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The effects of bendroflumethiazide/potassium chloride versus hydrochlorothiazide/amiloride on blood pressure and serum electrolytes in patients with mild to moderate hypertension seen in general practice. 苯并氟甲肼/氯化钾与氢氯噻嗪/阿米洛利对轻至中度高血压患者血压和血清电解质的影响
Pub Date : 1986-01-01
F Jørgensen, P Bredesgaard, P Johansen

The effects of 5 mg bendroflumethiazide plus 15 mmol potassium chloride versus 50 mg hydrochlorothiazide plus 5 mg amiloride on blood pressure and serum electrolytes were investigated in a 12-week, open, randomized study with parallel treatment groups. Forty-five patients with previously untreated hypertension and 33 hypertensive patients previously treated with thiazides until 1 month before allocation to the present treatments, completed the trial. Systolic and diastolic blood pressures were reduced significantly during treatment with both drug combinations. Significant negative correlations between initial serum potassium levels and the thiazide-induced decrease were observed. Mean potassium concentrations decreased by 0.39 mmol/l with bendroflumethiazide/potassium chloride and by 0.30 mmol/l with hydrochlorothiazide/amiloride. It is concluded that both treatments were effective and well tolerated in controlling patients with mild to moderate hypertension, and that the difference in the mean serum potassium concentration between the two treatments was not statistically significant.

在一项为期12周、开放、随机、平行治疗组的研究中,研究了5mg苯德鲁氟甲肼加15mmol氯化钾与50mg氢氯噻嗪加5mg阿米洛利对血压和血清电解质的影响。45名既往未接受治疗的高血压患者和33名既往接受噻嗪类药物治疗的高血压患者在分配到当前治疗前1个月完成了试验。在两种药物联合治疗期间,收缩压和舒张压均显著降低。初始血清钾水平与噻嗪类药物引起的下降呈显著负相关。苯并氟甲肼/氯化钾组平均钾浓度降低0.39 mmol/l,氢氯噻嗪/阿米洛利组平均钾浓度降低0.30 mmol/l。综上所述,两种治疗方法对控制轻中度高血压患者均有效且耐受性良好,两种治疗方法的平均血钾浓度差异无统计学意义。
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引用次数: 0
[Clinical and instrumental evaluation by multiple colonic manometry of tiropramide, trimebutine and octylonium bromide in the irritable colon: I. Administration by single i.v]. [替罗普胺、曲美布汀和溴化辛溴铵在易激结肠中的多重结肠测压的临床和仪器评价:1 .单次静脉给药]。
Pub Date : 1986-01-01
M Galeone, F Stock, G Moise, D Cacioli, E Benazzi, A Riva

Sixty out-patients with acute or sub-acute irritable colon were randomly allocated to receive a single intravenous dose of 50 mg tiropramide, 50 mg trimebutine maleate or 10 mg octilonium bromide. Before and after injection, multiple colonic manometry was performed, monitoring tonus, intensity and frequency of sinusoid contraction waves, transitories and vibrations, as well as the voluntary contraction capacity. Significant variations in tonus were not observed with any drug, but, while tiropramide left unmodified the voluntary contractile ability, a significant inhibition was observed with trimebutine and octilonium. The overall power of spontaneous colonic contractions did not vary significantly with tiropramide, whereas some decrease was observed with trimebutine, and a substantial one with octilonium. Moreover, while with tiropramide and, to a lesser extent, with trimebutine there was a significant redistribution of muscular power so as to increase phasic propulsion waves and to decrease the ineffective transitory and vibrational contractions, with octilonium only a decreased wave amplitude was recorded without alteration of the frequency of transient spasms. Based on these observations, tiropramide was evaluated as being at least as effective an antispasmodic as octilonium and at least as effective a synchronizer as trimebutine, while setting itself aside from both reference drugs as it was the only one to act contemporarily as both an antispasmodic and a synchronizer.

