洋地黄类药物的相互作用与合并用药

洋地黄类药物的相互作用与合并用药蔡志坚（江苏省句容县人民医院２１２４００）洋地黄类药物是具有正性肌力作用的强心甙，目前最常用的是地高辛、西地兰和毒毛旋花子甙等。本文就临床常用的洋地黄类药物与其它药物配伍时的相互作用重点叙述如下。１影响洋地黄类在胃肠道...     

心得安合并用药的相互作用

心得安是临床常用的β-受体阻滞剂。它与其他药物并用时,有的可产生协同作用,增强疗效,有的则产生不良反应。现综述如下:1.与血管扩张药及噻嗪类利尿药伍用。单独用心得安降压效果为52～65%,且可     

心得安合并用药的相互作用

药物相互作用在临床工作中甚为重要,两种或两种以上的药物合用,可能出现协同作用,也可能出现拮抗作用。如不熟悉药物的相互作用,会给病人造成危害。笔者根据国内外有关文献,浅谈一下有关心得安合并用药的相互作用,以供同道们参考。     

合并用药的定量分析

鉴于对合并用药后果的定义和计算存有争议[1]，本文先规定了各种合并用药后果的定义，然后简评几种有代表性的计算方法，最后提出建议公式。1关于合并用药后果的定义我国高等医药院校统编教材《药理学》对协同作用（synergism）;桔抗作用（antagonism）有明确的定义[2]。协同有增强和相加之区别[3]。增强（Potentiation，potentialization或supra-addition）指联用后的效应大于各药单用之和（有不少学者将此称为协同）;若等于各药效应之和则为相加（addition）。但药理学教科书的这一定义未指明联合用药后，是某一药物还是所有合用药物的作…     

抗生素联合用药中药物的相互作用

抗生素是临床上最常用的处方药,而抗生素的联合用药在临床上也比较常见。它主要用于增强药物的抗菌活动,扩大抗菌谱,减少微生物耐药性的产生,由于各种抗生素有不同的作用机理,因此各种药物可发生明显的相互作用,包括药物配伍禁忌,抗菌活性的增强和拮抗作用,药代动力学的改变和药效学反应的改变。药物间相互作用的临床重要性可随药物剂量,给药途径,给药时间,疗程及患者的基础疾患或药物遗传等而变化,抗生素的联合应用也可增加药物的不良反应或抗菌拮抗作用。     

环丙沙星合并用药之相互作用

环丙沙星合并用药之相互作用刘洪云王海波（山东省五莲县人民医院２６２３００）刘涛（山东省潍坊市立第二医院）环丙沙星（Ｃｉｐｒｏｆｌｏｘａｃｉｎ，ＣＰＦＸ）属第三代氟喹诺酮类抗菌药，对各种革兰阴性、革兰阳性菌均有较强的抗菌作用。本文仅就其药物的相互作用加...     

抗生素在联合用药中的相互作用

在临床实践中，由于合并多种药物治疗或先后次序使用，因药物间的相互作用，可导致药物的作用和效应发生变化。可使作用增强或减弱，作用的持久性也可以延长或缩短，其后果可以表现为有益的的治疗作用，也可以表现为有害的不良反应。     

药物相互作用在评价合理用药中的意义

<正>目前,临床用药几乎不存在一次只用一种药物的情况,合并用药的核心是增强药效,减少用量及不良反应,降低副作用,随着多种药物合用病例数的增加,药物不良反应率也在迅速上升,其中药物相互作用是药物不良反应和毒性反应的重要原因。因此,研究药物的相互作用对评价合理用药更有指导意义。     

对100例临床用药中不良相互作用的分析

为了更好地协助临床医生合理、安全地使用药物,我们对本院内科病房100例患者的临床用药做了随机调查分析,现阐述如下:在100名患者中,主要是心血管系统和呼     

尿中普萘洛尔对映体葡醛酸苷的HPLC测定

建立了人尿中普萘洛尔对映体葡醛酸苷无需水解、直接测定的HPLC法.采用生物合成获得普萘洛尔葡醛酸苷,并经C18固-液萃取纯化、浓集,作为对照品储备液.采用荧光检测器,激发波长和发射波长分别为310和339nm.线性范围0.0232～5.8μmol/L,r=0.9999.平均回收率为99.8%±5.01%,日内和日间精密度分别小于1.08%和2.86%.     

