格拉司琼预防妇科腹腔镜术后恶心呕吐的临床观察

目的探讨预防性应用新型高选择性5-HT3受体拮抗剂格拉司琼预防妇科腹腔镜术后恶心、呕吐的效果。方法择期行妇科腹腔镜手术的患者80例,均接受全身麻醉,随机分为2组,A组(对照组,n=40),在手术结束前静脉注入0.9%生理盐水3 mL;B组(格拉司琼组,n=40),在手术结束前静脉给予格拉司琼3 mg。观察术后24 h恶心、呕吐的发生率。结果术后24 h内格拉司琼组恶心、呕吐的发生率显著低于对照组(P<0.01)。结论格拉司琼能安全、有效地预防妇科腹腔镜术后恶心、呕吐的发生。     

格拉司琼复合地塞米松对腹腔镜胆囊切除术后恶心呕吐影响的研究

目的:观察格拉司琼复合地塞米松对腹腔镜胆囊切除术后的镇吐效果。方法:随机将A SAⅠ~Ⅱ120例择期行腹腔镜胆囊切除的患者分为3组,每组40例。格拉司琼复合地塞米松组(G+D组)于术毕时静脉注射格拉司琼8 m g和地塞米松5 m g;格拉司琼组(G组)于术毕时静脉注射格拉司琼8 m g;对照组(C组)则于术毕时静脉注射生理盐水5 mL。观察术后24 h内患者恶心、呕吐的发生情况。结果:G+D组恶心发生率为5%(2/40),明显低于G组的17.5%(7/40)和C组的35%(14/40)(P<0.05)。G+D组呕吐发生率为2.5%(1/40),明显低于G组的15%(6/40)和C组的32.5%(13/40)。G组恶心、呕吐发生率亦明显低于C组(P<0.05)。结论:格拉司琼复合地塞米松控制腹腔镜胆囊切除术后恶心呕吐发生的效果优于单纯使用格拉司琼。     

阿扎司琼联合地塞米松预防腹腔镜胆囊切除恶心呕吐的疗效观察

目的:观察阿扎司琼联合地塞米松对预防腹腔镜胆囊切除术后恶心呕吐(post-operative nausea and vomiting,PONV)的疗效.方法:选择腹腔镜胆囊切除手术患者80例,随机分为4组,每组20例.A组:麻醉诱导前静脉注射生理盐水2 mL,手术缝皮时静脉注射阿扎司琼10 mg,B组:麻醉诱导前静脉注射地塞米松10 mg,手术缝皮时静脉注射生理盐水2 mL;C组:麻醉诱导前静脉注射地塞米松10 mg,手术缝皮时给予阿扎司琼10 mg;D组:麻醉诱导前和手术缝皮时均给予生理盐水4 mL.观察并记录四组患者术后24小时恶心呕吐发生的例数、程度与不良反应.结果:术后24小时内,A、B、C三组恶心呕吐发生率较D组低,差异有统计学意义(P<0.05),A B两组问的恶心呕吐发生率差异无显著性(P>0.05),C组术后恶心呕吐发生率较A、B两组低,差异有显著性(P<0.05).结论:阿扎司琼联合地塞米松能有效预防腹腔镜胆囊切除术患者术后恶心呕吐,效果较单用阿扎司琼或地塞米松更佳.     

格拉司琼预防妇科腹腔镜术后恶心呕吐疗效观察

目的：观察格拉司琼预防妇科腹腔镜术后恶心呕吐的疗效。方法：60例ASAⅠ-Ⅱ级妇科疾病择期行腹腔镜手术患者随机分为对照组（A）和格拉司琼组（B），各30例。A组在麻醉诱导前静脉滴注0．9％生理盐水10ml；B组在麻醉诱导前静脉滴注格拉司琼3mg。结果：B组PONV发生率和程度明显低于A组，差异有显著性（P〈0．05）。结论：格拉司琼显著降低妇科腹腔镜术后24小时内恶心呕吐的发生率，对预防妇科腹腔镜术后恶心呕吐有明显效果。     

