• 대한약리학회지
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• 제28권1호
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• pp.41-48
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• 1992

국소마취제인 bupivacaine의 심근억제작용에 관한 기전을 규명하기 위하여, bupivacaine에 의해 수축력이 감소된 흰쥐 적출심장에 대한 각종 대사기질의 영향을 관찰한 바 다음과 같은 결과를 얻었다. 1. Krebs-Ringer glucose medium에 현수한 적출심방의 수축력은 0.01% bupivacaine에 의해 약 50% 감소되었다. 2. Pyruvate, acetate 및 fructose는 bupivacaine 억제심방의 수축력을 증가시켰으나, 정상 Krebs-Ringer medium에서의 수축력에는 현저한 영향이 없었다. 3. Glucose는 bupivacaine 억제심방의 수축력에는 별 영향이 없었으나, 정상 Krebs-Ringer medium에서의 수축력은 증가시켰다. 4. Pyruvate, acetate 및 fructose는 hypertonic medium에 의해 억제된 심방의 수축력에 영향이 없었으나, glucose는 약간의 수축력 증가를 보였다. 5. 각종 대사기질중 pyruvate가 bupivacaine 억제심방의 수축력을 최대로 증가시켰다. 이상의 결과는 bupivacaine이 심근의 glucose 섭취를 억제하거나, 해당과정을 통한 glucose의 이용을 억제하였음을 시사한다. 나아가서, bupivacaine에 의한 대사억제는 심근의 해당과정에서의 phosphofructokinase step이전의 단계에서 작용함을 시사하고 있다.

• Journal of Dental Anesthesia and Pain Medicine
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• 제19권4호
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• pp.209-215
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• 2019

Background: Pain is an unpleasant sensation ranging from mild localized discomfort to agony and is one of the most commonly experienced symptoms in oral surgery. Usually, local anesthetic agents and analgesics are used for pain control in oral surgical procedures. Local anesthetic agents including lignocaine and bupivacaine are routinely used in varying concentrations. The present study was designed to evaluate and compare the efficacy of 0.25% and 0.5% bupivacaine for postoperative analgesia in infraorbital nerve block. Methods: Forty-one patients undergoing bilateral maxillary orthodontic extraction received 0.5% bupivacaine (n = 41) on one side and 0.25% bupivacaine (n = 41) on the other side at an interval of 7 d. The parameters evaluated for both the bupivacaine concentrations were onset of action, pain during procedure (visual analog scale score [VAS]), and duration of action. The results were noted, tabulated, and analyzed using the Wilcoxon signed rank test. Results: The onset of action of 0.5% bupivacaine was quicker than that of 0.25% bupivacaine, but the difference was not statistically significant (P = 0.306). No significant difference was found between the solutions for VAS scores (P = 0.221) scores and duration of action (P = 0.662). Conclusion: There was no significant difference between 0.25% bupivacaine and 0.5% bupivacaine in terms of onset of action, pain during procedure, and duration of action. The use of 0.25% bupivacaine is recommended.

• The Korean Journal of Pain
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• 제18권2호
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• pp.181-186
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• 2005

Background: Hydromorphone has an intermediate lipid solubility range that falls between morphine and fentanyl. Lipophilic activity during opioid epidural administration is important in relation to both the side effects and analgesic efficacy. The purpose of this study was to compare epidural hydromorphone and fentanyl when concomitantly infused with bupivacaine in patients undergoing a thoracotomy. Methods: Seventy-seven thoracotomy patients, with patient-controlled epidural analgesia (PCEA), were blindly allocated into two groups [group F (n = 34); 0.1% bupivacaine and fentanyl $5{\mu}g/ml$, group H (n = 34); 0.1% bupivacaine and hydromorphone $16{\mu}g/ml$)]. The basal PCEA rate and demand dose were 4 ml/hr and 3 ml, respectively. The visual analogue scale (VAS) for pain, and pruritus, sedation and nausea were measured at 6, 12 and 24 hours after the operation. Results: There were no significant differences in the VAS pain scores and the incidences of pruritus, nausea and sedation between the two groups. The total infused volume after 24 hours was lower in H compared to that of F group (P < 0.05). Conclusions: We conclude that epidural hydromorphone or fentanyl administration has a similar analgesic efficacy and shows similar incidences of side effects, when concomitantly infused with bupivacaine, in the management of acute pain following a thoracotomy.

