单次静脉注射丙帕他莫后对乙酰氨基酚的血浆和脑脊液浓度。
Plasma and cerebrospinal fluid concentrations of paracetamol after a single intravenous dose of propacetamol.
作者信息
Bannwarth B, Netter P, Lapicque F, Gillet P, Péré P, Boccard E, Royer R J, Gaucher A
机构信息
URA CNRS 1288, Faculté de Médecine de Nancy, France.
出版信息
Br J Clin Pharmacol. 1992 Jul;34(1):79-81. doi: 10.1111/j.1365-2125.1992.tb04112.x.
Abstract
Since the antipyretic and probably the analgesic effects of paracetamol are, at least in part, centrally mediated, its plasma and cerebrospinal fluid (CSF) concentrations were measured in 43 patients with nerve-root compression pain. Each subject was given a short i.v. infusion of 2 g propacetamol, a prodrug which is hydrolysed to paracetamol within 7 min. Single blood and CSF samples were drawn concomitantly in each patient at intervals between 20 min and 12 h. Maximum CSF drug concentrations were observed at the 4th hour, subsequent concentrations exceeding those in plasma. The elimination half-life of paracetamol calculated from pooled data was shorter in plasma (2.4 h) than in CSF (3.2 h). The time-course of paracetamol in CSF may parallel that of analgesic effect.
摘要
由于对乙酰氨基酚的退热作用以及可能的镇痛作用至少部分是由中枢介导的，因此对43例神经根压迫性疼痛患者测量了其血浆和脑脊液（CSF）浓度。每位受试者接受了2g丙帕他莫的短时间静脉输注，丙帕他莫是一种前体药物，在7分钟内可水解为对乙酰氨基酚。在每位患者中，于20分钟至12小时的间隔时间内同时采集单次血液和脑脊液样本。在第4小时观察到脑脊液药物浓度最高，随后的浓度超过血浆浓度。根据汇总数据计算得出，对乙酰氨基酚在血浆中的消除半衰期（2.4小时）短于在脑脊液中的消除半衰期（3.2小时）。脑脊液中对乙酰氨基酚的时间进程可能与镇痛作用的时间进程平行。
相似文献
1
Plasma and cerebrospinal fluid concentrations of paracetamol after a single intravenous dose of propacetamol.单次静脉注射丙帕他莫后对乙酰氨基酚的血浆和脑脊液浓度。
Br J Clin Pharmacol. 1992 Jul;34(1):79-81. doi: 10.1111/j.1365-2125.1992.tb04112.x.
2
Cerebrospinal fluid pharmacokinetics of paracetamol after intravenous propacetamol in a former preterm infant.一名前早产儿静脉注射丙帕他莫后对乙酰氨基酚的脑脊液药代动力学
Br J Clin Pharmacol. 2004 Feb;57(2):224-5. doi: 10.1046/j.1365-2125.2003.01990.x.
3
Bioequivalence study comparing a new paracetamol solution for injection and propacetamol after single intravenous infusion in healthy subjects.在健康受试者单次静脉输注后，比较一种新的注射用扑热息痛溶液和丙帕他莫的生物等效性研究。
Int J Clin Pharmacol Ther. 2004 Jan;42(1):50-7. doi: 10.5414/cpp42050.
4
Pharmacokinetics and analgesic effects of intravenous propacetamol vs rectal paracetamol in children after major craniofacial surgery.小儿重大颅面外科手术后静脉注射丙帕他莫与直肠给予对乙酰氨基酚的药代动力学及镇痛效果比较
Paediatr Anaesth. 2008 Jul;18(7):582-92. doi: 10.1111/j.1460-9592.2008.02619.x. Epub 2008 May 8.
5
Tolerance and pharmacokinetics of propacetamol, a paracetamol formulation for intravenous use.
Fundam Clin Pharmacol. 1992;6(6):259-62. doi: 10.1111/j.1472-8206.1992.tb00119.x.
