薄层扫描法测定血浆中盐酸氟桂利嗪浓度及药物动力学

血浆中盐酸氟桂利嗪经硼酸缓冲液酸化后，正戊烷－异丙醇（９８：２）提取其原型，加酸使成盐溶于无机相中，再加碱后用二氯甲烷提取，样品点于硅胶ＧＦ２５４薄层板上，以环己烷－丙酮－氯仿（９：３：５）为展开剂。氟桂利嗪在２５４ｎｍ紫外灯下呈紫色斑点，Ｒｆ＝０．５４，于ＣＳ－９３０薄层扫描仪上测定，λｓ＝２１５ｎｍ、λｇ＝３１０ｎｍ，线性范围０．３￣８μｇ，平均回收率９０．０２％。用此法测定了氟桂利嗪血药浓度     

Flunarizine induces a transient loss of tyrosine hydroxylase immunoreactivity in nigrostriatal neurons

Neurotoxic effects of flunarizine (Fz), a selective calcium channel blocker, on the nigrostriatal dopamine system was investigated. Systemic injections of Fz to mice resulted in a transient loss of tyrosine hydroxylase (TH) immunoreactive nigrostriatal neurons without cell loss. TH immunoreactivity in these neurons was greatly reduced as rapidly as one day after drug administration (regardless of dosage used) and thereafter recovered in both dose- and time-dependent manners. Such a novel neurotoxic action of Fz may constitute a morphological substrate for reversible drug-induced parkinsonian signs described in recent clinical case reports.     

三例儿童交替性偏瘫的回顾性分析

目的探讨儿童交替性偏瘫病因、临床特点、治疗效果。方法回顾性分析3例儿童交替性偏瘫患者的病因、临床表现及疗效。结果本组3例患者起病年龄均小于18个月,反复发作的交替性偏瘫；进行性的智能障碍,其中1例伴有短暂眼球震颤及眼球活动障碍,1例伴有张力障碍性姿势异常；睡眠可缓解无力及锥体外系症状,应用氟桂嗪治疗后,2例患者发作频率及持续时间降低,1例无效。结论本病病因不明,多为散发,临床表现为18月内起病的发作性交替性偏瘫,辅助检查无特征性改变,氟桂利嗪治疗部分有效。     

Effect of nilvadipine on the voltage-dependent Ca channels in rat hippocampal CA1 pyramidal neurons

Effects of nilvadipine on the low- and high-voltage activated Ca²⁺ currents (LVA and HVA I_Ca, respectively) were compared with other organic Ca²⁺ antagonists in acutely dissociated rat hippocampal CA1 pyramidal neurons. The inhibitory effects of nilvadipine, amlodipine and flunarizine on LVA I_Ca were concentration- and use-dependent. The apparent half-maximum inhibitory concentrations (IC₅₀s) at every 1- and 30-s stimulation were 6.3×10⁻⁷ M and 1.8×10⁻⁶ M for flunarizine, 1.9×10⁻⁶ M and 7.6×10⁻⁶ M for nilvadipine, and 4.0×10⁻⁶ M and 8.0×10⁻⁶ M for amlodipine, respectively. Thus, the strength of the use-dependence was in the sequence of nilvadipine>flunarizine>amlodipine. Nilvadipine also inhibited the HVA I_Ca in a concentration-dependent manner with an IC₅₀ of 1.5×10⁻⁷ M. The hippocampal CA1 neurons were observed to have five pharmacologically distinct HVA Ca²⁺ channel subtypes consisting of L-, N-, P-, Q- and R-types. Nilvadipine selectively inhibited the L-type Ca²⁺ channel current which comprised 34% of the total HVA I_Ca. On the other hand, amlodipine non-selectively inhibited the HVA Ca²⁺ channel subtypes. These results suggest that the inhibitory effect of nilvadipine on the neuronal Ca²⁺ influx through both LVA and HVA L-type Ca²⁺ channels, in combination with the cerebral vasodilatory action, may prevent neuronal damage during ischemia.     

