Update on local anesthetics: focus on levobupivacaine

Burlacu, Crina; Buggy, Donal J.

doi:10.2147/tcrm.s1433

Cited by 128 publications

(132 citation statements)

References 88 publications

(106 reference statements)

Supporting

Mentioning

122

Contrasting

Unclassified

Order By: Relevance

“…The major mechanism for bupivacaine depression of cardiac conduction is considered to be the fast block of Na + channels during action potential transmission, which results in slow recovery from block during diastole [23] . Recently, levobupivacaine, a single enantiomer of bupivacaine, has been introduced as a new long-acting LA with potentially reduced toxicity compared with bupivacaine [24] . Even so, bupivacaine has not been replaced in the market, probably due to the lack of perceived safety benefits and/or the consideration of additional costs for the switch to levobupivacaine, which is ~57% more expensive than bupivacaine [22] .…”

Section: Discussionmentioning

confidence: 99%

Voltage-dependent blockade by bupivacaine of cardiac sodium channels expressed in Xenopus oocytes

et al. 2014

View full text Add to dashboard Cite

Bupivacaine ranks as the most potent and efficient drug among class I local anesthetics, but its high potential for toxic reactions severely limits its clinical use. Although bupivacaine-induced toxicity is mainly caused by substantial blockade of voltage-gated sodium channels (VGSCs), how these hydrophobic molecules interact with the receptor sites to which they bind remains unclear. Na v 1.5 is the dominant isoform of VGSCs expressed in cardiac myocytes, and its dysfunction may be the cause of bupivacainetriggered arrhythmia. Here, we investigated the effect of bupivacaine on Na v 1.5 within the clinical concentration range. The electrophysiological measurements on Na v 1.5 expressed in Xenopus oocytes showed that bupivacaine induced a voltageand concentration-dependent blockade on the peak of I Na and the half-maximal inhibitory dose was 4.51 μmol/L. Consistent with other local anesthetics, bupivacaine also induced a use-dependent blockade on Na v 1.5 currents. The underlying mechanisms of this blockade may contribute to the fact that bupivacaine not only dose-dependently affected the gating kinetics of Na v 1.5 but also accelerated the development of its open-state slow inactivation. These results extend our knowledge of the action of bupivacaine on cardiac sodium channels, and therefore contribute to the safer and more efficient clinical use of bupivacaine.

show abstract

Section: Discussionmentioning

confidence: 99%

Voltage-dependent blockade by bupivacaine of cardiac sodium channels expressed in Xenopus oocytes

et al. 2014

View full text Add to dashboard Cite

show abstract

“…We used low-volume high-concentration longacting LA for maximal duration of analgesic effect via a single-injection ISB. 17,18 The blinded researcher then selected a sealed envelope and gave the envelope to the unblinded study team member. The unblinded member of the study team prepared the medication in a room adjacent to the operating theatre.…”

Section: Randomization Techniquementioning

confidence: 99%

Thermal quantitative sensory testing to assess the sensory effects of three local anesthetic solutions in a randomized trial of interscalene blockade for shoulder surgery

Sermeus

Hans

Schepens

et al. 2015

Can J Anesth/J Can Anesth

View full text Add to dashboard Cite

Thermal quantitative sensory testing to assess the sensory effects of three local anesthetic solutions in a randomized trial of interscalene blockade for shoulder surgery Les tests sensoriels quantitatifs thermiques utilisés pour évaluer les effets sensoriels de trois solutions d'anesthésiques locaux dans une étude randomisée de blocs interscaléniques pour les chirurgies de l'épaule Methods This was a prospective randomized trial in patients scheduled for arthroscopic shoulder surgery under general anesthesia and US-ISB. Participants and observers were blinded for the study. We assigned the study participants to one of three groups: 0.5% levobupivacaine 15 mL, 0.5% levobupivacaine 15 mL with 1:200,000 epinephrine, and 0.75% ropivacaine 15 mL. We performed thermal QST within dermatomes C4, C5, C6, and C7 before infiltration and 30 min, six hours, ten hours, and 24 hr after performing the US-ISB. In addition, we used QST, a semi-objective quantitative testing method, to measure the onset, intensity, duration, extent, and functional recovery of the sensory block. We also measured detection thresholds for cold/warm sensations and cold/heat pain. Results Detection thresholds for all thermal sensations within the ipsilateral C4, C5, C6, and C7 dermatomes increased rapidly (indicating the development of a hypoesthetic state) and reached a steady state after 30 min. This lasted for approximately ten hours and returned to normal detection thresholds by 24 hr. There were no differences detected between the three groups at 24 hr

show abstract

“…Levobupivacaine and ropivacaine, new long-acting local anesthetics are S(-) enantiomers of two structurally similar molecules, 1-butyl-2' ,6'-pipecoloxylidide and 1-propyl-2' ,6'-pipecoloxylidide, respectively (18,19) and are been developed as safer alternatives to bupivacaine. Though less lipid-soluble than bupivacaine, ropivacaine is a long-acting spinal anesthetic.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the effects of ketamine on spinal anesthesia with levobupivacaine or ropivacaine

Zhang

Lin

Wen-bo

2016

Experimental and Therapeutic Medicine

View full text Add to dashboard Cite

Abstract. Spinal anesthesia or regional anesthesia is a potent anesthetic procedure. Additional modalities have been sought to increase the duration of block in spinal anesthesia. Ketamine is an N-methyl-D-aspartate (NMDA) receptor blocker that has an anesthetic effect when injected intrathecally and has a synergic effect with bupivacaine. Ketamine also has potent analgesic properties. The present study investigated the effect of intrathecally administered ketamine on spinal anesthesia with levobupivacaine or ropivacaine. Sprague-Dawley rats at post-natal day 21 were exposed to spinal anesthesia with 0.5% levobupivacaine or 0.5% ropivacaine. Separate groups of rats were treated with intrathecal ketamine at a 5 or 10 mg/kg bodyweight dose along with ropivacaine or levobupivacaine. The thermal and mechanical withdrawal latencies of the animals were determined using hot plate and von Frey filaments, respectively. A rotarod apparatus was employed to assess the capacity of the rats to rotate the spindle at 24 h following anesthesia. The gait of the rat pups was also assessed. Intrathecal administration of ketamine resulted in dense blocks and extended the duration of spinal blocks as evidenced by thermal latencies and responses to von Frey filaments. The latency to fall was shorter in rats exposed to ketamine along with ropivacaine or levobupivacaine spinal anesthesia. The gait parameters were also more disturbed upon ketamine administration. In conclusion, ketamine administration with ropivacaine or levobupivacaine increased the intensity and duration of spinal blockade, thereby increasing the anesthetic effects.

show abstract

Update on local anesthetics: focus on levobupivacaine

Cited by 128 publications

References 88 publications

Voltage-dependent blockade by bupivacaine of cardiac sodium channels expressed in Xenopus oocytes

Voltage-dependent blockade by bupivacaine of cardiac sodium channels expressed in Xenopus oocytes

Thermal quantitative sensory testing to assess the sensory effects of three local anesthetic solutions in a randomized trial of interscalene blockade for shoulder surgery

Evaluation of the effects of ketamine on spinal anesthesia with levobupivacaine or ropivacaine

Contact Info

Product

Resources

About