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Bupivacaine toxicity

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https://www.readbyqxmd.com/read/29232206/bupivacaine-indirectly-potentiates-glutamate-induced-intracellular-calcium-signaling-in-rat-hippocampal-neurons-by-impairing-mitochondrial-function-in-cocultured-astrocytes
#1
Yuan Xing, Nan Zhang, Wei Zhang, Lei-Ming Ren
BACKGROUND: Bupivacaine induces central neurotoxicity at lower blood concentrations than cardiovascular toxicity. However, central sensitivity to bupivacaine is poorly understood. The toxicity mechanism might be related to glutamate-induced excitotoxicity in hippocampal cells. METHODS: The intracellular free Ca concentration ([Ca]i), mitochondrial membrane potential, and reactive oxygen species generation were measured by fluorescence and two-photon laser scanning microscopy in fetal rat hippocampal neurons and astrocytes...
December 12, 2017: Anesthesiology
https://www.readbyqxmd.com/read/29232029/the-effects-of-subconjunctival-bupivacaine-lidocaine-and-mepivacaine-on-corneal-sensitivity-in-healthy-horses
#2
Maggie R Jinks, Robin L Fontenot, Robert W Wills, Caroline M Betbeze
OBJECTIVE: To compare the efficacy and duration of effect of three local anesthetics on corneal sensitivity when administered subconjunctivally in horses. ANIMALS STUDIED: Eight healthy adult horses. PROCEDURE: A randomized, masked, crossover study design was used, with a two-week washout period between trials. The subconjunctival space of the randomly selected eye was injected with 0.2 mLs of bupivacaine (0.5%), lidocaine (2%), mepivacaine (2%), or saline...
December 12, 2017: Veterinary Ophthalmology
https://www.readbyqxmd.com/read/29145932/lipid-emulsion-more-than-reversing-bupivacaine-cardiotoxicity-potential-organ-protection
#3
Negar Motayagheni, Sheshanna Phan, Ala Nozari, Anthony Atala
Efforts to develop a treatment for bupivacaine cardiotoxicity led to the discovery that Intralipid, a popular brand of intravenous lipid emulsion, could be used not only as an effective treatment for anesthetic-induced cardiac arrest, but also as a means of reversing many other toxicities. Contradictory data exist regarding the mechanism of action of lipid emulsion, a combination of fatty acids traditionally used in parenteral nutrition. Some researchers attribute the effects to lipophilicity and the individual characteristics of the lipids, while other data demonstrate a direct empowering mechanism through cellular upstream and downstream pathways...
2017: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29115971/local-anaesthetics-or-their-combination-with-morphine-and-or-magnesium-sulphate-are-toxic-for-equine-chondrocytes-and-synoviocytes-in-vitro
#4
L M Rubio-Martínez, E Rioja, M Castro Martins, S Wipawee, P Clegg, M J Peffers
BACKGROUND: Chondrotoxic effects of local anaesthetics are well reported in humans and some animal species but knowledge on their toxic effects on synoviocytes or equine chondrocytes or the effects on cellular production of inflammatory cytokines is limited. The purpose of this study was to evaluate the in vitro effects of local anaesthetics, morphine, magnesium sulphate (MgSO4) or their combinations on cell viability and pro-inflammatory cytokine gene expression of equine synoviocytes and chondrocytes...
November 7, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/29111148/effects-of-opioid-and-nonopioid-analgesics-on-canine-wheal-formation-and-cultured-human-mast-cell-degranulation
#5
Eric Schmidt-Rondon, Zhenping Wang, Shelle A Malkmus, Anna Di Nardo, Keith Hildebrand, Linda Page, Tony L Yaksh
Mast cell (MC) degranulation has been implicated in the side effect profile of a variety of clinically useful agents. Thus, after intrathecal delivery, formation of space-occupying, meningeally-derived masses may be related to local MC degranulation. We systematically characterized degranulating effects of opioid and nonopioid analgesics on cutaneous flares in the dog and in primary human MC (hMC) cultures. METHODS: Dogs were anesthetized with IV propofol and received intradermal (ID) injections (50μL)...
