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酯类局部麻醉药氯普鲁卡因的代谢与测定

Metabolism and measurement of chloroprocaine, an ester-type local anesthetic.

作者信息

O'Brien J E, Abbey V, Hinsvark O, Perel J, Finster M

出版信息

J Pharm Sci. 1979 Jan;68(1):75-8. doi: 10.1002/jps.2600680123.

DOI:10.1002/jps.2600680123
PMID:758470
Abstract

Blood levels of intact chloroprocaine were determined using a GLC procedure capable of detecting as little as 10 ng of chloroprocaine/ml of blood. It was necessary to detective plasma cholinesterases in collected samples by adding echothiophate iodide to blood sampling tubes. An extraction procedure, followed by a TLC separation and spectrodensitometric assay, was developed for measurement of the metabolite 2-chloro-4-aminobenzoic acid in plasma and urine. With these procedures, data were obtained showing that chloroprocaine is hydrolyzed rapidly by plasma cholinesterases. No unchanged drug could be detected in any blood samples obtained from volunteers who received chloroprocaine by intravenous infusion or from obstetric patients who had epidural anesthesia during labor and delivery. Blood levels of 2-chloro-4-amino-benzoic acid rose promptly with the administration of chloroprocaine and declined rapidly after drug administration. Most of the metabolite was recovered in urine.

摘要

使用一种气相色谱法(GLC)来测定血液中完整的氯普鲁卡因水平,该方法能够检测低至每毫升血液10纳克的氯普鲁卡因。有必要通过向血样采集管中添加碘依可酯来检测采集样本中的血浆胆碱酯酶。开发了一种提取程序,随后进行薄层色谱(TLC)分离和光密度测定法,用于测量血浆和尿液中的代谢物2 - 氯 - 4 - 氨基苯甲酸。通过这些程序获得的数据表明,氯普鲁卡因被血浆胆碱酯酶迅速水解。在接受静脉输注氯普鲁卡因的志愿者或在分娩期间接受硬膜外麻醉的产科患者采集的任何血样中,均未检测到未变化的药物。2 - 氯 - 4 - 氨基苯甲酸的血药浓度在给予氯普鲁卡因后迅速上升,并在给药后迅速下降。大部分代谢物在尿液中回收。

相似文献

1
Metabolism and measurement of chloroprocaine, an ester-type local anesthetic.酯类局部麻醉药氯普鲁卡因的代谢与测定
J Pharm Sci. 1979 Jan;68(1):75-8. doi: 10.1002/jps.2600680123.
2
Fetal acidosis, 2-chloroprocaine, and epidural anesthesia for cesarean section.胎儿酸中毒、2-氯普鲁卡因与剖宫产硬膜外麻醉
Am J Obstet Gynecol. 1985 Feb 1;151(3):322-4. doi: 10.1016/0002-9378(85)90295-9.
3
Intrapartum paracervical block anesthesia with 2-chloroprocaine.分娩期用2-氯普鲁卡因行宫颈旁阻滞麻醉。
Am J Obstet Gynecol. 1983 May 1;146(1):16-22. doi: 10.1016/0002-9378(83)90920-1.
4
Continuous Epidural Analgesia Using an Ester-Linked Local Anesthetic Agent, 2-Chloroprocaine, During Labor: A Case Report.分娩期间使用酯类局部麻醉药2-氯普鲁卡因进行连续硬膜外镇痛:一例报告
A A Case Rep. 2017 Jun 1;8(11):297-299. doi: 10.1213/XAA.0000000000000494.
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Plasma levels of 2-chloroprocaine in obstetric patients and their neonates after epidural anesthesia.
Anesthesiology. 1980 Jul;53(1):21-5. doi: 10.1097/00000542-198007000-00005.
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The half-life of 2-chloroprocaine.2-氯普鲁卡因的半衰期。
Anesth Analg. 1986 Mar;65(3):273-8.
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Continuous chloroprocaine infusion for thoracic and caudal epidurals as a postoperative analgesia modality in neonates, infants, and children.持续输注氯普鲁卡因用于新生儿、婴儿和儿童胸段及骶管硬膜外术后镇痛。
Paediatr Anaesth. 2016 Jan;26(1):84-91. doi: 10.1111/pan.12807. Epub 2015 Nov 4.
8
2-Chloroprocaine for local perineal infiltration.用于局部会阴浸润的2-氯普鲁卡因。
Am J Obstet Gynecol. 1987 Nov;157(5):1275-8. doi: 10.1016/s0002-9378(87)80313-7.
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The chloroprocaine controversy.氯普鲁卡因之争
Am J Obstet Gynecol. 1981 Jun 1;140(3):237-9. doi: 10.1016/0002-9378(81)90266-0.
10
[Peridural analgesia in labor. Comparison between bupivacaine and 2-chloroprocaine].[分娩时的硬膜外镇痛。布比卡因与2-氯普鲁卡因的比较]
Cah Anesthesiol. 1986 Mar-Apr;34(2):95-8.

引用本文的文献

1
Block-dependent sedation during epidural anaesthesia is associated with delayed brainstem conduction.硬膜外麻醉期间的节段依赖性镇静与脑干传导延迟有关。
Br J Anaesth. 2004 Aug;93(2):228-34. doi: 10.1093/bja/aeh192. Epub 2004 Jun 25.
2
Epidural morphine does not affect the duration of action of epidural 2-chloroprocaine following Caesarean section.剖宫产术后,硬膜外吗啡不影响硬膜外2-氯普鲁卡因的作用持续时间。
Can Anaesth Soc J. 1983 Nov;30(6):598-602. doi: 10.1007/BF03015229.