Mattia C, Coluzzi F
Department of Anaesthesiology, Intensive Care Medicine and Pain Therapy, University of Rome La Sapienza, Viale del Policlinico 155, 00198 Rome, Italy.
Minerva Anestesiol. 2005 Oct;71(10):565-84.
In the light of the most recent acquisitions published in the international literature, this review analyzes the pharmacologic features and modes of use of tramadol, one of the most widely used, on a worldwide scale, analgesic agents in acute and chronic pain of moderate to severe intensity. The action of the 2 enantiomers of tramadol--which exert different pharmacologic effects--and of metabolite M1, is differentiated. The global activity of tramadol results from the sum of their specific actions. Data of kinetics show a very high oral bioavailability and the sustained-release (SR) formulations assure a 24-h coverage through the constant blood levels. Data reported in the relevant literature show that tramadol is effective in the treatment of arthrosic and neuropathic pain, with a value of Number Needed to Treat (NNT) of 3.4, and in the mixed nociceptive-neuropathic pain, especially in persistent or chronic pain. Moreover, tramadol maintains a good tolerability profile in the elderly subjects and a good analgesic efficacy in the long-term treatments with reduced pharmacological interactions and a low incidence of constipation. These global features assured its inclusion into the most recent guidelines on the management of chronic pain. Furthermore, data from literature showed that tramadol is devoid of immunosuppressive activity, has a poor tendency to tolerance and a minimum risk of addiction and abuse.
根据国际文献中最近发表的研究成果，本综述分析了曲马多的药理学特性和使用方式。曲马多是全球范围内治疗中重度急慢性疼痛最常用的镇痛药之一。曲马多的两种对映体发挥不同的药理作用，其代谢物M1的作用也有所不同。曲马多的整体活性是其特定作用之和。动力学数据显示其口服生物利用度非常高，缓释（SR）制剂可通过恒定的血药浓度确保24小时的覆盖。相关文献报道的数据表明，曲马多在治疗关节疼痛和神经性疼痛方面有效，治疗所需人数（NNT）为3.4，在混合性伤害性-神经性疼痛中，尤其是持续性或慢性疼痛中也有效。此外，曲马多在老年患者中耐受性良好，在长期治疗中镇痛效果良好，药物相互作用减少，便秘发生率低。这些整体特性确保其被纳入最新的慢性疼痛管理指南。此外，文献数据表明，曲马多没有免疫抑制活性，耐受性倾向低，成瘾和滥用风险最小。
