新袢利尿药：托拉塞米

托拉塞米(Jovasemide,Torsemide,商品名Demadex)为一新的袢利尿药,其作用与布美他尼及呋塞米相似,新近美国FDA已批准此新药用于治疗充血性心力衰竭、肾脏或肝脏疾病所致的水肿,亦可用于治疗高血压病。既可口服,也可静注。 1 作用机制 托拉塞米属吡啶磺酰脲类,降低血压的剂量几乎没有起到利尿作用,抗高血压作用的     

新一代强效利尿药——托拉塞米

托拉塞米（torasemide）是新一代高效髓袢利尿药，1993年在德国上市。2004年我国SFDA批准生产针剂（商品名特苏尼）。托拉塞米起效迅速，静脉注射后10min即起效，达峰时间为1-2h。体内半衰期为3．8h，作用持续时间长达5-8h。80％经肝脏代谢，20％以原形经肾脏排泄。有独特的醛固酮拮抗作用，使K^＋等电解质排泄量明显减少。长期应用不易产生利尿抵抗，患耐受性好。托拉塞米可作为顽固性心衰的一线用药，可有效地改善心衰的症状、体征和血流动力学指标，增加钠排泄。此药对肾功能无影响，适合急性和慢性肾衰的治疗。在发挥利尿作用的同时，还抑制肾素-血管紧张素-醛固酮系统活性，阻断腹水恶性循环，是治疗肝硬化腹水的有效药物。[第一段]     

长效袢利尿药托拉塞米临床研究进展

托拉塞米是一种新型长效吡啶磺酰脲类袢利尿药,作用于髓袢升支粗段,抑制氯和钠的重吸收而产生利尿排钠作用,本品能有效治疗高血压和水肿．不良反应较轻。     

托拉塞米在肾移植病人围手术期的应用

目的:通过对比托拉塞米与呋塞米的利尿作用,探讨托拉塞米在肾移植病人围手术期中的应用价值。方法:肾移植术后病人52例,分为2组。托拉塞米组26例,男性16例,女性10例,年龄(31±s 10)a,围手术期中应用托拉塞米100 mg+氯化钠注射液500 mL,iv,qd;呋塞米组26例,男性15例,女性11例,年龄(29±9)a,围手术期中应用呋塞米400 mg·d~(-1)+氯化纳注射液500 mL,iv,qd。2组均治疗7 d为一个疗程。观察手术前和术后每日尿钾、钠及血钾、钠的含量,血压、血肌酐和24 h尿量变化情况。监测2组病人环孢素全血谷值血药浓度。结果:手术后托拉塞米组24 h尿钠、血钠含量和血肌酐与呋塞米组比较,无显著差异(P>0.05)。托拉塞米组血钾的含量和24 h尿量高于呋塞米组,差异非常显著(P<0.01)。呋塞米组24 h尿钾含量高于托拉塞米组,差异非常显著(P<0.01)。2组血压和环孢素全血谷值血药浓度比较无显著差异(P>0.05)。不良反应发生率托拉塞米组8%(2/26),呋塞米组69%(18/26),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,在增加病人尿量的同时不影响环孢素全血谷值血药浓度,减少了肾移植病人不良反应的发生,是一种比呋塞米更加适合肾移植围手术期利尿药物。     

利尿药降压致低钾血症53例临床分析

利尿药是目前抗高血压药物的一大基石,尤其因其低廉的价格而广泛应用于社区临床。近年来,随着高血压患病率、知晓率、治疗率的不断提高,利尿药的应用也大大增加,随之而来的不良反应病例迅速增加,特别是低钾血症患者在日常门诊中经常可见。     

新型袢利尿剂托拉塞米

综述托拉塞米的药理作用、药动学、临床应用、药物不良反应和药物经济学。托拉塞米属吡啶磺酰脲类袢利尿剂，作用于髓袢升支粗段，抑制Cl^ 和Na^ 的重吸收，产生利尿、利钠和其他作用。其生物利用度高，半衰期相对较长，血浆蛋白结合率较高。临床试验表明，托拉塞米治疗高血压和慢性肾功能衰竭、肝功能不全或心力衰竭患者的水肿和其他症状有效，不良反应较轻。药物经济学分析表明，托拉塞米通过降低住院率和再住院率而降低总花费。     

两种二氢吡啶衍生物的合成和降压活性

两种二氢吡啶衍生物的合成和降压活性张三奇１）（第四军医大学西京医院药剂科，西安７１００３２）招明高冯锐２）梅其炳赵德化（第四军医大学药理学教研室，西安７１００３２）关键词二氢吡啶衍生物；合成；降压活性１，４二氢３，５吡啶二羧酸酯类化合物是一类重要...     