• The Korean Journal of Pain
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• 제27권3호
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• pp.229-238
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• 2014

Background: A toxic dose of bupivacaine produces vasodilation in isolated aortas. The goal of this in vitro study was to investigate the cellular mechanism associated with bupivacaine-induced vasodilation in isolated endothelium-denuded rat aortas precontracted with phenylephrine. Methods: Isolated endothelium-denuded rat aortas were suspended for isometric tension recordings. The effects of nifedipine, verapamil, iberiotoxin, 4-aminopyridine, barium chloride, and glibenclamide on bupivacaine concentration-response curves were assessed in endothelium-denuded aortas precontracted with phenylephrine. The effect of phenylephrine and KCl used for precontraction on bupivacaine-induced concentration-response curves was assessed. The effects of verapamil on phenylephrine concentration-response curves were assessed. The effects of bupivacaine on the intracellular calcium concentration ($[Ca^{2+}]_i$) and tension in aortas precontracted with phenylephrine were measured simultaneously with the acetoxymethyl ester of a fura-2-loaded aortic strip. Results: Pretreatment with potassium channel inhibitors had no effect on bupivacaine-induced relaxation in the endothelium-denuded aortas precontracted with phenylephrine, whereas verapamil or nifedipine attenuated bupivacaine-induced relaxation. The magnitude of the bupivacaine-induced relaxation was enhanced in the 100mM KCl-induced precontracted aortas compared with the phenylephrine-induced precontracted aortas. Verapamil attenuated the phenylephrine-induced contraction. The magnitude of the bupivacaine-induced relaxation was higher than that of the bupivacaine-induced $[Ca^{2+}]_i$ decrease in the aortas precontracted with phenylephrine. Conclusions: Taken together, these results suggest that toxic-dose bupivacaine-induced vasodilation appears to be mediated by decreased calcium sensitization in endothelium-denuded aortas precontracted with phenylephrine. In addition, potassium channel inhibitors had no effect on bupivacaine-induced relaxation. Toxic-dose bupivacaine-induced vasodilation may be partially associated with the inhibitory effect of voltage-operated calcium channels.

• International Journal of Oral Biology
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• 제32권2호
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• pp.45-49
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• 2007

In this study, the cytotoxicity of commonly used local anesthetics was evaluated on odontoblasts which are essential for pulpal homeostasis in vitro. Local anesthetics, such as articaine, bupivacaine, levobupivacaine, lidocaine, mepivacaine, prilocaine, and procaine, were tested on the odontoblast cell line, MDPC-23. The concentration-and time-dependent cytotoxic effects of local anesthetics on odontoblasts were measured by MTT assay. Among local anesthetics treated for 18 h, only bupivacaine significantly showed cell death in a concentration-($LC_{50}=1.2mM$) and time-dependent manner. To confirm cell death induced by bupivacaine, the observation of cell morphology and FACS using Annexin V and propidium iodide (PI) staining were performed. As a result of Annexin V and PI staining, as well as the morphological change, only bupivacaine induced apoptotic cell death on odontoblasts when compared with levobupivacaine and lidocaine. These results suggest that bupivacaine might affect normal pulpal integrity even after uneventful local anesthesia.

