Lee C R, McTavish D, Sorkin E M
Adis International Limited, Auckland, New Zealand.
Drugs. 1993 Aug;46(2):313-40. doi: 10.2165/00003495-199346020-00008.
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.
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。