Pharmacokinetics, metabolism and renal excretion of sulfatroxazole and its 5-hydroxy- and N4-acetyl-metabolites in man

Hydroxylation is the predominant pathway of metabolism for sulfatroxazole in the body, accounting for 70 per cent of the dose. Fifteen per cent of the dose is acetylated unimodally and 10 per cent is excreted unchanged. The half-lives of sulfatroxazole and its metabolites 5-hydroxysulfatroxazole and N4-acetylsulfatroxazole are approximately 22 h after administration of sulfatroxazole. N4-acetylsulfatroxazole, taken as parent drug, is eliminated by renal excretion (92 per cent of the dose). The initial elimination half-life of N4-acetylsulfatroxazole is 4.5 h, which later increases to 70 h as the result of the acetylation-deacetylation equilibrium. Probenecid inhibits the renal excretion of the metabolites 5-hydroxy- and N4-acetylsulfatroxazole. Inhibition of the N4-acetyl metabolite favours the deacetylation, which results in an increase of the T 1/2 of sulfatroxazole from 20 to 30 h. The protein binding value of sulfatroxazole is 84 per cent, that of N4-acetylsulfatroxazole is 37 per cent. Sulfatroxazole is excreted renally by passive processes, while the metabolites are excreted by both passive and active processes.     

Performance and comparison of the Cockcroft-Gault and simplified Modification of Diet in Renal Disease formulae in estimating glomerular filtration rate in a Chinese Type 2 diabetic population.

AIMS: Our aim was to assess performances of the Cockcroft-Gault and simplified Modification of Diet in Renal Disease (MDRD) formulae in estimating glomerular filtration rate (GFR) in Chinese diabetic populations and their association with vascular risks. METHODS: A total of 1009 patients with Type 2 diabetes were categorized into low estimated GFR groups (GFR < 60 ml/min/1.73 m(2)) and control groups by the two equations. The performances of these formulae were assessed at different stages of kidney function. Carotid artery intima-media thickness (IMT) and the prevalence of diabetic retinopathy or albuminuria were compared among the groups. The ability of these formulae to identify established vascular risk markers using sensitivity, specificity, positive and negative predictive values were also compared. RESULTS: The prevalence of low estimated GFR was 32.7% with the Cockcroft-Gault formula and 5.2% with the MDRD formula, respectively. In low estimated GFR subjects by the MDRD formula, IMT was significantly thicker than those by the Cockcroft-Gault formula (1.2 mm vs. 1.0 mm; P < 0.05), with a higher prevalence of albuminuria (78.4 vs. 52.8%, P < 0.05) and diabetic retinopathy (46.5 vs. 30.5%; P < 0.05). The Cockcroft-Gault formula gave a specificity of 71.7% and a sensitivity of 37.0%, and the MDRD formula gave a specificity of 96.6% and a sensitivity of 7.9% in estimating low GFR relevant for established vascular risks. CONCLUSIONS: These formulae performed differently in Chinese diabetic populations. The simplified MDRD formula is minimally superior to the Cockcroft-Gault formula for its high specificity and positive predictive values in estimating low GFR relevant for vascular risks.     

Heart insufficiency in traumatic arteriovenous fistulas

Objective: To analyse the incidence, clinical presentation, and outcome of heart insufficiency in patients with chronic arteriovenous fistulas (AVF). Methodology: From 1991 to 2000 we treated 49 patients with traumatic AVF. The present study included 19 patients with AVF present for 6 months or longer, as it was presumed that these AVF will have an impact on cardiac overload. There were 16 male and three female patients with a mean age of 36 years (17–59). The time from injury to admission varied from 6 months to 33 years. Cardiological examination checked for dyspnoea and palpitation. ECG, chest X‐ray and ECHO‐cardiography were also performed. All AVF were deleted, magistral vessels reconstructed, non‐magistral obliterated, either surgically or by percutaneous embolization. Results: Mean follow up was 44.2 months (3–93). Serious heart insufficiency was seen in two patients only, with AVF in the subclavial vessels. Both suffered from serious heart disease prior to the therapeutic procedures that resulted in iatrogenic AVF, so it was difficult to connect heart insufficiency to the AVF alone. Despite surgical closure of AVF and intensive medical treatment, signs of heart insufficiency remained in both patients. Signs of cardiac overload were seen in six patients with long‐standing AVF in major vessels. Except for one patient who refused surgical closure of femoral AVF, the remaining five were symptom free for cardiac overload during the follow‐up period. Conclusion: In our series, heart insufficiency was an infrequent complication in long‐standing AVF, even when major vessels were involved.     

活体亲属肾移植手术的17例报告

目的总结活体亲属肾移植的临床经验。方法对供、受者进行全面的免疫学检查，对供者行IVU检查了解分侧肾功能，行DSA或MRA、螺旋CT血管三维成像检查了解血管的变异情况之后，开放式手术摘取供肾13例，经后腹腔镜活体供肾摘取4例，按常规方法移植给受者。免疫抑制方案为环孢素A（或FK506）、霉酚酸酯（或硫唑嘌呤、雷帕鸣）、强的松三联免疫抑制剂。结果13例开放式手术时间1．5～3．0h，平均2．0h；热缺血时间1．0～1．5min，平均1．2min；术中出血量60～200ml，平均140ml，术中及术后均未输血；术后住院7～10d，平均8d。4例后腹腔镜手术时间3．0～4．5h，平均3．5h；热缺血时间2．5～3．5min，平均2．8min；术中出血量60～100ml，平均75ml，术中及术后均未输血；术后3～5d出院。移植肾血液循环恢复后10～40s泌尿，平均20s。1例受者术后45d发生轻微的急性排斥反应，应用激素冲击3d后逆转，其余受者均无并发症。随访4～60个月，人／肾存活率为100％，移植肾功能良好。结论活体亲属肾移植安全可行，取左肾尽量靠近腹主动脉壁切断肾动脉，取右肾切取少许下腔静脉片。     

