Effect of the Intracerebroventricular Injection of Dopamine on Blood Pressure in the Spontaneously Hypertensive Rat

To examine the role of the central dopaminergic system in blood pressure regulation, dopamine was injected into the cerebral lateral ventricles of conscious, unrestrained spontaneously hypertensive rats (SHR), deoxycorticosterone (DOC)-salt hypertensive rats and Wistar-Kyoto normotensive rats (WKY). Intracerebroventricular (i.c.v.) injection of dopamine produced a significant dose-dependent decrease in blood pressure in the SHR as well as in the WKY and DOC-salt hypertensive rats. However, the SHR were significantly more sensitive than were the other 2 groups of rats. In the SHR, this central depressor effect of dopamine was significantly attenuated by pretreatment with i.c.v. metoclopramide, but not by phentolamine, suggesting that central dopamine receptors rather than α-adrenoceptors are involved in the mediation of the actions of dopamine in the brain. These results suggest that the central dopaminergic system plays a more important role in the regulation of blood pressure in the SHR than in the WKY and DOC-salt hypertensive rats.     

Comparison of dexamethasone,metoclopramide, and their combination in the prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy

Background Postoperative nausea and vomiting (PONV) are one of the most common complaints following anesthesia and surgery. This study was designed to evaluate the efficacy of dexamethasone, metoclopramide, and their combination to prevent PONV in patients undergoing laparoscopic cholecystectomy. Methods A total of 160 ASA physical status I and II patients were included in this randomized, double blind, placebo-controlled study. Patients were randomly assigned to 4 groups (n = 40 each): group 1 consisting of control patients administered 0.9% NaCl; group 2 patients received metoclopramide 10 mg just before the end of anesthesia; group 3 patients received dexamethasone 8 mg after the induction of anesthesia; and group 4 patients received dexamethasone 8 mg after the induction of anesthesia and metoclopramide 10 mg before the end of anesthesia. The incidence of PONV, mean visual analog pain scores at rest and on movement, time to the first request for analgesia, side effects, and well-being score were recorded during the first 24 h postoperatively. Results Data were analyzed using one-way analysis of variance (ANOVA) and the χ² test, with p < 0.05 considered statistically significant. The total incidence of PONV was 60% with placebo, 45% with metoclopramide, 23% with dexamethasone, and 13% with the combination of dexamethasone plus metoclopramide. None of the dexamethasone plus metoclopramide group patients (p < 0.05 versus groups 1 and 2) and one dexamethasone group patient (p < 0.05 versus group 1) required antiemetic rescue, as compared with four patients in the metoclopramide group and six patients in the placebo group. Pain scores, the time to the first request for analgesia, and side effects were similar across the study groups. Conclusions Dexamethasone and the combination of dexamethasone plus metoclopramide were more effective in preventing PONV than metoclopramide and placebo.     

HPLC法测定甲氧氯普胺中有关物质的含量

目的:建立以高效液相色谱法测定甲氧氯普胺中有关物质含量的方法。方法:色谱柱为C18,流动相为乙腈-0.02mol.L-1磷酸溶液(19∶81),流速为1.0mL.min-1,检测波长为275nm,柱温为室温,进样量为20μL;以主成分自身对照法计算有关物质的含量。结果:在该色谱条件下,甲氧氯普胺与杂质能完全分离;杂质限量在0.05%～4.0%范围内测得的峰面积与样品自身对照溶液的浓度呈良好的线性关系;甲氧氯普胺的最小检出量为0.3ng,其有关物质的含量均小于0.26%。结论:本方法简便、准确、灵敏度高、专属性强,可用于甲氧氯普胺中有关物质的检测。     

胃复安联合苯海拉明与昂丹司琼治疗化疗后不良反应的观察

目的将两种化疗止吐方法的疗效进行比较,寻找一种高效价廉的止吐方法。方法将200例恶性肿瘤化疗后呕吐患者随机分为胃复安联合苯海拉明止吐治疗组(100例)和昂丹司琼止吐治疗组100例,观察止吐效果和不良反应。结果对于轻度恶心呕吐者,胃复安联合苯海拉明止吐效果与昂丹司琼相近,差异无统计学意义(P>0.05),但对于重度恶心呕吐者,昂丹司琼止吐效果优于胃复安联合苯海拉明(P<0.05)。结论胃复安联合苯海拉明与昂丹司琼对于轻度呕吐的止吐效果均良好,但胃复安联合苯海拉明较昂丹司琼明显价廉。对于重度呕吐者,昂丹司琼的止吐效果较好。     

多潘立酮和甲氧氯普胺治疗呃逆的临床观察

目的探讨呃逆的治疗方法。方法将呃逆患者73例按咨询顺序随机分为2组,多潘立酮组37例,给予多潘立酮10mg顿服,如1h后无效再服1次;甲氧氯普胺组36例,给予甲氧氯普胺10mg,如1h后无效再服1次。2组疗程均为1d,比较2组临床疗效。结果多潘立酮组治疗呃逆显效时间快于甲氧氯普胺组,而且疗效优于甲氧氯普胺组,差异均有统计学意义（P〈0.01）。结论多潘立酮治疗呃逆效果优于甲氧氯普胺。     

Preparation and comparative evaluation of sustained release metoclopramide hydrochloride matrix tablets

