反相高效液相色谱法测定托拉噻米胶囊中托拉噻米的含量

目的建立高效液相色谱法测定托拉噻米胶囊中托拉噻米的含量。方法以岛津Sh impack CLC(M)C18(250 mm×4.6 mm,5μm)为色谱柱,以甲醇-0.02 mol.L-1磷酸二氢钾溶液(用磷酸调节pH至3.0)(65∶35)为流动相,检测波长为UV291 nm,流速为0.9 ml.min-1。结果托拉噻米在2~24μg.ml-1范围内具有良好线性关系(r=0.999 9),平均加样回收率为99.73%,相对标准差为0.17%;三批样品的标示百分含量(%)分别为99.8、100.1及100.4。结论本方法准确、灵敏度高、重现性好,可用于托拉噻米胶囊的含量测定。     

高效液相色谱法测定托拉塞米片中托拉塞米及其有关物质的含量

目的:建立高效液相色谱法测定托拉塞米片中托拉塞米及其有关物质的含量。方法:以岛津ShimpackCLC(M)C18(250mm×4.6mm,5μm)为色谱柱;以甲醇-0.02mol·L-1磷酸二氢钾溶液(用磷酸调节pH至3.0)(65∶35)为流动相;UV检测波长291nm;流速0.9mL·min-1。结果:托拉塞米在2～24mg·L-1范围内具有良好线性关系(r=0.9999),平均加样回收率为99.73%,RSD为0.17%(n=9);3批样品的标示百分含量(%)分别为99.80,100.10,100.40,有关物质的百分含量分别为0.58,0.45,0.39。结论:本方法准确、灵敏,重现性好,可用于托拉塞米片及其有关物质的含量测定。     

Torasemide in chronic heart failure: results of the TORIC study

BACKGROUND: Diuretics such as torasemide are commonly used to treat chronic heart failure (CHF). AIMS: The objective of the TOrasemide In Congestive Heart Failure (TORIC) Study was to investigate the safety, tolerability and efficacy of torasemide in CHF patients compared to furosemide or other diuretics in an open-label, non-randomised, post-marketing surveillance trial. METHODS: The present analysis shows the findings of 1377 patients with New York Heart Association (NYHA) class II-III CHF who received diuretic therapy with torasemide 10 mg/day orally (n=778) vs. patients who received furosemide 40 mg/day orally (n=527) or other diuretics (n=72) on top of their existing standard CHF therapy for 12 months. Besides safety and tolerability, efficacy was assessed by documentation of mortality, morbidity, functional class and serum potassium levels every 3 months. RESULTS: TORIC confirmed the safety and tolerability of torasemide in CHF patients. Mortality was significantly lower in the torasemide (n=17, 2.2%) than in the furosemide/other diuretics group (n=27, 4.5%) (P<0.05). Functional improvement as assessed by NYHA class was observed in more patients who received furosemide torasemide (n=356, 45.8%) than those who received furosemide/other diuretics (n=223, 37.2%) (P=0.00017). At the end of the study abnormally low serum potassium levels were observed in fewer torasemide (n=95, 12.9%) than furosemide/other diuretics patients (n=102, 17.9%) (P=0.013). CONCLUSION: Torasemide is safe and well tolerated in CHF patients. Although not designed as a mortality study, TORIC suggests a lower mortality amongst CHF patients treated with torasemide compared to furosemide/other diuretics. A functional improvement and a lower incidence of abnormal serum potassium levels were also observed in patients receiving torasemide as compared to those receiving furosemide/other diuretics.     

托拉塞米在重症心脏联合瓣膜置换病人围手术期中的应用

目的:通过对比托拉塞米与呋塞米的利尿作用,探讨托拉塞米在重症心脏联合瓣膜置换病人围手术期中的应用价值。方法:重症心脏联合瓣膜置换病人60例,随机分为2组。托拉塞米组30例,男性6例,女性24例,年龄(54±s 12)a,围手术期中应用托拉塞米静脉注射治疗;呋塞米组30例,男性5例,女性25例,年龄(54±12)a,围手术期中应用托拉塞米静脉注射治疗。观察用手术前及手术后1,3,7,14d,24h尿中钾、钠、肌酐的含量。结果:手术后,2组24h尿钠、钾和肌酐含量均增高,与手术前比较差异非常显著(P<0.01);手术后3d起,托拉塞米组24h尿钾、钠含量低于呋塞米组,肌酐含量高于呋塞米组,差异非常显著(P<0.01)。不良反应发生率托拉塞米组10％(3/30),呋塞米组80％(24/30),差异非常显著(P<0.01)。结论:托拉塞米具有排钠又相对保钾的作用,减少了不良反应的发生,是一种比呋塞米更加适合于重症联合心脏瓣膜置换术病人的围手术期利尿药物。     

