羟丙甲纤维素和聚维酮对氯硝西泮与羟丙基-β-环糊精包合作用的影响

采用相溶解度法考察羟丙甲纤维素（HPMC）和聚维酮（PVP）对水溶液中氯硝西泮与羟丙基-β-环糊精（HP-β-CD）包合作用的影响。以UV法测定氯硝西泮在溶液中的浓度。无论水溶液中是否存在HP—β—CD，PVP均能增加氯硝西泮的溶解度（P〈0．01）：HPMC作用不明显。     

丁螺环酮与氯硝西泮治疗焦虑症对照研究

目的比较丁螺环酮与氯硝西泮治疗焦虑症的效果。方法对68例焦虑症病人，随机分组丁螺环酮组38例，氯硝西泮组30例。结果丁螺环酮与氯硝西泮对焦虑的疗效无明显差异，治疗第8周，两组不良反应相仿。结论丁螺环酮治疗焦虑症，不良反应少，是一种安全有效的抗焦虑药。     

坦度螺酮与氯硝西泮治疗广泛性焦虑症的疗效分析

目的探讨坦度螺酮与氯硝西泮治疗广泛性焦虑症的疗效差异。方法 80例广泛性焦虑症患者随机分为观察组和对照组。观察组患者给予坦度螺酮治疗,对照组给予氯硝西泮治疗。疗程为4周。观察两组疗效。治疗前和治疗后采用汉密尔顿焦虑量表评分。观察两组不良反应发生情况。结果观察组患者总有效率(87.5%)和对照组总有效率(90.0%)比较,差异无统计学意义(P>0.05);观察组患者治疗后的汉密尔顿焦虑量表评分和对照组患者治疗后的汉密尔顿焦虑量表评分比较,差异无统计学意义(P>0.05)。观察组不良反应发生率低于对照组,差异有统计学意义(P<0.05)。结论坦度螺酮与氯硝西泮治疗广泛性焦虑症均有较好疗效,但坦度螺酮的不良反应少于氯硝西泮。     

高效液相色谱法测定病儿氯硝西泮的血药浓度

目的 :建立测定血清中氯硝西泮血药浓度的高效液相色谱 (HPLC)法。方法 :血清中的氯硝西泮在弱碱性条件下经叔丁基甲醚提取 ,以α 溴苯乙酮为内标 ,流动相为甲醇∶乙腈∶正己烷 (5 5∶10∶35 ) ,紫外检测波长 2 30nm的RP/C18 HPLC测定。结果 :在 5～ 10 0 0 μg·L- 1范围内 ,氯硝西泮和内标的峰面积之比与浓度呈良好的线性关系 ,r =0 .9995 ,平均回收率大于 97% ,日内和日间RSD <5 %。结论 :采用反相HPLC法准确、灵敏、简便 ,适用于氯硝西泮的血药浓度测定及临床药动学研究。     

本期新旧药名对照

<正> amiodarone胺碘酮(乙胺碘呋酮、安律酮,Atlansil, Cordarone, Trangorex, Tranquerone); atenolol阿替洛尔(氨酰心安、苯氧胺,Tenormin);bezafibrate苯扎贝特(降脂苯酰、必降脂,Bezalip);captopril卡托普利(巯甲丙脯酸、甲巯丙脯酸,Capoten, Lopirin, SQ-14225); chlorphenamidine氯苯甲脒(氯苯脒、杀虫脒、克死螨、氯二甲甲脒);cimetidine西咪替丁(甲氰咪胍、甲腈咪胍、甲腈咪胺);cinnarizine桂利嗪(桂益嗪、肉桂苯哌嗪、脑益嗪,Midronal),clonidine可乐定(氯压定、可乐宁、可乐亭、血压得平、110降压片、压泰生、催压降,Catapres, Catapresan); debrisoquine异喹胍(胍哇定,Declinax, Equifen     

迟发性运动障碍的药物治疗进展

本文报告迟发性运动障碍应用维生素Ｅ、氯硝西泮、苯妥英钠、氯氮平、左旋千金藤立定、硝苯地平、泰必利、丁螺环酮诸药的治疗进展。     

抗寄生虫药物临床应用近况

介绍几种药物－－复方阿苯达唑、蒿甲醚联合甲氟喹、哟喹酮，甲苯达唑在临床抗寄生虫方面的应用及疗效。     

本期新旧药名对照

<正> amiodarone胺碘酮(乙胺碘呋酮、安律酮,Co-rdarone);anagrelide阿那格雷(氯咪喹酮);brom-ocriptine溴隐亭(溴麦亭、溴麦角隐亭、溴麦角环肽);captopril卡托普利(甲硫丙脯酸、巯甲丙脯酸,Capoten,Lopirin,SQ-14225);carbamazepine卡马西平(痛惊宁、痛可宁、立痛定、退痛、痛痉宁、叉颠宁、氨甲酰苯(艹卓)、酰胺咪嗪、卡巴咪嗪,Finlepsin,Neurotol,Stazepine,Tegretol);carbidopa卡比多巴(甲基多巴肼、卡别多巴,α-methyldopa hy-drazine,MK-485,HMD,Hydrazinomethyldopa,     

