33% of examiners measured the aorta as an outer/inner or leading edge dimension, and 20% measured it as an outer/outer dimension. The percent uncertainty for the measurement (1.97 SD divided by the mean) showed a mean of 13.8% for the 25 packets of five echoes measured using the former criteria and 24.2% using the latter criteria. For ventricular chamber and cavity measurements, almost one-half of the examiners used the peak of the QRS and one-half of the examiners used the onset of the QRS for determining end-diastole. Estimates of the percent of measurement uncertainty for the septum, posterior wall and left ventricular cavity dimension in this study were 10--25%. They were much higher (40--70%) for the right ventricular cavity and right ventricular anterior wall. The survey shows significant interobserver and interlaboratory variation in measurement when examining the same echoes and indicates a need for ongoing education, quality control and standardization of measurement criteria. Recommendations for new criteria for measurement of M-mode echocardiograms are offered.
SUMMARY Etidocaine given by intravenous infusion has been compared, using a double-blind technique, with bupivacaine and lignocaine
in respect of toxic symptoms and signs. The degree of toxicity is affected considerably by the rate of drug infusion. At 10
mg/min subjects could tolerate twice the dose of etidocaine as bupivacaine. Tolerance to etidocaine was less at 20 mg/min
but still compared favourably with bupivacaine at 10 mg/min. Considering the difference in potency of the two agents it was
considered that the therapeutic ratios would not be substantially different. Lignocaine at 20 mg/min was better tolerated
than etidocaine. Venous plasma concentration during these experiments showed a more rapid decrease in the case of etidocaine
compared with bupivacaine, but the concentrations were unhelpful in predicting the toxic effects. Similarly electroencephalography
revealed no abnormalities in spite of marked subjective and objective signs of toxicity.
An echocardiogram from the left ventricle may be used to estimate left ventricular volume and rate of circumferential fiber shortening, to measure posterior wall and interventricular septal thickness and to evaluate the normality of septal motion. Extended application of this technique in this laboratory has emphasized the need for a more standardized means of transducer location and direction. The effect of placing the ultrasonic transducer in several intercostal spaces along the left sternal border was tested in 14 patients. Variability in the left ventricular dimension and the difference in this dimension from end-diastole to end-systole were greater than for duplicate measurements from the same interspace. A system has been developed for more consistent placement of the transducer in each patient, using intracardiac landmarks and observation of transducer orientation to record specific cardiac structures.
The clinical tolerance to local anaesthetic drugs can be assessed from a knowledge of their pharmacokinetic behaviour, their absorption properties and the effects produced by controlled i.v. infusions. Pharmacokinetic behavior can be calculated from the plasma concentrations of the drugs injected i.v. in non-toxic doses. Absorption properties can likewise be determined from plasma concentrations following injection at various sites. Acute toxicity can be assessed by i.v. infusion of toxic doses into volunteers. The dosage required to produce symptoms can be compared with other drugs. Such dosage is considerably affected by the rate of injection. The venous plasma concentrations at the height of toxicity are unreliable guides to toxicity. Experiences using the new local anaesthetic etidocaine are reported.
Ropivacaine (S-(-)-1-propyl-2',6'-pipecoloxylidide) is a new local anesthetic that is structurally related to mepivacaine and bupivacaine. The comparative effects of ropivacaine and bupivacaine on motor function were assessed in the laboratory rat and dog. (It was not possible to accurately evaluate sensory blockade in these models.) Several concentrations of both agents were injected in the region of the sciatic nerve of the rat and into the lumbar epidural or subarachoid space in the dog. Epidural blockade was also performed utilizing solutions of ropivacaine and bupivacaine which contained epinephrine (1:200,000). The rat sciatic block studies indicate that at concentrations of 0.5 and 0.75%, ropivacaine had a slightly shorter time of onset and duration of motor blockade than did bupivacaine. In the epidural and spinal studies in the dog, ropivacaine was less potent and had a shorter duration of motor blockade than did bupivacaine at equal drug concentrations. A 1.0% solution of ropivacaine produced epidural motor blockade similar in onset and duration to that achieved with a 0.75% solution of bupivacaine. Epinephrine did not significantly prolong the duration of motor blockade of either agent after epidural administration.
