右酮洛芬胶囊用于镇痛的随机双盲对照临床试验

目的:评价右酮洛芬(dexketoprofen)胶囊的临床镇痛效果和不良反应。方法:采用多中心随机双盲平行对照的方法,以酮洛芬(ketoprofen)胶囊为对照药,用于治疗轻、中度疼痛;1d给药用于治疗痛经,一周给药用于治疗骨科慢性疼痛。以疼痛强度差(PID)、疼痛缓解率(PAR)、有效率等作为镇痛效果判定指标。结果:治疗痛经时,试验组与对照组PID值的差异无统计学意义。用于骨科慢性疼痛时,用药后PID增加,用药4d后PID值基本稳定,试验组与对照组PID值的差异无统计学意义。1d给药和一周给药试验组与对照组的完全缓解率、明显缓解率组间差异均无统计学意义。1d给药和一周给药的试验组与对照组的总有效率都在90%以上;两组总有效率差值的95%置信区间在(-15.0%,15%)等效界值内,表明试验药与对照药等效。不良反应主要有胃不适、恶心等。结论:右酮洛芬为治疗轻、中度疼痛的镇痛药。其不良反应较轻。25mg的右酮洛芬与50mg酮洛芬镇痛效果等效。     

国产与进口二氟尼柳的实验性镇痛和抗炎作用的比较

目的 :观察国产二氟尼柳 (diflunisal)的镇痛和抗炎作用。方法 :镇痛用小鼠热板法和醋酸引起的小鼠扭体模型实验 ,抗炎用二甲苯引起的小鼠耳肿胀和角叉菜胶引起的大鼠足跖肿胀实验。结果 :镇痛实验结果表明国产二氟尼柳可显著延长小鼠热板法的痛阈值 ,抑制醋酸引起小鼠扭体模型的ED50 为 1 2 .46mg·kg-1(9.79～ 1 5 .86mg·kg-1) ;抗炎实验表明二氟尼柳抑制二甲苯引起小鼠耳肿胀的ED50 为 1 1 .1 0mg·kg-1(8.93～1 3 .81mg·kg-1) ,抑制角叉菜胶引起大鼠足跖肿胀的ED50 (用药后 6h)为 1 0 .5 6mg·kg-1(8.47～ 1 3 .1 7mg·kg-1)。结论 :国产二氟尼柳的镇痛和抗炎作用与进口品相近。     

酮洛芬的脊髓镇痛作用及其机制

目的研究酮洛芬的脊髓镇痛作用及作用机制。方法采用温浴法、热板法观察动物痛阈变化。结果鞘内注射（ｉｔｈ）酮洛芬１．６～３．２ｍｇ·ｋｇ－１具有明显镇痛作用，全身用药需１６ｍｇ·ｋｇ－１才具有同等镇痛效应。ｉｔｈ与ｉｐ药物有效剂量比为１∶１０。ｉｔｈ用药，作用可被ｉｐ利血平、ｓｃ哌唑嗪、育亨宾阻滞。结论酮洛芬具有脊髓镇痛作用，其机制与ＮＥ－α受体系统介导的内源性镇痛系统密切相关     

反相高效液相法测定右酮洛芬含量

酮洛芬是一种a-芳基丙酸非甾体抗体炎药物。右酮洛芬(dexketoprofen)多用拆分法得到的酮洛芬的光学异构体[1]，其作用几乎为同剂量酮洛芬的2倍，镇痛作用强，起效迅速，不良反应少[2]。目前我国处于新药研制阶段。本实验采用反相HPLC法测定右酮洛芬含量，方法简便，结果准确。     

酮洛芬的合成

对硝基苯乙酮经缩酮保护、缩合、脱保护、还原、重氮脱氨制得3-乙酰基二苯甲酮,再经Darzens反应制得酮洛芬,总收率44.6%.     