氯硝西泮与盐酸氯丙嗪治疗酒依赖的对照研究

氯硝西泮与盐酸氯丙嗪对照治疗酒依赖者 70例 ,每组各 3 5例。治疗期间 ,两组戒断症状均在 1 0天内消失。两药相比 ,氯硝西泮治疗起效迅速 ,副反应较盐酸氯丙嗪轻、少。氯硝西泮系苯二氮类药物 ,虽可能产生依赖 ,但未见数日内应用氯硝西泮产生依赖的临床报道 ,故临床上对酒依赖治疗可推广应用     

1989年美国FDA批准的新药

1989年美国FDA共批准23种新药上市,复审时间8～77个月。3个产品:盐酸氯米帕明、氯扎平、盐酸甲氟喹被FDA 评为最高等级1A 级,说明这些药品获得重要的疗效。3个是罕用药品,即甘西克洛维钠(ganciclovir sodium,DHPG)、盐酸司立吉林、甲氟喹。23种新药及其用途如下:·腺苷,Lyphomed、Medco Research 产,商品名Adenocard,用于治疗阵发性室上性心动过速。·盐酸氯米帕明(clomipramine HCl),     

Anticonvulsant activity of a new 1,4-benzodiazepine in rodents and the baboon Papio papio

RU 31124, a new anticonvulsant 1,4-benzodiazepine was compared with clonazepam in a series of tests in rats and mice. It demonstrated greater anticonvulsant potency whilst having equivalent sedative properties to clonazepam. This profile of activity was confirmed in the photosensitive baboon, Papio papio, in which RU 31124 provided long-lasting protection against convulsions at doses having little or no sedative side effects.     

Involvement of the "peripheral" benzodiazepine receptor type (omega 3) in the tolerance to the electroencephalographic effects of benzodiazepines in rats: comparison of diazepam and clonazepam

Rapid tolerance to the sedative effect of large doses of diazepam (10 mg/kg IV), but not of large doses of clonazepam (2 mg/kg IV) occurs in rats after 5 days of treatment on a once-a-day regimen. Electroencephalographic (EEG) studies show that such behavioral tolerance is associated with a decreased induction of spindle bursts and with an increased induction of 20-30 Hz waves (beta-like activity). Administration of clonazepam plus the agonist of the "peripheral" benzodiazepine receptor type (omega 3) Ro 5-4864 (4 mg/kg IV) for 5 days induces signs of behavioral and EEG tolerance to sedative effects of the benzodiazepine agonist. In animals treated for 5 days with diazepam plus the omega 3 antagonist PK 11195 (5 mg/kg IV), no signs of EEG and behavioral tolerance are observed. These results suggest that omega 3 type activation influences the development of rapid tolerance to the sedative effect of diazepam in rats.     

临床合并应用镇静催眠药对阿司匹林酯酶活性的影响

目的探讨镇静催眠药(咪达唑仑、苯巴比妥和氯硝西泮)对阿司匹林酯酶活性的影响,指导阿司匹林临床个体合理化给药,保证用药的安全性。方法采用高效液相色谱法测定培养体系中阿司匹林(ASA)和水杨酸(SA)的浓度,以CSA/(CASA+CSA)比值反应阿司匹林酯酶的活性。通过在培养体系中加入或不加咪达唑仑、苯巴比妥和氯硝西泮时阿司匹林酯酶活性的变化,分析上述镇静催眠药对阿司匹林酯酶活性的影响。结果咪达唑仑对阿司匹林酯酶活性有一定的抑制作用,抑制率为27.94%(P<0.05),苯巴比妥和氯硝西泮对阿司匹林酯酶活性有一定的增强作用,增强率分别为8.83%(P<0.05)和0.66%(P>0.05)。结论咪达唑仑、苯巴比妥与阿司匹林合用时应注意药物间的相互作用。     

Comparative characteristics of the psychotropic activity of "atypical" tranquilizers in an experiment

Experiments on animals were made to study pharmacological activity of "atypical" tranquilizers (nitrazepam, flunitrazepam, clobasam, tacitin, clonazepam, depakin) according to the classical methods for determination of pharmacological activity of typical anxiolytics. As regards the spectrum of pharmacological activity, "atypical" tranquilizers differ from classical anxiolytics. The anxiolytic effect exhibited by the latter group drugs with the exception of clonazepam develops in the presence of the sedative manifestations. The data obtained attest to the necessity of a comprehensive methodological approach to the assessment of "atypical" tranquilizers.     