• Journal of Chest Surgery
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• 제26권7호
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• pp.538-542
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• 1993

An approach to the treatment of post-operative pain by the injection of bupivacaine into the pleural space through an intrapleural cathter has been studied. Among 24 thoracotomy patients, bupivacaine was injected only to experimental group[ 12 patients ] when the patient was able to head up for oneself during recovery from anesthesia. The pain and ROM[ range of motion ] scores, respiration rate, PaCO2 level of both experimental and control group were measured at the time of head-up and 30 and 120 minutes thereafter.The scores of pain and ROM of experimental group were significantly[ P value < 0.05 ] decreased in 30 minutes and 120 minutes after bupivacaine injection compared with those of control group but respiration rate and PaCO2 level were not changed significantly. With this result, we can suggest that intrapleural injection of bupivacaine is useful for pain relief following thoracotomy.

• The Korean Journal of Pain
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• 제29권4호
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• pp.229-238
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• 2016

Background: The goal of this in vitro study was to investigate the effect of lipid emulsion on vasodilation caused by toxic doses of bupivacaine and mepivacaine during contraction induced by a protein kinase C (PKC) activator, phorbol 12,13-dibutyrate (PDBu), in an isolated endothelium-denuded rat aorta. Methods: The effects of lipid emulsion on the dose-response curves induced by bupivacaine or mepivacaine in an isolated aorta precontracted with PDBu were assessed. In addition, the effects of bupivacaine on the increased intracellular calcium concentration ($[Ca^{2+}]_i$) and contraction induced by PDBu were investigated using fura-2 loaded aortic strips. Further, the effects of bupivacaine, the PKC inhibitor GF109203X and lipid emulsion, alone or in combination, on PDBu-induced PKC and phosphorylation-dependent inhibitory protein of myosin phosphatase (CPI-17) phosphorylation in rat aortic vascular smooth muscle cells (VSMCs) was examined by western blotting. Results: Lipid emulsion attenuated the vasodilation induced by bupivacaine, whereas it had no effect on that induced by mepivacaine. Lipid emulsion had no effect on PDBu-induced contraction. The magnitude of bupivacaine-induced vasodilation was higher than that of the bupivacaine-induced decrease in $[Ca^{2+}]_i$. PDBu promoted PKC and CPI-17 phosphorylation in aortic VSMCs. Bupivacaine and GF109203X attenuated PDBu-induced PKC and CPI-17 phosphorylation, whereas lipid emulsion attenuated bupivacaine-mediated inhibition of PDBu-induced PKC and CPI-17 phosphorylation. Conclusions: These results suggest that lipid emulsion attenuates the vasodilation induced by a toxic dose of bupivacaine via inhibition of bupivacaine-induced PKC and CPI-17 dephosphorylation. This lipid emulsion-mediated inhibition of vasodilation may be partly associated with the lipid solubility of local anesthetics.

• 약학회지
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• 제45권6호
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• pp.623-633
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• 2001

Various bupivacaine-loaded microspheres were prepared using poly(d,1-lactide) (PLA) and poly(d,1-lactic-co-glycolide) (PLGA) by a solvent evaporation method for the sustained release of drug. The effects of process conditions such as drug loading, polymer type and solvent type on the characteristics of microspheres were investigated. The prepared microspheres were characterized for their drug loading, size distribution, surface morphology and release kinetics. Drug loading efficiency and yield of PLGA micro- spheres were higher than those of PLA microspheres. The prepared microspheres had an average particle size below 5${\mu}{\textrm}{m}$. The particle size range of microspheres was 1.65~2.24${\mu}{\textrm}{m}$. As a result of SEM, the particle size of PLA microspheres was smaller than that of PLGA microspheres. In morphology studies, microspheres showed a spherical shape and smooth surface in all process conditions. In thermal analysis, bupivacaine-loaded microspheres showed no peaks originating from bupivacaine. This suggested that bupivacaine base was molecular-dispersed in the polymer matrix of microspheres. The release pattern of the drug from microspheres was evaluated for 96 hours. The initial burst release of bupivacaine base decreased with increasing the molecular weight of PLGA, and the drug from microspheres released slowly. In conclusion, bupivacaine-loaded microspheres were successfully prepared from poly(d,1-lactide) and poly (d,1- lactic-co-glycolide) polymers with different molecular weights allowing control of the release rate.

