不同厂家盐酸氟西汀胶囊溶出度的比较

氟西汀是一种选择性5-羟色胺再摄取抑制剂（SSRI）。主要用于治疗抑郁症，此外，对强迫症、贪食症、惊恐发作和经前期焦虑障碍等也有效。固体制剂的溶出度是影响其体内生物利用度和临床疗效的主要因素。笔者选择3个厂家生产的盐酸氟西汀胶囊进行溶出度的比较，旨在考察不同厂家同类产品的内在质量，以期为国内生产厂家和临床应用提供参考。     

社交焦虑障碍的药物治疗

社交焦虑障碍是常见的焦虑障碍之一.目前临床常用治疗药物主要有选择性5-羟色胺再摄取抑制剂(SSRI)、选择性5-羟色胺和去甲肾上腺素再摄取抑制剂(SSNRI)及苯二氮(艹卓)类药物等.本文综述药物治疗近况.     

新型抗抑郁药临床应用评价

近20多年来,一系列新型抗抑郁药陆续用于临床,由于疗效确切、安全性好、不良反应少,现已成为帮助很多心理(精神)疾病患者解除痛苦的常用药物.在这些抗抑郁药中三类药物使用最多,第一类称为选择性5-羟色胺再摄取抑制剂(SSRI),产品有:氟西汀(fluoxetine)、帕罗西汀(paroxetine)、舍曲林(sertraline)、氟伏沙明(fluvoxamine)和西酞普兰(citalopram)及艾司西酞普兰(escitalopram);第二类称为5-羟色胺和去甲肾上腺素双重再摄取抑制剂(SNRI),产品有:文拉法辛(venlafaxine)和度洛西汀(dLuloxetine);第三类称为去甲肾上腺素和特异性5-羟色胺能抗抑郁剂(NaSSA),现有产品如米氮平(mirtazapine).     

LC-MS/MS法测定人血浆中帕罗西汀及其药动学

帕罗西汀（Paroxetine）属强力、高度选择性的5-羟色胺（5-HT）再摄取抑制剂。其抗抑郁作用和治疗强迫性神经症、惊恐障碍及社交焦虑症的疗效被认为与其所具有的特异性抵制脑神经的5-HT再摄取有关。     

72例惊恐障碍患者的医疗费用调查

目的 调查惊恐障碍患者的医疗费用及选择性5羟色胺再摄取抑制剂(SSRIs)帕罗西汀对惊恐障碍的疗效.方法 调查72例患者的医疗费用、病程、就诊次数、所做的主要辅助检查的种类及次数.同时用焦虑、抑郁量表观察了帕罗西汀对惊恐障碍的疗效.结果 惊恐障碍患者有较长的病程,病程中接受了很多不必要的辅助检查同时花费了大量的医疗费用.帕罗西汀能明显降低惊恐障碍患者的焦虑、抑郁的评分.结论 惊恐障碍患者在确诊前有较长的病程,花费了大量的医疗费用.帕罗西汀是一种治疗惊恐障碍的安全、有效的药物.     

氟西汀治疗高血压伴抑郁障碍的临床研究

目的评价5-羟色胺再摄取抑制剂氟西汀治疗高血压伴抑郁障碍的疗效及安全性. 方法采用随机单盲模拟对照试验,共68例高血压伴抑郁障碍患者随机分为氟西汀组与多塞平组各34例,在常规抗高血压药物治疗基础上,氟西汀组用氟西汀20mg*d -1,多塞平组用多塞平75mg*d-1,随访12周,以高血压症状计分及Zung积分减少50%或以上为治疗有效,用Zung抑郁自评量表评定疗效,治疗时出现的症状量表(TESS)评定安全性.结果氟西汀组有效率79.41%,多塞平组73.53%,2组疗效差异无显著性(P ＞0.05).起效时间氟西汀组3～4周,多塞平组6～8周,2组比较差异有显著性(P＜0 .05).不良反应发生率氟西汀组38.2%,多塞平组70.6%,2组比较差异有显著性(P＜ 0.05).结论氟西汀治疗高血压伴抑郁障碍有效且较安全.     

WHO《Signal》药物不良反应选载(7)

选择性5-羟色胺再摄取抑制剂引起高血压反应过去,英国医学会(UMC)发布的药物信息中 并未提及选择性5-羟色胺再摄取抑制剂(SSRIs)会引起高血压的不良反应.然而,美国1999出版的<医师案头参考>(PDR)中已经提到氟西汀和帕罗西汀常常会引起高血压.迄今,UMC已经收到了785份使用SSRIs期间引起高血压的报告(见表1).     

选择性5-羟色胺再摄取抑制剂的系统回顾与用药指南

选择性５－羟色胺（５－ＨＴ）再摄取抑制剂（ＳＳ－ＲＩ）用于治疗抑郁症已有１５年。最早用于临床的是齐美定（ｚｉｍｅｌｄｉｎｅ），因出现Ｇｕｉｌｌａｉｎ－Ｂａｒｒｅ综合征很快遭淘汰。尽管氯米帕明和文拉法辛有抑制５－ＨＴ再摄取的作用，但它们及其主要代谢产物也具有抑制去甲肾上腺素再摄取的作用；奈法唑酮及其代谢物有拮抗５－ＨＴ２Ａ受体的作用，但对人体５－ＨＴ的转运作用微弱。这里仅讨论５种市售的ＳＳＲＩ类药物，西酞普兰，氟西汀，氟伏沙明，帕罗西汀和舍曲林。本文系统回顾了ＳＳＲＩ药物间的各种比较研究，着重评估…     

氟西汀致全面性强直-阵挛发作1例

氟西汀(fluoxetine)是选择性5-羟色胺(5-HT)再摄取抑制剂,用于抑郁症、强迫症、神经性贪食症的治疗[1,2].过量服用氟西汀可致癫痫性大发作,但治疗量氟西汀致全面性强直-阵挛发作的病例 ,作者未见文献报道,现报道如下.     

抗抑郁药 氟西汀(Fluoxetine)

商品名 Prozac 化学名 N-甲基-3-苯基-3-(对三氟甲基苯氧基)丙胺盐酸盐药效分类抗抑郁药开发单位 (美)Eli Lilly 上市厂商 (美)Eli Lilly 药理作用本品为选择性5-羟色胺(5-HT)再摄取抑制剂。5-HT对许多疾病有作用,增强或降低5-HT功能可使某些疾病的临床症状得到改善。在含5-HT神经中,氟西汀抑制5-HT再摄取,间接地延长和增加5-HT作用,对治疗抑郁症等疾病有效。本品抑制5-HT摄取比抑制NE或多巴胺强     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.