银丹心脑通软胶囊联合氟桂利嗪治疗偏头痛的疗效观察

目的探讨银丹心脑通软胶囊联合氟桂利嗪治疗偏头痛的临床疗效。方法选择偏头痛患者85例,并随机分为观察组和对照组,对照组40例单纯采用氟桂利嗪治疗,观察组45例在对照组的基础上加用银丹心脑通胶囊治疗,用药1个月后开始评价两组的临床疗效及症状量化评分。结果观察组的总有效率为91.11%,明显优于对照组的80%,两组比较差异有统计学意义(P<0.05);观察组的症状量化评分显著低于对照组,差异有统计学意义(P<0.05)。结论银丹心脑通软胶囊联合氟桂利嗪治疗偏头痛能有效地减轻或终止头痛的发作,缓解伴发症状,提高疗效,预防头痛复发,值得临床推广应用。     

养血清脑颗粒与盐酸氟桂嗪胶囊治疗偏头痛临床疗效观察

目的：对照观察养血清脑颗粒与直艏囊治疗偏头痛的疗效。方法：将137例偏头痛患分成3组,对养血清脑颗粒和氟桂嗪以及两药合用治疗偏头痛的疗效进行比较,结果：氟桂嗪治疗偏头痛的疗效与献报道基本一致,养血清脑颗粒与氟桂嗪疗效基本相同,联合用药显效率显提高。结论：养血清脑颗粒是一种有效的偏头痛的治疗药物,与氟桂嗪合用可提高疗效。     

盐酸氟桂利嗪的改进措施

目的:探索盐酸氟桂利嗪原料质量的改进措施。方法:采用相转移催化剂和先进的工艺路线。结果:盐酸氟桂利嗪原料收率与质量明显提高,精制难度降低。结论:改进措施有效地提高了盐酸氟桂利嗪原料的质量。     

相转移催化剂在盐酸氟桂利嗪合成中的应用

目的:研究相转移催化剂十六烷基三甲基溴化铵(CTMAB)对合成盐酸氟桂利嗪的影响。方法:用肉桂基哌嗪和二氟苯基溴甲烷为原料,以二氯甲烷为溶剂,KOH为催化剂,十六烷基三甲基溴化铵(CTMAB)为相转移催化剂合成盐酸氟桂利嗪。结果:最佳条件为:n(肉桂基哌嗪)∶n(二氟苯基溴甲烷)∶n(KOH)=1∶1∶1.3,2g十六烷基三甲基溴化铵/1mol二氟苯基溴甲烷,反应时间4h,反应温度42℃,收率可达92.7%。结论:相转移催化剂十六烷基三甲基溴化铵(CTMAB)对合成盐酸氟桂利嗪的产品收率和质量均有较大的提高。     

Effects of flunarizine on electrical and mechanical responses of smooth muscle cells in basilar and ear arteries of the rabbit

Summary The effects of flunarizine on electrical and mechanical responses of smooth muscle tissues of the rabbit basilar and ear arteries to transmural stimulation, highpotassium solution (high-K), 5-hydroxytryptamine and noradrenaline were studied. In the basilar artery, 10^–6 M flunarizine (69 min application) blocked spike potentials generated by outward current stimuli or transmural stimulation without change in the resting membrane potential or membrane resistance. The spike potentials generated in the ear artery were attenuated by a long exposure (up to 2 h) to a high concentration of flunarizine (10^–6 M). Membrane depolarizations produced by high-K, noradrenaline or 5-hydroxytryptamine were not blocked by flunarizine. Flunarizine inhibited smooth muscle contractions produced by transmural stimuli, high-K, noradrenaline or 5-hydroxytryptamine in both arteries, however the inhibition developed slowly, and the ear artery required a longer period of incubation with flunarizine than the basilar artery. The inhibitory effects of flunarizine on basilar artery were more marked against transmural stimulation or high-K induced contractions than against agonist-induced contractions.     