60例急性或亚急性结肠易激门诊患者随机分配接受单次静脉注射剂量50mg替罗普胺、50mg马来酸曲美布汀或10mg溴化奥替溴铵。注射前后行多次结肠测压,监测张力、正弦收缩波强度、频率、瞬缩、振动及自主收缩能力。任何药物均未观察到张力的显著变化,但是,虽然替罗普胺未改变自愿收缩能力,但曲美布汀和奥替隆对张力有明显的抑制作用。替罗普胺对自发结肠收缩的总强度没有显著影响,而曲美布汀和奥替溴铵则有一定程度的降低。此外,使用替罗普胺和曲美布汀(在较小程度上),肌肉力量的重新分配显著增加了相推进波,减少了无效的短暂性和振动性收缩,而使用奥替溴铵只记录了减少的波幅,而没有改变短暂性痉挛的频率。基于这些观察结果,替罗普胺被评估为至少与奥替溴胺一样有效的抗痉挛药,至少与曲美布汀一样有效的同步剂,同时将自己与两种参考药物分开,因为它是唯一一种同时作为抗痉挛药和同步剂的药物。
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引用次数: 0
A parallel group comparison of tenoxicam and piroxicam in patients with ankylosing spondylitis. 替诺昔康与吡罗西康治疗强直性脊柱炎的平行组比较。
Pub Date : 1986-01-01
H A Bird, P Le Gallez, C Astbury, D Looi, V Wright

Tenoxicam (20 mg/day) and piroxicam (20 mg/day) were compared in a double-blind, parallel group study over 4 weeks in 30 patients with ankylosing spondylitis. Both tenoxicam and piroxicam reduced spinal pain, but the improvement was greater with piroxicam. Tenoxicam and piroxicam were equally effective at improving duration of morning stiffness. Slight improvement was seen with other symptoms with both treatments. Patients were slightly more tolerant of piroxicam than tenoxicam and most patients elected to continue on their particular therapy at the end of the study.

在一项为期4周的双盲平行组研究中,对30例强直性脊柱炎患者进行了替诺昔康(20mg /天)和吡罗昔康(20mg /天)的比较。替诺昔康和吡罗西康均可减轻脊柱疼痛,但吡罗西康的改善更大。替诺昔康和吡罗西康在改善晨僵持续时间方面同样有效。两种治疗方法对其他症状均有轻微改善。患者对吡罗西康的耐受性略高于替诺西康,大多数患者在研究结束时选择继续他们的特定治疗。
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引用次数: 0
Dose linearity and other pharmacokinetics of ofloxacin: a new, broad-spectrum antimicrobial agent. 新型广谱抗菌药物氧氟沙星的剂量线性及药代动力学。
Pub Date : 1985-01-01
M Verho, V Malerczyk, E Dagrosa, A Korn

After oral administration of a single dose of ofloxacin (100, 300 or 600 mg) to 13 healthy male volunteers in an open, randomized crossover study, concentrations of the unchanged drug were estimated at various times in serum and urine, over 28 hours and 48 hours, respectively. Each dose was followed by a wash-out period of 1 week. Ofloxacin concentrations were determined using both high pressure liquid chromatography (HPLC) and a microbiological assay. The measurements obtained were compared by linear distribution independent regression, and were found to be equivalent, indicating no major metabolism of ofloxacin. Maximum serum concentrations (Cmax) of ofloxacin after administration of 100, 300 or 600 mg were, respectively, 1.0, 3.4 and 6.9 mg/ml (HPLC, median values). A linear relationship between Cmax and dose was demonstrated within the range tested (coefficient of correlation r = 0.88). The same applied to AUC0-28 (r = 0.98) and to urinary recovery of the drug (r = 0.98). Time to reach Cmax varied between 0.5 and 1.1 hours (median values), indicating rapid absorption of the drug. Biological half-life (t1/2 beta) was determined by fitting a two-compartment open model to the date: t1/2 beta was in the range 5.6 to 6.4 hours (HPLC, median values) and was not relevantly dose-dependent. Urinary concentrations of ofloxacin remained above 1 microgram/ml, i.e. above the minimum inhibitory concentrations (MIC90) for most bacterial strains at all dosages tested, for at least 36 hours after drug administration. General tolerability was good; no side-effects were reported.

在一项开放、随机交叉研究中,13名健康男性志愿者口服单剂量氧氟沙星(100,300或600mg)后,分别在28小时和48小时内,在不同时间估计血清和尿液中不变药物的浓度。每次给药后为1周的洗脱期。采用高压液相色谱法和微生物法测定氧氟沙星浓度。通过线性分布独立回归对测量结果进行比较,发现结果相当,表明氧氟沙星无主要代谢。给药100mg、300mg和600mg后,氧氟沙星的最大血清浓度(Cmax)分别为1.0、3.4和6.9 mg/ml (HPLC中值)。Cmax与剂量在测试范围内呈线性关系(相关系数r = 0.88)。AUC0-28 (r = 0.98)和尿中药物回收率(r = 0.98)也是如此。达到Cmax的时间在0.5至1.1小时之间变化(中位数),表明药物的快速吸收。生物半衰期(t1/2 β)通过拟合两室开放模型确定:t1/2 β在5.6至6.4小时范围内(HPLC,中位数),不相关的剂量依赖性。在给药后至少36小时,尿中氧氟沙星浓度保持在1微克/毫升以上,即在所有测试剂量下,高于大多数细菌菌株的最低抑制浓度(MIC90)。总体耐受性良好;没有副作用的报道。
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引用次数: 0
Oral nifedipine in hypertensive emergencies. 口服硝苯地平治疗高血压急症。
Pub Date : 1985-01-01
T Alexander, J Jose, D Mathai, D Dennison, B M Pulimond

