盐酸多沙普仑的临床应用

［摘要］盐酸多沙普仑为非特异性呼吸兴奋药，能直接兴奋延髓呼吸中枢与血管运动中枢，广泛应用于兴奋中枢神经。其在临床上可作为全麻术后催醒药物，可预防术后肺部并发症，治疗术后寒战和急性中毒等，也可与麻醉性镇痛药等合用。随着对该药研究的不断深入，其在临床中的应用日益广泛。该文对盐酸多沙普仑的临床应用现状以及面临的主要问题进行综述。     

安钠咖治疗低颅压综合征4例疗效观察

安钠咖系中枢神经兴奋药.临床主要用于抢救中枢性呼吸衰竭.笔者于1998年至2002年使用安钠咖静脉注射治疗低颅压综合征4例,取得满意疗效.     

国内外咖啡因的产销分析

咖啡因是一种主要的兴奋中枢神经的药品,它能振奋精神,消除疲劳,改进思维活动,提高工作效率。较大剂量可直接兴奋延髓脑呼吸中枢及血管运动中枢,使呼吸加深、加快。本品主要用于对麻醉药、镇静催眠药的中毒和各种疾病所致的呼吸、循环衰竭等疾患的抢救。据美国食品研究所的专家检测,它与肿瘤发生无关。据报道,     

呼吸兴奋药──多沙普仑投入生产

呼吸兴奋药──多沙普仑投入生产多沙普仑（ｄｏｘａｐｒａｍ）为非特异性呼吸兴奋药，主要作用于颈动脉和主动脉化学感受器，增加剂量时，可兴奋呼吸中枢，近年来列入颈动脉窦兴奋药类，能明显增加潮气量和呼吸频率。国内临床应用于处理麻醉引起的呼吸抑制，术后催醒和中...     

减肥药氟苯丙胺试制成功

氟苯丙胺(Fenfluramine)是近年来国外文献报道中比较成熟和效果较为理想的减肥药。减肥效果明显,一般于服药后每星期可减轻体重2磅左右。副反应如厌食等较小。它不具有中枢神经兴奋作用,高血压和糖尿病患者也可应用。据国外生产厂报道,经临床使用九百多万病例,未见有成瘾性报道。     

何谓促进智能药物?怎样进行药理学研究?

<正> 促进智能药物(nootropic drug)是指选择性作用大脑皮质,具有激活、保护和促进受损神经细胞功能恢复的一类药物(如Piracetam、Oxiracetam和Vin-camina等。其对中枢神经系的作用并不是通过网状系统和嗅脑,而是直接对大脑皮质产生作用的。它们不影响行为、也无镇静或兴奋作用。因此,促进智能药物有可能作为一类新颍的第六类精神药物位于精神抑制药(安定药)、抗抑郁药、抗焦虑药、精神兴奋药和致幻药等五类经典精神药之后。这类药物是通过对脑细胞中生物能量代谢(葡萄糖、ATP、蛋白质、RNA和类脂)的同化作用,改善与精神功能(记忆、学习和回答问题)相关的脑整合机理。它们的作用不是如精神兴奋药那种短暂的中枢兴奋作用,而是一种较持     

尼可刹米呼吸兴奋作用机制的探讨

研究了尼可刹米、戊四唑、洛贝林对乌拉坦麻醉猫、兔在几种不同给药途径时兴奋呼吸的阈量。在猫、尼可刹米静脉注射兴奋呼吸的阈量平均为24.9 mg/kg,椎动脉注射阈量为静脉量的1/35,窦区局部给药阈量约为静脉量的1/6。戊四唑静脉注射兴奋呼吸的阈量平均为8.5mg/kg,椎动脉注射阈量约为静脉量的1/4.5,窦区局部给药阈量约为静脉量的1/3,但部分动物在5 mg/kg时抑制呼吸。洛贝林静脉注射兴奋呼吸的阈量为0.5 mg/kg,椎动脉注射阈量为静脉量的1/10,但半数动物呈呼吸抑制反应,窦区局部给药阈量约为静脉量的1/8.5。 在兔,尼可刹米静脉注射兴奋呼吸的阈量平均为40.8 mg/kg,椎动脉注射阈量约为静脉量的1/10,窦区局部给药阈量约为静脉量的1/8,但有较多的动物反呈呼吸抑制反应。 戊四唑静脉注射兴奋呼吸的阈量为14.9 mg/kg,椎动脉注射阈量约为静脉量的1/3,窦区给药则多数动物呈现呼吸抑制反应。 洛贝林静脉注射兴奋呼吸的阈量为2.2 mg/kg,椎动脉注射阈量为静脉量的1/8。窦区局部给药阈量约为静脉量的1/6。 从以上结果,我们认为尼可刹米和戊四唑一样主要是兴奋呼吸中枢,但在较大剂量时也可观察到尼可刹米通过窦区反射性地兴奋呼吸。而一般认为主要是作用于颈动脉体反射性兴奋呼吸的洛贝林,似亦有中枢机制同时存在。     