肝素镇痛作用的动物实验

近年来肝素在临床的新用途日益增加，其中临床用于镇痛就有许多文献报道，但未见有对动物实验镇痛作用的研究。为证实肝素新的药理作用和用途，以给临床应用提供科学依据，我们作了肝素对大白鼠光幅射热甩尾法和小鼠热板法两种镇痛作用实验，结果表明：肝素有明显镇痛作用。     

牛黄解毒滴丸解热镇痛和抗炎作用实验

目的：观察牛黄解毒滴丸的解热镇痛和抗炎作用。方法：采用2,4-二硝基酚大鼠致热法观察其解热作用;小鼠扭体法、热板刺激法观察其镇痛作用;小鼠耳部肿胀法、大鼠蛋清足肿胀法观察其抗炎作用。结果：牛黄解毒滴丸显著降低2,4-二硝基酚所致大鼠升高的体温;明显减轻和抑制热板所致的小鼠疼痛及醋酸所致的小鼠扭体反应;抑制二甲苯所致的小鼠耳肿胀和蛋清所致的大鼠足肿胀。结论：牛黄解毒滴丸对实验大鼠、小鼠具有良好的解热、镇痛和抗炎作用。     

桂皮醛解热镇痛抗炎作用的实验研究

目的：观察桂皮醛解热镇痛抗炎作用。方法：采用酵母发热大鼠模型，观察桂皮醛解热作用；采用小鼠扭体法和热板法，观察桂皮醛镇痛作用；通过小鼠耳肿胀及对腹腔毛细血管通透性的影响观察桂皮醛抗炎作用。结果：桂皮醛能显著减轻酵母所致大鼠发热反应，明显提高热板痛阈和抑制醋酸所致扭体反应，亦能显著抑制腹腔毛细血管通透性的增高及二甲苯所致小鼠耳廓肿胀。结论：桂皮醛具有明显的解热镇痛抗炎作用。     

解热镇痛消炎药的处方用药调查分析

本文分析华山医院１９９４年１月至１９９４年１２月每月１日门诊处方１２５１８张，其中含解热镇痛消炎药处方数占总处方数的１５．１％，男女之比１：０．８７，５０～７０岁年龄组为其主要用药对象。非甾体消炎药的ＤＤＤｓ排序依次为阿斯匹林，芬必得，扶他林；解热镇痛药ＤＤＤｓ排序依次为帕尔克、康泰克、克感敏。９３．９２％的处方为单独用药，大部分药品的ＤＵＩ＜１，提示在用量上无明显滥用情况。     

人血浆中右酮洛芬浓度的HPLC法测定

目的：建立 HPLC 法测定人血浆中右酮洛芬的浓度。方法：血浆样品用乙醚作为萃取剂萃取,以萘普生为内标;采用 DiamonsiL C18 色谱柱（5 μm,4.6 mm×200 mm）;流动相为乙腈-5 mol/L 磷酸盐缓冲液（27∶73）,pH 值为 6.9,流速为 1.0 mL/min;检测波长为 260 nm。结果：右酮洛芬血浆样品的线性范围为 0.078-5.000 μg/mL（r＝0.999 6）;方法回收率和萃取回收率分别为 99.5%-101.9% 和 70.8%-73.8%（n＝5）,日内、日间 RSD 分别为 5.5%-10.8% 和 6.4%-9.4%（n＝5）。结论：本法简便、准确、灵敏度高、专属性强,适用于人血浆中右酮洛芬浓度的测定。     

Comparative study of analgesic efficacy and morphine-sparing effect of intramuscular dexketoprofen trometamol with ketoprofen or placebo after major orthopaedic surgery

AIMS: Multimodal analgesia is thought to produce balanced and effective postoperative pain control. A combined therapy with nonsteroidal anti-inflammatory drugs (NSAIDs) and opiates could result in synergistic analgesia by acting through different mechanisms. Currently there are very few parenterally administered NSAIDs suitable for the immediate postoperative period. Therefore, this study was undertaken to assess the analgesic efficacy, relative potency, and safety of parenteral dexketoprofen trometamol following major orthopaedic surgery. METHODS: One hundred and seventy-two patients elected for prosthetic surgery, were randomized to receive two intramuscular injections (12 hourly) of either dexketoprofen 50 mg, ketoprofen 100 mg or placebo in a double-blind fashion. Postoperatively, the patient's pain was stabilized, then they were connected to a patient- controlled analgesia system (PCA) of morphine for 24 h (1 mg with 5 min lockout). RESULTS: The mean cumulative amount of morphine (CAM) used was of 39 mg in the dexketoprofen group and 45 mg in the ketoprofen group vs 64 mg in the placebo group. (Reduction in morphine use was approximately one-third between the active compounds compared with placebo (adjusted mean difference of -25 mg between dexketoprofen and placebo and -23 mg between ketoprofen and placebo. These differences were statistically significant: P 相似文献   