Metoclopramide hydrochloride (MCP) is commonly used for the management of gastrointestinal disorders. Frequent administration and the undesired side effects (extra pyramidal symptoms) of the drug on the central nervous system due to the fluctuations of its plasma concentrations may lead to patient incompliance, and hence, improper therapy. Therefore, the present work will be devoted to formulate the drug in sustained release formulations. MCP was incorporated in 12 formulae containing different polymers and/or different polymer ratios. These polymers were hydroxypropylmethyl cellulose (HPMC), carboxymethylcellulose (CMC) and ethyl cellulose (EC). Sodium starch glycolate (SSG) was added to some formulae in different amounts in order to soften and/or disintegrate the tablets. Both direct compression and granulation techniques were used to prepare the tablets. The physical properties were found to be satisfactory for all the formulae. The dissolution profiles of the tablets were constructed using the change-over method. The drug release involved a combination of both diffusion and polymer-chain relaxation mechanisms. The time required to release 50% of MCP ranged from 1.2 to more than 8 h. Direct compression and dry granulation techniques produced sufficient sustaining of the drug release. However, the pellets made by wet granulation released MCP in about 2 h, i.e., pelletization spheronization technique was not effective in sustaining the drug.     

Effects of metoclopramide on gastric motility measured by short-term bio-impedance

AIM： To analyze the accuracy of short-term bio-impedance as a means of measuring gastric motility. METHODS： We evaluated differences in the shortterm electrical bio-impedance signal from the gastric region in the following conditions： （1） fasting state, （2） after the administration of metoclopramide （a drug that induces an increase in gastric motility） and （3） after food ingestion in 23 healthy volunteers. We recorded the real component of the electrical impedance signal from the gastric region for 1000 s. We performed a Fast Fourier Transform （FFT） on this data and then compared the signal among the fasting, medicated, and postprandial conditions using the median of the area under the curve, the relative area under the curve and the main peak activity. RESULTS： The median of the area under the curve of the frequency range in the region between 2-8 cycles per minute （cpm） decreased from 4.7 cpm in the fasting condition to 4.0 cpm in the medicated state （t = 3.32, P = 0.004）. This concurred with the decrease seen in the relative area under the FFT curve in the region from 4 to 8 cpm from 38.3% to 26.6% （t = 2.81, P = 0.012） and the increase in area in the region from 2 to 4 cpm from 22.4% to 27.7%, respectively （t = -2.5, P = 0.022）. Finally the main peak position also decreased in the region from 2 to 8 cpm. Main peak activity in the fasting state was 4.72 cpm and declined to 3.45 cpm in the medicated state （t = 2.47, P = 0.025）. There was a decrease from the fasting state to the postprandial state at 3.02 cpm （t = 4.0, P = 0.0013）. CONCLUSION： Short-term electrical bio-impedance can assess gastric motility changes in individuals experiencing gastric stress by analyzing the area medians and relative areas under the FFT curve.     

胃复安引起锥体外系综合症68例临床分析

目的探讨胃复安引起锥体系综合症的临床表现及预防。方法我科门诊和住院患者使用胃复安引起锥体外系综合征的68例病人停用胃复安，给予肌注阿品或654—2，部分病人服用安坦。结果68例中50例痉挛性斜颈和舌肌运动障碍者经治疗后20min-24h内锥体外系症状全部消失，18例于40h后好转，3d后症状全部消失。结论立即停药和及时治疗，所有患者的锥体外系症状可在短期内好转或消失。     

赛格恩预防CHOP方案治疗非霍奇金淋巴瘤致胃肠道反应分析

目的:观察赛格恩(国产盐酸托烷司琼注射液)防治非霍奇金淋巴瘤(NHL)化疗所致恶心、呕吐的疗效.方法:34例病人随机分为A组和B组.A组:化疗前20分钟赛格恩5 mg,静脉推注;B组:化疗前20分钟,苯海拉明20 mg,肌肉注射,化疗后4小时、8小时,胃复安20 mg,肌肉注射.结果:A组预防恶心有效率显著高于B组(88.2%vs 67.6%,P＜.05),预防呕吐有效率亦高于胃复安组(91.1%vs 70.6%,P＜0.05).赛格恩的主要不良反应包括便秘、头痛等,病人均能耐受.结论:赛格恩能较好的防治化疗所致恶心、呕吐.     

Nutzen und Risiko von hochdosiertem Metoclopramid im Vergleich zu hochdosiertem Haloperidol oder Triflupromazin bei cisplatin-induziertem Erbrechen

Summary The antiemetic efficacy of metoclopramide (MCL, Paspertin®, loading infusion 0.5 mg/kg body wt./h over 2 h, maintenance infusion 0.25 mg/kg/h over 24 h) has been compared with haloperidol (HAL, Haldol®, 1/10 of MCL dosage) and with triflupromazine (TFP, Psyquil®, 1/2 of MCL dosage) in two sequential analyses, against the emetic effects of cisplatin (60–90 mg/m²).After treating 14 and 8 pairs of patients respectively, MCL was significantly (=0.05) more effective than HAL or TFP. Only 1 of the 14 patients in the HAL group and 0 of 8 in the TFP group were totally protected against emesis, in contrast to 6 of 14 patients and 3 of 8 in the MCL groups. In order to quantify the benefit/risk relationship of the antiemetic drugs studied the number of prevented emetic episodes (in comparison to previous insufficient treatment) was related to the incidence of major undesired effects (i.e. dystonia and/or akathisia). This relationship was 17.8 and 12.1 for the two MCL groups; for HAL and TFP it was only 5.8 and 4.6, respectively.The high antiemetic selectivity of MCL against cisplatin-induced emesis is probably related to the still unknown action of MCL on the gastrointestinal motility. A high neuroleptic potency, with or without additional anticholinergic activity, is apparently not essential for high antiemetic protection against cisplatin.

---

Abkürzungen HAL Haloperidol - MCL Metoclopramid - TFP Triflupromazin