尼可刹米呼吸兴奋作用机制的探讨

研究了尼可刹米、戊四唑、洛贝林对乌拉坦麻醉猫、兔在几种不同给药途径时兴奋呼吸的阈量。在猫、尼可刹米静脉注射兴奋呼吸的阈量平均为24.9 mg/kg,椎动脉注射阈量为静脉量的1/35,窦区局部给药阈量约为静脉量的1/6。戊四唑静脉注射兴奋呼吸的阈量平均为8.5mg/kg,椎动脉注射阈量约为静脉量的1/4.5,窦区局部给药阈量约为静脉量的1/3,但部分动物在5 mg/kg时抑制呼吸。洛贝林静脉注射兴奋呼吸的阈量为0.5 mg/kg,椎动脉注射阈量为静脉量的1/10,但半数动物呈呼吸抑制反应,窦区局部给药阈量约为静脉量的1/8.5。在兔,尼可刹米静脉注射兴奋呼吸的阈量平均为40.8 mg/kg,椎动脉注射阈量约为静脉量的1/10,窦区局部给药阈量约为静脉量的1/8,但有较多的动物反呈呼吸抑制反应。戊四唑静脉注射兴奋呼吸的阈量为14.9 mg/kg,椎动脉注射阈量约为静脉量的1/3,窦区给药则多数动物呈现呼吸抑制反应。洛贝林静脉注射兴奋呼吸的阈量为2.2 mg/kg,椎动脉注射阈量为静脉量的1/8。窦区局部给药阈量约为静脉量的1/6。从以上结果,我们认为尼可刹米和戊四唑一样主要是兴奋呼吸中枢,但在较大剂量时也可观察到尼可刹米通过窦区反射性地兴奋呼吸。而一般认为主要是作用于颈动脉体反射性兴奋呼吸的洛贝林,似亦有中枢机制同时存在。     

多沙普仑用于全麻术后催醒的临床观察

多沙普仑又名吗苯哌酮,为一非特异性呼吸兴奋药,多沙普仑有可靠的呼吸兴奋作用和安全范围大的特点,临床效果显著[1].国产多沙普仑近年开始推广使用,我们将其用于全麻术后催醒,取得明显效果,现报告如下.     

呼吸兴奋药──佳苏仑投入批量生产

呼吸兴奋药──佳苏仑投入批量生产本刊特约通讯员张玉玲佳苏仑（盐酸多沙普仑）原料药及其注射液日前由江苏徐州第三制药厂投入批量生产。佳苏仑为一非特异性呼吸兴奋药，主要作用于颈动脉和主动脉化学感受器，当剂量增加时，可兴奋呼吸中枢。近年列入颈窦兴奋药一类。它...     

Possible role of brain dopaminergic systems in the memory effects of central stimulants

In experiments on male Wistar rats trained and tested for memory retention on an active avoidance task in a maze, it was found that haloperidol at doses of 0.2 and 2 mg/kg injected intraperitoneally one hour prior to or immediately after training impaired learning and/or memory. The central stimulants caffeine (20 mg/kg), strychinine (1 mg/kg) and amphetamine (1 mg/kg) injected intraperitoneally immediately after training improved long-term retention; the central stimulants administered at the same doses but in combination with haloperidol (2 mg/kg) after training did not manifest their retention-facilitating effect. It is assumed that dopaminergic mechanisms underlie learning and memory processes in active avoidance conditioning and that an optimum activity of these mechanisms is necessary for the memory-facilitating effect of the central stimulants to appear.     

