Enantiomer Of Racemic Bupivacaine Research Articles

Comparison of Equivalent Doses of Intrathecal Hyperbaric Levo-bupivacaine and Hyperbaric Bupivacaine for Caesarean Section: A Prospective Randomised Double-Blind Study

Introduction: Subarachnoid Block (SAB) with Hyperbaric Bupivacaine (HB) is the most common anaesthetic technique for Lower Segment Caesarean Section (LSCS). Levo-bupivacaine, an enantiomer of racemic bupivacaine, has been developed to provide anaesthesia with the same effectiveness but with better haemodynamic stability. Aim: To compare the effectiveness of hyperbaric levobupivacaine to HB in achieving sensory and motor blocks in Caesarean Section(CS) using equivalent doses. Materials and Methods: Eighty parturients aged 18-38 years with no co-morbidities were randomly divided into two groups receiving equivalent doses of HB and hyperbaric levobupivacaine for SAB. The effectiveness of the two drugs was compared in terms of the time taken to achieve sensory and motor blocks, as well as the time for block regression for two segments for sensory block and the return of motor block assessed by the ability to flex the ankle joint. Adverse events such as a fall in Systolic Blood Pressure (SBP) and the dose of vasopressor were noted for the two groups. Results: The time taken to attain a T6 dermatomal block level was 2.43±1.00 and 2.80±1.51 (p-value 0.08) for the bupivacaine and levo-bupivacaine groups, respectively. Complete motor block of the lower limb was achieved in 4.85±1.67 and 5.15±1.82 (p-value 0.53). However, the time to 2-segment regression for sensory block was significantly faster in the levo-bupivacaine group than in the bupivacaine group (125.9±28.56 minutes and 109.13±28.84 minutes, respectively, p-value 0.009). Regression from motor block was also found to be highly statistically significant (158.38±34.92 minutes for bupivacaine and 138.75±25.71 minutes for the levobupivacaine group, p-value 0.006). Spinal-induced hypotension was comparable in both groups, but the bupivacaine group needed a much higher repetition of dose of vasopressor than the levo-bupivacaine group. Conclusion: Levo-bupivacaine is comparable to its racemic isomer bupivacaine in achieving anaesthesia when administered Intrathecally (IT) for CS. However, with equivalent doses, the duration of action is significantly shorter with hyperbaric levobupivacaine. Dose adjustment might be required with hyperbaric levo-bupivacaine based on the duration of the surgery. Haemodynamic stability is also similar with both drugs.

Comparison of Intrathecal Bupivacaine with Levobupivacaine using Fentanyl as an Adjuvant for Transurethral Resection of Prostate-A Randomised Controlled Trial

Introduction: Transurethral Resection of Prostate (TURP) is a common surgical procedure performed for Benign Prostatic Hypertrophy (BPH), most commonly under Spinal Anaesthesia (SA). It is generally tolerated well by the elderly but since they suffer from several co-morbidities, therefore, it is desirable to avoid hypotension following SA, in these patients. Levobupivacaine, a pure S enantiomer of racemic bupivacaine has emerged as a safe alternative to bupivacaine with similar efficacy and better pharmacokinetic profile. Aim: To compare the efficacy of intrathecal levobupivacaine with bupivacaine using fentanyl as adjuvant in TURP. Materials and Methods: This randomised controlled trial was conducted at Pandit BD Sharma Postgraduate Institute of Medical Sciences, Rohtak, Haryana, India, between March 2022 to September 2022. Fifty patients, 50-80 years of age, American Society of Anaesthesiologists (ASA) I-III, posted for TURP under SA, were included in the study and divided into two groups: group B (n=25): Inj. bupivacaine (0.5%) hyperbaric 12.5 mg+25 µg fentanyl citrate, group L (n=25): Inj. levobupivacaine (0.5%) isobaric 12.5mg+25µg fentanyl citrate. Onset of sensory and motor block, time to onset of maximum sensory and motor block, Heart Rate (HR), Systolic Bood Pressure (SBP), Diastolic Bood Pressure (DBP) and Mean Arterial Pressures (MAP) were recorded. Data analysis was done with the help computer software using Statistical Package for the Social Sciences (SPSS), version 24.0. Means, standard deviations, Chi-square, t-values and p-values were calculated, p-value <0.05 was considered significant at 95% confidence level. Results: Demographic data of the patients was comparable. The mean time to onset of sensory block in group B was significantly faster (3.72±0.96 min) than group L (4.47±0.73 min). The mean time to onset of motor block was faster in group B (4.74±0.91 min) than group L (7.57±1.51 min). HR was lower in group B, after SA at 5, 10, 15, 20, 30, and 45 min after SA. Group B recorded a lower SBP, DBP and MAP following SA, compared to group L (p<0.001). The duration of analgesia was significantly longer in group B (232.80±14.07 min vs 221.80±15.47 min in group L) (p<0.05). No adverse effects were reported from either of the groups. Conclusion: Levobupivacaine provided very stable haemodynamics, good quality analgesia and muscle relaxation intraoperatively. Postoperative analgesia was clinically similar to bupivacaine, no adverse effects were reported. Thus, levobupivacaine is a safe and reliable alternative to bupivacaine for elderly patients undergoing TURP