格拉司琼术前和术后预防性给药对预防术后恶心呕吐效果的比较

目的研究格拉司琼在术前和术后预防性给药预防行腹腔镜胆囊切除术患者术后恶心呕吐(PONV)的效果。方法90例全麻下行腹腔镜胆囊切除术患者随机分为3组,每组30例。Ⅰ组(对照组)不预防性给药;Ⅱ组(术前格拉司琼组)于麻醉诱导前给予格拉司琼3mg;Ⅲ组(术后格拉司琼组)手术结束时给予格拉司琼3mg。记录术后24h内恶心呕吐的发生情况及用药情况。结果Ⅱ组患者在术后24h内恶心呕吐发生率为20.0%,略高于Ⅲ组的16.7%,但无显著性差异(P>0.05);Ⅱ、Ⅲ组与Ⅰ组的46.7%相比,恶心呕吐的发生率和程度明显降低(P<0.05),术后应用止吐药物剂量亦明显低于Ⅰ组(P<0.05)。结论在手术前或手术结束时,应用本研究所用剂量的格拉司琼预防术后恶心呕吐的效果相当。     

格拉司琼单独或联合药物预防胆囊手术术后恶心呕吐的护理

目的 总结腹腔镜胆囊手术后格拉司琼单独或联合药物防治恶心呕吐的护理措施.方法 90例择期腹腔镜胆囊切除术患者随机分成3组.A组为对照组术时给予生理盐水5 ml.B组格拉司琼组术中静脉注射格拉司琼8 mg.C组联合组,术中静脉注射长托宁1 mg +格拉司琼.观察术后24 h患者的恶心呕吐情况.结果 A、B、C组患者术后恶心呕吐发生率分别为83.3%、30.0%、12.0%(P<0.05或P<0.01).结论 本研究提示术中静脉注射格拉司琼与长托宁能有效防止腹腔镜术后恶心呕吐.     

氟哌利多、格拉司琼预防腹腔镜胆囊切除术后恶心呕吐疗效观察

目的:比较氟哌利多、格拉司琼预防腹腔镜胆囊切除术后恶心呕吐的临床疗效.方法:选择 120例ASA Ⅰ一Ⅱ级择期腹腔镜胆囊切除术病人,按入院编号随机分为三组,各40例.A组诱导前 5 min 静注氟哌利多 2.5 mg,B组在开始缝皮前静注格拉司琼3 mg、C组(对照组)静注生理盐水10 mL.结果:术后24 h内恶心呕吐发生率A组17.5%、B组15%,明显低于C组50%(P＜0.05),A组与 B组比较差异无显著性(P＞0.05).结论:氟哌利多和格拉司琼均可显著降低腹腔镜胆囊切除术后恶心呕吐发生率.     

格拉司琼联合甲氧氯普胺预防腹腔镜胆囊切除术后恶心呕吐的疗效观察

目的：探讨术前预防性应用格拉司琼合用甲氧氯普胺预防腹腔镜胆囊切除术后恶心、呕吐的疗效。方法：择期行腹腔镜下胆囊切除术患者120例,随机分为3组,每组40例,分别为空白对照组、试验组I和试验组II。空白对照组不进行任何干预措施,试验组I和试验组II分别在腹腔充气前5min给予格拉司琼3mg和格拉司琼3mg联合甲氧氯普胺20mg。观察手术后24h内恶心呕吐发生率。结果：术后恶心呕吐发生率试验组均明显低于空白对照组（P＜0.01）;试验组II低于试验组I（P＜0.05）。结论：格拉司琼联合甲氧氯普胺能有效预防腹腔镜胆囊切除术后恶心呕吐的发生。     

阿扎司琼应用于胸腔镜的镇吐效果评价

目的评价阿扎司琼应用于胸腔镜术后的镇吐效果。方法随机将ASAⅠ～Ⅱ120例择期行胸腔镜术后的患者分为2组(各60例):阿扎司琼(A组)于术毕静脉注射阿扎司琼10mg(2mL);胃复安(B组)于术毕静脉注射胃复安10mg(2mL)。观察术后24h内患者的恶心、呕吐情况。结果 A组恶心呕吐发生率为(10%),明显低于B组(30%),比较差异有显著意义(P<0.05)。结论阿扎司琼和胃复安均能减少胸腔镜术后的恶心、呕吐发生率,但在镇吐效果上阿扎司琼明显优于胃复安。     

