保妇康凝胶联合诺氟沙星治疗宫颈糜烂50例疗效观察

目的：探讨保妇康凝胶联合诺氟沙星治疗宫颈糜烂的临床效果。方法将100例宫颈糜烂患者根据随机数字表法分为观察组和对照组各50例。观察组给予保妇康凝胶和诺氟沙星联合治疗，对照组单独给予治糜灵栓治疗，比较两组患者临床症状的变化，并对临床疗效进行评价。结果观察组治愈率为86.00%，明显高于对照组的74.00%，临床症状评分改善较对照组明显，且其临床症状消失的时间短于对照组，差异均有统计学意义(P<0.05)。结论保妇康凝胶与诺氟沙星合用比治糜灵栓治疗宫颈糜烂效果更佳，且治愈时间上明显较优，值得临床上推广应用。     

Carboxylesterase catalyzed 18O-labeling of carboxylic acid and its potential application in LC-MS/MS based quantification of drug metabolites

LC-MS quantification of drug metabolites is sometimes impeded by the availability of internal standards that often requires customized synthesis and/or extensive purification. Although isotopically labeled internal standards are considered ideal for LC-MS/MS based quantification, de novo synthesis using costly isotope-enriched starting materials makes it impractical for early stage of drug discovery. Therefore, quick access to these isotope-enriched compounds without chemical derivatization and purification will greatly facilitate LC-MS/MS based quantification. Herein, we report a novel ¹⁸O-labeling technique using metabolizing enzyme carboxylesterase (CES) and its potential application in metabolites quantification study. Substrates of CES typically undergo a two-step oxygen exchange with H₂¹⁸O in the presence of the enzyme, generating singly- and doubly-¹⁸O-labeled carboxylic acids; however, unexpected hydrolytic behavior was observed for three of the test compounds – indomethacin, piperacillin and clopidogrel. These unusual observations led to the discovery of several novel hydrolytic mechanisms. Finally, when used as internal standard for LC-MS/MS based quantification, these in situ labeled compounds generated accurate quantitation comparable to the conventional standard curve method. The preliminary results suggest that this method has potential to eliminate laborious chemical synthesis of isotope-labeled internal standards for carboxylic acid-containing compounds, and can be developed to facilitate quantitative analysis in early-stage drug discovery.     

Acute myocardial infarction after sumatriptan administration for cluster headache

Abstract The pain of cluster headache attacks is severe, excruciating and selectively responsive to subcutaneous sumatriptan. Serious cardiovascular events attributed to sumatriptan are extremely rare and have most often been reported in patients at significant cardiovascular risk, or in overt cardiovascular disease. They also have occurred, however, in patients without evidence of cardiovascular disease. We describe a 42-year-old man with episodic cluster headache without history of coronary artery disease who was admitted to our coronary care unit for acute myocardial infarction after 3 h of subcutaneous injection of sumatriptan. During hospitalisation cluster headache attacks were successfully treated with e.v. indomethacin.     

雷公藤双层栓的研制

介绍了雷公藤双层栓的制备和质量检查。雷公藤双层栓的上层为空白层,下层为含药层。空白层可有效地阻止后端所释药物向上扩散,从而避免相当部分药物经门肝系统吸收,因此可明显提高其生物利用度。     

The effect of indomethacin and metamizole on ureteral motility and urine flow in sheep

Summary The objective of this study was to evaluate the effect of two non-steroid anti-inflammatory drugs, indomethacin and metamizole, on ureteral peristalsis during acute occlusion similar to the situation in renal colic. In 12 pentobarbital anesthetized sheep, both ureters were cannulated and the frequency of ureteral contractions, urine flow, mean ureteral pressure and blood pressure were recorded during 10-min control and i.v. drug administration periods. Both indomethacin (1–2 mg/kg) and metamizole (60–120 mg/kg) showed a dose dependent reduction in peristaltic frequency without reduction of the mean pressure. In addition, the pressure amplitude of the peristaltic waves was also lowered, particularly with indomethacin. Only indomethacin reduced the urine flow. Arterial blood pressure was elevated by both drugs, particularly after the first dose of indomethacin. It can be concluded that indomethacin and metamizole reduce ureteral peristaltic frequency, probably blocking the impulse transmission at the ureteropelvic junction.For the partial fulfillment of a Master's degree in Pharmacology     

