新型镇痛药——盐酸他喷他朵

Tapentadol HCl:a novel analgesics

盐酸他喷他朵是一种新型的具有双重功效的中枢止痛剂,它既是μ型阿片受体激动剂同时又抑制中枢去甲肾上腺素再摄取,是迄今为止研发的第一个同时具有上述两种药理作用的单一分子药物。该药镇痛谱广,包括各种急性和慢性疼痛。对各种疼痛模型中包括神经病理性痛在内的多种大鼠疼痛模型有效,镇痛作用是吗啡的1/2～1/3。临床应用副反应轻微,耐受良好。

Tapentadol HCl is a single molecule, centrally acting oral analgesic with a dual mode of action： mu-opioid receptor agonism and norepinephrine reuptake inhibition. It exhibited analgesic effects in a wide range of animal models of acute pain and chronic neuropathic and inflammatory pain using various routes of administration （IV, IP, and P0）. The potency of tapentadol HCl was between morphine and tramadol. In clinical use, Tapentadol HCI has mild adverse events and welltolerated for the relief of moderate-to-severe pain.