October 27, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29084192/transient-left-ventricular-dysfunction-due-to-coronary-spasm-after-spinal-anesthesia-with-bupivacaine-a-case-report
#6
Waldemar Elikowski, Małgorzata Małek-Elikowska, Marek Słomczyński, Karolina Horbacka, Jarosław Bartkowski, Bartosz Kalawski
Bupivacaine is a long-acting local anesthetic (LA) used for cutaneous infiltration, peripheral nerve blocks, epidural and spinal anesthesia. However, its application may result in cardiovascular complications such as: hypotension, bradycardia, cardiac arrest and toxic myocardial injury. The authors describe a 53-year-old male with a history of cigarette smoking, admitted for an elective inguinal hernia surgery. Before surgery, the patient received subarachnoid injection of bupivacaine (20 mg). After the operation, he developed transient hypotension...
October 23, 2017: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/29055733/qx-oh-levobupivacaine-fixed-dose-combination-to-provide-a-long-acting-postoperative-pain-of-knee-surgery-in-rodents
#7
WenLing Zhao, Jun Yang, YuJun Zhang, Jin Liu, WenSheng Zhang
Although total knee arthroplasty (TKA) is a commonly performed procedure, anesthetic efficacy in post-surgical pain remains an issue. Exparel (45mM liposome bupivacaine), a relatively long-acting local anesthetic, has shown efficacy in blocking peripheral nerve or periarticular infiltration to achieve better post-TKA analgesia. In the present work, we tested whether a fixed-dose combination of QX-OH (35mM) and levobupivacaine (10mM) (QX-OH/LB) could confer longer-lasting pain relief and reduce periarticular tissue toxicity compared to liposome bupivacaine (45mM) after TKA operation...
October 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29042063/-pharmacokinetic-and-clinical-effects-of-two-bupivacaine-concentrations-on-axillary-brachial-plexus-block
#8
Leonardo H C Ferraro, Alexandre Takeda, Cleber N Barreto, Bernadete Faria, Nilson A Assunção
INTRODUCTION: The risk of systemic bupivacaine toxicity is a persistent problem, which makes its pharmacokinetic study fundamental for regional anesthesia safety. There is little evidence of its influence on plasma peak at different concentrations. The present study compares two bupivacaine concentrations to establish how the concentration affects this drug plasma peak in axillary brachial plexus block. Postoperative latency and analgesia were also compared. METHODS: 30 patients were randomized...
October 14, 2017: Revista Brasileira de Anestesiologia
https://www.readbyqxmd.com/read/28982145/encapsulation-of-ropivacaine-in-a-combined-donor-acceptor-ionic-gradient-liposomal-system-promotes-extended-anesthesia-time
#9
Camila Morais Gonçalves da Silva, Michelle Franz-Montan, Cíntia Elisabeth Gomez Limia, Lígia Nunes de Morais Ribeiro, Mário Antônio Braga, Viviane Aparecida Guilherme, Camila Batista da Silva, Bruna Renata Casadei, Cíntia Maria Saia Cereda, Eneida de Paula
Ropivacaine is a local anesthetic with similar potency but lower systemic toxicity than bupivacaine, the most commonly used spinal anesthetic. The present study concerns the development of a combined drug delivery system for ropivacaine, comprised of two types of liposomes: donor multivesicular vesicles containing 250 mM (NH4)2SO4 plus the anesthetic, and acceptor large unilamellar vesicles with internal pH of 5.5. Both kinds of liposomes were composed of hydrogenated soy-phosphatidylcholine:cholesterol (2:1 mol%) and were prepared at pH 7...
2017: PloS One
https://www.readbyqxmd.com/read/28913485/an-in-vitro-study-of-the-release-capacity-of-the-local-anaesthetics-from-siloxane-matrices
#10
Gabriela Preda, Alexandru Florin Rogobete, Dorel Săndesc, Ovidiu Horea Bedreag, Carmen Alina Cradigati, Mirela Sarandan, Marius Papurica, Sonia Elena Popovici, Monica Dragomirescu
AIMS: In the field of anaesthesia and intensive care, the controlled release systems capable of delivering constantly local anaesthetics are of interest because of the advantages brought to pain management. In this paper we presented the release profiles by usage of siloxane matrices of two common local anaesthetics, lidocaine and bupivacaine, analysed in vitro. METHODS: The siloxane matrices were obtained in accordance with the methods described in the specialized literature, tetraethoxysilane (TEOS) and tetramethoxysilane (TMOS) were used as precursors...