Propranolol pharmacokinetics and pharmacodynamics after single doses and at steady-state

Summary The duration and extent of cardiac beta-blockade and their relationship to propranolol pharmacokinetics were assessed in nine healthy volunteers. Each subject received 160 mg of regular propranolol (R), 160 mg of sustained-release propranolol (SR) and no drug (control), both as single doses and once daily for 7 days.After single doses and at steady-state, both products caused a decrease in exercise heart rate for at least 24 h, compared to control. The time course of effect was similar to the time course of serum propranolol concentration. The oral clearance of propranolol decreased from single doses to steady-state for both R and SR; however, the difference achieved statistical significance only for R. These changes were reflected in mean accumulation ratios (AUC steady-state 0–24 h/AUC single dose 0-infinity) of 1.49 and 1.68 for R and SR, respectively.The pharmacokinetic data are consistent with a decrease in intrinsic hepatic clearance of propranolol, leading to an increase in bioavailability at steady-state. Despite a two-fold difference in the bioavailability of R and SR, there was no difference in the area under the effect-time curve at steady-state.Presented in part at the IIIWorld Conference on Clinical Pharmacology and Therapeutics, Stockholm, Sweden, July 1986     

新药生殖毒性试验规范性操作介绍

生殖毒性试验是毒理学试验中较为复杂和繁琐、技术要求较高的试验。现从实验技术人员资质要求、试验前准备、试验期观察、试验记录、供试品、对照品的配制和给予、亲本动物的剖杀和检查、与专题负责人沟通确认等方面介绍作为技术人员如何做好安全性评价中的生殖毒性试验工作。     

普萘洛尔与维拉帕米治疗药物性窦性心动过速的比较

目的：用双盲对照法比较普萘洛尔与维拉帕米治疗抗精神病药所致窦性心动过速（简称窦速）的疗效。方法：因服抗精神病药物后引起窦速１００例，分为甲、乙２组。甲组５０例（男性３１例，女性１９例；年龄３２±ｓ１３ａ）采用普萘洛尔１０ｍｇ，ｐｏ，ｔｉｄ×２ｗｋ．乙组５０例（男性３１例，女性１９例；年龄３３±１２ａ）采用维拉帕米２０ｍｇ，ｐｏ，ｔｉｄ×２ｗｋ。结果：甲组痊愈４３例，有效７例；乙组痊愈１９例，有效２１例，无效１０例，经Ｒｉｄｉｔ分析法统计，Ｐ＜０．Ｏ５；２组均无明显不良反应。结论：治疗抗精神病药物性引起的窦速普萘洛尔优于维拉帕米。     

Sustained Propranolol Delivery and Increased Oral Bioavailability in Dogs Given a Propranolol Laurate Salt

Pharmaceutical Research -     

The action of benzodiazepine antagonist Ro 15-1788 on the effects of GABA-ergic drugs

Summary The interaction of Ro 15-1788 (5 mg kg^–1 i.p.), a benzodiazepine antagonist, with GABA-ergic drugs muscimol (1.4 mg kg^–1 i.p.), fenibut (100 mg kg^–1 i.p.) and baclofen (5 mg kg^–1 i.p.) was examined in behavioural and biochemical studies in rats. All the above-mentioned GABA-ergic drugs produced motor depression and with the exception of muscimol, where anti-aggressive effect was evident, fenibut and baclofen showed only slight antiagressive properties. Ro 15-1788 attenuated the motor depression produced by these compounds but potentiated their antiaggressive effect. Moreover, it was found that Ro 15-1788 itself possessed dose-related antiagressive properties. Fenibut increased, whereas muscimol and Ro 15-1788 decreased, the GABA content in the rat striatum. Ro 15-1788 and all the studied GABA-ergic compounds increased the level of the dopaminc metabolite 3,4-dihydroxyphenylacetic acid (DOPAC) in the striatum. In spite of this no further increase of DOPAC was observed after concomitant use of Ro 15-1788 with GABA-ergic drugs. The action of investigated GABA-ergic drugs via GABA receptors linked to benzodiazepine receptors is suggested.     

