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注射用碘美普尔在实验动物中的药效学作用。

Pharmacodynamic effects of iomeprol for injection in experimental animals.

作者信息

Cipolla P, Tirone P, Luzzani F, de Haën C

机构信息

Research and Development Division, Bracco SpA, Milan, Italy.

出版信息

Eur J Radiol. 1994 May;18 Suppl 1:S32-42. doi: 10.1016/0720-048x(94)90092-2.

Abstract

Iomeprol for injection is a new nonionic triiodinated contrast medium for diagnostic radiology, which combines low osmolality with low viscosity. The effects of iomeprol for injection on the cardiovascular system, blood parameters, renal function and the central nervous system were studied after intravascular administration to several animal species of doses at least as high as the highest presumed clinical doses. The following observations were made with respect to the central circulatory system: moderate and short-lasting increases of left ventricular end-diastolic pressure and cardiac output, no significant effects on heart rate either in vitro or in vivo, some episodes of arrhythmia and ventricular fibrillations only at doses far higher than the highest presumed clinical ones, no significant increases in diastolic and systolic coronary flow. The following observations were made with respect to peripheral circulation: no significant changes on blood pressure, moderate and short-lasting increases in renal and pulmonary arterial flow, together with a decrease in peripheral vascular resistance, no crossing of the blood-brain barrier in healthy animals. Cardiovascular and haemodynamic changes were all significantly milder than those induced by ionic contrast media (CM) and were similar to effects caused by some other nonionic contrast media. When injected into the femoral artery of rats, iomeprol was shown to be less algogenic than iopamidol and iohexol. In comparison with the same reference CM, iomeprol affected to a lesser extent the filterability of red blood cells in vitro and showed a less marked effect on their deformability. When administered intravenously at very high dosages, iomeprol had no effect on the glomerular filtration rate, but increased both renal blood flow and diuresis. Proteinuria and enzymuria were also increased, albeit more transiently. The neurotolerance of iomeprol for injection after intravenous administration was higher than or at worst equal to that of iopamidol and iohexol. Iomeprol is therefore a promising new contrast agent particularly suitable for intravascular use in humans.

摘要

注射用碘美普尔是一种用于诊断放射学的新型非离子型三碘造影剂,它兼具低渗透压和低粘度的特点。在对几种动物物种进行血管内给药、剂量至少高达最高推测临床剂量后,研究了注射用碘美普尔对心血管系统、血液参数、肾功能和中枢神经系统的影响。关于中心循环系统有以下观察结果:左心室舒张末期压力和心输出量有中度且持续时间较短的增加,体外和体内对心率均无显著影响,仅在远高于最高推测临床剂量时出现一些心律失常和心室颤动发作,舒张期和收缩期冠状动脉血流量无显著增加。关于外周循环有以下观察结果:血压无显著变化,肾和肺动脉血流量有中度且持续时间较短的增加,同时外周血管阻力降低,健康动物中未出现血脑屏障穿透现象。心血管和血流动力学变化均明显比离子型造影剂(CM)引起的变化轻微,且与其他一些非离子型造影剂产生的影响相似。当注入大鼠股动脉时,碘美普尔显示出比碘帕醇和碘海醇的致痛性更低。与相同的对照CM相比,碘美普尔在体外对红细胞过滤性的影响较小,对其变形性的影响也不太明显。以非常高的剂量静脉给药时,碘美普尔对肾小球滤过率无影响,但增加了肾血流量和尿量。蛋白尿和酶尿也有所增加,尽管更短暂。静脉给药后注射用碘美普尔的神经耐受性高于或最差等于碘帕醇和碘海醇。因此,碘美普尔是一种有前景的新型造影剂,特别适合在人体血管内使用。

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