钆喷酸葡胺注射液不良反应的文献分析

目的分析钆喷酸葡胺注射液发生不良反应特点及相关因素,为临床合理用药提供参考。方法对万方数据库2002～2012年发表的文献进行检索,对涉及钆喷酸葡胺注射液不良反应病例的信息进行分类统计分析。结果发生不良反应的男女比例为1：1．2,多数不良反应发生在用药后30min内。非过敏反应有59例（44％）;轻度过敏性反应有47例（35％）;中度过敏性反应10例（8％）;重度过敏性反应18例（13％）,其中死亡有6例（4％）。结论虽然钆喷酸葡胺注射液不良反应发生率较低,但仍可引起严重的过敏反应,甚至休克死亡,由于其使用多在缺少临床医护监护的影像诊断科,所以更应加强其监测。     

钆喷酸葡胺致不良反应误吸二例

目的探讨钆喷酸葡胺在头部伽玛刀放疗患者行磁共振增强定位时的不良反应和安全性。方法报道2例钆喷酸葡胺不良反应致误吸及抢救经过。结果钆喷酸葡胺存在不良反应,在某种特殊情况下,会导致误吸。结论钆喷酸葡胺的不良反应发生率虽低,但其在头部伽玛刀放疗患者行磁共振增强定位时有误吸现象发生,应引起足够的重视,且应做好用药前的告知、预防误吸训练及用药中的急救准备工作。     

我院钆喷酸葡胺对比剂致8例不良反应分析

目的:促进临床合理使用钆喷酸葡胺对比剂。方法:观察我院3657例按0.2～0.4mL·kg-1剂量静脉注射钆喷酸葡胺注射液后不良反应的发生情况。结果:3657例中共有8例发生不良反应,不良反应发生率为0.218%,其中轻度过敏反应5例、中度过敏反应1例、非过敏反应2例,未见重度过敏反应和死亡病例。结论:钆喷酸葡胺作为静脉注射磁共振成像对比剂,不良反应发生率低,临床应用比较安全,但也应引起重视,细心观察,及时处理。     

钆喷酸葡胺脂质体在小鼠体内的分布与药代动力学

目的研究钆喷酸葡胺脂质体在小鼠体内的分布与药代动力学。方法应用ICP发射光谱分析法定量测定了钆喷酸葡胺及其脂质体在小鼠心、肝、脾、肺、肾及血中的钆浓度。结果钆喷酸葡胺及其脂质体在小鼠体内的血药时程变化符合二室模型。钆喷酸葡胺脂质体保持了相对较高的血药浓度 ,并且在肝脾中的分布明显增加。结论钆喷酸葡胺脂质体具有肝脾靶向性     

钆喷酸葡胺对比剂行冠状动脉CTA诊断及临床安全性分析

目的：对钆喷酸葡胺对比剂代替碘对比剂行美国GE 64排128层螺旋冠状动脉CT血管造影（CTA）的临床安全性及得到影像诊断图像的效果进行分析。方法选取2013年10月至2014年3月在该院就诊的40例临床高度怀疑冠状动脉粥样硬化性心脏病（冠心病）患者,同时对碘剂过敏,伴甲状腺功能亢进、糖尿病、基础肾功能不全等,均运用钆喷酸葡胺行冠状动脉CTA检查,观察钆喷酸葡胺对比剂的不良反应,并由5位专家对冠状动脉主干、分支进行分析并作出诊断。结果各患者冠状动脉显像都非常清晰,CT值测量准确,由5位专家分别对冠状动脉狭窄程度进行判断,均可达到诊断目的。40例患者运用钆喷酸葡胺剂量为44.1～60.0 mL,平均（48.0±9.7）mL。钆喷酸葡胺按0．6 mL/kg给药,40例患者均未发生过敏反应。结论对碘对比剂有严重反应的患者,用钆喷酸葡胺作对比剂代替行GE 64排128层螺旋冠状动脉CTA非常安全,得到图像效果基本可以达到诊断目的。     

钆喷酸葡胺对比剂的临床安全性分析

目的 探讨钆喷酸葡胺对比剂的不良反应,以利其安全使用.方法 对医院1500例静脉注射钆喷酸葡胺对比剂发生不良反应的病例进行分类分析,观察不良反应发生及处置过程.结果 发生钆喷酸葡胺不良反应12例,不良反应发生率为0.80%;其中轻度不良反应11例,重度不良反应1例.结论 静脉注射钆喷酸葡胺对比剂的不良反应发生率低,但严重不良反应一旦发生可危急生命,应引起临床重视.     

