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安乃近代谢物的唾液水平、生物利用度与镇痛效果之间的关系。

Relationship between saliva levels of metamizol metabolites, bioavailability and analgesic efficacy.

作者信息

Rohdewald P, Drehsen G, Milsmann E, Derendorf H

出版信息

Arzneimittelforschung. 1983;33(7):985-8.

PMID:6684934
Abstract

Salivary levels of the metabolites of metamizol (N-methyl-, N-acetyl- and 4-aminoantipyrine) were determined after the intake of film-coated metamizol (Novalgin) tablets and metamizol (Novalgin) solution. Cortical evoked potentials, pain ratings and thresholds of sensation were monitored following tooth pulp stimulation after administration of metamizol tablets. Within the different groups of subjects a remarkable degree of reproducibility was obtained for the metabolite concentrations in saliva. At 20 min after drug intake a more rapid absorption was demonstrable for the solution in comparison to the tablets. The metabolite levels were correlated to the simultaneously recorded pain response demonstrating that the analgesic efficacy can only be attributed to the two metabolites N-methyl- and -4-amino-antipyrine.

摘要

在摄入薄膜包衣的安乃近(诺瓦经)片和安乃近(诺瓦经)溶液后,测定了安乃近(N-甲基-、N-乙酰-和4-氨基安替比林)代谢物的唾液水平。在服用安乃近片后,对牙髓进行刺激,监测皮质诱发电位、疼痛评分和感觉阈值。在不同组的受试者中,唾液中代谢物浓度具有显著程度的可重复性。服药后20分钟,与片剂相比,溶液的吸收更快。代谢物水平与同时记录的疼痛反应相关,表明镇痛效果仅归因于两种代谢物N-甲基-和-4-氨基-安替比林。

相似文献

1
Relationship between saliva levels of metamizol metabolites, bioavailability and analgesic efficacy.安乃近代谢物的唾液水平、生物利用度与镇痛效果之间的关系。
Arzneimittelforschung. 1983;33(7):985-8.
2
[Dose-dependence of the analgesic action of metamizol].
Anaesthesist. 1988 Mar;37(3):150-5.
3
Dose-dependent pharmacokinetics of metabolites of dipyrone in saliva.安乃近代谢产物在唾液中的剂量依赖性药代动力学。
Eur J Drug Metab Pharmacokinet. 1988 Apr-Jun;13(2):105-11. doi: 10.1007/BF03191311.
4
The effects of analgesics on pain-related somatosensory evoked potentials.镇痛药对疼痛相关体感诱发电位的影响。
Agents Actions Suppl. 1986;19:75-88.
5
[Metamizol--a new effective analgesic with a long history. Overview of its pharmacology and clinical use].[安乃近——一种历史悠久的新型有效镇痛药。其药理学与临床应用概述]
Cas Lek Cesk. 2000 Jul 19;139(14):440-4.
6
[Metamizol--acute overdose with suicidal intent].[安乃近——有自杀意图的急性过量服用]
Dtsch Med Wochenschr. 1983 Nov 18;108(46):1761-4. doi: 10.1055/s-2008-1069822.
7
Pharmacokinetics of metamizol metabolites.安乃近代谢物的药代动力学。
Agents Actions Suppl. 1986;19:199-204.
8
Surfactant influence on disintegration time and other characteristics of propyphenazone-metamizol tablets.表面活性剂对安乃近-保泰松片崩解时间及其他特性的影响
Acta Pharm Hung. 1988 Jul;58(4):153-7.
9
Pharmacokinetics of metamizol metabolites in healthy subjects after a single oral dose of metamizol sodium.单次口服安乃近钠后,健康受试者体内安乃近代谢物的药代动力学。
Eur J Clin Pharmacol. 1990;38(1):61-5. doi: 10.1007/BF00314805.
10
[Elimination of caffeine and metamizol in in vivo characterization of cytochrome P-450 dependent biotransformation reactions in aged humans].
Pharmazie. 1985 Nov;40(11):787-90.

引用本文的文献

1
Dose evaluation of intravenous metamizole (dipyrone) in infants and children: a prospective population pharmacokinetic study.静脉注射甲灭酸(安痛定)在婴儿和儿童中的剂量评估:一项前瞻性群体药代动力学研究。
Eur J Clin Pharmacol. 2019 Nov;75(11):1491-1502. doi: 10.1007/s00228-019-02720-2. Epub 2019 Aug 7.
2
Novel bioactive metabolites of dipyrone (metamizol).新型吡罗昔康(灭痛定)生物活性代谢产物。
Bioorg Med Chem. 2012 Jan 1;20(1):101-7. doi: 10.1016/j.bmc.2011.11.028. Epub 2011 Nov 25.
3
Clinical pharmacokinetics of dipyrone and its metabolites.
安乃近及其代谢产物的临床药代动力学。
Clin Pharmacokinet. 1995 Mar;28(3):216-34. doi: 10.2165/00003088-199528030-00004.
4
Pyrazolone derivatives.吡唑啉酮衍生物
Drugs. 1986;32 Suppl 4:60-70. doi: 10.2165/00003495-198600324-00006.
5
Dose-dependent pharmacokinetics of metabolites of dipyrone in saliva.安乃近代谢产物在唾液中的剂量依赖性药代动力学。
Eur J Drug Metab Pharmacokinet. 1988 Apr-Jun;13(2):105-11. doi: 10.1007/BF03191311.
6
Effect of age on the pharmacokinetics of dipyrone.年龄对安乃近药代动力学的影响。
Eur J Clin Pharmacol. 1989;36(5):513-6. doi: 10.1007/BF00558078.
7
Effects of pentazocine and acetylsalicylic acid on pain-rating, pain-related evoked potentials and vigilance in relationship to pharmacokinetic parameters.
Agents Actions. 1990 Mar;29(3-4):342-59. doi: 10.1007/BF01966467.