MEGX (hydrochloride)
(Synonyms: 去乙基利多卡因) 目录号 : GC45508
An active metabolite of lidocaine
Cas No.:7729-94-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
MEGX is an active metabolite of lidocaine.1 It is formed via N-deethylation of lidocaine by the hepatic cytochrome P450 (CYP) isoform CYP3A4. Topical administration of MEGX (2% v/v) reduces thrombus formation in a hamster model of laser-induced microvascular injury.2 Plasma levels of MEGX following lidocaine administration have been used to monitor declining liver function in patients with cirrhosis.1
References
1. Reichel, C., Skodra, T., Nacke, A., et al. The lignocaine metabolite (MEGX) liver function test and P-450 induction in humans. Br. J. Clin. Pharmacol. 46(6), 535-539 (1998).
2. Luostarinen, V., Evers, H., Lyytik•inen, M.T., et al. Antithrombotic effects of lidocaine and related compounds on laser-induced microvascular injury. Acta Anaesthesiol. Scand. 25(1), 9-11 (1981).
| Cas No. | 7729-94-4 | SDF | |
| 别名 | 去乙基利多卡因 | ||
| Canonical SMILES | CC1=CC=CC(C)=C1NC(CNCC)=O.Cl | ||
| 分子式 | C12H18N2O.HCl | 分子量 | 242.7 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1203 mL | 20.6016 mL | 41.2031 mL |
| 5 mM | 0.8241 mL | 4.1203 mL | 8.2406 mL |
| 10 mM | 0.412 mL | 2.0602 mL | 4.1203 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Analgesic efficacy of articaine hydrochloride for velvet antler removal in red deer ( Cervus elaphus) and analysis of drug residues in the harvested velvet antlers
N Z Vet J 2019 Sep;67(5):228-233.PMID:31034783DOI:10.1080/00480169.2019.1611503.
Aims: To investigate the analgesic efficacy of articaine hydrochloride for antler removal in red deer (Cervus elaphus) following S/C administration as a ring block, and to quantify the residue concentrations of articaine compared to lignocaine in the harvested antlers. Methods: Articaine hydrochloride (40 mg/mL) was administered to 10 male red deer as a ring block around the base of each antler at 1 mL/cm of pedicle circumference. Analgesia was evaluated by determining the response to a saw cut test every 1-minute, until no response was observed. Behaviour during and following removal of antlers was also recorded. Twenty commercially harvested velvet antlers were also collected following S/C administration of 2% lignocaine hydrochloride. A liquid chromatography-mass spectrometry (LC-MS) method for quantification of residues of articaine and lignocaine in velvet antlers was developed and validated. Results: In red deer administered 4% articaine hydrochloride as a ring block, the median interval to analgesia was 4 (min 3, max 5) minutes and no deer showed withdrawal responses during antler removal. There were no signs of toxicity or adverse effects up to 2 hours after administration. The sample preparation method developed for the LC-MS was simple and had acceptable extraction recoveries of articaine and lignocaine from the velvet antlers. The lower limits of quantification of lignocaine and articaine were 5 and 50 ng/g, respectively. Mean concentrations of articaine in antlers following ring block with 4% articaine hydrochloride were 1.50 (SD 1.09) mg/kg, and of lignocaine following ring block with 2% lignocaine hydrochloride were 0.66 (SD 0.71) mg/kg. Conclusions and clinical relevance: A ring block with 4% articaine hydrochloride at a dose of 1 mL/cm of pedicle circumference provided effective analgesia for velvet antler removal in red deer. The LC-MS method developed and validated to quantify articaine and lignocaine was simple and sensitive. Based on these results, articaine hydrochloride appears to be an effective alternative to lignocaine hydrochloride for velvet antler removal. However, further studies to evaluate the safety and residue concentrations of articaine and articainic acid are required before it can be recommended for use in deer.Abbreviations: DMA: 2,6-dimethylaniline; LC-MS: Liquid chromatography-mass spectrometry; MEGX: Monoethylglycinexylidide; MRL: Maximum residue level.