Pharmacological treatment of ADHD and the short and long term effects on sleep

There is growing research focusing on the sleep problems of children with attention-deficit/hyperactivity disorder (ADHD) in recent years. High incidence of sleep disorders in children with ADHD may be associated with a substantial impact on their quality of life and exacerbation of ADHD symptoms. The core symptoms of ADHD can be effectively treated by various medications, including methylphenidate (MPH), amphetamine, pemoline, and the newly FDA-approved extended-release α2 adrenergic agonists. However, most of them are known to affect patients' sleep because of their pharmacological actions on dopaminergic and/or noradrenergic release in the central nervous system. Previous studies have found increased incidence of insomnia and sleep disturbances in ADHD children treated with CNS (central nervous system) stimulants. In contrast, recent prospective, double-blind, placebo-controlled trials concluded that MPH, by objective polysomnographic or actigraphic measurements, did not cause significant sleep problems in children or adolescents with ADHD. Given the fact that sleep quality and core symptoms of ADHD are highly correlated, it is imperative that we understand the effects of ADHD medications on sleep while prescribing either CNS stimulants or non-CNS stimulants. Here we will concisely review the pharmacological treatments of ADHD, and provide the relevant data discussing their short- and long-term effects on sleep.     

小剂量甲强龙联合呼吸兴奋剂在治疗慢性阻塞性肺疾病合并呼吸衰竭中的疗效评价

目的：分析小剂量甲强龙对慢性阻塞性肺疾病合并呼吸衰竭患者的治疗效果和并发症情况。方法分析2010年3月至2015年10月接收的85例慢性阻塞性肺疾病合并呼吸衰竭患者临床相关资料,根据患者治疗方法不同,分为甲强龙组(40例)和对照组(45例),治疗组为小剂量甲强龙(40 mg)+呼吸兴奋剂(可拉明0.75 mg+洛贝林6 mg),对照组为单纯使用呼吸兴奋剂(可拉明0.75 mg+洛贝林6 mg),分析2组患者心率、呼吸等相关指标。结果2组患者治疗结束后,心率和呼吸指标、氧分压、二氧化碳分压等血气指标、FEV1/FVC和FEV1占预计值肺功能指标、肺动脉压及C反应蛋白的水平较治疗前均改善,甲强龙组显著优于对照组( P <0.05)。甲强龙组总有效率为92.3%显著高于对照组的74.3%( P <0.05)。结论小剂量甲强龙在慢性阻塞性肺疾病合并呼吸衰竭患者的治疗中疗效显著,主要体现在其对患者的心率和呼吸指标的改善,血气和肺功能、肺动力水平的提高,C反应蛋白水平的降低,对于无禁忌证的慢性阻塞性肺疾病患者来说,甲强龙在治疗中值得推荐应用。     

Addictiveness of Central Stimulants

Central stimulants have been abused since their inception and we are currently in the midst of a cocaine epidemic that challenges our resources and capabilities. Through their actions on powerful endogenous reward centers, central stimulants produce intense euphoria that reinforces subsequent usage and eventual dependence. Considerable evidence indicates that the activation of dopamine circuits mediates stimulant reward. With regard to cocaine, it has been hypothesized that depletion of central dopamine leads to craving. Euphoria and craving, the key dynamics of stimulant addiction, may therefore result largely from neurochemical alterations of dopamine systems in the brain's reward center. Progressive deterioration of the stimulant addict involving medical, psychiatric, and psychosocial impairment occcurs rapidly, underscoring the addiction potential of these agents. Tolerance, sensitization and withdrawal phenomena are discussed from clinical and neurochemical perspecitives.     

Effects of caffeine and doxapram perfusion on local cerebral glucose utilization in conscious rats

The quantitative autoradiographic 2-[14C]deoxyglucose method was used to measure the effects of a continuous infusion of the respiratory stimulants, caffeine or doxapram, 18 mg/kg per h, on local cerebral glucose utilization in the adult male rat. Local cerebral glucose utilization was measured in 54 cerebral structures from different systems. Caffeine induced widespread increases in energy metabolism, resulting in a significant increase in glucose utilization in 25 structures out of the 54 studied. These increases were distributed within all systems studied, sensory, extrapyramidal motor, limbic and hypothalamic systems. In addition, caffeine induced a non-significant, 10-15%, increase in local cerebral glucose utilization in central respiratory areas. Doxapram infusion did not change the rates of glucose utilization in any of the structures. The rates of local cerebral glucose utilization were significantly lower after doxapram than after caffeine exposure in five cerebral areas, among which were three central respiratory areas. The results confirm the absence of side-effects of doxapram as compared to caffeine when used as respiratory stimulant, especially in neonates. These results also favor a preferentially central action of caffeine on respiratory areas and a more peripheral action of doxapram on chemoreceptors, at least at therapeutic levels.     

