Romagnoli A, Keats A S
Int J Clin Pharmacol Res. 1986;6(6):451-5.
Ciramadol, an agonist-antagonist analgesic of lesser milligram potency than morphine, given intravenously at 30 mg/70 kg produced respiratory depression equivalent to that observed with morphine 10 mg/70 kg. Respiratory depression was measured in terms of drug induced displacement of the carbon dioxide response curve of healthy volunteers. In contrast to the progressive respiratory depression by each 10 mg/70 kg increment of morphine, further doses of ciramadol up to 90 mg/70 kg failed to increase respiratory depression. The ceiling of respiratory depression by ciramadol was half the ceiling previously demonstrated for nalbuphine and dezocine. Ceiling respiratory depression may be a general characteristic of agonist-antagonist type analgesics in contrast to pure agonist analgesics.
环拉马朵是一种激动 - 拮抗型镇痛药，其毫克效价比吗啡低，静脉注射30mg/70kg时产生的呼吸抑制与10mg/70kg吗啡所观察到的相当。呼吸抑制是根据药物引起的健康志愿者二氧化碳反应曲线的位移来测量的。与吗啡每增加10mg/70kg导致的渐进性呼吸抑制不同，进一步增加环拉马朵剂量至90mg/70kg并未增加呼吸抑制。环拉马朵呼吸抑制的上限是先前纳布啡和地佐辛所显示上限的一半。与纯激动型镇痛药相比，呼吸抑制上限可能是激动 - 拮抗型镇痛药的一个普遍特征。