English

BACKGROUND: There are always efforts to find a better and safer local anaesthetic along with adjuvants in epidural anaesthesia. Bupivacaine is a long acting, effective local anaesthetic that is commonly administered in anaesthesia practice. Despite its undoubted efficacy, bupivacaine is associated with cardiotoxicity and neurotoxicity. Central nervous system (CNS) and cardiovascular adverse reactions reported after inadvertent intravascular or intravenous regional anesthesia have been linked to R (+) isomer of bupivacaine. So Levobupivacaine, the pure S (-) - enantiomer of racemic bupivacaine, was developed as an alternative to bupivacaine. Levobupivacaine is increasingly used in the clinical practice because of its safer pharmacological profile and faster protein binding rate AIM: This study was conducted to evaluate the onset and duration of analgesia, extent and duration of sensory and motor block, sedation and side effects of Dexmedetomidine and Clonidine when used as adjuvants to Levobupivacaine in epidural anaesthesia for lower limb orthopaedic surgeries. MATERIALS AND METHODS:A prospective randomized study was carried out in the department of Anaesthesia at Rajarajeswari Medical College and Hospital which included 50 adult patients between the ages of 21 and 60 years (of ASA I/II grade) who underwent lower limb orthopaedic surgeries. The patients were randomly allocated into two groups; levobupivacaine + dexmedetomidine (LD) and levobupivacaine + clonidine (LC), comprising of 25 patients each. Group LD was administered 18 ml of 0.5% epidural levobupivacaine and 1.5 µg/kg of dexmedetomidine, while group LC received admixture of 18 ml of 0.5% levobupivacaine and 2 µg/kg of Clonidine. Onset of analgesia, sensory and motor block levels, sedation, duration of analgesia and side effects were observed. STATISTICAL ANALYSIS: The data obtained was subjected to statistical analysis using analysis of variance, student t test, chi-square test and Fisher Exact test. The Statistical Software namely SAS 9.2,SPSS 15.0,Stata 10.1,MedCalc 9.0.1,Sysatat 12.0 and R environment ver.2.11.1 were also used for the analysis of the data and Microsoft word and Excel have been used to generate graphs,tables etc. The value of P 0.05). CONCLUSION: Dexmedetomidine is a better neuraxial adjuvant when compared to clonidine for providing early onset of sensory and motor blockade levels, adequate sedation and a prolonged post-operative analgesia with better success rate and increased patient satisfaction.