不同剂量氟伐他汀调整高脂血症疗效比较

目的 :研究不同剂量氟伐他汀调整高脂血症的疗效及不良反应。方法 :氟伐他汀 4 0mgq .n .组 37例 ,2 0mgq .n .组33例 ,服药 4周。结果 :4 0mg组服药后血清总胆固醇降低32 .4 % ,2 0mg组降低15 .7% ,P <0 .0 5。两组降低甘油三酯及升高高密度脂蛋白胆固醇的差异不显著。结论 :氟伐他汀 4 0mgq .n .降低血清总胆固醇的作用明显优于氟伐他汀 2 0mgq .n .。     

Effect of piracetam on urea-induced myoclonus in rats]

Piracetam [2-oxo-1-pyrrolidineacetamide], a cyclic GABA, has been used in Europe for the treatment of patients with cognitive disorders. We investigated the effect of piracetam on urea-induced myoclonus in rats. Myoclonus was induced by intraperitoneal injection of 4.5 g/kg urea, and was recorded with EMG and video apparatus. The incidence of induced myoclonus decreased significantly by intraperitoneal injection of 300 mg/kg piracetam and oral administration of 0.3-10 mg/kg clonazepam. Furthermore, the combined application of 100 mg/kg piracetam and 0.03-0.1 mg/kg clonazepam was effective in ameliorating the myoclonus, although separate administrations were not effective. These findings suggest that piracetam is an effective drug for treating myoclonus, particularly when it is used in combination with clonazepam.     

2007—2012年天津医科大学第二医院口服镇静催眠药应用分析

了解2007-2012年我院口服镇静催眠药的使用情况及用药趋势,为临床合理用药提供依据。方法：根据我院医院信息系统（CHIS）中2007-2012年口服镇静催眠药的原始数据资料,采用世界卫生组织（WHO）推荐的限定日剂量（DDD）分析法,对各年口服镇静催眠药的销售金额、用药频度（DDDs）、限定日费用（DDC）等进行比较分析。结果：2007-2012年我院口服镇静催眠药的销售金额和DDDs基本呈增长趋势,DDC稳中有降。艾司唑仑、劳拉西泮、氯硝西泮等苯二氮蕈类药的DDDs均较高,以唑吡坦为代表的新型非苯二氮革类药用量增长迅速。结论：我院口服镇静催眠药应用基本合理,其中苯二氮革类药占主导地位,新型非苯二氮革类药用量也有逐年上升趋势,前景广阔。进一步加强精神药品的监督管理仍是今后工作的重点。     

舒眠胶囊中非法添加氯苯那敏的检测方法研究

目的:建立舒眠胶囊中非法添加氯苯那敏的检测方法。方法:采用LC-MS/MS筛查非法添加镇静催眠药地西泮、氯硝西泮、艾司唑仑为阴性。一级质谱扫描图检出几个未知成分大峰,通过GC-MS法谱库检索推测出含有违法添加氯苯那敏,用马来酸氯苯那敏对照品进行确证。结果:应用本法检测出舒眠胶囊中违法添加的马来酸氯苯那敏每粒含2.7mg。结论:该法简便、快捷,灵敏度高、专属性强,可作为检测中药制剂及保健食品中非法掺入化学药马来酸氯苯那敏的有效手段。     

Clonazepam in the treatment of protracted depression: a hundred-case report]

Clonazepam, which presently is recommended for the treatment of seizure disorders, has been reported to be useful as an adjunctive treatment for depression. The purpose of this paper was to examine the suitable adjunctive dose and the characteristics of clonazepam for the treatment of protracted depression. A hundred protracted depressive patients treated with clonazepam were studies by the retrospective method. A daily dose of 3.0 mg clonazepam as augmentation expressed high effectiveness (78.4%) on protracted depression. Most of the improved patients showed a rapid onset of action within two weeks. Gender, age, phase number, family history of psychosis, and clinical symptoms did not change the effectiveness of clonazepam treatment. A daily dose of at least 3.0 mg clonazepam as augmentation of ongoing antidepressant treatment should be considered for protracted depressive patients with suboptimal improvement. Unipolar depression was significantly more effective than bipolar depression on clonazepam treatment. The clear-cut difference in response to unipolar and bipolar depression suggests that the underlying abnormality in unipolar depression is not the same as that in bipolar depression. A continuance of clonazepam after improvement disturbed the recurrence of depression, and it seems that clonazepam augmentation has a preventive effect.     

The pharmacological profile of chlordesmethyldiazepam and other benzodiazepines

The pharmacological profile of chlordesmethyldiazepam was studied in mice and compared with that of other benzodiazepines (diazepam, lorazepam, clonazepam, nitrazepam, oxazepam, flunitrazepam, medazepam and chlordiazepoxide). All the drugs were administered perorally and their anticonvulsive activity (antagonism towards pentetrazole-induced clonic convulsions), anxiolytic action (the four-plate test), myorelaxant activity (the rota-rod test), sedative effect (inhibition of the locomotor activity) and neurotoxic effect (abolition of the righting reflex) were estimated. Chlordesmethyldiazepam revealed an anticonvulsive action (ED50 = 0.11 mg/kg), anxiolytic activity (MED = 2 mg/kg), myorelaxant action (ED50 = 17.5 mg/kg), sedative effect (ED50 = 34 mg/kg) and neurotoxic action (NTD50 = 190 mg/kg). Considering the potency of action (ED50) in respective tests and the therapeutic indices (NTD50/ED50 ratio), chlordesmethyldiazepam in respect of its profile resembles most lorazepam and diazepam.