Pancuronium

潘库溴铵
  • 文章类型: Journal Article
    维库溴铵,罗库溴铵,和潘库溴铵被广泛用作非去极化肌肉松弛剂。使用这种肌肉松弛剂时,偶尔会出现过敏反应甚至死亡的情况。快速测定血液中这些肌松药的浓度可以为早期临床诊断提供有价值的信息。作为季铵化合物,这些肌肉松弛剂是高度极性的。因此,它们不能有效地保留在具有常规流动相的反相色谱柱上。这些季铵肌肉松弛剂主要通过离子对色谱法分离。使用离子配对试剂可以帮助提高季铵肌肉松弛剂的保留能力。然而,由于流动相中离子配对试剂引起的离子抑制,MS检测的灵敏度显着降低。此外,离子配对试剂会污染MS系统。建立了高效液相色谱-串联质谱(HPLC-MS/MS)同时测定血液中3种季铵盐类肌松药含量的方法。稀释血液样品并进行高速离心。上清液在BondElutAL-N固相萃取柱上纯化,然后通过0.45μm微孔膜过滤。季铵肌肉松弛剂在ZIC-cHILIC分析柱上分离(50mm×2.1mm,3.0μm),梯度洗脱。乙腈和0.1%甲酸水溶液用作流动相。通过串联MS与电喷雾电离(ESI)源在正和多反应监测(MRM)模式下分析分离的化合物。维库溴铵的基质效应,罗库溴铵,血中潘库溴铵占88.1%~95.4%。维库溴铵的校准曲线,罗库溴铵,和潘库溴铵在每个范围内都表现出良好的线性关系,所有相关系数(R2)均>0.996。维库溴铵的检测限,罗库溴铵,潘库溴铵为0.2-0.8ng/mL,相应的定量限为0.5-2.0ng/mL。维库溴铵的回收率,罗库溴铵,潘库溴铵占92.8%至110.6%,相对标准偏差(RSD)为3.2%-9.4%。这个方法很灵敏,准确,易于操作,它可以用来快速测定维库溴铵,罗库溴铵,和血中的潘库溴铵.
    Vecuronium, rocuronium, and pancuronium are widely used as non-depolarizing muscle relaxants. There have been occasional cases of allergic reactions and even death when using such muscle relaxants. Rapid determination of the concentration of these muscle relaxants in blood can provide valuable information for early clinical diagnosis. As quaternary ammonium compounds, these muscle relaxants are highly polar. Hence, they cannot be retained effectively on reversed-phase chromatographic columns with conventional mobile phases. These quaternary ammonium muscle relaxants are mainly separated by ion-pair chromatography. Using an ion-pairing reagent can help improve the retention capabilities of quaternary ammonium muscle relaxants. Nevertheless, the sensitivity of MS detection is significantly decreased because of ionic inhibition caused by the ion-pairing reagent in the mobile phase. Furthermore, ion-pairing reagents can pollute the MS system. A method based on high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was established for the simultaneous determination of the three quaternary ammonium muscle relaxants in blood. The blood samples were diluted and subjected to high-speed centrifugation. The supernatant was purified on a Bond Elut AL-N solid phase extraction column and then filtered through a 0.45 μm microporous membrane. The quaternary ammonium muscle relaxants were separated on a ZIC-cHILIC analytical column (50 mm×2.1 mm, 3.0 μm) with gradient elution. Acetonitrile and 0.1% formic acid aqueous solution were used as mobile phases. The separated compounds were analyzed by tandem MS with an electrospray ionization (ESI) source in positive and multiple reaction monitoring (MRM) modes. The matrix effects of vecuronium, rocuronium, and pancuronium in blood were 88.1% to 95.4%. The calibration curves for vecuronium, rocuronium, and pancuronium showed good linear relationships in each range, and all correlation coefficients (R2) were > 0.996. The limits of detection of vecuronium, rocuronium, and pancuronium were 0.2-0.8 ng/mL, with the corresponding limits of quantification being 0.5-2.0 ng/mL. The recoveries of vecuronium, rocuronium, and pancuronium were 92.8% to 110.6%, with relative standard deviations (RSDs) of 3.2%-9.4%. This method is sensitive, accurate, and easy to operate, and it can be used to rapidly determine vecuronium, rocuronium, and pancuronium in blood.
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    文章类型: English Abstract
    OBJECTIVE: To investigate the haemodynamic and respiratory changes following intravenous administration with midazolam, pavulon or both of them in the patients having incoordination between spontaneous breathing and mechanical ventilation.
    METHODS: Thirty patients having incoordination between spontaneous breathing and mechanical ventilation were randomly assigned to receiving intravenous injection of pavulon (group 1), midazolam (group 3), and both (group 2) respectively with 10 cases in each group. The degree of coordination between spontaneous breathing and mechanical ventilation, blood pressure (BP), heart rate (HR), respiration frequency (RF), oxygen saturation of pulse (SpO(2)) were observed before the medication and at 5, 15, 30 and 60 minutes following the administration of drugs in all the patients.