The inhibition of amine oxidase and the central stimulating action of the stereoisomeric amphetamines and 1-phenylethylamines

The stereoisomers of amphetamine and 1-phenylethylamine have been studied in the rat both as central stimulants and as inhibitors of amine oxidase from brain, liver, and kidney. There was no correlation between these two effects; thus it is unlikely that the central stimulating action of amphetamine is due to inhibition of amine oxidase.     

苯丙胺类兴奋剂所致精神障碍临床特征及治疗分析

目的：总结苯丙胺类兴奋剂所致精神障碍的临床特征及治疗。方法：对120例符合CCMD-3诊断标准的苯丙胺类兴奋剂所致精神障碍患者进行临床特征及治疗的总结和分析。结果：滥用苯丙胺者以青少年居多,男女性别差异不大,文化素质普遍偏低,职业以无业和个体为主。常见临床表现为心慌烦躁、兴奋、发热、血压升高、抑制、消瘦、性欲亢进、食欲下降、抑郁、激越和精神病症状,部分病人有口腔和鼻粘膜溃疡、震颤、行走不稳和肌张力增高等类帕金森氏病样症状等。治疗以对症治疗为主,但类帕金森氏病样症状治疗效果不佳。结论：苯丙胺类兴奋剂是一类对生理和心理有显著伤害的中枢兴奋剂,治疗以对症治疗为主,并辅以心理治疗,总体疗效尚佳。     

Antihypertensive drugs interacting with central imidazoline (I1)-receptors

Central imidazoline (I(1))-receptors have been recognised as targets of a new class of centrally acting antihypertensives. The stimulation of these I(1)-receptors induces peripheral sympatho-inhibition and a reduction of (elevated) blood pressure. Moxonidine and rilmenidine are the prototypes of this new class of centrally acting antihypertensives. These imidazoline receptor stimulants are effective antihypertensives with a haemodynamic profile which is attractive from a pathophysiological point of view. Since both moxonidine and rilmenidine have a much weaker affinity for central (2)-adrenoceptors than classic centrally acting drugs, for example, clonidine and alpha-methyl-DOPA, the side-effects profile of the I(1)-receptor stimulants is significantly better. The imidazoline (I(1))-receptor stimulants are the subject of the current survey. They appear to offer the possibility of developing centrally acting antihypertensives with the same attractive haemodynamic characteristics as the classic alpha(2)-adrenoceptor stimulants, but with clearly better tolerability. Their potential use in the treatment of congestive heart failure and the metabolic syndrome is subject to clinical investigation.     

Montelukast: new preparation. No current use in asthma

(1) Montelukast, an antiasthmatic drug belonging to the leukotriene antagonist family, has two indications in France: as adjunctive treatment for mild to moderate chronic asthma when regular inhaled steroid therapy and short-acting inhaled beta 2 stimulants "on demand" are inadequate; and in the prevention of effort-induced asthma. (2) The clinical file on montelukast contains no methodologically acceptable comparisons with reference treatments. (3) Several placebo-controlled trials have shown the efficacy of montelukast, with an improvement in clinical scores and respiratory function tests in chronic asthma; and prevention of effort-induced asthma. (4) In chronic asthma montelukast has not been compared with oral or inhaled long-acting beta 2 stimulants, or with sustained-release theophylline in patients inadequately controlled by steroid therapy. (5) In effort-induced asthma, only two trials have compared montelukast to salmeterol. On the basis of preliminary results the authors concluded that montelukast was superior in both studies. (6) Clinical trials showed no clear difference in the frequency of side effects in patients on montelukast and those on a placebo. However, montelukast may possibly be associated with the Churg and Strauss syndrome in rare cases. (7) Montelukast is an expensive drug.     

Mefenorex (Rondimen)

Mefenorex, N-(3-chloropropyl)-alpha-methylphenethylamine, (RONDIMEN), is included in the list of centrally acting stimulants and/or hallucinogens or related compounds to be considered by a World Health Organization (WHO) Expert Committee in 1985 for possible scheduling under the Convention on Psychotropic Substances, 1971. The therapeutic efficacy of mefenorex as an adjunctive support in the treatment of obesity for limited periods of time, as well as its ability to be well tolerated, has been amply demonstrated. There have been no reports of actual abuse. There have been no reports of illicit trafficking, falsification of packages or materials, or clandestine laboratories manufacturing the compound. Data from preclinical and clinical studies do not suggest a potential for abuse similar to that of amphetamine or related compounds. Moreover, the lack of pulmonary hypertension with mefenorex has been demonstrated in both preclinical and clinical studies. There have been no reports of any public health or social problems associated with mefenorex use. The compound is a well-tolerated anorectic agent with little central stimulant activity.