A study was carried out to evaluate the efficacy and tolerance of oral nifedipine in hypertensive emergencies. Eleven consecutive patients with very high blood pressure requiring emergency reduction were included in the study. Nifedipine (10 mg) was given orally at 6-hourly intervals and blood pressure, pulse, serum electrolytes, urea, creatinine and uric acid were monitored. A reduction in blood pressure was noted within 10 minutes, with a significant reduction occurring within 30 minutes (reduction of systolic blood pressure by 8.11% and diastolic blood pressure by 9.38%). The maximum reduction in blood pressure occurred within 90 minutes (reduction of systolic blood pressure by 20.78% and diastolic blood pressure by 21.74%) and remained at this level for 4 hours, after which a mild increase in blood pressure was noted. At 6 hours, the reduction in blood pressure was 15.41% and diastolic reduction was 17.94%. The reduction in blood pressure was found to be directly correlated with the pre-treatment blood pressure. There was no significant alteration in the pulse rate or blood chemistry. No side-effects were noted during the study. It is suggested that oral nifedipine is a simple, effective and well-tolerated alternative to parenteral therapy in the management of hypertensive emergencies.

本研究旨在评价口服硝苯地平治疗高血压急症的疗效和耐受性。连续11例需要紧急降压的高血压患者被纳入研究。每隔6小时口服硝苯地平10 mg,监测血压、脉搏、血清电解质、尿素、肌酐、尿酸。血压在10分钟内降低,30分钟内显著降低(收缩压降低8.11%,舒张压降低9.38%)。最大的血压下降发生在90分钟内(收缩压下降20.78%,舒张压下降21.74%),并保持在这个水平4小时,之后血压轻度升高。6小时时,血压降低15.41%,舒张降低17.94%。血压的降低被发现与治疗前的血压直接相关。脉搏率和血液化学没有明显变化。研究期间未发现任何副作用。提示口服硝苯地平是一种简便、有效、耐受性良好的非肠外治疗高血压急症的替代方法。
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引用次数: 0
Cytoprotective approach to peptic ulcer therapy: a preliminary dose-finding clinical investigation with triletide. 细胞保护方法对消化性溃疡的治疗:初步剂量发现的临床研究与三叶肽。
Pub Date : 1985-01-01
C A Maggi, D Ferrari

Thirty out-patients with gastric (8) or duodenal (22) ulcers were randomly assigned to receive a daily dose of 1.0, 1.5 or 2.0 g triletide over a period of 8 weeks. Endoscopic findings and overall clinical rating indicated that triletide effectively accelerated ulcer healing in a proportion of patients (73% of responders), with a trend for better response at doses higher than 1 g/day, regardless of the ulcer location. Heartburn, epigastric pain and concomitant antacid consumption improved significantly in each dose group, but to a significantly greater extent in the highest dose group than in either mid-dose or low-dose groups. Tolerance of treatment was good at all dose levels, and no significant variations in routine haematology, haematochemistry or renal function tests were observed. It is suggested, therefore, that triletide provides an effective and well-tolerated new means to promote ulcer healing, both gastric and duodenal, with easily graded symptomatic relief by modifying the daily dose.