189例磁共振对比剂钆喷酸普胺致不良反应病例的文献分析

目的:分析磁共振对比剂钆喷酸葡胺所致不良反应的特点,为钆喷酸葡胺的安全使用提供参考。方法:利用"中国知网"数据库,以"钆喷酸葡胺""不良反应"为关键词,搜索2000年—2014年发表的有关钆喷酸葡胺致不良反应的文献报道,分析其不良反应的特点。结果:钆喷酸葡胺致不良反应病例189例,发生非过敏反应病例为39例(20.64%)、轻度过敏反应病例为100例(52.91%)、中度过敏反应病例为30例(15.87%)和重度过敏性反应病例为20例(10.58%),其中死亡病例为6例(3.17%)。结论:钆喷酸葡胺存在严重过敏反应以及致病亡的风险,应及早做好使用前不良反应的预案及提高医技科室应急抢救能力是至关重要的。     

钆喷酸葡胺致罕见不良反应脑病1例及文献复习

<正>钆喷酸葡胺(gadopentetate dimeglumine)是一种广泛运用于磁共振成像(MRI)的造影剂。无机钆盐是有毒的,可产生急性抗凝血作用,也会造成患者嗜睡和呼吸抑制,但是有机钆螯合物在临床上用于核磁共振增强扫描,其所造成的不良反应及其并发症很少。由于螯合的保护作用,静脉内注射钆喷酸葡胺造影剂所产生的毒性比无机钆盐低20倍。但国内仍有钆喷酸葡胺引起不良反应甚至患者死亡的报道~([1])。笔者在临床工作中遇到1例由钆喷酸葡胺引起脑病的罕见不良反应的病例,     

钆喷酸葡胺注射液380例临床观察

钆喷酸葡胺注射液主要成分为钆喷酸二葡甲胺,其化学名称为:二氯[N,N-双][2-{双(羟甲基)氨基}乙基]甘氨醉酰基(5-)钆酸(2-)复合1-脱氧-1(甲氨基) -D-葡葡糖醇(1:2),是目前临床MRI检查所使用的顺磁性造影剂。顺磁性离子钆(Gd 3)具有很强的     

磁共振成像前列腺动态增强扫描中钆双胺与钆喷酸葡胺的应用效果对比分析

目的研究分析钆双胺与钆喷酸葡胺在磁共振成像前列腺动态增强扫描中的应用效果。方法选取2012年10月至2014年10月在我院确诊收治的84例前列腺疾病患者作为研究对象,将所有患者随机分为对照组和观察组各42例,对照组患者给予钆喷酸葡胺增强扫描,观察组患者给予钆双胺增强扫描,观察两组患者的扫描效果和安全性。结果两组患者的动态强化效果和不良反应发生率相比,差异无统计学意义(P>0.05)。结论双胺与钆喷酸葡胺在磁共振成像前列腺动态增强扫描中均具有显著的增强效果,能够有效减少不良反应,安全可靠,值得临床大力推广。     

钆喷酸葡胺注射液致尿失禁1例

1病例资料患者,女,58岁,两年前病理切片检查怀疑"鼻咽癌",2012年6月10日来我院核磁共振室行MRI检查。既往患有"高血压",目前服用阿司匹林肠溶胶囊(商品名:伯基)0.1 g qd,苯磺酸氨氯地平片(商品名:络活喜)2.5 mg qd,血压控制在120~130/70~75 mmHg。否认药物及其他过     

Pharmacokinetics after discontinuous intravenous administration of azlocillin

In severe, sometimes life-threatening infections azlocillin (Securopen) is administered in single doses up to 10 g in order to increase therapeutic efficacy. Therefore the serum concentrations and urinary excretion of azlocillin were investigated in 2 healthy volunteers and in 11 patients after intravenous injection (5 min) of 2 g followed by intravenous infusion of 2 g/h over 4 h. The serum concentrations increased during infusion in patients up to a median concentration of 317 mg/l. The median serum concentrations decreased down to 94 mg/l at 2 h, 43 mg/l at 4 h and 11 mg/l at 6 h after the end of infusion. 24-h urinary excretion in patients was 54.3%. Serum half-life from the last five serum concentrations (6-10 hours after start of administration) calculated amounts to a median half life of 100 min (range 60-180 min). The study showed, that using this dose and kind of administration high serum concentrations can be maintained over many hours, sufficiently high also for life threatening and difficult-to-treat infections, if administered at intervals of 12 hours.     