    RESULTS: Incoordination between spontaneous breathing and mechanical ventilation, fast RF, decreased SpO(2) were observed before the drug in all patients. Improvement of respiratory was significant in group 2. Patients in group 2 were in excellent coordination between spontaneous breathing and mechanical ventilation, reaching 100% within 30 minutes after administration, and lasting longer. The haemodynamics maintained stable and a significant improvement in respiration and SpO(2) were found. BP and HR were elevated significantly, and RF and hypoxemia were improved, and the degree of coordination between spontaneous breathing and mechanical ventilation reached 100% 5 minutes after the drug, but with shorter duration in group 1. There were no obvious changes in BP, HR, RF and hypoxemia, and the degree of coordination between spontaneous breathing and mechanical ventilation was lowest in group 3.
    CONCLUSIONS: The combined use of midazolam and pavulon has little influence on circulation, and it also can maintain the coordination between spontaneous breathing and mechanical ventilation. It is suggested that the combined use of midazolam and pavulon is an optimal way to improve the ventilatory function in mechanical ventilation.
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  • 文章类型: Journal Article
    Nasopharyngeal (NPT) and rectal (RT) temperatures were continuously monitored in 51 adult or pediatric patients undergoing cardiac surgical procedures until 1 hour after the termination of cardiopulmonary bypass (CPB). The measurement also included the lowest NPT achieved and the dwelling time at that temperature on CPB, the rewarming time, the time on CPB, and the time that the chest remained opened after CPB. After the termination of CPB, the decrease of NPT (afterdrop) was significantly greater in the adult group than in the pediatric group. The mean decrease in adult patients was 1.34 +/- 0.65 degrees C versus 0.63 +/- 0.8 degrees C in pediatric patients. The combination of the NPT at the end of bypass (EndNPT), body weight times the EndNPT, and the dwelling of the lowest temperature times the EndNPT could predict 45% of the afterdrop. It is concluded that afterdrop occurs to a lesser degree in pediatric patients than in adults. This may be due to more efficient supplying of external heat to pediatric patients in whom there is a larger body surface area to weight ratio.
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    文章类型: Journal Article
    Ketamine has many neuromuscular effects in vitro. Its neuromuscular effects in vivo have been controversial and inconsistent. To systematically examine its neuromuscular effects over a wide dose range and its interaction with all popular nondepolarizing neuromuscular relaxants, the effects of ketamine 2, 5, and 10 mg/kg IV were studied on a continuous but incomplete (50%) neuromuscular block preestablished by an IV infusion of d-tubocurarine, atracurium, vecuronium, and pancuronium. Indirectly stimulated adductor pollicis muscle response of monkeys anesthetized with 0.5-1.0% halothane in oxygen were quantified. Ketamine in the absence of a neuromuscular relaxant had no effect on the thumb twitch. In a dose-dependent manner, ketamine significantly enhanced the 50% depression of the thumb twitch preestablished by a constant IV infusion of each of the four muscle relaxants studied. Ketamine 2 mg/kg potentiated the neuromuscular relaxants in the following order of magnitude: vecuronium greater than atracurium greater than d-tubocurarine greater than pancuronium. However, with a 10 mg/kg dose of ketamine, pancuronium became as potentiated as was vecuronium, i.e., pancuronium = vecuronium greater than atracurium greater than d-tubocurarine. It is concluded that in the primate, ketamine potentiates all nondepolarizing muscle relaxants in a dose-dependent manner.