Comparison of intrathecal hyperbaric bupivacaine and levobupivacaine for Cesarean section

Background Levobupivacaine is a relatively new amide local anesthetic, and it has been already investigated in epidural and locoregional techniques, but more has to be known regarding its characteristics in spinal anesthesia. Aims The aim of our study was to compare clinical and anesthetic features of levobupivacaine and racemic bupivacaine when intrathecally administered in patients undergoing elective Cesarean section. Patients and methods Hundred patients of ASA I and II were randomized to receive an intrathecal injection of one of two local anesthetic solutions. Each patient in group L ( n = 50) received 2 ml of isobaric levobupivacaine 5 mg/ml (10 mg) with 15 μg of fentanyl, whereas each patient in group B ( n = 50) received 2 ml of hyperbaric bupivacaine (10 mg) with 15 μg of fentanyl. The parameters studied were onset and total duration of sensory block, onset and total duration of motor block, the quality of intraoperative anesthesia, hemodynamic alterations, and any intraoperative and postoperative complications. Results There were no significant differences in demographic or surgical variables between the two groups. There was no significant difference in the quality of anesthesia and intraoperative side effects in the two groups. Time to complete regression of motor blockade was statistically lower in group L (135 ± 15.6 vs. 145 ± 20.5 min; P 12 level in group L (168.3 ± 15.6 vs. 172.2 ± 20.5 min; P > 0.005) was nonsignificant when compared with group B. Conclusion Levobupivacaine, the pure S (-) enantiomer of racemic bupivacaine, is an equally effective local anesthetic for spinal anesthesia for Cesarean section, compared with racemic bupivacaine.

Does levobupivacaine have a benefit over bupivacaine in our practice?

Background The well-known toxic effects of bupivacaine on central nervous system and cardiovascular system were a base for the development of new long-acting local anesthetics. Levobupivacaine is the pure S(-)-enantiomer of racemic bupivacaine. This study compares the efficacy of levobupivacaine as against bupivacaine by epidural clinical study and by different routes in animal study. Materials and methods Evaluation of the analgesic activities by the hot plate method was carried out in nine groups of mice. Each four groups were injected intraperitoneally with either levobupivacaine or bupivacaine. The control group received saline. The hemodynamic effects of levobupivacaine and bupivacaine were carried out on the isolated rabbit's heart and anesthetized cats for carotid blood pressure and ECG. Thirty patients undergoing limb surgery were randomized to receive 15 ml of 0.5% levobupivacaine or bupivacaine through epidural needle. Intraoperative blood pressure and heart rate were recorded. Onset time of sensory and motor block, time to T 10 sensory block, complete motor block, quality of analgesia, and times for two segment regressions were detected. Results Experimentally, the intensity and duration of analgesia produced by levobupivacaine was more than that of bupivacaine. Both drugs induced significant dose-dependent negative inotropic effect, but it was lesser in levobupivacaine than in bupivacaine. An amount of 2 mg/kg levobupivacaine produced a significant rise in blood pressure and 4 mg/kg significantly decreased it, whereas 1 and 2 mg/kg bupivacaine produced a significant decrease in blood pressure. The ECG pattern of levobupivacaine showed no abnormalities, but bupivacaine at a dose of 2 mg/kg produced significant bradycardia and ECG changes. Cardiac arrest and death of cats occurred when 4 mg/kg of bupivacaine was injected. Clinically, the onset time of sensory block, time to T 10 sensory block and time to complete motor block are lower with bupivacaine than with levobupivacaine. Conclusion We found, based on the current pharmacodynamics evidence from this experimental and clinical study, that levobupivacaine has good analgesic activity and less cardiodepressant effect, and it offers advantages over bupivacaine.

Local anesthesia for treatment of hernia in elder patients: Levobupicavaine or Bupivacaine?