Activated charcoal and the absorption of ferrous sulfate in rats

The treatment of iron poisoning has typically not included the administration of activated charcoal due to the lack of evidence supporting its efficacy. Several in vitro studies have demonstrated good adsorption of iron in a variety of pH ranges that were comparable to those found with other drugs for which activated charcoal is clinically used. This study was designed to determine whether activated charcoal altered the gastrointestinal absorption of toxic doses of iron as ferrous sulfate in an in vivo model. Seventy-five male Sprague-Dawley rats were randomly assigned into 5 groups: control given only distilled water; 100 mg elemental Iron and water; 1:1 charcoal to iron; 2:1 charcoal to iron; and 4:1 charcoal to iron. All treatments were administered consecutively by gavage within 5 min. Physiological measurements and blood samples were taken at 0, 1, 4 and 8 h after treatment. There were no consistent differences in physiological measurements among the 5 groups. Mean serum iron concentrations did not differ among Groups 2, 3, 4 and 5 at the 4 sampling times except at I h between Groups 4 and 5. The area under the curve for serum iron concentrations did not differ among the treatment groups. Activated charcoal did not alter the extent of iron absorption in the experimental model.     

The effect of rate of drug administration on the extent and time course of phencyclidine distribution in rat brain, testis, and serum.

The goal of these studies was to examine the relationship between the rate of phencyclidine (PCP) administration and PCP tissue distribution. The time course of PCP distribution in serum, brain, and testis after rapid (i.v.) and slow (s.c.) administration was studied. Brain and serum PCP concentrations after an i.v. bolus dose (1 mg/kg at 900 microg/min) were highest at 30 s and decreased biphasically, with serum concentrations decreasing 30 times faster than brain concentrations during the early phase. Consequently, the brain-to-serum PCP concentration ratio increased from 8:1 at 30 s to 14:1 at 20 min before equilibrating at a ratio of 3:1 that remained constant from 1 to 8 h. In contrast, the testis-to-serum ratio increased slowly from 1:1 to 12:1 over 4 h, and then remained constant. In a separate group of animals, an s.c. infusion of PCP (18 mg/kg/day or 3.6 microg/min) produced a brain-to-serum ratio (6:1) that remained constant throughout the 96-h infusion. Testis-to-serum ratios increased from 4:1 at 1 h to 12:1 at 8 h and then remained constant for 96 h. Steady-state infusion of a pharmacologically inactive dose (2.5 mg/kg/day) produced a brain-to-serum ratio (3:1) that was significantly lower than the ratio (6:1) after infusion of the three pharmacologically active doses (10-25 mg/kg/day). The temporary high brain PCP concentrations and the dynamic disequilibrium between brain and serum concentrations after rapid i.v. administration could provide a better understanding of the preference of the human drug abuser for rapid rates (e.g., i.v. or smoking) of drug administration.     

Intestinal permeability to glucose after experimental traumatic brain injury: effect of gadopentetate dimeglumine administration

Traumatic injuries are the leading cause of mortality in individuals aged 1-44 years, and brain injury significantly contributes to the outcome in nearly one half of all deaths from trauma. At the intestinal level, traumatic brain injury (TBI) induces profound effects, including gastrointestinal mucosa ischaemia and motility dysfunction. However, nothing is known concerning the effect of TBI on the intestinal absorption of glucose. Hence, the aim of this study was to investigate the effect of TBI on the intestinal absorption of glucose by investigating the effect of TBI on the jejunal mucosal-to-serosal apparent permeability (AP-to-BL P(app)) to two glucose model substrates, (3)H-2-deoxy-D-glucose ((3)H-DG) and (3)H-3-O-methyl-D-glucose ((3)H-OMG), and to (14)C-sorbitol. Additionally, we tested if gadopentetate dimeglumine administration could prevent any of the changes observed after TBI. Traumatic brain injury induced an increase in the AP-to-BL P(app) to (3)H-DG. After a 100-min. perfusion of the jejunum, the AP-to-BL P(app) to (3)H-DG in TBI rats was almost 70% higher than in the control rats. There was no change, however, in the AP-to-BL P(app) to neither (3)H-OMG nor (14)C-sorbitol. Interestingly enough, gadopentetate dimeglumine was able to prevent the increase in the AP-to-BL P(app) to (3)H-DG observed after TBI. Given the differences in transport characteristics between (3)H-DG and (3)H-OMG, our results point to the possibility of the Na(+)-independent glucose transporter 2 (GLUT2) being activated by TBI (as the P(app) to (3)H-DG, a GLUT2 substrate, was increased) and the Na(+)-dependent glucose co-transporter (SGLT1) being inhibited by TBI (as the P(app) to (3)H-OMG, a GLUT2 and SGLT1 substrate, remained unchanged). Moreover, gadopentetate dimeglumine prevented these changes associated with TBI.     