2种疗效判断标准对洛索洛芬治疗类风湿关节炎的评价

目的 :国内、美国风湿病学会 (ACR) 2种疗效判断标准评价洛索洛芬 (loxoprofen)治疗类风湿关节炎 (RA)的疗效及不良反应。方法 :选择 5 0例 ,年龄 (4 8±s 13)a ,4 0～ 69aRA活动期病人 (男女不限 ) ,口服洛索洛芬 60mg ,tid× 4wk ,比较用药前后关节压痛数、关节肿胀数、血沉、C反应蛋白等临床及实验室指标的变化 ,用国内、ACR不同疗效判断标准评价洛索洛芬治疗RA的疗效及不良反应。结果 :洛索洛芬治疗RA的总有效率达 74 %(国内标准 )和 80 % (ACR标准 ) ,2种疗效判断标准无显著差异 ,各项临床及实验室指标均有显著改善 ,不良反应发生率 10 % ,未出现危及生命的不良反应。结论 :洛索洛芬治疗RA安全、有效     

Studies on the antiinflammatory,immunoregulatory, and analgesic actions of melatonin

In order to develop melatonin (MT) as a potential new drug for the treatment of diseases with inflammation, pain, and abnormal immune responses, the effects and mechanisms of MT on inflammation, immunoregulation, and nociception were studied systematically. MT (40–160 mg/kg, ip) had significant analgesic effects in the hot-plate, writhing, and tail-flick models, with a marked dose- and time-dependence. The onset of its analgesia about 30–60 min after ip, was slower than that of pethidine, but the duration was longer (about 1.5–2 h). The analgesia was also induced by icv MT (0.25 mg/kg) injection. A lower dose of MT (10 mg/kg) could enhance the analgesic effect of pethidine, which was blocked by naloxone (10 mg/kg). MT (100 mg/kg, ip) decreased the content of beta-endorphin in the hypothalamus and pituitary. The analgesia of MT could be attenuated by pretreatment with reserpine (30 mg/kg, ip) or phentolamine (10 mg/kg, ip). CaCl₂ (230 mg/kg) could antagonize the analgesia of MT. EGTA and verapamil had opposite effects to CaCl₂. No tolerance and dependence to MT was found in mice. Further studies showed that MT could enhance the functions of T and B lymphocytes and macrophages in vitro and in adjuvant arthritis, and inhibit the disturbance of immune cells. MT could inhibit the swelling of hindpaw induced by carrageenin and complete Freund's adjuvant. These factors suggest that MT possesses marked antiinflammatory, immunoregulatory, and analgesic effects which may be related to the system of opiate, monoamine, and Ca²⁺ modulation. Drug Dev. Res. 39:167–173. © 1997 Wiley-Liss, Inc.     

类风湿关节炎338例药物治疗16年回顾性分析

目的 :了解类风湿关节炎 (RA)药物治疗及治疗方案的远期疗效及安全性。方法 :82例单种使用非甾类消炎药 (NSAIDs) ,2 56例用慢作用抗风湿药 (SAARDs) ,其中 113例为单种SAARDs治疗 ,95例为联合用药 ,4 8例为轮换用药。结果 :1,2 ,3,5a和 10a以上治疗坚持率轮换用药组为 94 % ,77% ,69 % ,4 4 %和 13 %。而联合用药组为 81% ,4 7% ,39% ,19%和 4 % ,单种SAARDs用药组为59 .3 % ,33.6% ,2 2 .1% ,7.0 %和 2 .7% ,NSAIDs组为 13 % ,2 % ,2 % ,0和 0。单种SAARDs用药组、联合用药组和轮换用药组治疗RA临床显效率分别为 33.6% ,34 %和 38%。单种用药组、联合用药组和轮换用药组均无发生严重不良反应。结论 :SAARDs治疗方案坚持率高 ,疗效好 ,不良反应轻。     

