Bupivacaine toxicity

Background: Levobupivacaine is an attractive alternative to racemic bupivacaine for spinal anesthesia due to the lower potential for cardio-toxicity and faster recovery profile. This study was designed to compare isobaric levobupivacaine with hyperbaric racemic bupivacaine with respect to intraoperative quality of anesthesia and the postoperative recovery profile in patients undergoing inguinal hernia surgery. Methods: A total of 100 ASA 1 and 2 patients, aged 18-60 years, undergoing elective daycare unilateral inguinal hernia surgery, were randomized into two groups...

Objective: This study reports a preclinical evaluation of an alginate/chitosan nanoparticle formulation containing NovaBupi®, a racemic bupivacaine (BVC) containing 25% dextrobupivacaine and 75% levobupivacaine. Methods: New Zealand White rabbits (n=6) received intraoral or intrathecal injections of BVC 0.5% or BVC 0.5%-loaded alginate-chitosan nanoparticles (BVCALG ). BVC plasma levels and pharmacokinetic parameters were determined in blood samples of these rabbits...

BACKGROUND: Systemic toxicity of local anesthetics is predominantly complicated by their myocardial toxicity. Especially long-acting local anesthetics exert a negative inotropic effect that has been described at lower concentrations than defined for blockade of myocardial ion channels. We evaluated the negative inotropic effect of bupivacaine at a concentration described for clinical toxicity testing the hypothesis that negative inotropy is a result of reduced Ca sensitivity rather than blockade of ion channels...

Peripheral nerve blocks are becoming increasingly popular for perioperative use as anesthetics and analgesics in small animals. This prospective study was performed to investigate the duration of motor and sensory blockade following use of bupivacaine for ultrasound-guided femoral and sciatic nerve blocks in dogs and to measure the plasma concentrations of bupivacaine that result from these procedures. Six dogs were anesthetized twice using a randomized cross-over design. At the first anesthetic, dogs were assigned to receive either an ultrasound-guided femoral nerve block or sciatic nerve block with 0...

Objective In orthopedic joint injection, the most frequently used local anesthetics are ropivacaine, bupivacaine, and 1% or 2% lidocaine. The aim of this study was to examine effects of these various anesthetics on the viability of human chondrocytes. Our hypothesis was that all local anesthetics tested damage human chondrocytes in vitro. Methods Primary human chondrocytes were isolated and cultured from 6 donated human knee joints (mean age of donors 61.2 years). Local anesthetics were added to these cultures...

BACKGROUND: The optimal local-anaesthetic (LA) dose for transversus-abdominis-plane (TAP) block is unclear. In this meta-analysis, we aimed to determine whether TAP blocks for Caesarean delivery (CD) with low-dose (LD) LA demonstrated non-inferiority in terms of analgesic efficacy, compared with high-dose (HD) LA. METHODS: A literature search was performed for randomised controlled trials examining the analgesic efficacy of TAP blocks vs control after CD. The different dosing used in these studies was classified as HD or LD (bupivacaine equivalents >50 or ≤50 mg per block side, respectively)...

The experimental use of lipid emulsion for local anesthetic toxicity was originally identified in 1998. It was then translated to clinical practice in 2006 and expanded to drugs other than local anesthetics in 2008. Our understanding of lipid resuscitation therapy has progressed considerably since the previous update from the American Society of Regional Anesthesia and Pain Medicine, and the scientific evidence has coalesced around specific discrete mechanisms. Intravenous lipid emulsion therapy provides a multimodal resuscitation benefit that includes both scavenging (eg, the lipid shuttle) and nonscavenging components...

The American Society of Regional Anesthesia and Pain Medicine's Third Practice Advisory on local anesthetic systemic toxicity is an interim update from its 2010 advisory. The advisory focuses on new information regarding the mechanisms of lipid resuscitation, updated frequency estimates, the preventative role of ultrasound guidance, changes to case presentation patterns, and limited information related to local infiltration anesthesia and liposomal bupivacaine. In addition to emerging information, the advisory updates recommendations pertaining to prevention, recognition, and treatment of local anesthetic systemic toxicity...

The synthesis of multifunctional spirocycles was achieved from common cyclic carboxylic acids (cyclobutane carboxylate, cyclopentane carboxylate, l-proline, etc.). The whole sequence included only two chemical steps-synthesis of azetidinones, and reduction into azetidines. The obtained spirocyclic amino acids were incorporated into a structure of the known anesthetic drug Bupivacaine. The obtained analogues were more active and less toxic than the original drug. We believe that this discovery will lead to a wide use of spirocyclic building blocks in drug discovery in the near future...

Objectives: To evaluate the knowledge of ophthalmologists regarding local anesthesia toxicity syndrome (LATS) and intravenous lipid emulsion used in treatment, and to raise awareness of this issue. Materials and Methods: A questionnaire comprising 14 questions about demographics, local anesthesia (LA) use, toxicity, and treatment methods was administered to ophthalmologists at different hospitals. Results: The study included 104 ophthalmologists (25% residents, 67...

BACKGROUND: Interscalene brachial plexus blocks have been a routinely performed method of anesthesia for shoulder surgery that decreases the need for general anesthesia, length of stay, and recovery time. We describe a case of bupivacaine toxicity after an interscalene block. CASE REPORT: The patient was a 66-year-old man who presented to our Emergency Department by emergency medical services from an ambulatory surgery center where he had undergone rotator cuff surgery, with bradycardia and hypotension...

Context: Brachial plexus block is effective with good postoperative analgesia in upper limb surgery has gained importance as it safe, low cost, and maintains stable hemodynamics intraoperatively. To decrease the onset time and prolong the duration of nerve block bicarbonate, opioids (morphine, fentanyl, etc.), sympathomimetic agents (epinephrine, phenylephrine, etc.), α-2 agonists (clonidine and dexmedetomidine), calcium channel blocker (verapamil), magnesium sulfate, etc., were studied with local anesthetics and their isomers...

BACKGROUND: The relatively short duration of effect of local anesthetics has been addressed by encapsulation in drug delivery systems. Codelivery with a single compound that produces an adjuvant effect on nerve block but without intrinsic local anesthetic properties can further prolong the nerve block effect. Here, we investigated whether codelivery of more than 1 encapsulated adjuvant compound can further enhance nerve blockade. METHODS: Liposomes loaded with bupivacaine (Bup), dexamethasone phosphate (DexP), or dexmedetomidine (DMED) were synthesized and its in vitro drug release profiles were determined...

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...

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...

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...

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...

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)...

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...

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...