Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM'S NMIMS, V.L. Mehta Road, Vile Parle West, Mumbai, 400056, India.
Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM'S NMIMS, V.L. Mehta Road, Vile Parle West, Mumbai, 400056, India.
Biomed Pharmacother. 2019 Mar;111:443-451. doi: 10.1016/j.biopha.2018.12.085. Epub 2018 Dec 27.
Patients with chronic non-malignant pain report impairment of physical and social life along with psychological state affecting their overall quality of life. The purpose of managing pain is to reduce the trauma and improve the patient comfort with better quality of life. Tramadol is a centrally acting weak μ-opioid receptor analgesic and is a racemic mixture of (+)-tramadol and (-)-tramadol enantiomers. Tramadol is used worldwide and is listed in many medical guidelines for pain management. The (+)-tramadol has greater affinity for μ-opioid receptor and provides additional prevention of 5- hydroxy tryptamine reuptake, while the (-)-tramadol is a successful noradrenaline reuptake inhibitor and intensifies its release by activating the auto receptor. Tramadol is prescribed to relieve moderate to severe pain management in patients. Tramadol does not show much serious adverse effects without any dependency potential in therapeutic doses as seen in other opioids, like morphine. Tramadol metabolite M1 also has μ-opioid receptor agonist activity, but it faces poor blood brain barrier permeability. In this review, we report the complete updated status of Tramadol along with its chemistry, synthesis, pharmacology, medicinal uses, adverse effects and its combinations available in the market. We have also covered Tramadol patents so that a complete overview provides a broader perspective for future designing of its derivatives and increase their potential use for pain management in terminal cancer patients.
慢性非恶性疼痛患者报告身体和社会生活受损，以及影响整体生活质量的心理状态。管理疼痛的目的是减轻创伤，提高患者舒适度，提高生活质量。曲马多是一种中枢作用的弱μ-阿片受体镇痛药，是（+）-曲马多和（-）-曲马多对映异构体的外消旋混合物。曲马多在世界范围内使用，并被列入许多医学指南用于疼痛管理。（+）-曲马多对μ-阿片受体具有更高的亲和力，并提供额外的 5-羟色胺再摄取预防，而（-）-曲马多是一种成功的去甲肾上腺素再摄取抑制剂，并通过激活自动受体来增强其释放。曲马多被开处方用于缓解中重度疼痛管理患者。曲马多在治疗剂量下没有表现出像吗啡等其他阿片类药物那样的严重不良反应和潜在的依赖性。曲马多代谢物 M1 也具有μ-阿片受体激动剂活性，但它的血脑屏障通透性较差。在这篇综述中，我们报告了曲马多的完整更新状态，包括其化学、合成、药理学、药用用途、不良反应以及市场上的组合。我们还涵盖了曲马多的专利，以便全面概述为其衍生物的未来设计提供更广阔的视角，并增加它们在晚期癌症患者疼痛管理中的潜在用途。