利尿药与其它药物的配伍问题

利尿药为临床常用药,与一些药物配伍使用时能产生不良反应,应注意避免。     

托拉塞米的利尿作用和安全性

目的 观察健康受试者口服托拉塞米的利尿作用和安全性。方法 19名健康男性受试者单次口服不同剂量托拉塞米5,10和20 mg(n=9)或连续7天每日口服托拉塞米10 mg(n=10)。观察血压,尿量,24 h尿钾、钠、氯和血钾、钠、氯,心率,呼吸,心电图和心电监测,血常规,尿常规,血生化等指标。 结果 5,10,20mg 3组单次服药后24 h总尿量分别为2.24,2.60和3.17 L(P<0.05),24 h尿钾、钠、氯的排泄随托拉塞米剂量增加而略增加(P>0.05)。连续服药,首次药后的24h尿量及尿钾、钠、氯的量最多。单次和连续给药后血钾、钠、氯均未见下降,甘油三脂增加0.1~0.4 mmol.L-1(P<0.05)。4例受试者出现药物不良反应。 结论 在5~20 mg,托拉塞米利尿作用随剂量增加而增加,国人对托拉塞米耐受性良好。     

托拉塞米对重度心力衰竭的短期临床疗效观察

目的探讨托拉塞米对重度心力衰竭的短期临床疗效及副作用。方法58例重度心力衰竭分为托拉塞米组与呋塞米组,在心衰常规治疗方法相同的情况下,比较两组对心衰患者总有效率、尿量、浮肿消退、血钾、血钠、血Cr变化。结果托拉塞米组总有效率明显优与呋塞米组（93．7％ vs 82．1％P〈0．05）存在显著性差异;尿量（2600ml vs 2100ml）,存在显著差异（P〈0．05）;浮肿消退：托拉塞米组明显消退95．8％,呋塞米组63．6％存在显著差异（P〈0．05）．在每日补钾相同情况下,托拉塞米组血钾上升0．2mmol·L^-1未发生新的低血钾,呋塞米组血钾下降0．1mmol·L^-1低血钾发生率两组存在显著差异（P〈0．05）,两组对血钠、血Cr影响无显著性差异。结论托拉塞米对重度心力衰竭患者有较好的短期疗效、利尿作用强、浮肿消退率高、副作用相对较少。     

Evaluation in man of bumetanide,a new diuretic agent

Summary Bumetanide, a new diuretic, has been studied in ten healthy volunteers, who received single oral doses of 0.125 to 1.50 mg. It was potent and had, a rapid action; the maximum effect occurred within 60 to 90 min and lasted for 5 to 6 h. Within 60–90 min of a 1 mg dose the urine volume increased from 1 to about 10 ml/min and sodium excretion from about 100 µEq/min to about 1000 µEq/min. There was only a slight increase in potassium excretion. The mean total urinary volume during the first six hours after 1 mg of bumetanide was approximately 1500 ml. The increase of diuresis and saluresis after 0.125 mg was slight. In the dosage range of 0.125 to 1.0 mg there was a linear relationship between dose and increase in urinary volume and sodium excretion. Increasing the dose from 1.0 to 1.5 mg did not produce a correspondingly larger diuresis. The optimal range of doses of bumetanide appears to lie between 0.25 to 1.00 mg, according to the present results obtained in ten healthy volunteers.     

Ketanserin combined with a beta-blocker or diuretic in essential hypertension. A multicentre study

Summary The antihypertensive effect of ketanserin 40 mg b.d. in combination with a beta-adrenergic blocking agent or a diuretic was assessed in an open study in 35 patients with essential hypertension, who had not responded to treatment with beta-blockers, diuretics or their combination.The ketanserin/beta-blocker combination decreased mean sitting systolic/diastolic blood pressure (SBP/DBP) from 169/107 mm Hg to 156/91 mm Hg at the end of the 12-week active treatment period. The decrease in systolic blood pressure was significant only at Week 8, while the decrease in diastolic blood pressure was highly significant at all times. A significant reduction in heart rate by 10 beats·min^–1 was observed with the ketanserin + -blocker combination.The ketanserin/diuretic combination led to a significant reduction in mean SBP/DBP from 164/106 mm Hg to 146/92 mm Hg after 12 weeks, with no significant change in heart rate. Body weight slightly increased in both groups.There were significantly fewer adverse reactions with the ketanserin/diuretic combination than with the ketanserin/beta-blocker combination.The results indicate a potentially useful therapeutic role for ketanserin in combination with beta-blockers or diuretics.     

Valsartan, a new angiotensin II antagonist for the treatment of essential hypertension: efficacy and safety compared to hydrochlorothiazide

Objective: To compare the antihypertensive efficacy of a new angiotensin II antagonist, valsartan, with a reference therapy, hydrochlorothiazide (HCTZ). Methods: In this double-blind study, 167 adult outpatients with mild-to-moderate essential hypertension were randomly allocated in equal number to receive valsartan 80 mg or HCTZ 25 mg for 12 weeks. In patients whose blood pressure (BP) remained uncontrolled after 8 weeks of monotherapy, atenolol 50 mg was added to the initial treatment. Patients were assessed at 4, 8 and 12 weeks. The primary efficacy variable was change from baseline in mean sitting diastolic BP (SDBP) at 8 weeks. Secondary variables included change in sitting systolic BP (SSBP) and responder rates (percentage of patients with SDBP <90 mmHg or drop ≥10 mmHg compared to baseline) at 8 weeks. Results: Valsartan and HCTZ were both effective at lowering diastolic and systolic blood pressure at all time points. Similar falls were seen in both groups with no significant differences between treatments. For the primary variable (decrease in SDBP) there was no significant difference between treatments. For SSBP there was also no significant difference observed. Responder rates at 8 weeks were 74% for valsartan and 62% for HCTZ (P = 0.10). Both treatments were well tolerated, both as monotherapy, and when combined with atenolol 50 mg per day. Conclusion: The data show valsartan 80 mg to be as effective as HCTZ in the treatment of mild-to-moderate hypertension. The results also show valsartan to be well tolerated when taken alone or in combination with atenolol. Received: 7 March 1996 / Accepted in revised form: 29 July 1996     

