Bupivacaine toxicity

Inhibition of actin remodeling in nerves modulates action potential propagation and therefore could be used to treat acute pain. N-001 is a novel protein analgesic engineered from several C. Botulinum toxins. N-001 targets sensory neurons through ganglioside GT1b binding and ADP-ribosylates G-actin reducing actin remodeling. The activity and efficacy of N-001 was evaluated previously in vitro and in a mouse inflammatory pain model. To assess the relevance of N-001 for treatment of acute post-surgical pain, the current study evaluated the efficacy of N-001 in a mouse hind-paw incision model by peri-incisional and popliteal nerve block administration combined with mechanical testing...

BACKGROUND/IMPORTANCE: Anesthesiologists frequently use truncal catheters for postoperative pain control but with limited characterization of dosing and toxicity. OBJECTIVE: We reviewed the published literature to characterize local anesthetic dosing and toxicity of paravertebral and transversus abdominis plane catheters in adults. EVIDENCE REVIEW: We searched the literature for bupivacaine or ropivacaine infusions in the paravertebral or transversus abdominis space in humans dosed for 24 hours...

BACKGROUND/IMPORTANCE: Despite over 30 years of use by pediatric anesthesiologists, standardized dosing rates, dosing characteristics, and cases of toxicity of truncal nerve catheters are poorly described. OBJECTIVE: We reviewed the literature to characterize dosing and toxicity of paravertebral and transversus abdominis plane catheters in children (less than 18 years). EVIDENCE REVIEW: We searched for reports of ropivacaine or bupivacaine infusions in the paravertebral and transversus abdominis space intended for 24 hours or more of use in pediatric patients...

Chronic disease patients (cancer, arthritis, cardiovascular diseases) undergo long-term systemic drug treatment. Membrane transporters in ocular barriers could falsely recognize these drugs and allow their trafficking into the eye from systemic circulation. Hence, despite their pharmacological activity, these drugs accumulate and cause toxicity at the non-target site, such as the eye. Since around 40% of clinically used drugs are organic cation in nature, it is essential to understand the role of organic cation transporter (OCT1) in ocular barriers to facilitate the entry of systemic drugs into the eye...

Classical local anesthetics are unsuitable to treat regional pain lasting several days due to their limited duration and systemic toxicity. Self-delivery nano systems without excipients were designed for long-term sensory blocks. 1a self-assembled into different vehicles with different fractions of intermolecular π-π stacking, transported itself into nerve cells, and released single molecules slowly to achieve long-term duration for rats' sciatic nerve block for 11.6 h in water, 12.1 h in water with CO2 and 3...

Local anesthetic (LA) compounds decrease the permeability of the ion channels to sodium, which in turn, diminishes the rate of depolarization. These agents (a.k.a. -caines) are also used to depress mucosal sensations, e.g., gag reflex in the form of topical anesthetics. Overdose of LA can lead to local anesthetic systemic toxicity (LAST), which is the precursor of potentially lethal consequences on clinical grounds. There is a wide array of possible presentations of LAST, from mild findings, such as temporary hypertensive events, to serious conditions, including refractory cardiac dysfunction, dysrhythmias and prearrest situations...

This study was to explore the application value of chromosome ten (PTEN) - phosphatidylinositol 3-kinase (PI3K) - protein kinase B (AKT) signaling pathway in the treatment of Bupivacaine toxicity to neuronal cells under the regulation of fat emulsion. Neurons in the hippocampus of newborn rats were treated with Bupivacaine and fat emulsion and divided into five groups. The activity and action potential of neurons in each group were measured and Nissl's staining was performed. The results showed that the neuron activity of Bupivacaine group (42...

BACKGROUND: Subarachnoid block is used in most of urological surgeries and finding the best possible drug has always been a challenge. Bupivacaine's pure enantiomers ropivacaine and levobupivacaine have lesser systemic toxicity. Isobaric solution has extra benefit of not affecting the intrathecal dispersion of drug. Dexmedetomidine when added intrathecally provides longer duration of analgesia and anaesthesia. Aim of this study is to compare onset, duration of the block with both the drugs along with their hemostability and postoperative analgesia...

PURPOSE: Various sustained-release formulations incorporate high bupivacaine concentrations but data on local toxicity is lacking. This study explores local toxic effects of highly concentrated (5%) bupivacaine compared to clinically used concentrations in vivo following skeletal surgery, to assess the safety of sustained-release formulations with high bupivacaine concentrations. METHODS: Sixteen rats underwent surgery, in which screws with catheters affixed were implanted in the spine or femur in a factorial experimental design, allowing single-shot or continuous 72 h local administration of 0...

BACKGROUND: Bupivacaine/Meloxicam combination is the first extended-release dual-acting local anesthetic (DALA) that provides 72 h. of postoperative pain relief. It reduces opioid use after surgery and manages pain better than bupivacaine alone over 72 h. it overcomes surgical site inflammation with a new synergistic mode of action that combines bupivacaine with a low dosage of meloxicam. OBJECTIVE: In today's pharmaceutical research, we take great care to only use non-toxic solvents that pose no threat to either humans or the environment...

