Rooks W H
Scientific Information Department, Syntex Research, Palo Alto, CA 94303.
Pharmacotherapy. 1990;10(6 ( Pt 2)):30S-32S.
Ketorolac tromethamine is a highly potent member of a class of compounds having both analgesic and antiinflammatory activity. In animal pain models using underlying inflammation, ketorolac markedly inhibited the pain response and increased the pain threshold; it did not exhibit any narcotic or central nervous system depressant effects. It was also active in rat models of acute and chronic inflammation and pyresis. These activities are mediated primarily by potent prostaglandin cyclooxygenase inhibitory activity. Mild central nervous system and cardiovascular effects occurred only at doses far greater than those required for analgesic and antiinflammatory activity. Solutions of ketorolac tromethamine are not irritating. When given intramuscularly to rabbits (0.31-5% solutions), no drug-related irritation or changes in serum creatine phosphokinase were seen. The agent was not irritating when applied to the skin or eyes (less than or equal to 0.5% solutions) of animals.
酮咯酸氨丁三醇是一类兼具镇痛和抗炎活性的化合物中效力很强的一种。在利用潜在炎症的动物疼痛模型中，酮咯酸显著抑制疼痛反应并提高痛阈；它未表现出任何麻醉或中枢神经系统抑制作用。它在急性和慢性炎症及发热的大鼠模型中也有活性。这些活性主要由强大的前列腺素环氧化酶抑制活性介导。仅在远高于镇痛和抗炎活性所需剂量时才会出现轻微的中枢神经系统和心血管效应。酮咯酸氨丁三醇溶液无刺激性。给兔子肌肉注射（0.31 - 5%溶液）时，未观察到与药物相关的刺激或血清肌酸磷酸激酶变化。将该制剂应用于动物皮肤或眼睛（≤0.5%溶液）时无刺激性。
