Glauser F L, Powers D, Fischer P, Egan P, Smeltzer D, Lewis J, Smith W R, Morton M
Am Rev Respir Dis. 1977 Jan;115(1):83-8. doi: 10.1164/arrd.1977.115.1.83.
Noncardiogenic pulmonary edema has been reported to follow the intravenous use of ethchlorvynol (Placidyl) in both human clinical and animal experimental situations. In a further attempt to define ethchlorvynol-pulmonary tissue inter-relations, we measured ethchlorvynol concentrations in venous and arterial blood and lung and liver tissue of dogs after intravenous injection of 15 to 25 mg of the drug per kg of body weight. In 10 dogs, the mean +/- SEM lung concentrations 1, 3, and 5 min after injection were 70 +/- 20, 50 +/- 13, and 24 +/- 9 mug per g of tissue, respectively. Simultaneous mean +/- SEM venous contrations were 75 +/- 40, 29+/-5, and 22 +/- 5 mug per ml of blood, respectively. During minutes 1 and 3, the liver concentrations were lower than those found in the lung. In an additional 3 dogs, injection of ethchlorvynol into the portal vein led to higher concentrations (at all sample times) in the liver when compared to the lung. In vitro lung slice studies using ethchlorvynol labeled with iodine-131 revealed no active energy-dependent uptake. Intravenously administered ethchlorvynol rapidly fluxes into and out of lung tissue, apparently following the laws of diffusion.
据报道,在人类临床和动物实验中,静脉使用乙炔氯戊烯醇(安宁)后会出现非心源性肺水肿。为了进一步明确乙炔氯戊烯醇与肺组织的相互关系,我们在每千克体重静脉注射15至25毫克该药物后,测量了犬的静脉血、动脉血以及肺和肝组织中的乙炔氯戊烯醇浓度。在10只犬中,注射后1、3和5分钟时,肺组织中药物浓度的平均值±标准误分别为每克组织70±20、50±13和24±9微克。同时,静脉血中药物浓度的平均值±标准误分别为每毫升血液75±40、29±5和22±5微克。在第1和第3分钟时,肝脏中的药物浓度低于肺中的浓度。在另外3只犬中,将乙炔氯戊烯醇注入门静脉后,与肺相比,肝脏中的药物浓度(在所有采样时间)更高。使用碘-131标记的乙炔氯戊烯醇进行的体外肺切片研究显示,不存在依赖能量的主动摄取。静脉注射的乙炔氯戊烯醇显然遵循扩散规律,能迅速进出肺组织。