BackgroundInguinal hernia is one of the most common diseases in the elderly. Treatment of this pathology is exclusively surgical and relies almost always on the use of local anesthesia. While in the past hernia surgery was carried out mainly by general anesthesia, in recent years there has been growing emphasis on the role of local anesthesia.MethodsThe aim of our study was to compare intra-and postoperative analgesia obtained by the use of levobupivacaine to the same obtained by bupivacaine. Bupivacaine is one of the main local anesthetics used in the intervention of inguinal hernioplasty. Levobupivacaine is an enantiomer of racemic bupivacaine with less cardiotoxicity and neurotoxicity. The study was conducted from March 2011 to March 2013. We collected data of eighty patients, male and female, aged between 65 and 86 years, who underwent inguinal hernioplasty with local anesthesia.ResultsEvaluation of intra-operatively pain shows that minimal pain is the same in both groups. Mild pain was more frequent in the group who used levobupivacaine. Moderate pain was slightly more frequent in the group who used bupivacaine. Only one reported intense pain. Two drugs seem to have the same effect at a distance of six, twelve, eighteen and twentyfour hours. Bupivacaine shows a significantly higher number of complications, as already demonstrated by previous studies. Degree of satisfaction expressed by patients has been the same in the two groups. Levobupivacaine group has shown a greater request for paracetamol while patients who experienced bupivacaine have showed a higher request of other analgesics.ConclusionsClinical efficacy of levobupivacaine and racemic bupivacaine are actually similar, when used under local intervention of inguinal hernioplasty. In the field of ambulatorial surgery our working group prefers levobupivacaine for its fewer side effects and for its easy handling.

Comparative study between Levobupivacaine and Bupivacaine for hernia surgery in the elderly

BackgroundThe inguinal hernia is one of the most common diseases in the elderly. Treatment of this type of pathology is exclusively surgical and relies almost always on the use of local anesthesia. While in the past hernia surgery was carried out mainly by general anesthesia, in recent years there has been growing emphasis on the role of local anesthesia.MethodsThe aim of our study was to compare intra-and postoperative analgesia obtained by the use of levobupivacaine compared with that of bupivacaine. Bupivacaine is one of the main local anesthetics used in the intervention of inguinal hernioplasty. Levobupivacaine is an enantiomer of racemic bupivacaine with less cardiotoxicity and neurotoxicity. The study was conducted from April 2010 to May 2012. We collected data of forty male patients, aged between 73 and 85 years, who underwent inguinal hernioplasty with local anesthesia for the first time.ResultsMinimal pain is the same in both groups. Mild pain was more frequent in the group who used bupivacaine, moderate pain was slightly more frequent in the group who used levobupivacaine, and the same for intense pain. It is therefore evident how Bupivacaine is slightly less preferred after four and twenty four hours, while the two drugs seem to have the same effect at a distance of twelve and forty-eight hours. Bupivacaine shows a significantly higher number of complications, as already demonstrated by previous studies. The request for an analgesic was slightly higher in patients receiving levobupivacaine.ConclusionsAfter considering all these elements, we can conclude that the clinical efficacy of levobupivacaine and racemic bupivacaine are essentially similar, when used under local intervention of inguinal hernioplasty.

Levobupivacaine for Regional Anesthesia and Pain Management

Levobupivacaine is an enantiomer of racemic bupivacaine with a safe pharmacological profile. We present a review of levobupivacaine and its current clinical use in regional anaesthesia and pain management. The pharmacokinetic and pharmacodynamic profile of levobupivacaine is discussed and a qualitative review of studies involving levobupivacaine for regional anaesthesia is presented. Comparisons of levobupivacaine with other local anaesthetic agents as well as studies looking at different doses of levobupivacaine are overviewed.

A Comparison of Epidural Analgesia using 0.1% Levobupivacaine or 0.2% Levobupivacaine Combined with Sufentanil after Major Abdominal Surgery