Interleukin-1 inhibits keratan sulfate production by rabbit chondrocytes: Possible role of prostaglandin E2

We investigated the importance of prostaglandin E2 (PGE2) release in interleukin-1 (IL-1)-induced inhibition of aggrecan synthesis by chondrocytes. Keratan sulfate (KS) production was measured in parallel with PGE2 release in chondrocytes. IL-1 inhibited KS production and stimulated PGE2 release. In the presence of PGE2, there was a dosedependent decrease in baseline KS production. Indomethacin and dexamethasone partially blocked the IL-1-induced PGE2 release while KS production recovered. Our results suggest that IL-1 inhibits KS production, in part, by stimulating the release of PGE2.     

消炎痛对人胃癌上皮细胞BGC-823的作用

目的 :探讨非甾体类抗炎药 (NSAIDs)消炎痛 (indomethacin ,IND)对人胃癌细胞BGC - 82 3的作用 ,以期为非甾体类抗炎药对胃癌的防治作用提供理论依据。方法 :采用DNA条带分析以及流式细胞仪分别从定性及定量的角度观察不同浓度的消炎痛引起的BGC - 82 3细胞凋亡情况 ;MTT法分析不同浓度的消炎痛对BGC - 82 3细胞增殖的影响。结果 :低浓度的消炎痛可引起BGC - 82 3细胞的凋亡并且呈现量效关系 ;MTT分析发现 :消炎痛可抑制BGC - 82 3细胞的增殖 (P <0 .0 5)。结论 :NSAIDs有抑制胃癌细胞增殖、诱导其凋亡的作用 ,提示NSAIDs是一类预防胃肠道肿瘤的可行性药物     

乙酰胆硷和电刺激迷走神经对HC1引起的大鼠胃粘膜损伤的保护作用

本工作观察了乙酰胆硷(Ach)和电刺激迷走神经对0.6N HCl引起的胃粘膜出血性损伤的保护作用,发现皮下注射50μg/kg的氯化Ach和电刺激膈下迷走神经5min,可明显降低HCl引起的胃粘膜出血量,这一作用可被消炎痛及阿托品所阻断。提示这种保护作用是通过依赖于M-受体的内源性前列腺素。     

卡前列甲酯栓阴道给药、舌下含服预防产后出血

目的观察卡前列甲酯栓（卡孕栓）对产后出血发生的影响及其副作用。方法将正常足月妊娠阴道分娩者８０例随机分成３组，其中２组为卡孕栓实验组，以不同给药途径分为阴道用药组（２５例）与舌下含服组（２５例），对照组（３０例）则常规静脉推注麦角新碱。结果３组产妇的第３产程平均时间分别是７．６４、５．５２和６．４４ｍｉｎ，无明显统计学差异（Ｐ＞０．０５）；产后２ｈ内的平均出血量，对照组（２６０．８３ｍｌ）与卡孕栓阴道给药组（１９０．２８ｍｌ）及舌下含服组（１９９．８０ｍｌ）相比均有显著差异（Ｐ＜０．００１）；两卡孕栓组间则未见差异。两实验组产妇均未发生明显副反应。结论卡孕栓预防产后出血的效果优于麦角新碱，其阴道用药及舌下含服都是有效给药途径。     

Practical guidelines for physicians in the management of febrile seizures

Recent studies have shown that adequate medication can prevent the recurrence of febrile seizures (FS). It has also been clarified that the vast majority of, though not all, FS patients follow a benign course. Then, questions arise as to whether or not FS should be prevented, particularly in light of the risks of side effects from drugs. Which kinds of FS can be prevented, if necessary? The guidelines presented here are aimed primarily at helping general practitioners in considering how to manage FS most appropriately. The guidelines stress that judgements should be individualized, while referring to a few specific ‘warning factors’. The guidelines follow a ‘laissez-faire’ principle for the majority of FS cases, whereas intermittent therapy with diazepam and continuous medication with either phenobarbital or valproate are indicated in other limited cases meeting respective definite criteria.