BACKGROUND: Peritendinous injection of local anesthetics, alone or in combination with corticosteroids, is widely used in the treatment of tendinopathies. Toxicity of local anesthetics has been demonstrated in many cells, including myocytes, chondrocytes, and neurons. Bupivacaine and lidocaine are known to have time- and dose-dependent cytotoxicity in these cells. The effects of these agents on the tendon remain unknown. PURPOSE: To show histological and biomechanical effects after the injection of different local anesthetics and steroids, both single and combined, at different concentrations into the peritendinous sheath of rat Achilles tendon...

Currently, lipid emulsion (LE) is widely used in the treatment of local anesthetic systemic toxicity (LAST). Additionally, LE has been shown to be effective to ameliorate intractable cardiovascular collapse evoked by toxicity of lipid soluble non-local anesthetic drug. The goal of this review focused on the underlying mechanism of LE treatment in the drug toxicity including LAST, LE treatment, and further research direction. We searched the relevant articles using following keywords: "local anesthetic systemic toxicity or LAST or toxicity or intoxication or poisoning" and "Intralipid or lipid emulsion"...

Nanoparticles are heterologous small composites that are usually between 1 and 100 nanometers in size. They are applied in many areas of medicine with one of them being drug delivery. Nanoparticles have a number of advantages as drug carriers which include reduced toxic effects, increased bioavailability, and their ability to be modified for specific tissues or cells. Due to the exciting development of nanotechnology concomitant with advances in biotechnology and medicine, the number of clinical trials devoted to nanoparticles for drug delivery is growing rapidly...

Local anesthetics are commonly used in farm animals to provide analgesia for painful procedures but can cause adverse effects at high systemic concentrations. The pharmacokinetics and efficacy of a long-acting sucrose acetate isobutyrate (SAIB) bupivacaine formulation following cornual nerve block in calves were compared to lidocaine. Fourteen calves were randomly assigned to one of the treatment groups (i) 5% Bupivacaine-SAIB (BUP-SAIB), n = 7; or (ii) 2% lidocaine (LID), n = 7. Cornual nerve block was performed, and duration of effective analgesia was evaluated by nociceptive threshold testing using a hand-held pressure algometer...

Infusion of lipid emulsion for drug overdose arose as a treatment for local anaesthetic systemic toxicity (LAST) initially based on laboratory results in animal models with the subsequent support of favourable case reports. Following successful translation to the clinic, practitioners also incorporated lipid emulsion as a treatment for non-local anaesthetic toxicities but without formal clinical trials. Recent clinical trials demonstrate a benefit of lipid emulsion in antipsychotic, pesticide, metoprolol and tramadol overdoses...

Background Levobupivacaine toxicity reports are rare, and when they do occur, toxic symptoms are frequently treatable with minimal morbidity and mortality. However, levobupivacaine has not entirely replaced bupivacaine in clinical practice. Moreover, the experience of intrathecal anesthesia with levobupivacaine is not well documented. Hence, the purpose of this study is to assess the quality and duration of sensory and motor blockade of levobupivacaine and its side effects, if any, compared to intrathecal bupivacaine during infraumbilical surgeries...

PURPOSE: Transurethral resection of bladder tumour (TURBT) is done under general anaesthesia (GA) with muscle relaxation to prevent obturator jerk and bladder perforation. TURBT under spinal anaesthesia (SA) with obturator nerve block (ONB) may prevent the obturator jerk while eliminating the disadvantages of GA. OBJECTIVES: To assess the outcome of TURBT under SA and ONB. METHODS: Patients undergoing TURBT for lateral wall tumours from 01...

BACKGROUND: Long-lasting local anesthetic use for perioperative pain control is limited by possible cardiotoxicity (e.g., arrhythmias and contractile depression), potentially leading to cardiac arrest. Off-target cardiac sodium channel blockade is considered the canonical mechanism behind cardiotoxicity; however, it does not fully explain the observed toxicity variability between anesthetics. The authors hypothesize that more cardiotoxic anesthetics (e.g., bupivacaine) differentially perturb other important cardiomyocyte functions (e...

PURPOSE: Discoblock is effective in relieving discogenic low back pain, but it can also cause intervertebral disk degeneration (IDD). The effect of species, concentration and volume of local anesthetics on IDD with discoblock have not been reported. The purpose was to study the effect of species, concentration and volume of local anesthetics on IDD in rats undergoing discoblock. METHODS: The effects of local anesthetics on nucleus pulposus cell (NPC) viability in vitro were studied...

Background: Topical local analgesic and anaesthetic agents have been used both pre- and immediately post-harvest on split-thickness skin graft (STSG) donor site wounds (DSW). There is no systematic review of their effectiveness in providing post-harvest analgesia, or of the possible toxic effects of systemic absorption. This study is designed to address the question of which agent, if any, is favoured over the others and whether there are any safety data regarding their use. Methods: Systematic literature review of randomised controlled trials of topical agents applied to STSG DSWs, with a view to providing analgesia...