Background: Continuous epidural analgesia with an opioid-local anesthetic combination is an effective strategy for postoperative pain relief after abdominal surgery. Levobupivacaine, the pure S (−) enantiomer of racemic bupivacaine, is similar to its native agent for anesthetic efficacy but has less cardiotoxic and neurotoxic potential than the bupivacaine. We compared the efficacy and safety of 0.1% levobupivacaine with sufentanil or 0.2% levobupivacaine with the same dose of suentanil for patient-controlled epidural analgesia after major abdominal surgery. Methods: Forty patients scheduled for major abdominal surgery under general anesthesia were randomized to receive either 0.1% levobupivacaine with sufentanil 0.75μg/ml (n = 20) or 0.2% levobupivacaine with sufentanil 0.75μg/ml (n = 20) for postoperative epidural analgesia using a patient-controlled analgesia pump at a rate of 3 ml/h and bolus dose of 2 ml on demand. Visual analogue scale (VAS) pain scores at rest, on coughing, during mobilization from the supine to the sitting position and on ambulation were assessed during 48 hours following the surgery. In addition, degree of motor block and mobilization, additional analgesic requirements and adverse effects were assessed. Results: There were no significant differences in VAS pain scores at rest, on coughing, during mobilization from the supine to the sitting position and on ambulation. There were no signi ficant differences in mean volume of local anesthetic consumption, additional analgesic requirements, degree of motor block and mobilization and the incidence of adverse effects. Conclusions: 0.1% levobupivacaine with sufentanil provided comparable postoperative epidural analgesia and incidences of adverse effects to 0.2% levobupivacaine with the same dose of suentanil in patients undergoing major abdominal surgery. (Korean J Anesthesiol 2008; 54: 307∼14)

Pharmacokinetics of levobupivacaine 0.25% following caudal administration in children under 2 years of age

Levobupivacaine, the S(-)enantiomer of racemic bupivacaine is less cardiotoxic than racemic bupivacaine and the R(+)enantiomer dexbupivacaine, while retaining similar local anaesthetic properties and potency to racemic bupivacaine. The pharmacokinetic profiles of the two bupivacaine enantiomers differs and that of racemic bupivacaine may be age dependent. We examined the pharmacokinetics of levobupivacaine after its single shot caudal epidural administration in children. An open-label phase 2 study was undertaken to examine the pharmacokinetics of levobupivacaine 0.25% 2 mg kg(-1) in 49 children aged less than 2 yr, after single shot caudal epidural administration. Plasma concentrations were determined at intervals up to 60 min after caudal injection. Time to peak plasma concentration (T(max)) ranged between 5 and 60 min (median 30 min) and was reached later in children aged less than 3 months (P<0.005). Peak plasma concentration (C(max)) ranged between 0.41 and 2.12 micro g ml(-1) (median 0.80, mean (SD) 0.91 (0.40) micro g ml(-1)). After the caudal epidural administration of levobupivacaine 2 mg kg(-1) in children less than 2 yr of age, C(max) was within the accepted safe range for racemic bupivacaine. T(max) varied and occurred later in some children, particularly those aged less than 3 months. Sampling in future pharmacokinetic studies in this age group should extend beyond 60 min.

Spinal anesthesia with 0.5% S(−)-bupivacaine for elective lower limb surgery

Background and Objectives. This study examines the clinical effects of the subarachnoid administration of levobupivacaine, the S(−)-enantiomer of racemic bupivacaine. Methods. An open, noncomparative study was performed on 20 patients undergoing elective lower limb surgery. Three milliliters of a plain solution of 0.5% S(−)-bupivacaine (15 mg) was administered via the L2 or L3 interspace with the patient in the sitting position. Following injection, the patients were immediately placed supine. Spread of sensory analgesia, degree of motor block, and hemodynamic parameters were recorded. Results. Satisfactory surgical anesthesia was achieved in 18 patients. The median time to onset of analgesia was 2 minutes (ranging 2–10 minutes) and the median duration of analgesia was 388 minutes (range, 295–478 minutes). This group of patients achieved complete motor block, with a median onset time of 5 minutes (2–10 minutes) and duration of 266 minutes (range, 170–415 minutes). Sensory block height was inadequate for surgery in 2 patients, who received supplemental anesthesia. Conclusions. The results suggest that S(−)-bupivacaine can provide satisfactory surgical anesthesia, but the spread of the plain solution is unpredictable.