October 2016: Romanian Journal of Anaesthesia and Intensive Care
https://www.readbyqxmd.com/read/28844768/systemic-safety-of-liposomal-bupivacaine-in-simultaneous-bilateral-total-knee-arthroplasty
#11
Bryan D Springer, J Bohannon Mason, Susan M Odum
BACKGROUND: Intraoperative periarticular injections (PAIs) with local anesthetic are an important component of multimodal pain control in total joint arthroplasty. Liposomal bupivacaine is an extended-release formulation of bupivacaine designed to provide extended pain relief, approved for use in a single surgical site. The systemic safety profile for use in simultaneous bilateral TKA (bTKA) with a full dose in each knee has not been evaluated. The purpose of this study was to determine the safety and pharmacokinetics of bilateral full-dose PAI liposomal bupivacaine in the blood collected in patients undergoing simultaneous bTKA...
August 1, 2017: Journal of Arthroplasty
https://www.readbyqxmd.com/read/28751934/activation-of-p47phox-as-a-mechanism-of-bupivacaine-induced-burst-production-of-reactive-oxygen-species-and-neural-toxicity
#12
Yu-Jie Li, Wei Zhao, Xu-Jiao Yu, Feng-Xian Li, Zi-Ting Liu, Le Li, Shi-Yuan Xu
Bupivacaine has been shown to induce neurotoxicity through inducing excessive reactive oxygen species (ROS), but the underlying mechanism remains unclear. NOX2 is one of the most important sources of ROS in the nervous system, and its activation requires the membrane translocation of subunit p47phox. However, the role of p47phox in bupivacaine-induced neurotoxicity has not been explored. In our in vitro study, cultured human SH-SY5Y neuroblastoma cells were treated with 1.5 mM bupivacaine to induce neurotoxicity...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28745230/bupivacaine-s75-r25-loaded-in-nanostructured-lipid-carriers-factorial-design-hplc-quantification-method-and-physicochemical-stability-study
#13
Gustavo Henrique Rodrigues Da Silva, Ligia Nunes de Moraes Ribeiro, Viviane Guilherme, Simone Ramos de Castro, Márcia Cristina Breitkreitz, Eneida de Paula
Bupivacaine is the most used local anesthetic in surgical procedures, producing prolonged anesthesia. The major limiting factor for the clinical use of bupivacaine comes from its systemic toxicity. Nanostructured lipid carriers (NLC) are vehicles for sustained drug delivery that are able to minimize the toxicity and to increase the action time of lipophilic drugs. This work reports a 22 factorial design, which elucidate the role of the lipids mixture in the NLC, towards an optimized formulation. It also provides a new method for Bupivacaine S75:R25 (BVCS75) quantification in NLC...
July 26, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28727583/serum-bupivacaine-concentration-after-periarticular-injection-with-a-mixture-of-liposomal-bupivacaine-and-bupivacaine-hcl-during-total-knee-arthroplasty
#14
Michael J Buys, Marian F Murphy, Christine M Warrick, Nathan L Pace, Jeremy M Gililland, Christopher E Pelt, Byron R Bankhead, John L Patzkowsky, Ken B Johnson
BACKGROUND AND OBJECTIVES: A relatively new technique to reduce postoperative pain for total knee arthroplasty is to inject a mixture of 266 mg of liposomal bupivacaine and 125 mg of 0.25% bupivacaine HCl with epinephrine 1:300,000 around the knee joint at the time of surgery. Currently, no publications report serum bupivacaine concentrations over time after periarticular injection of liposomal mixed with free bupivacaine. This information is important to ensure safe serum bupivacaine concentrations are maintained especially when considering supplemental or rescue peripheral nerve blocks...
September 2017: Regional Anesthesia and Pain Medicine
https://www.readbyqxmd.com/read/28692439/lipid-emulsion-in-local-anesthetic-toxicity
#15
Martyn Harvey, Grant Cave
PURPOSE OF REVIEW: Enthusiasm for regional anesthesia has been driven by multimodal benefits to patient outcomes. Despite widespread awareness and improved techniques (including the increasing use of ultrasound guidance for block placement), intravascular sequestration and the attendant risk of local anesthetic systemic toxicity (LAST) remains. Intravenous lipid emulsion (ILE) for the treatment of LAST has been endorsed by anesthetic regulatory societies on the basis of animal study and human case report data...