Pharmacokinetics of intravenous, subcutaneous, and topical administration of lidocaine hydrochloride and metabolites 3-hydroxylidocaine, monoethylglycinexylidide, and 4-hydroxylidocaine in horse
J Vet Pharmacol Ther 2018 Dec;41(6):825-837.PMID:30028024DOI:10.1111/jvp.12695.
Intravenous (iv), subcutaneous (sq), and topical (tp) lidocaine was administered to six horses in a cross-over, randomized design study. Samples were collected for up to 72 hr. Compartmental models were used to investigate the pharmacokinetics of (LD) and its metabolites 3-hydroxylidocaine (3-OH), 4-hydroxylidocaine (4-OH), and monoethylglycinexylidide (MEGX). Metabolites 3-OH and 4-OH were present in conjugated forms, whereas LD and metabolite MEXG were present primarily in the un-conjugated form. Plasma concentrations of LD after iv administration (100 mg) were described by three-compartment model with an additional three compartments to describe the elimination of metabolites. Median (range) elimination micro-constants (Ke ) for LD, 3-OH, 4-OH, and MEXG were 4.12 (2.62-6.23), 1.25 (1.10-2.15), 1.79 (1.22-2.39), and 1.69 (1.03-1.99)/hr, respectively. Median (range) values of alpha (t½α ), beta (t½β ), and gamma (t½γ ) half-lives were 0.08 (0.07-0.13), 0.57 (0.15-1.25), and 4.11 (0.52-7.36) hr. Plasma concentrations of LD after sq (200 mg) administration were described by absorption and two-compartment elimination model. The median (range) of the LD absorption half-life (t½ab ) was 0.47 (0.29-0.61) hr. The Ke for LD, 3-OH, 4-OH, and MEXG was 3.91 (1.48-9.25), 1.00 (0.78-1.08), 1.76 (0.96-2.11), and 1.13 (0.69-1.33)/hr. The median (range) of t½α and t½β was 0.15 (0.06-0.27) and 3.04 (2.53-6.39) hr. Plasma concentrations of LD after tp (400 mg) application were described by one-compartment model with a t½ab of 8.49 (5.16-11.80) hr. The Ke for LD, 3-OH, and MEXG was 0.24 (0.10-0.81), 0.41 (0.08-0.93), and 0.38 (0.26-1.14)/hr.
Lidocaine Intraoperative Infusion Pharmacokinetics during Partial Hepatectomy for Living Liver Donation
Anesthesiology 2023 Jan 1;138(1):71-81.PMID:36512707DOI:10.1097/ALN.0000000000004422.
Background: Postoperative pain associated with open partial hepatectomy can be intense and persistent. The multimodal approach used to lessen this problem includes an intraoperative intravenous infusion of lidocaine hydrochloride. Decreased hepatic metabolism after resection raises concerns about safe lidocaine dosing in this patient population. The hypothesis was that the elimination clearance of lidocaine and its metabolites, monoethylglycinexylidide and glycinexylidide, is reduced after a partial hepatectomy, as reflected by observed plasma concentrations that are higher and have a longer half-life than expected based on pharmacokinetic modeling (estimated for normal liver function). Secondarily, this study postulated that plasma concentrations of lidocaine, monoethylglycinexylidide, and glycinexylidide do not reach toxic concentrations with institutional protocol up to 24 h after surgery. Methods: Blood samples were collected from 15 patients undergoing a partial hepatectomy for living liver donation, at the following specific time points: before and immediately after induction of anesthesia, during hepatectomy, 30 min after hepatectomy completion, at case end, and 24 h after the end of surgery. Plasma concentrations of lidocaine and metabolites were measured by liquid chromatography-mass spectrometry. The population lidocaine pharmacokinetics were estimated, and total body weight and the fraction of remaining liver mass as potential model covariates were evaluated. The detection of any lidocaine, monoethylglycinexylidide, or glycinexylidide toxic plasma concentrations at any time point during and after hepatectomy were also evaluated. Results: The typical value for lidocaine elimination clearance was 0.55 ± 0.12 l/min (± standard error of the estimate) which, on average, was reduced to about one third of the baseline clearance, 0.17 ± 0.02 l/min, once the donor graft was surgically isolated, and remained so for 24 h according to the current data and model. The fraction of remaining liver was a significant covariate for the posthepatectomy lidocaine clearance' such that if 50% of the liver is removed the clearance is reduced by approximately 60%. Plasma concentrations of lidocaine and its metabolites remained below their theoretical combined toxic threshold concentrations throughout the surgical and postoperative course in all patients, with one exception obtained near induction of anesthesia. Plasma lidocaine concentrations decreased at case end and postoperatively, while metabolite concentrations continued to rise at the end of surgery with reduction postoperatively. Pharmacokinetic modeling revealed that the only significant covariate in the model was the fraction of liver remaining after isolation of the donor graft. Conclusions: Intravenous lidocaine infusions are an acceptable option for multimodal pain management in patients undergoing a hepatectomy for living donation if the lidocaine infusion is stopped when the liver resection is complete. Clearance of lidocaine is decreased proportionally to the remaining liver mass, which should guide lidocaine infusion administration or dosing adjustments for patients undergoing liver resection surgery.