Pharmacokinetics, pharmacodynamics, and tolerability of a generic formulation of exenatide: a randomized, open-label, single- and multiple-dose study in healthy Chinese volunteers

A randomized, open-label, dose-escalating study was designed to assess the pharmacokinetics, pharmacodynamics and tolerability of single and multiple subcutaneous administrations of exenatide in 24 healthy Chinese volunteers. The effects of gender on the pharmacokinetics of exenatide were also evaluated. Subjects were randomized to receive a single and multiple subcutaneous doses of 5 or 10?μg of exenatide. Following the single dose subjects received exenatide twice daily on days 2-4 and once on day 5. Sequential blood samples were collected at regular intervals from 0 to 8?h after single administration. Concomitantly the serum glucose concentrations were measured in each sample. Tolerability was assessed using physical examination, vital signs, laboratory analysis, and by interview of subjects. Pharmacokinetic parameters for exenatide after subcutaneous administration of a single dose of 5-10?μg were as follows: Cmax=77.7 (13.9) and 136.1 (15.2) pg/mL; AUC0-t=184.2 (49.7) and 309.7 (52.3) pg·h/mL; AUC0-∞=225.8 (77.4) and 365.4 (68.8) pg·h/mL; tmax (median [range])=1.00 (0.75-1.50) and 1.00 (0.75-1.50) h; t1/2 (mean [range])=1.4 (0.7-3.2) and 1.8 (1.0-2.5) h, respectively. Because of its short t1/2, Css, min could not be detected in any plasma samples prior to daily dosing on days 3-5. Pharmacokinetic parameters for exenatide after administration of multiple doses of 5 or 10?μg were as follows: Cmax=81.2 (12.2) and 144.5 (13.3) pg/mL; AUC0-t=181.1 (39.4) and 275.6 (45.0) pg·h/mL; AUC0-∞=217.2 (44.8) and 313.3 (48.4) pg·h/mL; tmax=1.10 (0.75-1.25) and 1.00 (1.00-1.25)?h; t1/2=1.6 (0.8-2.2) and 1.4 (0.9-2.7)?h, respectively. Both doses of exenatide were associated with significant reductions in serum glucose concentrations (P<0.001) when compared to baseline levels. Mean percentage of maximal decline for serum glucose concentrations after single and multiple doses were 15.6% and 19.9% for 5?μg, respectively; as well as 26.3% and 28.7% for 10?μg, respectively. 12 of the 24 subjects reported a total of 75 adverse events. The rate increased with higher doses of exenatide: after 5?μg only one subject experienced at least 1 adverse event but following 10?μg 11 subjects were affected. 2 subjects receiving the higher dose of 10?μg exenatide dropped out because of adverse events (nausea and vomiting). The most common adverse events were of gastrointestinal origin (e.?g. decreased appetite, nausea and vomiting) and of mild severity. In conclusion, in healthy Chinese subjects, AUC and Cmax increased in proportion to the dose, whereas t1/2 was independent of dose. The pharmacokinetic parameters after multiple dosing were consistent with those after single doses. No significant gender differences were noted for pharmacokinetic variables. Both exenatide doses were associated with significant reductions in serum glucose levels. Adverse events were mainly of gastrointestinal origin and their incidence was dose-dependent.     

Safety of high-dose iron sucrose infusion in hospitalized patients with chronic kidney disease.