氯诺昔康联合地塞米松超前镇痛用于下肢手术的临床观察

目的：研究氯诺昔康联合地塞米松超前镇痛应用于下肢手术的镇痛效果及安全性。方法：将100例骨科下肢择期手术患者随机分为四组,A组：氯诺昔康（8mg溶于2mL注射用水）＋地塞米松（10mg,2mL）组;B组：氯诺昔康（8mg溶于2mL注射用水）＋生理盐水（2mL）组;C组：地塞米松（10mg,2mL）＋生理盐水（2mL）组;D组：单纯生理盐水（4mL）组。各组于术前30min静注相应药物,术中患者采用连续硬膜外麻醉,术后予静脉自控镇痛（PCIA,2mL／h,48h）。记录术后2、4、8、12、24、48h各时点的视觉模拟评分（VAS）与术后48h最痛程度（PD）评分、术后2d平均疼痛程度（MD）评分来评价其镇痛效果,以舒适度分级（BCS）~睡眠障碍度分级（SS）来评价患者对术后镇痛的满意程度,记录术后各组辅助镇痛药物的使用情况,同时观察恶心、呕吐、皮肤瘙痒、嗜睡、切口感染、延迟不愈等相关不良反应。结果：D组术后2、4、8、12、24、48hVAS评分高于A、B两组（P〈0．05）,同时BCS分级低于A、B两组（P〈0．05）：A组术后2j4、8、12h的VAS评分低于B组（P〈0．05）;术后48h内A组的PD、MD、SS评分均低于其他三组（P〈0．05）,A、B两组辅助镇痛药物的使用量明显少于C、D组（P〈0．05）,恶心、呕吐的发生率A组低于其他三组（P〈0．05）。结论：氯诺昔康联合地塞米松超前镇痛用于骨科手术,能有效缓解术后疼痛,提高患者对镇痛的满意程度,同时减少术后辅助镇痛药物的使用及相关不良反应。     

萘丁美酮治疗类风湿关节炎

目的 :评估萘丁美酮对类风湿关节炎 (RA)的疗效和安全性。方法 :76例RA病人分 2组 ,萘丁美酮组 4 6例 ,男性 14例 ,女性 32例 ,年龄 4 5a±s 11a(2 2～ 68a) ,给萘丁美酮片 1g ,po ,qd× 4wk。双氯芬酸组 30例 ,男性 6例 ,女性 2 4例 ,年龄 4 4a± 10a(2 6～ 64a) ,给双氯芬酸 5 0mg ,po ,qd× 4wk。观察其临床疗效、实验室指标和不良反应。结果 :萘丁美酮组总有效率为 91% ,明显高于双氯芬酸组 (73% ,P <0 .0 5 ) ,2组治疗后临床各指标均有明显改善 (P <0 .0 1) ,萘丁美酮组不良反应为 15 % ,明显低于双氯芬酸组 (37% ,P <0 .0 5 )。结论 :萘丁美酮对RA具有良好疗效和较低的不良反应     

Validation of ICD-9 codes with a high positive predictive value for incident strokes resulting in hospitalization using Medicaid health data

PURPOSE: To validate ICD 9 codes with a high positive predictive value (PPV) for incident strokes. The study population consisted of Tennessee Medicaid enrollees aged from 50 to 84 years. METHODS: We identified all patients who were hospitalized with a discharge diagnosis of stroke between 1999 and 2003 using highly specific codes (ischemic stroke ICD 9-CM codes 433.x1, 434 [excluding 434.x0], or 436; intracerebral hemorrhage [431]; and subarachnoid hemorrhage [430]). We reviewed medical records of a systematic sample of 250 cohort members. We randomly selected 10-30 eligible records for review from hospitals with at least 10 stroke hospitalizations. RESULTS: We reviewed 231 charts (93% of total sampled), and 205 (89%) met study criteria for new outpatient stroke. Of the 205 confirmed new outpatient strokes, 196 had stroke listed as the primary discharge diagnosis (PPV = 96%). However, 46 (23%) of the 196 patients identified by the primary diagnosis also had a remote stroke history (recurrent stroke not incident). Thus the PPV of the primary discharge diagnosis for identifying incident stroke decreased to 74%. When we applied an algorithm that restricted our population to those with stroke as the primary diagnosis and excluded patients with any prior outpatient diagnosis of stroke, we identified incident stroke events with more precision (PPV = 80%). CONCLUSION: The PPV of incident strokes was 80% using our strategy of primary discharge diagnosis and excluding prior outpatient diagnoses of stroke. Although an unknown percentage of incident strokes are missed, this group of proven incident stroke patients can be used for etiologic studies of medication exposures.