格拉司琼联合阿托品预防腹腔镜胆囊切除术后恶心呕吐的护理体会

目的探讨腹腔镜胆囊切除术后格拉司琼联合阿托品预防术后恶心呕吐的护理体会。方法选择2010年9月至2012年9月期间实施腹腔镜胆囊切除术的患者120例,随机分为对照组（静脉注射生理盐水5mL）、格拉司琼组（静脉注射格拉司琼3mg）以及联合给药组（肌肉注射阿托品1mg和静脉注射格拉司琼3mg）,每组各40例,术后24h观察患者恶心、呕吐情况,并进行比较。结果与对照组（80．00％）相比,格拉司琼组术后恶心呕吐发生率（30．00％）明显降低（P〈0．05）;与格拉司琼组相比,联合给药组术后恶心呕吐发生率（10．00％）显著降低（P〈0．05）。结论格拉司琼联合阿托品能有效降低腹腔镜胆囊切除术后恶心呕吐的发生率,值得临床推广。     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Synthesis and anti-nociceptive and anti-inflammatory effects of gaultherin and its analogs

The synthesis of gaultherin (1) and its analogs was carried out to provide 11 glycosides under phase-transfer catalytic conditions. The activities of all synthesized compounds were evaluated by nitric oxide production inhibitory assay in vitro. Methyl 2-O-(4-O-β-d-galactopyranosyl)-β-d-glucopyranosylbenzoate (5f) showed significantly anti-nociceptive and anti-inflammatory effects by the evaluation in vivo. Structure–activity relationships within these compounds were discussed.     

Interaction of estrone and estradiol with DNA and protein of liver and kidney in rat and hamster in vivo and in vitro

[6,7-³H] Estrone (E) and [6,7-³H]estradiol-17 (E₂) have been synthesized by reduction of 6-dehydroestrone and 6-dehydroestradiol with tritium gas. Tritiated E and E₂ were administered by oral gavage to female rats and to male and female hamsters on a dose level of about 300 g/kg (54 mCi/kg). After 8 h, the liver was excised from the rats; liver and kidneys were taken from the hamsters. DNA was purified either directly from an organ homogenate or via chromatin. The radioactivity in the DNA was expressed in the units of the Covalent Binding Index, CBI = (mol chemical bound per mol DNA-P)/(mmol chemical administered per kg b.w.). Rat liver DNA isolated via chromatin exhibited the very low values of 0.08 and 0.09 for E and E₂, respectively. The respective figures in hamster liver were 0.08 and 0.11 in females and 0.21 and 0.18 in the males. DNA isolated from the kidney revealed a detectable radioactivity only in the female, with values of 0.03 and 0.05 for E and E₂, respectively. The values for male hamster kidney were < 0.01 for both hormones. The minute radioactivity detectable in the DNA samples does not represent covalent binding to DNA, however, as indicated by two sets of control experiments. (A) Analysis by HPLC of the nucleosides prepared by enzyme digest of liver DNA isolated directly or via chromatin did not reveal any consistent peak which could have been attributed to a nucleoside-steroid adduct. (B) All DNA radioactivity could be due to protein contaminations, because the specific activity of chromatin protein was determined to be more than 3,000 times higher than of DNA. The high affinity of the hormone to protein was also demonstrated by in vitro incubations, where it could be shown that the specific activity of DNA and protein was essentially proportional to the concentration of radiolabelled hormone in the organ homogenate, regardless of whether the animal was treated or whether the hormone was added in vitro to the homogenate.Carcinogens acting by covalent DNA binding can be classified according to potency on the basis of the Covalent Binding Index. Values of 10³–10⁴ have been found for potent, 10² for moderate, and 1–10 for weak carcinogens. Since estrone is moderately carcinogenic for the kidney of the male hamster, a CBI of about 100 would be expected. The actually measured limit of detection of 0.01 places covalent DNA binding among the highly unlikely mechanisms of action. Similar considerations can be made for the liver where any true covalent DNA binding must be below a level of 0.01. It is concluded that an observable tumor induction by estrone or estradiol is unlikely to be due to DNA binding.Paper presented at the Satellite Symposium of the European Society of Toxicology, Rome, March 29, 1983     