Comparison of the calcium entry blockers nimodipine and flunarizine on human cerebral and temporal arteries: role in cerebrovascular disorders

Summary The effect of the calcium entry blockers flunarizine and nimodipine on isolated human cerebral and temporal arteries has been studied.Flunarizine induced only weak relaxation of precontracted temporal arteries in contrast to the response seen in cerebral arteries. Nimodipine invariably induced strong relaxation of both types of vessel. The effect of the calcium entry blockers on potassium (K⁺)-, noradrenaline (NA)- and 5-hydroxytryptamine (5-HT)-induced contraction was also examined. In general, the K^–-induced contraction was inhibited by both calcium entry blockers, nimodipine being more potent than flunarizine, the cerebral artery being more sensitive. The response to K⁺ consisted of two phases; the second, slowly developing phase of contraction was more sensitive to either blocker than the initial, fast phase of contraction.Flunarizine was significantly more potent in inhibiting NA-induced contraction of the human cerebral than of the temporal artery, and there was no difference in its action on 5-HT-induced contraction of either artery. The same pattern was found for nimodipine, which was more potent in every aspect. Both calcium entry blockers induced a parallel shift in calcium-induced contraction studied by application of calcium to vessels preincubated in calcium free medium. Flunarizine was more potent on cerebral than on temporal arteries and there was no difference between the two vessels in this action of nimodipine. However, the latter was more potent than flunarizine in preventing calcium-induced contraction.The clinical implications of the two agents are discussed in relation to cerebrovascular disorders.     

Bay K 8644 induces a reversible spasticity-like syndrome in rats

The dihydropyridine Bay K 8644 exerts a positive modulation of Ca²⁺ channels. Administration of Bay K 8644 3–5 mg/kg i.p. to rats induces within 15 min a severe spasticity syndrome consisting of stiff tail, arched back, stretching and twisting of forelimbs and hindlegs and backwards motility and rolling over. The syndrome was effectively antagonized by nifedipine 3–30 mg/kg but not by the other Ca²⁺ channel blockers flunarizine, diltiazem and verapamil. Diltiazem even enhanced the spasticity. Diazepam 10–30 mg/kg i.p. completely blocked the spasticity whereas the other muscle relaxants (−)-baclofen and the β-carboline ZK 93423 were completely inactive. These findings with Bay K 8644 suggest that spasticity may be caused by changed Ca²⁺ homeostasis.     

缺血脑组织内皮素含量变化的实验研究

为探讨内皮素含量变化是否为缺血神经元损伤的危险因素及Ca~(2+)拮抗剂氟桂嗪对脑缺血的保护作用,采用放射免疫分析法,我们测定兔大脑中动脉阻断48小时后缺血区脑组织内皮素含量变化及氟桂嗪对其变化的影响。结果显示,缺血48小时后梗塞区脑组织内皮素含量明显升高(P<0.01),为对照组的10倍,而氟桂嗪能明显降低缺血区脑组织水、内皮素含量(P<0.05)。上述结果提示:缺血脑组织内皮素含量升高是导致缺血神经元损伤的重要因素,氟桂嗪对脑缺血有保护作用。     

儿童交替性偏瘫六例分析

目的探讨儿童交替性偏瘫（ＡＨＣ）的临床特点及治疗方法。方法对６例ＡＨＣ患儿的临床资料进行分析。结果６例患儿的临床特征为出生后１８个月起内病，频繁发作，持续数分钟至数小时；短暂的眼球震颤，肌张力异常，舞蹈徐动样动作，植物神经机能紊乱和认知机能减退；睡眠可缓解无力及锥体外系症状。应用氟桂嗪治疗后，１例患儿发作完全停止，其余５例患儿均显示发作频率和持续时间降低。结论本病的主要特征为１８个月内起病的发作性交替性偏瘫，伴锥体外系症状及智力障碍，氟桂嗪治疗本病有效     

The effects of flunarizine and pentoxifylline on vestibular blood flow in the guinea pig

Several authors have proposed that complications arising from vestibular disorders are the result of compromised circulation. The purpose of the current study was to assess the ability of flunarizine and pentoxifylline to increase peripheral vestibular blood flow (VBF), since flunarizine is a selective calcium-channel entry blocker that inhibits calcium-related contraction of smooth muscle, while pentoxifylline is a xanthine derivative that promotes microcirculation by affecting red blood cell malleability. Both of these treatment strategies have received considerable attention in clinics and laboratory, but their effects on blood flow are unclear. Changes in VBF were evaluated from the posterior semicircular canal ampulla in guinea pigs using a laser Doppler flowmeter. One group of animals was infused with pentoxifylline at concentrations of 10–40 mg/ml, while a second group was treated with 0.3–1.5 mg/kg flunarizine. VBF, blood pressure (BP) and heart rate (HR) were monitored continuously. Findings showed that pentoxifylline induced a concentration-dependent increase in VBF. In contrast, no increase in VBF occurred in response to flunarizine infusions. These studies suggest that the effectiveness of pentoxifylline in the clinical treatment of vestibular disorders may be the result of improved blood flow. Received: 8 April 1998 / Accepted: 11 May 1998