October 2017: Current Opinion in Anaesthesiology
https://www.readbyqxmd.com/read/28663643/comparison-between-conventional-and-ultrasound-guided-supraclavicular-brachial-plexus-block-in-upper-limb-surgeries
#16
Kiran Abhayakumar Honnannavar, Mahantesh Shivangouda Mudakanagoudar
INTRODUCTION: Brachial plexus blockade is a time-tested technique for upper limb surgeries. The classical approach using paresthesia technique is a blind technique and may be associated with a higher failure rate and injury to the nerves and surrounding structures. To avoid some of these problems, use of peripheral nerve stimulator and ultrasound techniques were started which allowed better localization of the nerve/plexus. Ultrasound for supraclavicular brachial plexus block has improved the success rate of the block with excellent localization as well as improved safety margin...
April 2017: Anesthesia, Essays and Researches
https://www.readbyqxmd.com/read/28655546/optimised-nlc-a-nanotechnological-approach-to-improve-the-anaesthetic-effect-of-bupivacaine
#17
Gustavo H Rodrigues da Silva, Lígia N M Ribeiro, Hery Mitsutake, Viviane A Guilherme, Simone R Castro, Ronei J Poppi, Márcia C Breitkreitz, Eneida de Paula
The short time of action and systemic toxicity of local anaesthetics limit their clinical application. Bupivacaine is the most frequently used local anaesthetic in surgical procedures worldwide. The discovery that its S(-) enantiomeric form is less toxic than the R(+) form led to the introduction of products with enantiomeric excess (S75:R25 bupivacaine) in the market. Nevertheless, the time of action of bupivacaine is still short; to overcome that, bupivacaine S75:R25 (BVCS75) was encapsulated in nanostructured lipid carriers (NLC)...
June 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28614364/serum-levels-of-bupivacaine-after-pre-peritoneal-bolus-vs-epidural-bolus-injection-for-analgesia-in-abdominal-surgery-a-safety-study-within-a-randomized-controlled-trial
#18
RANDOMIZED CONTROLLED TRIAL
Timothy H Mungroop, Ganapathy van Samkar, Bart F Geerts, Susan van Dieren, Marc G Besselink, Denise P Veelo, Philipp Lirk
BACKGROUND: Continuous wound infiltration (CWI) has become increasingly popular in recent years as an alternative to epidural analgesia. As catheters are not placed until the end of surgery, more intraoperative opioid analgesics might be needed. We, therefore, added a single pre-peritoneal bolus of bupivacaine at the start of laparotomy, similar to the bolus given with epidural analgesia. METHODS: This was a comparative study within a randomized controlled trial (NTR4948)...
2017: PloS One
https://www.readbyqxmd.com/read/28599806/pharmacokinetics-of-bupivacaine-after-bilateral-ultrasound-guided-transversus-abdominis-plane-block-following-cesarean-delivery-under-spinal-anesthesia
#19
B Trabelsi, R Charfi, L Bennasr, S Ben Marzouk, H Eljebari, N Jebabli, M Ben Sassi, S Trabelsi, H Maghrebi
BACKGROUND: Transversus abdominis plane block is an effective method of post-cesarean analgesia. There are no data available about plasma bupivacaine levels after this block in adults. This study aimed to assess bupivacaine pharmacokinetic parameters after ultrasound-guided transversus abdominis plane blocks following cesarean delivery under spinal anesthesia. METHODS: A prospective observational study in parturients undergoing elective cesarean delivery under hyperbaric bupivacaine spinal anesthesia was conducted...
November 2017: International Journal of Obstetric Anesthesia
https://www.readbyqxmd.com/read/28562387/lipid-resuscitation-in-acute-poisoning-after-a-decade-of-publications-what-have-we-really-learned
#20
Lotte C G Hoegberg, Sophie Gosselin
PURPOSE OF REVIEW: The decision to provide intravenous lipid emulsion (ILE) therapy as a treatment modality for the reversal of various drug toxicity was discovered in the last decade. Numerous publications, in both humans and animals attest to its clinical use, but current supporting evidence is inconsistent. RECENT FINDINGS: A recent systematic review reported evidence for benefit of ILE in bupivacaine toxicity. Human randomized trials, large observational studies as well as animal models of orogastric poisoning failed to report a clear benefit of ILE for nonlocal anesthetics poisoning...
August 2017: Current Opinion in Anaesthesiology
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