30名患有胃(8)或十二指肠(22)溃疡的门诊患者被随机分配接受每日剂量1.0、1.5或2.0 g三叶肽,持续8周。内窥镜检查结果和总体临床评分表明,三叶肽在一定比例的患者(73%的应答者)中有效地加速了溃疡愈合,并且无论溃疡位置如何,当剂量高于1 g/天时,有更好的反应趋势。胃灼热、胃脘痛和伴随的抗酸药消耗在各剂量组均有显著改善,但最高剂量组的改善程度明显大于中剂量组和低剂量组。所有剂量水平的治疗耐受性都很好,并且在常规血液学、血液化学或肾功能检查中没有观察到明显的变化。因此,提示三叶肽提供了一种有效且耐受性良好的促进胃溃疡和十二指肠溃疡愈合的新手段,通过改变日剂量可以很容易地逐步缓解症状。
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引用次数: 0
Preliminary human pharmacokinetics of triletide. 三叶肽人体药代动力学初步研究。
Pub Date : 1985-01-01
L Repossini

Six healthy volunteers were administered a single 1 g dose of triletide, orally, and blood concentrations of the parent drug determined by high pressure liquid chromatography over a 10-hour period. Analysis of both individual and pooled data indicated that triletide was well absorbed after oral administration, with a lag time of 0.3 hours and the blood peak was reached after about 1.1 to 1.3 hours. Metabolization to desmethyl, desacetyl, desmethyl-desacetyl and hydroxylated derivatives plays a major role in the biotransformation of the drug and thus in its disappearance from blood, the distribution half-life being about 1 hour. Elimination half-life ranged about 5 hours, thus suggesting a dosage schedule of 3-times daily for loading, while for maintenance a twice-daily schedule appears also suitable. The existence of deep compartments and, therefore, risks of accumulation appear to be excluded.

6名健康志愿者口服1克三肽,并在10小时内用高压液相色谱法测定母体药物的血液浓度。个体和汇总数据分析表明,口服三叶肽后吸收良好,滞后时间为0.3小时,约1.1 ~ 1.3小时血药浓度达到峰值。代谢成去甲基、去乙酰、去甲基-去乙酰和羟基化衍生物在药物的生物转化中起主要作用,从而使其从血液中消失,分布半衰期约为1小时。消除半衰期约为5小时,因此建议每天3次的剂量计划用于装载,而每天两次的剂量计划用于维持似乎也是合适的。深隔室的存在,因此,积累的风险似乎被排除在外。
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引用次数: 0
Flunitrazepam prevents succinylcholine-induced increase in intra-ocular pressure. 氟硝西泮可防止琥珀胆碱引起的眼压升高。
Pub Date : 1985-01-01
E Vatashsky, S Zaroura

Ninety-three patients scheduled for various elective surgical procedures were divided into three equal groups and had induction of anaesthesia with either thiopentone (5 mg/kg), thiopentone (5 mg/kg) plus gallamine (0.3 mg/kg), or with flunitrazepam (0.03 mg/kg). Four minutes after induction they received a bolus intravenous injection of succinylcholine (1 mg/kg). Intra-ocular pressure was measured before and after induction, and approximately 1 minute after succinylcholine. It was found that flunitrazepam prevented the increase in intra-ocular pressure better than thiopentone plus gallamine. In both these groups, the subsequent intravenous administration of succinylcholine slightly increased the pressure but to levels below that noted before anaesthesia was induced. However, intra-ocular pressure was significantly increased above baseline levels when succinylcholine was injected after induction with thiopentone alone. Flunitrazepam is recommended, therefore, as a possible alternative for thiopentone-gallamine induction with succinylcholine when an increase in intra-ocular pressure must be prevented.

93例计划进行各种选择性外科手术的患者被分为三组,分别使用硫喷妥酮(5mg /kg)、硫喷妥酮(5mg /kg)加胆碱胺(0.3 mg/kg)或氟硝西泮(0.03 mg/kg)诱导麻醉。诱导后4分钟,静脉注射琥珀酰胆碱(1mg /kg)。在诱导前后及使用琥珀胆碱后约1分钟测量眼压。氟硝西泮对眼压升高的抑制作用优于硫喷妥酮加胆碱胺。在这两组中,随后静脉给药琥珀胆碱使血压略有升高,但低于诱导麻醉前的水平。然而,当单独用硫喷妥诱导后注射琥珀胆碱时,眼压明显高于基线水平。因此,当必须防止眼压升高时,推荐氟硝西泮作为硫喷妥-胆碱诱导胆碱的可能替代品。
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引用次数: 0
Controlled clinical assessment of the efficacy and tolerance of triletide versus antacids in patients with gastric and duodenal ulcers. 三叶肽与抗酸药对胃溃疡和十二指肠溃疡患者的疗效和耐受性的对照临床评价。
Pub Date : 1985-01-01
H Hoetzinger

