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曲马多。对其药效学和药代动力学特性以及在急慢性疼痛状态下的治疗潜力的初步综述。

Tramadol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute and chronic pain states.

作者信息

Lee C R, McTavish D, Sorkin E M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1993 Aug;46(2):313-40. doi: 10.2165/00003495-199346020-00008.

DOI:10.2165/00003495-199346020-00008
PMID:7691519
Abstract

Tramadol is a centrally acting analgesic which possesses opioid agonist properties and activates monoaminergic spinal inhibition of pain. It may be administered orally, rectally, intravenously or intramuscularly. In patients with moderate to severe postoperative pain, intravenous or intramuscular tramadol has generally proved to be of equivalent potency to pethidine (meperidine) and one-fifth as potent as nalbuphine. Intravenous tramadol 50 to 150mg was equivalent in analgesic efficacy to morphine 5 to 15mg in patients with moderate pain following surgery; however, when administered epidurally tramadol was one-thirtieth as potent as morphine. Tramadol has demonstrated efficacy in a few studies in the short term treatment of chronic pain of various origins. Orally administered tramadol was found to be an effective analgesic in step 2 of the World Health Organization's guidelines for the treatment of patients with cancer pain. Tramadol is well tolerated in short term use with dizziness, nausea, sedation, dry mouth and sweating being the principal adverse effects. Respiratory depression has been observed in only a few patients after tramadol infusion anaesthesia. When used for pain relief during childbirth, intravenously administered tramadol did not cause respiratory depression in neonates. The tolerance and dependence potential of tramadol during treatment for up to 6 months appears to be low, although the possibility of dependence with long term use cannot be entirely excluded. Thus, evidence to date of the analgesic effectiveness of tramadol combined with a low respiratory depressant effect and low dependence potential in short term use, suggests that the drug may become a useful alternative to the opioid analgesics currently available for the treatment of patients with moderately severe acute or chronic pain.

摘要

曲马多是一种中枢性镇痛药,具有阿片类激动剂特性,并能激活单胺能对疼痛的脊髓抑制作用。它可以口服、直肠给药、静脉注射或肌肉注射。对于中度至重度术后疼痛患者,静脉注射或肌肉注射曲马多通常已证明其效力与哌替啶(度冷丁)相当,而效力仅为纳布啡的五分之一。在术后中度疼痛患者中,静脉注射50至150毫克曲马多的镇痛效果与5至15毫克吗啡相当;然而,硬膜外给药时,曲马多的效力仅为吗啡的三十分之一。曲马多在一些关于各种原因引起的慢性疼痛短期治疗的研究中已显示出疗效。在世界卫生组织癌症疼痛患者治疗指南的第2步中,口服曲马多被发现是一种有效的镇痛药。曲马多短期使用耐受性良好,主要不良反应有头晕、恶心、镇静、口干和出汗。仅在少数接受曲马多输注麻醉的患者中观察到呼吸抑制。用于分娩镇痛时,静脉注射曲马多不会导致新生儿呼吸抑制。曲马多在长达6个月的治疗期间产生耐受性和依赖性的可能性似乎较低,尽管不能完全排除长期使用产生依赖性的可能性。因此,迄今为止的证据表明,曲马多在短期使用中具有镇痛效果、低呼吸抑制作用和低依赖性可能性,这表明该药物可能成为目前用于治疗中度至重度急性或慢性疼痛患者的阿片类镇痛药的有用替代品。

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Tramadol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute and chronic pain states.曲马多。对其药效学和药代动力学特性以及在急慢性疼痛状态下的治疗潜力的初步综述。
Drugs. 1993 Aug;46(2):313-40. doi: 10.2165/00003495-199346020-00008.
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Tramadol: a new centrally acting analgesic.曲马多:一种新型中枢性镇痛药。
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[Effectiveness and tolerance of tramadol in cancer pain. A comparative study with respect to buprenorphine].曲马多治疗癌痛的有效性和耐受性。与丁丙诺啡的比较研究
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Analgesics in ophthalmic practice: a review of the oral non-narcotic agent tramadol.眼科临床中的镇痛药:口服非麻醉性药物曲马多综述
Optom Vis Sci. 1999 Jul;76(7):455-61. doi: 10.1097/00006324-199907000-00020.

