0.5%酮咯酸氨丁三醇眼液在飞秒激光LASIK手术中的应用与观察

目的观察0.5%酮咯酸氨丁三醇滴眼液在飞秒激光制作角膜瓣后对眼部刺激症的抑制效果。方法采用自身对照法观察30例（60只眼）接受飞秒激光手术的患者,右眼飞秒激光制作角膜瓣后立即滴用0.5%酮咯酸氨丁三醇滴眼液为试验组,左眼飞秒激光制作角膜瓣后不滴用任何眼液为对照组。观察左、右眼在等待气泡吸收的15分钟内,眼部刺激症状的表现程度。结果两组在眼部刺激症状表现程度上有明显差异,试验组30只眼中0级无眼部刺激反应的21只眼,占本组的70%;1级轻度反应8只眼,占本组26.6%;2级中度反应1只眼,占本组3.3%;对照组30只眼中0级无眼部刺激症状的4只眼,占本组13.3%;1级轻度19只眼,占本组63.3%;2级中度7只眼,占本组23.3%。两组进行fisherexacttest,P〈0.05。结论 0.5%酮咯酸氨丁三醇滴眼液属于非甾体抗炎药,可有效控制眼前节炎症消退,降低角膜敏感性,具有镇痛、消炎、抗敏感作用。通过对两组的比较分析,认为0.5%酮咯酸氨丁三醇滴眼液可有效缓解和抑制飞秒激光制作角膜瓣后的眼部刺激症状,有助于准分子激光切削时患者与医生的配合,提高手术效果,是安全和有效的。     

Pharmacokinetics of Ketorolac and p-Hydroxyketorolac Following Oral and Intramuscular Administration of Ketorolac Tromethamine

Ketorolac tromethamine (KT), a potent analgesic with cyclooxygenase inhibitory activity, was administered in an open, randomized, single-dose study of Latin-square design to 12 healthy male volunteers. Doses of 30 mg oral (po) and 30, 60, and 90 mg intramuscular (im) KT were administered in solution. Plasma samples were analyzed for ketorolac (K) and its inactive metabolite, p-hydroxyketorolac (PHK), by reversed-phase high-performance liquid chromatography (HPLC). The 30-mg im dose was found to be similar to the 30-mg po dose with respect to total AUC values for both K and PHK. The amount of PHK circulating in plasma was very low as judged by AUC ratios (PHK/K × 100) of 1.9 and 1.5% for the 30-mg po and im doses, respectively. The rate of absorption of K and formation of PHK, as determined by C _max and T _max values, was significantly slower following the im doses. Total AUC and C _max for K and PHK increased linearly with dose after im administration of 30, 60, and 90 mg of KT. The mean plasma half-life of K was remarkably consistent between po and im administration and was independent of dose, ranging from 5.21 to 5.56 hr. The plasma metabolic profile was similar following both routes of administration and graded im doses.     

The excretion of ketorolac tromethamine into breast milk after multiple oral dosing

Summary We have studied the transfer of the analgesic ketorolac tromethamine into breast milk in ten women aged between 22 and 35 years. Ketorolac administration was started between 2 and 6 days after delivery. The breast milk was not fed to the infant because of maternal antibiotic use (6 patients) or because of jaundice of the baby.10 mg of ketorolac was given four times daily for two days. Plasma and milk samples were collected on the two dosing days and on the first day after dosing. The plasma and milk were assayed for ketorolac concentrations by HPLC; the quantification limits were 10 ng·ml^–1 and 5 ng·ml^–1 respectively.The maternal plasma concentrations were within established ranges for ketorolac. In four patients the concentration of ketorolac in the milk was never above 5 ng·ml^–1. At 2 h after dosing on both Days 1 and 2 there were quantifiable concentrations of ketorolac in the milk. The range was 5.2 ng·ml^–1 to 7.9 ng·ml^–1. The ratio of breast milk: plasma concentrations of ketorolac ranged from 0.015 to 0.037.The maximum potential amount of ketorolac that an infant may be exposed to daily could range from 3.16 mg to 7.9 mg, assuming a consumption of between 400 ml and 1 l of breast milk. On a weight-adjusted basis this is equivalent to between 0.16% and 0.40% of the total daily maternal dose.Klinikum der Stadt Mannheim, Gynaecological Clinic, Mannheim, (until 1986: Krankenanstalt Rotes Kreuz, Munich)     

高效液相色谱法测定人体血浆中酮咯酸含量及其药动学

目的：建立高效液相色谱法测定血浆中酮咯酸浓度的方法.方法：色谱柱为Waters sunfire C18色谱柱（150 mm× 4.6mm,5 μm）,流动相为（0.02 mol·L^-1磷酸二氢钾溶液-乙腈（70∶30）,用磷酸调至pH 4.5,检测波长315 nm,测定酮咯酸的含量.结果：血样酮咯酸的保留时间为6.35 min,最低定量限为0.05 mg·L^-1,RSD小于20%,在0.05～8.0 mg·L^-1范围内呈良好线性关系,平均方法学回收率为95.40%～100.28%关系,平均提取回收率为95.79%～106.01%,批内和批间变异＜10%.结论：本法简便、快捷、灵敏,适用于酮咯酸人体临床药动学研究.     

