VanWagoner M, O'Toole M, Worah D, Leese P T, Quay S C
Salutar, Inc., Sunnyvale, California 94086.
Invest Radiol. 1991 Nov;26(11):980-6. doi: 10.1097/00004424-199111000-00010.
Twenty adult male volunteers were studied in an unblinded, ascending-dose study to evaluate the safety, tolerance, and pharmacokinetics of intravenously administered nonionic gadodiamide injection. Dosages administered were 0.05, 0.1, 0.2, and 0.3 mmol/kg. Subjects were monitored from 36 hours before, through 72 hours after administration. There were no clinically relevant changes in vital signs or electrocardiograms. No clinically significant changes occurred in blood or urine laboratory parameters, although a tendency for minor, transient elevations in serum iron levels 8 to 48 hours after administration was noted. These changes were not dose-related. Nine of 20 subjects reported at least one adverse event; all events were transient and of mild intensity, the most common being dizziness/lightheadedness and perversion of taste or smell. One subject reported discomfort consisting of mild stinging at the injection site during administration. Gadodiamide was excreted unmetabolized in the urine with greater than 95% recovery at 72 hours after administration. The serum elimination half-life was approximately 70 minutes.
对20名成年男性志愿者进行了一项非盲法、剂量递增研究，以评估静脉注射非离子型钆双胺注射液的安全性、耐受性和药代动力学。给药剂量分别为0.05、0.1、0.2和0.3 mmol/kg。在给药前36小时至给药后72小时对受试者进行监测。生命体征或心电图未出现临床相关变化。血液或尿液实验室参数未发生临床显著变化，不过在给药后8至48小时观察到血清铁水平有轻微、短暂升高的趋势。这些变化与剂量无关。20名受试者中有9人报告了至少一项不良事件；所有事件均为短暂性且强度较轻，最常见的是头晕/头轻脚重以及味觉或嗅觉异常。一名受试者报告在给药期间注射部位有轻度刺痛的不适感。钆双胺以未代谢形式经尿液排泄，给药后72小时回收率超过95%。血清消除半衰期约为70分钟。