盐酸普萘洛尔延迟起释缓释片释放的影响因素

通过体外释放度考察影响盐酸普萘洛尔延迟起释缓释片时滞及释药速率的因素,包括包衣层处方及释放条件.结果表明包衣材料的比例及包衣增重对制剂释放影响较大;增塑剂及抗粘剂用量在一定范围内影响药物释放;释放介质的pH及转速对释放影响较大,释放度测定方法及释放介质用量对释放基本无影响.     

The Effect of Propranolol on the Electroencephalogram in Normal and Ethanol Dependent Rats

Abstract: Electroencephalograms were recorded from scalp electrodes placed over the cerebral hemispheres of rats withdrawing from ethanol. The purpose was to investigate whether administration of the β-adrenergic receptor blocker propranolol changed the EEG during that condition. The animals were artificially ventilated with an air mixture of 70% N₂O:30% O₂ and PaO₂ PaCO₂ and mean arterial blood pressure were kept constant. There were no significant differences in EEG frequencies or amplitudes between abstinent animals and controls neither before nor 20 min. after intravenous administration of propranolol 2 mg/kg body weight. Similarly, there was no EEG changes during 3 min. of photic stimulation. It has been reported that electrophysiological abnormalities during physical ethanol dependence are generated in subcortical brain structures but the 4 day intoxication period used in the present study seems too short to involve the cerebral cortex.     

儿童用临时调配盐酸普萘洛尔口服混悬液的制备

目的：制备可用于分剂量给药的儿童临时调配盐酸普萘洛尔口服混悬液,并进行初步稳定性实验。方法：通过处方筛选和优化制备空白混悬液,并加入研细的市售盐酸普萘洛尔片制备临时调配的盐酸普萘洛尔口服混悬液。采用紫外分光光度法于289 nm波长处测定混悬液中盐酸普萘洛尔的含量。以离心实验和留样观察进行初步稳定性考察。结果：制备的混悬液均匀细腻,稳定性、分散性良好,各项检查符合相关规定。三次实验的平均回收率分别为96.24%、100.68%、95.10%（RSD分别为4.04%、0.82%、0.86%,n=3）。离心实验中样品外观未见分层,留样观察10 d成品性质稳定。结论：该制备工艺简单方便,药物分散简单快速;含量测定方法准确、可靠;成品性质稳定。     

Solubilization of Liposomes by Weak Electrolyte Drugs. I. Propranolol

The solubilization of dimyristoylphosphatidylcholine (DMPC) liposomes by a weak electrolyte drug, propranolol (PPL) hydrochloride, has been studied as a function of pH, [PPL], [DMPC], and temperature. The solubilization of liposomes at 40°C by 0.2 mM PPL occurred at different rates from 2.9 to 14.4 mM DMPC but converged at complete solubilization after 13 hr at pH 12.0. At the same [PPL], solubilization was complete after 18 days at pH 11.0, but incomplete solubilization occurred at pH 10.0 and not at all at lower pH's. In 14.4 mM DMPC liposomes, solubilization was gradual and proportional to the [PPL] from 0.001 to 0.10 mM up to 95 hr, then rapid thereafter. The [PPL] at which the solubilization efficiency began to increase rapidly was determined to be 0.078 mM. The rate of solubilization was also influenced by the fluidity of the bilayers, a sevenfold increase in the time for complete solubilization being observed upon cooling from 40 to 20°C. Surface tension (st) data confirmed a low critical micelle concentration (CMC) and continued decrease in the st above the CMC. It is concluded that the critical ratio of PPL to DMPC for solubilization occurs in localized regions of the bilayers, with total solubilization at different rates depending on the [PPL] and the physical properties of the liposomes. The processes may be used advantageously to prepare small vesicles or to extract lipids or proteins, more efficiently than detergents, from biological membranes.