Intramuscular ketorolac following total hip replacement with spinal anaesthesia and intrathecal morphine

We have studied the analgesic and morphine sparing effect of ketorolac tromethamine in 60 patients after total hip replacement under spinal anaesthesia.
In this double blind study 30 patients received ketorolac 30 mg IM 6 hourly postoperatively and the control group received saline. Analgesia was assessed by visual analogue pain scores (VAS) and morphine consumption by patient controlled analgesia (PCA). There was a significantly ( P <0.02) lower morphine consumption in the ketorolac group (7.1 ±8.6 mg; Mean±s.d.) when compared to the saline group (14.2±13.6 mg). Although there was a trend for lower VAS on the first postoperative night this was only significant at 10 hours postoperatively and the next morning at 08:00 hr. The incidence of side effects (emetic sequelae, pruritus and headache) were similar in both groups. It is concluded that ketorolac reduces the consumption of additional morphine in conjunction with intrathecal morphine but had no effects on the side effects.     

卡前列素氨丁三醇防治产妇产后出血的临床效果

目的：研究卡前列素氨丁三醇防治产妇产后出血的临床效果。方法2011年1月~2014年1月,选择90例存在宫缩乏力性产后出血因素的产妇进行研究,按随机数χ表法分为试验组(45例)与对照组(45例),两组产妇在胎儿娩出后均静脉滴注20 U缩宫素,在此基础上,试验组产妇宫肌注射或臀肌注射250μg卡前列素氨丁三醇,对照组产妇宫肌注射或臀肌注射20 U缩宫素。经处理后,比较两组产妇的产后2、24 h出血量,产后出血及不良反应发生情况。结果试验组产后2、24 h出血量及产后24 h血红蛋白下降值均显著少于对照组(P<0.05);试验组的产后出血发生率为11.1%,明显低于对照组(31.1%),两组比较,差异有统计学意义(χ2=5.4040,P=0.0201);试验组的不良反应发生率为13.3%,对照组为8.9%,两组比较,差异无统计学意义(χ2=0.4500,P=0.5023)。结论卡前列素氨丁三醇防治产妇产后出血的效果良好,安全性高,值得临床推广应用。     

Protective effect of intrathecal ketorolac in spinal cord ischemia in rats: a microdialysis study

BACKGROUND: The prevention of ischemic paraplegia after thoracoabdominal aortic surgery is challenging for both anesthesiologists and surgeons. In a previous study, we showed that intrathecal ketorolac pre-treatment protects rats against ischemic spinal cord injury. In the present study, using a microdialysis method, we investigated whether this neuroprotective effect was related to changes in the spinal cord release of nitric oxide (NO) or the excitatory amino acids (EAAs) aspartate and glutamate. METHODS: Rats were randomized to receive either intrathecal saline or ketorolac 60 microg (10 rats per group), 1 h before spinal cord ischemic injury induced by balloon inflation of a 2F Fogarty catheter in the thoracic aorta with maintenance of the proximal arterial blood pressure at 40 mmHg for 11 min, followed by reperfusion. Another 10 animals were used as the sham-operated control group. Ischemic injury was assessed by hind limb motor function. Cerebrospinal fluid dialysates were collected at baseline (before ischemia) and at 1, 2, 3, 4, 6, 12 and 24 h after the start of reperfusion, and were analyzed for EAAs using high-performance liquid chromatography and for NO metabolites using an NO analyzer. RESULTS: The results showed that intrathecal ketorolac attenuated spinal cord ischemic injury. Dialysate concentrations of NO and EAAs were increased after spinal cord ischemia, and this effect was inhibited by intrathecal administration of ketorolac. CONCLUSIONS: The results of this study suggest that the neuroprotective effect of intrathecal ketorolac in spinal cord ischemia in rats may be caused by a decrease in the spinal cord release of NO and EAAs.     

水囊压迫联合卡前列素氨丁三醇治疗产后出血的临床研究

探讨宫腔水囊压迫联合卡前列素氨丁三醇治疗产后出血的效果。方法对甘肃省白银市第一人民医院2011年8月至2013年12月收治的162例产后大出血患者的临床资料进行回顾性分析,采用宫腔水囊压迫联合卡前列素氨丁三醇治疗的82例为观察组,采用宫腔纱条填塞联合缩宫素治疗的80例为对照组,分析两组止血有效率、放置时间、取出时间、术后2 h及24 h出血量,再次出血率、子宫切除的情况。结果观察组止血有效率高于对照组(98.8%vs 92.5%,P0.05);产后2 h出血量少于对照组[(25.8±12.3)m L vs(41.1±9.6)m L,P0.05];再次出血发生率低于对照组(1.22%vs 3.75%,P0.05);子宫切除率低于对照组(1.22%vs 7.50%,P0.05)。结论宫腔水囊压迫联合卡前列素氨丁三醇治疗产后出血疗效显著,值得临床推广。     

米索前列醇与卡前列素氨丁三醇预防剖宫产产后出血的效果比较

目的 比较米索前列醇与卡前列素氨丁三醇预防高危产妇剖宫产产后出血的价值.方法 选择有产后出血倾向的高危孕妇113例(包括瘢痕子宫、前置胎盘、双胎、巨大儿、羊水过多),按随机数字表法分为观察组58例和对照组55例,观察组给予0.4 mg米索前列醇塞肛治疗,对照组给予肌肉注射卡前列素氨丁三醇250 μg.比较两组产后出血发生率、产后2 h和24 h的出血量、输血率,止血时间、近远期并发症等.结果 两组产后出血率比较差异无统计学意义(P>0.05);对照组产后2 h及24 h出血量、输血率、止血时间及子宫切除率均低于观察组,差异有统计学意义(P<0.05);两组不良反应发生率比较差异无统计学意义(P>0.05).结论 与米索前列醇相比,卡前列素氨丁三醇在剖宫产术产后出血的防治效果更优,可减少产后出血量和输血率,减少并发症的发生.