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  • 文章类型: Clinical Trial
    进行了一项随机交叉试验,以比较三种低剂量口服避孕药(OC)的药效学作用:Marvelon(150微克去氧孕酮(DSG)30微克乙炔雌二醇(EE),Mercilon(150微克DSG+20微克EE)和Microgynon(150微克左炔诺孕酮(LNG)+30微克EE)。没有OCs产生血清胆固醇的任何显著变化,LDL-C和载脂蛋白B。去氧孕烯OCs增加了甘油三酯,但Microgynon没有增加。然而,后者增加了葡萄糖耐量试验的葡萄糖和胰岛素反应,而Marvelon和Mercilon则没有影响。HDL-C随着Marvelon而增加,与Mercilon保持不变,与Microgynon降低。所有三种OC都增加了载脂蛋白AII,但只有DSGOC增加了载脂蛋白AI。所有OC都产生了相似的钙蓝蛋白增加,但Marvelon和Mercilon的SHBG增加要比Microgynon大得多。与DSGOCs相比,Microgynon降低的睾酮更多。与DSG相比,许多变化反映了LNG对代谢参数的强烈抗雌激素作用。除了对HDL-C的影响,Marvelon和Mercilon在代谢参数上几乎没有差异,这补充了两种OCs的大规模临床试验的结果。Mercilon,因此提供了一个非常令人满意的替代Marvelon。
    12名健康志愿者参加上海计划生育诊所,初产妇和婴儿中国,医院,参加了这项研究,口服避孕药(OCs)的处方:Marvelon(150mcgdesogestrel-DSG),Mercilon(150mcg的DSG),和Microgynon(150微克左炔诺格雷-液化天然气)。在一项随机交叉研究中,将患者分为6组,每组2人。在周期的第6天进行OC直至第21天,然后停止7天。每个OC使用3个月。在卵泡期的第6天和第9天以及黄体期的第21天和第22天之间的预处理周期中,禁食后采集血液样本以测定脂质,性激素结合球蛋白(SHGB),铜蓝蛋白,和睾丸激素。葡萄糖负荷后,在仅用Microgynon治疗的1,2和3小时,血糖和胰岛素显著升高.胰岛素与葡萄糖的总面积比没有显着变化,糖基化血红蛋白A1水平也没有显着变化。Marvelon(27%-43%)和Mercilon(29-40%)的血清甘油三酯浓度均显着增加。Marvelon的血清高密度脂蛋白(HDL)胆固醇浓度显着升高,但Mercilon的浓度较低,而HDL-C显著降低与Microgynon。血清低密度脂蛋白(LDL)胆固醇变化不显著,但LDL-C浓度随DSG制剂而下降,而随Microgynon增加。Marvelon和Mercilon的载脂蛋白A1和A2均显着增加。载脂蛋白A2随Microgynon增加。Marvelon的血清SHBG显着增加(335-380%)。血清睾丸激素浓度显着降低(Microgynon为33.2-40.4%),铜蓝蛋白值也是如此。强LNG在Microgynon中的抗雌激素感化产生了显著的代谢变更。Marvelon中30mcgEE和Mercilon中20mcgEE的作用是相等的。
    A randomised cross-over trial was performed to compare the pharmacodynamic actions of three low-dose oral contraceptives (OCs): Marvelon (150 micrograms desogestrel (DSG)+ 30 micrograms ethinyloestradiol (EE)), Mercilon (150 micrograms DSG + 20 micrograms EE) and Microgynon (150 micrograms levonorgestrel (LNG) + 30 micrograms EE). None of the OCs produced any significant changes in serum cholesterol, LDL-C and apoprotein B. Triglycerides were increased by the desogestrel OCs but not by Microgynon. The latter however increased the glucose and insulin responses to a glucose tolerance test whereas Marvelon and Mercilon had no effect. HDL-C increased with Marvelon, was unchanged with Mercilon and was decreased with Microgynon. Apoprotein AII was increased by all three OCs but only the DSG OCs increased apoprotein AI. All OCs produced similar increases in caeruloplasmin but the increase in SHBG was much greater with Marvelon and Mercilon than with Microgynon. Testosterone was reduced more with Microgynon than with the DSG OCs. Many of the changes reflect the strong anti-oestrogenic action of LNG on metabolic parameters compared to DSG. Except for the effect on HDL-C, there was little difference between Marvelon and Mercilon on metabolic parameters and this complements the findings from large-scale clinical trials of the two OCs. Mercilon, therefore provides a very satisfactory alternative to Marvelon.
    12 healthy volunteers attending the family planning clinic at Shanghai, First Maternity and Infant China, Hospital, enrolled in the study, Oral contraceptives (OCs) were prescribed: Marvelon (150 mcg of desogestrel--DSG), Mercilon (150 mcg of DSG), and Microgynon (150 mcg of levonorgestrel--LNG). The patients were divided into 6 groups of 2 persons each in a randomized cross-over study. OCs were taken on day 6 of the cycle up to day 21, then stopping for 7 days. Each OC was used for 3 months. During the pretreatment cycle between days 6 and 9 of the follicular phase and 21 and 22 of the luteal phase a blood sample was taken after fasting for determination of lipids, sex hormone binding globulin (SHGB), ceruloplasmin, and testosterone. After glucose loading, significant increases of glucose and insulin occurred at 1, 2, and 3 hours during treatment with Microgynon only. The ratio for total areas of insulin to glucose did not change significantly nor did glycosilated hemoglobin A1 levels. Serum triglyceride concentrations increased significantly for both Marvelon (27%-43%) and Mercilon (29-40%). Serum high density lipoprotein (HDL) cholesterol concentrations were significantly elevated with Marvelon but less so with Mercilon, while HDL-C decreased significantly with Microgynon. The serum low density lipoprotein (LDL) cholesterol changes were not significant, but LDL-C concentrations declined with DSG formulations and increased with Microgynon. Apoprotein A1 and A2 increased significantly for both Marvelon and Mercilon. Apoprotein A2 increased with Microgynon. Serum SHBG increased markedly with Marvelon (335-380%). Serum testosterone concentrations decreased significantly (33.2-40.4% with Microgynon) and so did ceruloplasmin values. The antiestrogenic effect of strong LNG in Microgynon produced significant metabolic changes. The effect of 30 mcg EE in Marvelon and 20 mcg EE of Mercilon was equal.
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