Capetola R J, McGuire J L, Rosenthale M E
Pharmacology. 1983;27 Suppl 1:1-13. doi: 10.1159/000137893.
A number of peripherally acting analgesics have become available in the past two decades for the treatment of mild to moderate pain of diverse etiology. The action of these agents is based on their putative ability to inhibit prostaglandin biosynthesis and attenuate hyperalgesia. Suprofen is a new and potent peripherally acting analgesic with anti-inflammatory and antipyretic properties which appears to inhibit prostaglandin synthetase in a tissue-selective manner. In preclinical studies, suprofen was shown to possess a wide separation of analgesic activity from gastrointestinal irritation. Suprofen appears to exert its pharmacological effect by inhibiting synthesis of prostaglandins from precursor arachidonic acid, inhibiting the pain induced by bradykinin, and by raising the threshold to pain induced by prostaglandins. The onset of action is rapid with peak analgesic effect reached in 1-2 h. Preclinical data suggest that suprofen may be an extremely valuable and versatile analgesic for the clinical management of pain.
在过去二十年里，已有多种外周作用性镇痛药可用于治疗各种病因引起的轻至中度疼痛。这些药物的作用基于其推测的抑制前列腺素生物合成和减轻痛觉过敏的能力。舒洛芬是一种新型强效外周作用性镇痛药，具有抗炎和解热特性，它似乎以组织选择性方式抑制前列腺素合成酶。在临床前研究中，舒洛芬显示出镇痛活性与胃肠道刺激之间有很大的分离度。舒洛芬似乎通过抑制前体花生四烯酸合成前列腺素、抑制缓激肽诱导的疼痛以及提高对前列腺素诱导疼痛的阈值来发挥其药理作用。起效迅速，1 - 2小时达到最大镇痛效果。临床前数据表明，舒洛芬可能是一种对疼痛临床管理极其有价值且用途广泛的镇痛药。