The local anaesthestic properties of 1-propyl-2',6'-pipecoloxylidide, a congener of mepivacaine and bupivacaine, and its enantiomers were compared in animals. The (S)-enantiomer (ropivacaine, LEA 103) produced a longer duration of sciatic nerve block and infiltration anaesthesia than the racemate and the (R)-form. Ropivacaine and bupivacaine were equally potent in terms of block of evoked action potential in vitro and minimum effective concentration in vivo. Ropivacaine 0.25-1.0% was distinctly longer acting than bupivacaine on infiltration, equally effective in sciatic and brachial plexus block and somewhat shorter lasting in epidural and spinal blockade. There were tendencies towards a greater benefit from the addition of adrenaline with ropivacaine in epidural anaesthesia and a shorter latency to block in some of the tests. Ropivacaine seems less vasodilative than bupivacaine and capable of producing some vasoconstriction over a wider range of low concentrations, which may explain its longer duration of intradermal anaesthesia. The somewhat shorter duration of central blockade of ropivacaine is probably a result of lesser lipid solubility. Ropivacaine was less toxic (i.v. and s.c. LD50-values) than bupivacaine but more toxic than lidocaine, and produced only weak local irritation. Due to a combination of interesting local anaesthetic properties and relative safety including cardiotoxic potential, we consider ropivacaine a candidate for further studies.
Pharmacokinetics seeks to provide a mathematical basis for the description and prediction of the time-course of drugs in the body and an understanding of the processes involved in drug absorption and disposition. In the context of regional anaesthesia, the application of kinetic principles helps specifically in the following ways: (1) To select safe doses for single anaesthetic procedures and safe rates for continuous nerve block techniques. (2) To choose the best agents for particular procedures. (3) To identify patients who may be at particular risk of developing systemic toxic reactions. (4) To understand events after inadvertent intravascular injection. In addition, knowledge of the pharmacokinetics of existing agents should contribute to the design of better local anaesthetics in the future. This review will concentrate on aspects of the systemic absorption and disposition of local anaesthetics. Processes involved in the local disposition of the agents at and near the site of injection also come under the heading of pharmacokinetics. However, understanding of these phenomena is more speculative, since it is based primarily upon spatio-temporal changes in anaesthetic effect, rather than chemical measurements. The reader is referred to reviews by Greene (1983,1985) and Tucker and Mather (1980,1986) for discussion of these aspects.
To assess the usefulness of B-scan ultrasonography in determining left ventricular geometry and function, 25 patients with various cardiac disorders were studied with B-scan imaging within 24 hours of performance of biplane cine angiography of the left ventricle. In 14 patients asynergy present on the left anterior oblique ventriculogram was also detected on the B-scan image. A good correlation was found between the area ejection fractions as determined from the B-scan and the ventriculographic silhouettes (r = 0.92). A good correlation was also found between the B-scan area ejection fraction and the biplane volume ejection fraction (r = 0.87), even in patients with left ventricular asynergy, in whom the quantification of left ventricular geometry and function by standard time-motion echocardiography may be inaccurate. Thus, B-scan ultrasonography appears to be a safe, noninvasive, easily repeated technic for the study of left ventricular geometry, ejection and segmental motion in patients with v...
1 The cardiac effects of disopyramide (D) and lignocaine (L) were measured and compared in normal volunteers (D n=4; L n=3) following the establishment of a series of three steady-state drug plasma concentrations spanning the therapeutic range (1.5-5 micrograms base ml-1). 2 During control and steady-state periods multiple measurements were made of heart rate, blood pressure, drug concentrations and echocardiographic measurement of cardiac dimensions and estimated left ventricular function. 3 No change in heart size or estimated function occurred with L except for a small increase in estimated cardiac output (+0.5 1 min-1) secondary to a small rise in heart rate (maximum +7 beats min-1). Blood pressure rose slightly (maximum +11 mmHg). 4 D caused an increase in heart size, marked at end systole (+0.63 cm), and a decrease in echo indices of ventricular function (25-33%). These changes were related to plasma drug concentration but were not reflected in cardiac output estimation since heart rate rose (+15 beats min-1). Blood pressure also rose (+10 mmHg). 5 Significant differences were shown between D and L at similar plasma drug concentrations. The negative inotropic effect of D may be greater than previously suggested and clinically important.
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