成骨细胞的功能与损伤和骨质疏松的防治

骨质疏松是一种全身性骨骼疾病,导致骨折风险增加。成人的骨量通过破骨细胞的骨吸收和成骨细胞的骨形成作用来维持动态平衡,治疗骨质疏松症的理想策略是抑制破骨细胞的骨吸收和/或增强成骨细胞的骨形成功能。目前针对保护成骨细胞及增强其功能的骨质疏松疗法相对较少。因此,本文针对成骨细胞相关功能蛋白、各种细胞损伤机制（内质网应激、氧化应激、机械过载、微小RNA和长链非编码RNA的影响等）及骨质疏松的治疗与预防作一综述,以期为针对增强成骨细胞功能的骨质疏松治疗策略提供新思路。     

益生菌与肿瘤防治

益生菌广泛存在于自然界中,通过维持宿主体内菌群平衡、影响肠屏障功能和调节免疫应答等作用,提高宿主健康水平,被公认为"肠道健康卫士".一些益生菌可以增强机体的免疫功能,抑制致癌物质,影响肿瘤细胞的基因表达,对肿瘤具有拮抗作用.大量研究表明,益生菌在未来的肿瘤防治中有很好的应用和发展前景.     

Modelling and simulation of variability and uncertainty in toxicokinetics and pharmacokinetics

Two important methodological issues within the framework of the variability and uncertainty analysis of toxicokinetic and pharmacokinetic systems are discussed: (i) modelling and simulation of the existing physiologic variability in a population; and (ii) modelling and simulation of variability and uncertainty when there is insufficient or not well defined (e.g. small sample, semiquantitative, qualitative and vague) information available. Physiologically based pharmacokinetic models are especially suited for separating and characterising the physiologic variability from the overall variability and uncertainty in the system. Monte Carlo sampling should draw from multivariate distributions, which reflect all levels of existing dependencies in the intact organism. The population characteristics should be taken into account. A fuzzy simulation approach is proposed to model variability and uncertainty when there is semiquantitative, qualitative and vague information about the model parameters and their statistical distributions cannot be defined reliably.     

Self-stimulation and amphetamine: Tolerance to d and l isomers and cross tolerance to cocaine and methylphenidate

The effects of the d and l isomers of amphetamine on self-stimulation responding were tested following acute and chronic administration. Tolerance and post-drug depression of responding occurred in tests with both isomers, indicating no role for p-hydroxynorephedrine (PHN) which is one of the metabolites of d-amphetamine. In the second experiment, d-amphetamine, methylphenidate and cocaine all produced quantitatively and qualitatively similar effects on self-stimulation responding following acute administration. Following chronic administration of d-amphetamine, animals showed tolerance to all three drugs, indicating cross-tolerance among them. These data are consistent with an hypothesis that tolerance and post-drug depression following chronic amphetamine treatment are the result of decreases in postsynaptic receptor sensitivity, which would lead to a decreased effectiveness of all three drugs, regardless of their pre-synaptic mechanisms.     

Short and Efficient Synthesis of Alkyl- and Aryl-Ortho-Hydroxy-Anilides and their Antibiotic Activity

Ortho-hydroxy-anilides are part of natural products like the new antibiotics platencin (A) and platensimycin (B). An important step in the total synthesis of these antibiotics or their derivatives is the preparation of the o-hydroxy-anilide partial structure. The presented method allows the preparation of o-hydroxy-anilides and o-dihydroxy-anilides from 2-nitrophenol esters in a one-step synthesis without protecting the hydroxy group. Aryl- and alkyl-anilides were prepared following this method as simple analogues of platensimycin (A). The resulting compounds were tested in an agar diffusion assay for their antibiotic potency.     

注射剂和滴眼剂中抑菌剂和抗氧剂的添加及检测

近年来随着注射剂和滴眼剂的广泛使用,由处方中抑菌剂和抗氧剂引起的不良反应已经逐步为人所知并引起药物研发人员的重视.本文就抑菌剂和抗氧剂添加的必要性、危害以及几种抑菌剂和抗氧剂的检测方法进行介绍,并提出通法检测的设想.