• The Korean Journal of Pain
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• 제12권1호
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• pp.48-53
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• 1999

Background: Despite the popularity of epidural bupivacaine-morphine infusions for postoperative pain management, the optimum concentrations and dosages of bupivacaine have not been determined. At present, due to the disadvantages conferred by intense motor block and the increased risk of toxicity, many trials focus on reducing bupivacaine concentration and thus the evaluation of concentrations less than 0.1% may be warranted. Methods: Forty patients having epiduro-general anesthesia for hysterectomy were randomly assigned to one of two study groups. As a mean of postoperative pain control, all received 2 mg of epidural morphine bolusly 1 hr before the end of surgery and continuous epidural infusion was started using a two-day Infusor containing 4 mg of morphine in 100 ml of 0.125% bupivacaine (Group 0.125B, n=20) or 100 ml of 0.0625% bupivacaine (Group 0.0625B, n=20). Study endpoints included visual analog scales (VAS) for pain during rest and movement, sensory change and motor blockade. They were assessed at 2, 4, 8, 16, 24, 32, 40 and 48 hrs postoperatively. Results: For VAS during rest, no significance could be found between two groups over the course of study. But for VAS during movement, the 0.125B group showed more satisfactory results especially during early postoperative periods. For the incidence of complications, the 0.125B group revealed greater frequency of sensory change (25.0%) and motor blockade (10.0%) compared with the 0.0625B group. Conclusion: This study suggests that 0.0625% bupivacaine with morphine via epidural route was sufficient for pain control during rest but it was not satisfactory during movement especially in early postoperative periods. We also recommend that careful attention to motor blockade should be paid when using 0.125% bupivacaine.

• Journal of Yeungnam Medical Science
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• 제7권2호
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• pp.121-130
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• 1990

영남대학교 마취과학교실에서 하지에 국한된 수술을 받는 환자 40예를 대상으로 각군 20예씩 0.5% 고비중 tetracaine 2ml와 0.5% 순수 bupivacaine 2.5ml을 사용하여 척추마취를 실시한 결과 다음과 같은 성적을 얻었다. 1. 각군의 연령, 성별, 신장 및 체중은 비슷하였다. 2. 양군 모두 감각차단이 $T_{12}$분절에 도달되는 시간은 4분정도였고, 감각차단 최고분절높이도 $T_{6-7}$이었으며 최고높이에 도달되는 시간도 20분 정도였다. 3. 운동차단정도도 양군이 비슷하여 10분에 대부분이, 20분이내에 전예에서 완전차단이 초래되었다. 4. Bupivacaine군은 감각차단이 $T_{12}$분절이상에서 유지된 시간이 3시간, 술후 진통시간이 7시간으로 tetracaine군보다 작용시 간과 진통시간이 의의있게 길었다(P<0.05). 5. 수축기 혈압의 감소는 bupivacaine군이 훨씬 적었으며(P<0.05), 혈압은 마취후 20~30분에 심하게 감소되었다. 6. 마취후 발생된 부작용은 전체 대상환자에서 두통(3예), 다리저림(5예), 배뇨곤란(3예) 및 배부통(4예) 등이었고 양군사이에 발생빈도의 차이는 없었다. 이 상의 결과로 bupivacaine 척추마취의 임상적 특징은 감각차단 및 운동차단이 나타나는 양상과 마취후 부작용은 고비중 tetracaine과 비슷하고, 고비중 tetracaine보다 혈압감소가 적고 작용시간이 걸고 술후 진통효과가 좋은 점등의 장점이 있으므로 0.5% 순수 bupivacaine은 하지수술을 위한 척추마취제로 유용하게 사용될 수 있을 것으로 사료된다.