托拉塞米的临床应用与评价

评价托拉塞米注射液在治疗水肿性疾病的利尿效果及安全性，对托拉塞米的作用机制、药效学、药动学、临床应用、安全性及用法用量进行综述。短期应用托拉塞米注射液治疗水肿性疾病利尿效果显著，不良反应少，值得临床推广应用。     

Renal excretory responses to single and repeated administration of diuretics in healthy subjects: Clinical connotations

Administration of an initial oral dose of hydrochlorothiazide 25 mg to healthy subjects is followed by increased 24-hour urinary outputs of sodium, chloride, and potassium. On the fourth day of once-daily dosing with hydrochlorothiazide 25 mg, 24-hour natriuresis and chloriuresis are no longer augmented, but the elevation in 24-hour kaliuresis that follows the first dose remains unchanged. Twenty-four-hour urinary calcium output is consistently reduced during repeated once-daily administration of hydrochlorothiazide 25 mg.The first oral dose of the loop diuretic torasemide augments the average natriuresis and kaliuresis in the 6 hours immediately after dosing in healthy subjects, in a dose-dependent fashion, within the 2.5 to 10-mg range. These increased urinary outputs are followed by rebounds below postplacebo values between 6 and 24 hours after dosing. As a result of this biphasic response, torasemide 2.5 mg qualifies as a nondiuretic formulation (it does not elevate 24-hour natriuresis), whereas torasemide 5 and 10 mg qualify as diuretic formulations. After the seventh dose of torasemide 5 or 10 mg during a regimen of once-daily therapy, 24-hour urinary sodium and chloride outputs no longer differ from their postplacebo counterparts. Twenty-four-hour kaliuresis tends to increase in a dose-dependent fashion after the first dose of torasemide (torasemide 2.5 and 5 mg do not augment it significantly), but this tendency is no longer present after the seventh once-daily dose, when torasemide (2.5, 5, or 10 mg) does not elevate the mean 24-hour kaliuresis. Twenty-four-hour calciuresis tends to increase in a dose-dependent manner (torasemide 2.5 mg does not elevate it significantly) after the first dose of torasemide; this calciuretic effect does not change in intensity after 7 days of once-daily treatment.     

Pharmacokinetics of torasemide and its metabolites in healthy controls and in chronic renal failure

Summary The pharmacokinetics of 20 mg torasemide i.v. has been studied in 7 healthy controls and 9 patients with varying degrees of renal impairment.Torasemide had a t_1/2 of about 4 h which was independent of kidney function, as the nonrenal clearance of torasemide was 3-times greater than its renal clearance. The active metabolite M1 and the main metabolite M5 were accumulated in chronic renal failure.In contrast to liver function, therefore, kidney failure does not have an important effect on the pharmacokinetics of torasemide.     

经典恒温法预测托拉塞米注射液的有效期

目的预测托拉塞米在室温下的有效期。方法采用HPLC法测定主药含量,用经典恒温法预测其有效期。结果托拉塞米的降解反应属一级反应,在室温(25℃)条件下的分解速度常数K25℃=5.186 9×10-6,该注射液在25℃时的有效期t0.9=2.32年。结论自制的托拉塞米注射液的有效期暂定为2年。     

托拉塞米及多巴胺联合静脉滴注治疗顽固性心力衰竭的观察与护理

目的观察大剂量托拉塞米联合多巴胺治疗顽固性心力衰竭的临床疗效。方法选择顽固性心力衰竭患者53例,随机分成2组：联合治疗组27例,在常规治疗基础上给予大剂量托拉塞米联合多巴胺治疗;对照组26例,给予常规治疗,治疗5～7d。观察患者血压、心率、尿量、肾功能及电解质等改善情况。结果治疗后,联合治疗组患者心率、体重、血钾、BNP下降,尿量、血钠、6min步行距离增加,NYH分级改善,水钠潴留明显减轻,与对照组比较,差异有统计学意义（P〈0．05）。结论托拉塞米联合多巴胺治疗顽固性心力衰竭具有较好疗效。