Postmarketing study of the use of flunarizine in vestibular vertigo and in migraine

Objective: This international postmarketing observational study of flunarizine was designed to evaluate, in routine clinical practice, the risk/benefit ratio of flunarizine in its approved indications, namely prophylaxis of migraine and treatment of vertigo. Comparator drugs were propranolol in migraine and betahistine in vertigo. The study was carried out by 498 general practitioners in Belgium, The Netherlands and Germany, whose participation had been requested by mail. In total 3186 patients were entered: 1601 in the two migraine cohorts and 1585 in the two vertigo cohorts. Results: In the migraine study, treatment results with propranolol tended to be somewhat better than those with flunarizine, but a selection bias cannot be excluded. There was no clear difference regarding efficacy between flunarizine and betahistine in the vertigo study. The safety evaluation focused on extrapyramidal symptoms (EPS) and depression. Overall, EPS were noted in only four patients, two in the vertigo-betahistine and two in the migraine-flunarizine cohort. A total of 70 patients developed depressive symptoms (34 in the flunarizine and 24 in the propranolol migraine cohorts, but only 7 in the flunarizine and 5 in the betahistine vertigo cohorts). Patients with migraine were clearly more prone to depression than patients with vertigo, regardless of their treatment. Additional risk factors for depression were a history of depression, and, in the migraine flunarizine cohort, a high number of previous migraine treatments. Received: 23 October 1995/Accepted in revised form: 20 February 1996     

自制中药粉剂中盐酸小檗碱的定量检测方法

目的测定自制中药粉剂中盐酸小檗碱的含量。方法采用薄层扫描法测定了盐酸小檗碱的含量。结果盐酸小檗碱在1～6μg间呈良好的线性关系,r=0.9975,平均回收率为97.95%,RSD为2.36%(n=5)。结论所建立的方法可靠准确地进行定量检测,可用于该制剂的质量控制。     

葛根素治疗颈性眩晕临床观察

以葛根素加半夏白术天麻汤治疗颈性眩晕45例，为治疗组；以西北灵加半夏白术天麻汤治疗42例，为对照组。通过两组临床疗效观察：治疗组显效27例，有效16例，无效2例，有效率为96．0％；对照组显效8例，有效24例，无效10例，有效率为77．0％，对比有显著性差异（P＜0．01）。     

半夏白术天麻汤加味治疗美尼尔氏病临床观察

[目的]观察半夏白术天麻汤加味治疗美尼尔氏病的临床疗效。[方法]将40例患者随机分为两组。治疗组22例口服加味半夏白术天麻汤治疗,对照组18例在维持营养及水电解质平衡的基础上,加服脑益嗪片、西比灵片治疗。两组治疗1个疗程(14d)进行疗效判定。[结果]治疗组临床治愈6例,显效9例,有效5例,无效2例,总有效率90.90%。对照组临床治愈3例,显效6例,有效4例,无效5例,总有效率72.20%。临床疗效治疗组优于对照组(P<0.05)。[结论]加味半夏白术天麻汤治疗美尼尔氏病疗效较好。     

托吡酯治疗慢性偏头痛的临床疗效观察

目的观察托吡酯治疗慢性偏头痛的临床疗效。方法选取我院2009年10月至2013年2月诊治的慢性偏头痛患者120例,随机分为两组,每组60例,治疗组予托吡酯治疗,对照组予氟桂利嗪治疗,治疗3个月,统计两组的治疗总有效率。结果两组的总有效率分别为78.33%和70.00%。托吡酯治疗组优于氟桂利嗪治疗组(P<0.05)。结论托吡酯治疗慢性偏头痛安全有效。     

萸竹定眩丸治疗颈性眩晕短期疗效观察

目的:观察萸竹定眩丸治疗颈性眩晕的短期疗效。方法:将河南省中医院脊柱科门诊收治的80例患者随机分为对照组和观察组,各40例。对照组服用盐酸氟桂利嗪胶囊治疗,治疗组在服用盐酸氟桂利嗪胶囊基础上加服萸竹定眩丸治疗。每组疗程均为4周1个疗程,1个疗程后根据改良Macnab标准评估临床疗效。结果:治疗组40例中优4例,良28例,可6例,差2例,有效率80%(32/40);对照组中优1例,良21例,可8例,差10例,有效率55%(22/40),两组差异有统计学意义(P<0.05)。结论:盐酸氟桂利嗪胶囊治疗颈性眩晕能取得一定临床疗效,但盐酸氟桂利嗪胶囊联合萸竹定眩丸临床疗效更显著。