Development,implementation and cost-effectiveness of a protocol for review of combination diuretic prescribing

AIMS: To determine the extent of inappropriate prescribing of combination diuretics and the cost implications of protocol implementation. METHODS: Pharmacist-run medication review clinics in two general practices in Bradford, UK. RESULTS: Sixty-one patients, mean +/- s.d. age 75.8 +/- 12.0 years, were reviewed. Thirty-six met protocol criteria; 30 (49.2%) patients had their potassium-sparing diuretics (PSDs) discontinued. Mean (95% confidence interval) reduction in serum potassium concentrations after intervention in these 30 patients was 0.26 (0.09, 0.43) mmol l(-1) (P < 0.01). Twenty-eight (93.3%) patients were within the reference range at follow-up; none was below. CONCLUSIONS: Of prescribed PSDs, 59% were found to be unnecessary. Using the developed protocol potentially improves drug safety and enables cost savings.     

甘露醇并活血利水中药治疗创伤性足踝部肿胀的疗效及安全性分析

目的探讨甘露醇并活血利水中药治疗创伤性足踝部肿胀的临床疗效和安全性。方法回顾性分析我院2007年3月至2012年5月收治的120例创伤性足踝部肿胀患者的临床资料。120例患者随机分为2组,每组60例。观察组采用甘露醇并活血利水中药进行治疗,对照组采用甘露醇单独治疗,对比两组的临床疗效。结果治疗后,两组患者足踝部肿胀情况均有所改善,其中观察组肿胀改善的总有效率为76.6%,明显高于对照组(56.6%,P<0.05);两组患者均未出现明显的不良反应。结论甘露醇联合活血利水中药治疗创伤性足踝肿胀安全性高,且疗效确切,较单用甘露醇治疗效果更明显。     

新型袢利尿剂托拉塞米治疗心衰进展

组织水肿是心衰发生、发展过程中的重要环节,袢利尿剂的应用是心衰治疗的重要组成部分.托拉塞米是一种新型的吡啶磺酰脲类袢利尿剂.近十余年的研究证实,托拉塞米在心衰的治疗方面有良好的作用:利尿作用更强、生物利用度更高、半衰期更长、作用更持久;对电解质、血糖、血脂代谢均无影响;主要在肝脏代谢.因此,对肾脏功能不全者不会产生蓄积,可以长期使用.本文就新型袢利尿剂托拉塞米治疗心衰的研究作一综述.     

利尿剂对老年高血压患者血压、血钾、尿酸及三酰甘油的影响

目的 探究利尿剂对老年高血压患者血压、血钾、尿酸及三酰甘油的影响,为该病临床治疗积累相关实践性经验.方法 选取本院心内科于2010年1月～2012年12月收治的102例高血压患者,根据服用降压药物的不同进行分组,分为利尿剂组（50例）和非利尿剂组（52例）.同时选取同期来院门诊或复查的老年高血压者（未服用降压药或自行停药1个月以上者）,设为对照组.结果 3组的血压、体质指数、肌酐、TC、HDL-C、LDL-C和LVEF差异无统计学意义（P＞0.05）;利尿剂组、非利尿剂组的收缩压、舒张压均低于对照组（P＜0.05）,利尿剂组的血钾低于非利尿剂组、对照组（P＜0.05）,尿酸和三酰甘油均高于非利尿剂组、对照组（P＜0.05）;继续服用利尿剂组的血钾低于停服利尿剂组,血尿酸高于停服利尿剂组（P＜0.05）.结论 老年高血压患者服用利尿剂与非利尿剂的降压效果相当,但长期服用会增高低血钾、高尿酸及高血脂发生率,因此,医生应指导服用利尿剂患者定期来院检测上述指标,并针对异常数值给予早期干预.     

藏西医结合治疗顽固性高血压临床疗效观察

目的探讨藏西医结合治疗顽固性高血压病的临床疗效。方法对512例顽固性高血压患者分别用藏西医结合治疗及西医治疗进行临床疗效对比观察分析。结果藏西医结合组的疗效明显优于西医组,两组比较有差异,P〈0．005,说明有显著性。结论在合理选择西药的同时加用藏药珊瑚七十味治疗顽固性高血压,收到了降压稳定及较为确切的逆转左心室肥大、动脉硬化等靶器官损害的疗效。