PURPOSE: The safety of high-dose iron sucrose infusion in hospitalized patients with chronic kidney disease was studied. METHODS: A retrospective analysis was conducted at a 478-bed community hospital. A medical informatics search was performed to identify all hospitalized patients who were prescribed i.v. iron sucrose to deliver elemental iron 300 mg every other day for three doses between January and December 2002. Patients were eligible for inclusion in the analysis if they had chronic kidney disease, had an estimated creatinine clearance of <60 mL/min, and were prescribed the above regimen. Information on iron administration, vital signs, hematologic values, and iron indexes was gathered from patients' medical records. Medical record review was also used to identify possible adverse events. RESULTS: A total of 73 patients met eligibility criteria and received a total of 167 doses of iron sucrose. Twenty adverse events were judged as possibly related to iron sucrose administration and included nausea (n = 8 events), reduced blood pressure (n = 4), vomiting (n = 2), dysgeusia (n = 2), constipation (n = 2), fatigue (n = 1), and anxiety (n = 1). The majority of these adverse events were low in severity, as determined by an objective scale. No severe adverse events occurred. There was no association between infusion rate and the occurrence of potential adverse events (p = 0.44). CONCLUSION: Every-other-day i.v. infusion of iron sucrose, to deliver elemental iron 300 mg/dose, was associated with adverse events that were relatively uncommon, minor in severity, and unlikely to require medical intervention.     

Acute iron intoxication: the efficacy of deferiprone and sodium biocarbonate in the prevention of iron absorption from the digestive tract.

To determine whether enteral deferiprone given after a loading dose of liquid iron interferes with iron absorption from the digestive tract, prospective randomized animal study was initiated using Sprague-Dawley rats. The rats were given 20 mg elemental iron/kg as a ferrous sulfate solution + 1 mEq sodium bicarbonate/kg, and then dosed orally with 150 mg deferiprone/kg immediately or after 15 min. Serum iron levels were measured at 1, 3, 5 and 24 h; feces were collected for 24 h. The 20 mg elemental iron/kg caused a significant and rapid increase in serum iron levels to > 350 micrograms/dL within 20 min of oral dosing. Deferiprone, if given immediately after the iron, produced a significant decrease in serum iron levels and a 2-fold increase in iron excretion in feces. Effectiveness was delayed when the deferiprone was given 15 min after the iron dosing. Enteral deferiprone might be useful in preventing cases of acute iron intoxication.     

Pharmacokinetics of recombinant human basic fibroblast growth factor in rabbits and mice serum and rabbits aqueous humor

AIM: To study the pharmacokinetics of recombinant human basic fibroblast growth factor (rhbFGF) in rabbits and mice after iv and postocular administration, and the changes of rhbFGF in rabbits aqueous humor after postocular administration. METHODS: After iv or postocular administration three doses of rhbFGF in rabbits and mice, rhbFGF concentration in serum and rabbit aqueous humor was determined by enzyme-linked immunosorbent assay. RESULTS: Serum concentration-time data of rabbits after iv administration of rhbFGF 1, 2, and 4 μg/kg were fitted to bi-exponential equations with half-lives of 0.9, 0.9, and 0.6 min for T1/2α and 7, 8, and 4.7 min for T1/2β. Plasma concentration-time data of mice after iv administration of rhbFGF 2.5, 5 and 10 μg/kg were fitted to bi exponential equations with half-lives of 0.4, 0.6, and 0.9 min for T1/2α　and 6, 5, and 7 min for T1/2β.The AUCs were linearly correlated to doses in both cases (rrabbit=0.997, rmouse=0.999). The serum concentrations of rhbFGF were very l     

静脉与口服铁剂比较对维持性血透患者肾性贫血的临床疗效

目的观察慢性肾功能不全患者静脉和口服补铁治疗肾性贫血的疗效、不良反应的发生情况以及对促红细胞生成素(EPO)使用效应的比较。方法病情稳定的48例维持性血透肾性贫血患者,随机的分为静脉组和口服组2组,每组24例,观察期10周。观察用药前、用药后4周、用药后8周、用药后10周的血红蛋白(Hb)、红细胞压积(Hct)、铁蛋白(SF)、不良反应以及应用促红细胞生成素剂量。结果2组患者的血红蛋白、红细胞压积、铁蛋白,治疗后均较治疗前有明显升高,而静脉组升高幅度显著于口服组(P<0.01);2组患者应用促红细胞生成素的剂量在治疗后较治疗前均有所减少,而静脉组减少明显(P<0.05)。结论静脉补铁能及时有效的补充肾性贫血患者所需的铁剂,使贫血状况改善,不良反应少,而且能增强促红细胞生成素效应,减少其用量。