6
Intravenous acetaminophen (paracetamol): comparable analgesic efficacy, but better local safety than its prodrug, propacetamol, for postoperative pain after third molar surgery.静脉注射对乙酰氨基酚（扑热息痛）：在第三磨牙手术后的术后疼痛治疗中，其镇痛效果相当，但局部安全性优于其前体药物丙帕他莫。
Anesth Analg. 2005 Jul;101(1):90-6, table of contents. doi: 10.1213/01.ANE.0000155297.47955.D6.
7
Pharmacokinetics of single dose intravenous propacetamol in neonates: effect of gestational age.新生儿单剂量静脉注射丙帕他莫的药代动力学：胎龄的影响
Arch Dis Child Fetal Neonatal Ed. 2004 Jan;89(1):F25-8. doi: 10.1136/fn.89.1.f25.
8
Pharmacokinetics of paracetamol in the neonate and infant after administration of propacetamol chlorhydrate.
Dev Pharmacol Ther. 1993;20(3-4):129-34. doi: 10.1159/000457553.
9
Tolerance and analgesic efficacy of a new i.v. paracetamol solution in children after inguinal hernia repair.一种新型静脉注射用扑热息痛溶液在儿童腹股沟疝修补术后的耐受性及镇痛效果
Paediatr Anaesth. 2005 Aug;15(8):663-70. doi: 10.1111/j.1460-9592.2004.01518.x.
10
Safety and pharmacokinetics of paracetamol following intravenous administration of 5 g during the first 24 h with a 2-g starting dose.在最初24小时内以2克起始剂量静脉注射5克对乙酰氨基酚后的安全性和药代动力学。
Clin Pharmacol Ther. 2007 Mar;81(3):401-5. doi: 10.1038/sj.clpt.6100064.
引用本文的文献
1
Highly prevalent geriatric medications and their effect on β-amyloid fibril formation.高患病率的老年医学药物及其对β-淀粉样纤维形成的影响。
BMC Neurol. 2024 Nov 14;24(1):445. doi: 10.1186/s12883-024-03930-7.
2
Evaluation of the mechanism of action of paracetamol, drotaverine, and peppermint oil and their effects in combination with hyoscine butylbromide on colonic motility: human study.对乙酰氨基酚、屈他维林和薄荷油的作用机制及其与丁溴东莨菪碱联合使用对结肠动力的影响评估：人体研究。
Front Pharmacol. 2024 Jul 10;15:1384070. doi: 10.3389/fphar.2024.1384070. eCollection 2024.
3
Synergistic Antinociceptive Effect of β-Caryophyllene Oxide in Combination with Paracetamol, and the Corresponding Gastroprotective Activity.氧化β-石竹烯与对乙酰氨基酚联合使用的协同镇痛作用及相应的胃保护活性。
Biomedicines. 2024 May 8;12(5):1037. doi: 10.3390/biomedicines12051037.
4
Multi-omics approach reveals dysregulated genes during hESCs neuronal differentiation exposure to paracetamol.多组学方法揭示了人胚胎干细胞在神经元分化过程中暴露于对乙酰氨基酚时的基因失调情况。
iScience. 2023 Aug 28;26(10):107755. doi: 10.1016/j.isci.2023.107755. eCollection 2023 Oct 20.
5
Acetaminophen: A hazard to immunotherapy.对乙酰氨基酚：免疫疗法的一种危害。
Ann Med Surg (Lond). 2022 Jul 31;80:104272. doi: 10.1016/j.amsu.2022.104272. eCollection 2022 Aug.
6
Optimal Timing of Intravenous Acetaminophen Administration for Postoperative Analgesia.静脉注射对乙酰氨基酚用于术后镇痛的最佳时机。
Anesth Prog. 2022 Jun 1;69(2):3-10. doi: 10.2344/anpr-69-02-05.
7
Modulation of Glycinergic Neurotransmission may Contribute to the Analgesic Effects of Propacetamol.甘氨酸能神经传递的调制可能有助于丙帕他莫的镇痛作用。
Biomolecules. 2021 Mar 25;11(4):493. doi: 10.3390/biom11040493.