A study was carried out in 30 out-patients with endoscopically confirmed active, benign gastric or duodenal ulceration to assess the comparative effectiveness and tolerance of treatment with triletide, a new synthetic tripeptide with anti-ulcer properties, with that of conventional antacids. Patients were allocated at random to receive treatment with either 1.6 g aluminium hydroxide and 1.6 g magnesium hydroxide per day or the antacids plus 1.5 g triletide per day over a period of 8 weeks. Heartburn and epigastric pain, monitored every other week, were significantly relieved by both treatments, but to a significantly greater extent (70% vs 20% on average, p less than 0.01) and significantly faster (p less than 0.01) in the presence of triletide. Endoscopic control showed that the patients who had triletide experienced complete healing in a significantly greater proportion (73% vs 27%, p less than 0.02) than those who had antacids only. The efficacy of treatments was the same, regardless of the actual ulcer location. Routine haematology and haematochemistry findings were unaffected by either treatment, and subjective possible side-reactions were limited to constipation (9 complaints overall) which is a well-known side-effect of antacid treatment. It would appear, therefore, that triletide is at least as well tolerated as antacids, while promoting the healing of peptic ulcers in a significantly greater proportion of patients and easing symptoms significantly faster and to a greater extent than antacids alone, regardless of the ulcer location.

本研究对30例经内窥镜确认为活动性良性胃或十二指肠溃疡的门诊患者进行了研究,以评估三肽(一种新型合成的具有抗溃疡特性的三肽)与常规抗酸药治疗的比较疗效和耐受性。患者被随机分配接受治疗,每天1.6 g氢氧化铝和1.6 g氢氧化镁或抗酸剂加1.5 g三肽,为期8周。每隔一周监测一次的胃灼热和胃脘痛,两种治疗均显著缓解,但在三叶肽存在时,缓解程度明显更大(70% vs 20%, p < 0.01),缓解速度明显更快(p < 0.01)。内窥镜对照显示,与仅使用抗酸药的患者相比,使用三肽的患者完全愈合的比例明显更高(73% vs 27%, p < 0.02)。无论溃疡的实际位置如何,治疗的效果都是相同的。常规血液学和血液化学结果均未受两种治疗的影响,主观可能的副作用仅限于便秘(总共9例),这是抗酸治疗的众所周知的副作用。因此,三联肽的耐受性至少与抗酸药一样好,同时促进消化性溃疡愈合的患者比例明显高于单独使用抗酸药,且缓解症状的速度和程度明显高于单独使用抗酸药,无论溃疡位置如何。
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引用次数: 0
Efficacy of penbutolol and a combination of a low dose of penbutolol with piretanide in the treatment of mild to moderate hypertension. 喷布托尔与小剂量喷布托尔联合吡雷他尼治疗轻中度高血压的疗效观察。
Pub Date : 1985-01-01
E Graml, M Verho, B Rangoonwala, R Englert, E Häringer, K Pahnke

A double-blind study was carried out in two parallel groups of patients with mild to moderate hypertension to assess the efficacy and tolerance of the combination 20 mg penbutolol plus 3 mg piretanide in comparison to 40 mg penbutolol alone over a period of 6 weeks. Active drug treatment in the 51 patients studied was preceded by a 2-week period of placebo. The results showed that in both groups there was an effective reduction in systolic and diastolic blood pressure compared with initial levels. Although there was no significant difference between the groups, the normalization of diastolic blood pressure (less than 95 mmHg) was achieved in 70% of the patients receiving the combination and in 59% of the patients treated with penbutolol alone. Pulse rate decreased in both groups, body weight only in the combination group. The biochemical and haematological parameters showed no clinically relevant changes during treatment with either drug regimens. Minor side-effects definitely or probably associated with the treatment were observed in both groups but were generally mild and did not interfere with treatment. No patient withdrew prematurely from the trial.

在两组轻度至中度高血压患者中进行了一项双盲研究,以评估20mg喷布托尔加3mg吡雷他尼与40mg喷布托尔单独联合使用的疗效和耐受性,为期6周。在研究的51名患者中,积极的药物治疗之前有2周的安慰剂期。结果显示,与初始水平相比,两组患者的收缩压和舒张压均有效降低。虽然两组之间没有显著差异,但70%的联合用药患者和59%的单用喷布托洛尔患者的舒张压达到了正常化(低于95 mmHg)。两组脉搏率均下降,仅联合用药组体重下降。两种药物治疗期间生化和血液学参数均无临床相关变化。在两组中都观察到轻微的副作用,这些副作用肯定或可能与治疗有关,但通常是轻微的,不会干扰治疗。没有患者过早退出试验。
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引用次数: 0
期刊
Pharmatherapeutica
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