Pharmacokinetics of lidocaine and its deethylated metabolite: dose and time dependency studies in man
J Pharmacokinet Biopharm 1982 Jun;10(3):265-81.PMID:7175699DOI:10.1007/BF01059261.
The concentrations of lidocaine and of its deethylated metabolite, MEGX, were measured in blood following the intravenous administration of 50 and 100 mg lidocaine hydrochloride, the oral administration of 100, 300, and 500 mg lidocaine hydrochloride monohydrate, and the oral administration of 300 mg lidocaine hydrochloride monohydrate every 8 h for seven doses, to three healthy volunteers. The range of values for the parameters defining the disposition kinetics of lidocaine were: terminal half-life, 50-231 min; total clearance, 13-17 ml/min/kg; initial dilution space, 0.13-2.5 liters/kg; and volume of distribution at steady state, 0.6-4.5 liters/kg. Lidocaine absorption from solution was rapid, but due to presystemic hepatic metabolism, the availability was low, the range of average values lying between 0.19 and 0.38. No dose or time dependency in lidocaine and monoethylglycinexylidide pharmacokinetics following the single dose studies of lidocaine were noted. Effective hepatic blood flow, based on total clearance and availability measurements, was estimated to be 18-27 ml/min/kg. The concentrations of MEGX were approximately one-third of those of lidocaine following intravenous lidocaine and were comparable following oral lidocaine, but as predicted, the dose normalized area under the MEGX concentration-time curve was constant and independent of the route of administration of lidocaine. In two subjects, the blood concentrations of lidocaine and MEGX following multiple doses of oral lidocaine were those predicted from the single dose studies. In the third subject, the degree of accumulation of lidocaine was greater than predicted. The reasons and mechanism for this difference between subjects on multiple dosing remains unclear.
Concentrations of monoethylglycinexylidide in body fluids of deceased patients after use of lidocaine for endotracheal intubation
Leg Med (Tokyo) 2000 Mar;2(1):31-5.PMID:12935463DOI:10.1016/s1344-6223(00)80006-1.
The objective of this study was to determine whether the postmortem concentrations in body fluids of monoethylglycinexylidide (MEGX), a major active metabolite of lidocaine, reflect the circulatory state during cardiopulmonary resuscitation following endotracheal intubation using lidocaine. The concentrations of lidocaine and MEGX in blood, pericardial fluid, bile and/or urine were measured for sixteen patients who had received endotracheal intubation using Xylocaine jelly, a 2% w/v lidocaine hydrochloride preparation. Lidocaine was detected in all of the sixteen cases. Of six patients who had survived 3 h to 10 d following endotracheal intubation, four were MEGX-positive and two were negative. No MEGX was detected in the other ten patients whose hearts had not resumed beating despite attempts at cardiopulmonary resuscitation. MEGX can be an indicator of the vital state of a patient during cardiopulmonary resuscitation; it shows the antemortem use of lidocaine under normal hepatic conditions.