8
Analgesic Effect of Acetaminophen: A Review of Known and Novel Mechanisms of Action.对乙酰氨基酚的镇痛作用：已知及新作用机制综述
Front Pharmacol. 2020 Nov 30;11:580289. doi: 10.3389/fphar.2020.580289. eCollection 2020.
9
Comparing the effects of ketorolac and Paracetamol on postoperative pain relief after coronary artery bypass graft surgery. A randomized clinical trial.比较酮咯酸和对乙酰氨基酚对冠状动脉搭桥手术后疼痛缓解的效果。一项随机临床试验。
J Cardiothorac Surg. 2020 May 11;15(1):80. doi: 10.1186/s13019-020-01125-y.
10
Development of a physiologically-based pharmacokinetic pediatric brain model for prediction of cerebrospinal fluid drug concentrations and the influence of meningitis.开发一种基于生理学的儿童脑药代动力学模型，用于预测脑脊液中的药物浓度以及脑膜炎的影响。
PLoS Comput Biol. 2019 Jun 13;15(6):e1007117. doi: 10.1371/journal.pcbi.1007117. eCollection 2019 Jun.
本文引用的文献
1
SITE OF ACTION OF NARCOTIC AND NON-NARCOTIC ANALGESICS DETERMINED BY BLOCKING BRADYKININ-EVOKED VISCERAL PAIN.通过阻断缓激肽诱发的内脏疼痛来确定麻醉性和非麻醉性镇痛药的作用部位。
Arch Int Pharmacodyn Ther. 1964 Nov 1;152:25-58.
2
Acetaminophen as an internal standard for calibrating in vivo electrochemical electrodes.对乙酰氨基酚作为用于校准体内电化学电极的内标物。
J Pharmacol Exp Ther. 1981 Oct;219(1):49-53.
3
A rapid quantitative determination of acetaminophen in plasma.血浆中对乙酰氨基酚的快速定量测定。
J Pharm Sci. 1982 Nov;71(11):1291-4. doi: 10.1002/jps.2600711128.
4
Pharmacokinetics of parenteral paracetamol and its analgesic effects in post-operative dental pain.
Eur J Clin Pharmacol. 1981;20(3):215-8. doi: 10.1007/BF00544600.
5
Inhibitory actions of desacetylation products of phenacetin and paracetamol on prostaglandin synthetases in neuronal and glial cell lines and rat renal medulla.非那西丁和对乙酰氨基酚去乙酰化产物对神经元和神经胶质细胞系以及大鼠肾髓质中前列腺素合成酶的抑制作用。
Life Sci. 1982 May 24;30(21):1783-91. doi: 10.1016/0024-3205(82)90314-9.
6
High-performance liquid chromatographic method for the determination of trace amounts of acetaminophen in plasma.用于测定血浆中痕量对乙酰氨基酚的高效液相色谱法。
J Pharm Sci. 1984 Jan;73(1):117-9. doi: 10.1002/jps.2600730132.
7
Inhibition of prostaglandin synthetase in brain explains the anti-pyretic activity of paracetamol (4-acetamidophenol).大脑中前列腺素合成酶的抑制作用解释了对乙酰氨基酚（4-乙酰氨基酚）的解热活性。
Nature. 1972 Dec 15;240(5381):410-1. doi: 10.1038/240410a0.
8
In vivo electrochemical recording of acetaminophen in non human primate brain.非人灵长类动物大脑中对乙酰氨基酚的体内电化学记录。
Life Sci. 1987 Jan 26;40(4):375-9. doi: 10.1016/0024-3205(87)90139-1.
9
High performance liquid chromatographic determination of paracetamol in human serum.高效液相色谱法测定人血清中的对乙酰氨基酚
Ann Biol Clin (Paris). 1986;44(2):139-41.
10
Central analgesic effect of paracetamol manifested by depression of nociceptive activity in thalamic neurones of the rat.对乙酰氨基酚的中枢镇痛作用表现为大鼠丘脑神经元伤害性活动的抑制。
Neurosci Lett. 1987 Jun 26;77(3):339-43. doi: 10.1016/0304-3940(87)90524-6.
Zotero 插件