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本文引用的文献

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Epidural tramadol for postoperative pain relief.硬膜外注射曲马多用于术后镇痛。
Anaesthesia. 1993 Apr;48(4):328-31. doi: 10.1111/j.1365-2044.1993.tb06955.x.
2
Complementary and synergistic antinociceptive interaction between the enantiomers of tramadol.曲马多对映体之间的互补性和协同性抗伤害感受相互作用。
J Pharmacol Exp Ther. 1993 Oct;267(1):331-40.
3
[Obstetrical analgesia with tramadol].[曲马多用于产科镇痛]
慢性肾脏病患者的阿片类药物处方:关于比较慢性肾脏病患者使用阿片类药物安全性和有效性的系统评价
Cureus. 2023 Sep 18;15(9):e45485. doi: 10.7759/cureus.45485. eCollection 2023 Sep.
4
Pain Management in Children Admitted to the Emergency Room: A Narrative Review.急诊室收治儿童的疼痛管理:一项叙述性综述
Pharmaceuticals (Basel). 2023 Aug 18;16(8):1178. doi: 10.3390/ph16081178.
5
CYP24A1 and CYP3A4 Levels, Renal, Hepatic Changes, and Incidence of Oxidative Stress in Tramadol-Alcohol Concomitant Misuse.曲马多与酒精同时滥用时CYP24A1和CYP3A4水平、肾脏和肝脏变化以及氧化应激发生率
Cureus. 2023 Mar 29;15(3):e36877. doi: 10.7759/cureus.36877. eCollection 2023 Mar.
6
A Meta-Analysis Showing the Quantitative Evidence Base of Preemptive Pregabalin for Postoperative Pain from Cancer-Related Surgery.一项荟萃分析显示了普瑞巴林预防性治疗与癌症相关手术术后疼痛的定量证据基础。
Medicina (Kaunas). 2023 Jan 31;59(2):280. doi: 10.3390/medicina59020280.
7
Current and emerging treatment options for premature ejaculation.早泄的当前和新兴治疗选择。
Nat Rev Urol. 2022 Nov;19(11):659-680. doi: 10.1038/s41585-022-00639-5. Epub 2022 Aug 25.
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Short-term mortality following tramadol poisonings in Denmark.丹麦曲马多中毒的短期死亡率。
Basic Clin Pharmacol Toxicol. 2022 Jul;131(1):83-92. doi: 10.1111/bcpt.13741. Epub 2022 May 17.
9
Investigating antimicrobial features and drug interactions of sedoanalgesics in intensive care unit: an experimental study.重症监护病房中镇静镇痛药的抗菌特性及药物相互作用研究:一项实验研究。
ADMET DMPK. 2021 Sep 6;9(3):219-226. doi: 10.5599/admet.1042. eCollection 2021.
10
The Relationship Between Postoperative Opioid Analgesia and Sleep Apnea Severity in Patients Undergoing Hip Arthroplasty: A Randomized, Controlled, Triple-Blinded Trial.髋关节置换术患者术后阿片类镇痛与睡眠呼吸暂停严重程度之间的关系:一项随机、对照、三盲试验
Nat Sci Sleep. 2022 Feb 25;14:303-310. doi: 10.2147/NSS.S348834. eCollection 2022.
Fortschr Med. 1980 Apr 24;98(16):632-4.
4
[A doubleblind comparison of tramadol and buprenorphine in the control of postoperative pain (author's transl)].曲马多与丁丙诺啡用于术后疼痛控制的双盲比较(作者译)
Anaesthesist. 1981 Dec;30(12):623-6.
5
[The clinical usefulness of Tramadol-infusion anaesthesia (author's transl)].曲马多静脉输注麻醉的临床效用(作者译)
Anaesthesist. 1981 Dec;30(12):619-22.
6
[The analgesic effectiveness of Tramal (tramadol) 100 mg for postoperative wound pain (author's transl)].曲马多100毫克对术后伤口疼痛的镇痛效果(作者译)
Schweiz Rundsch Med Prax. 1981 Mar 3;70(10):435-40.
7
[Infusion-controlled Tramal-anaesthesia (author's transl)].[输注控制的曲马多麻醉(作者译)]
Anaesthesist. 1980 Dec;29(12):673-4.
8
[Biotransformation of tramadol in man and animal (author's transl)].曲马多在人和动物体内的生物转化(作者译)
Arzneimittelforschung. 1981;31(11):1932-43.
9
[Hemodynamic and respiratory effects of tramadol during nitrous oxide-oxygen-artificial respiration and in the postoperative period].[曲马多在氧化亚氮-氧气-人工呼吸期间及术后的血流动力学和呼吸效应]
Anaesthesist. 1982 Nov;31(11):604-10.
10
[Is postoperative respiratory depression associated with tramadol infusion anesthesia?].[术后呼吸抑制与曲马多静脉输注麻醉有关吗?]
Anaesthesist. 1983 Feb;32(2):88.