后腹腔镜联合经尿道电切镜治疗上尿路移行细胞癌(附83例报告)

目的 探讨后腹腔镜联合经尿道电切镜治疗上尿路移行细胞癌的效果和安全性. 方法 2003年3月～2006年7月,我院采用后腹腔镜联合经尿道电切镜治疗83例上尿路移行细胞癌.经尿道袖状电切患侧输尿管口周围1.5 cm范围膀胱壁达膀胱外脂肪组织,采用后腹腔镜切除肾及全长输尿管.术后留置导尿管7 d.11例术后辅助放疗. 结果 83例手术均成功.手术时间115～205 min,平均156 min.术中出血50～150 ml,平均80 ml.无术中并发症.术后住院7～11 d,平均8.5 d.病理报告：82例上尿路移行细胞癌,1例肾盂上皮中～重度不典型增生.术后随访3～38个月,平均10.8月.术后12个月内行膀胱镜检查发现膀胱肿瘤6例,其中5例行经尿道膀胱肿瘤电切,1例行腹腔镜根治性膀胱全切术、左侧输尿管皮肤造口术.2例肾盂肿瘤（pT3 G3和pT2 G3）于术后3个月肝转移.2例输尿管中段肿瘤（pT3 G3和pT3 G2～3）术后6个月原位复发并肺转移.1例输尿管下段肿瘤（pT3 G3）术后6个月骨转移.失访1例.其余71例均未发现肿瘤复发、切口转移及远处转移. 结论 对于上尿路移行细胞癌,采用后腹腔镜联合经尿道电切镜行肾、输尿管全切及膀胱袖套状切除具有创伤小、安全、恢复快等优点,值得临床推广应用.     

盐酸丁咯地尔治疗椎-基底动脉供血不足的效果

①目的　观察盐酸丁咯地尔对椎 基底动脉供血不足的治疗作用。②方法　将 82例椎 基底动脉供血不足病人随机分为两组 ,治疗组 4 2例 ,给予盐酸丁咯地尔 2 5 0mL静滴 ,每日 1次 ;对照组 4 0例 ,给予维脑路通0 .5g、胞二磷胆碱 0 .5 g静滴 ,每日 1次 ,均治疗 7d。检测两组治疗前后血液流变学和血流动力学指标的变化。 ③结果　治疗后治疗组全血高切黏度明显低于对照组 ,椎动脉平均血流速度 (VA)明显快于对照组 ,差异均有显著性(t=3.96 0 ,P <0 .0 1 ;t=2 .0 92 ,P <0 .0 5 )。治疗组治疗后全血高切、低切和血浆黏度明显低于治疗前 ,差异有显著性 (t=2 .74 6～ 2 .95 1 ,P <0 .0 1 ) ;VA、基底动脉平均血流速度 (BA)和外周血管阻力指数 (PI)高于治疗前 ,差异有显著性 (t=2 .732～ 5 .1 0 4 ,P <0 .0 1 )。对照组治疗后血浆黏度、PI明显低于治疗前 ,VA高于治疗前 ,差异均有显著性 (t=2 .1 6 8～ 2 .732 ,P <0 .0 5 ) ;全血高切、低切黏度、BA治疗前后差异无显著性 (t=0 .346～ 2 .0 0 8,P >0 .0 5 )。④结论　盐酸丁咯地尔对椎 基底动脉供血不足有良好的改善作用 ,其疗效明显优于维脑路通加胞二磷胆碱的治疗效果     

重组大鼠肝再生增强因子对急性肾衰竭大鼠肾脏的保护作用

目的 探讨重组大鼠肝再生增强因子(rrALR)对庆大霉素所致急性肾衰竭（ARF）大鼠肾小管上皮细胞及肾功能的保护作用。 方法 雌性Wistar大鼠150只，随机分成5组，每组30只，即健康对照组，ARF模型组，模型+空质粒对照组（空质粒组），模型+rrALR干预组（ALR组）：根据给予rrALR的剂量不同分为ALR1组和ALR2组两个亚组。分别于实验的第4、8、12、16和21天每组随机抽取6只大鼠在留取血、尿标本后，处死大鼠并取肾组织标本。常规生化方法检测各组大鼠BUN、Scr和尿N-乙酰-β-D-葡萄糖苷酶（NAG）酶的变化；PAS染色观察各组大鼠肾组织病理学改变；免疫组化法检测大鼠肾组织中ALR和增殖细胞核抗原（PCNA）的表达；Western印迹法检测肾组织中ALR蛋白的表达量。 结果 ARF大鼠各组BUN、Scr及尿NAG酶水平在第4、8、12、16天时均较对照组显著升高（P < 0.05）。与模型组和空质粒组相比，ALR组BUN、Scr及尿NAG酶水平明显降低（P < 0.05）；肾组织病理损害程度在各时间点明显减轻；而肾组织的ALR蛋白表达增加（P < 0.05）；肾小管上皮细胞增殖活跃；PCNA阳性细胞呈弥漫性分布，增殖指数（PI）明显升高（P < 0.05）。 结论 rrALR对急性损伤的肾小管上皮细胞具有减轻病变和促进再生修复的作用，可明显改善ARF大鼠的肾功能。     

中药肾区渗透并常规治疗高血压性肾损害40例疗效观察

目的：观察中药肾区皮肤外敷渗透加西药常规治疗高血压肾损害结果。方法：将部分中药粉碎微细化处理，将另部分中药液化处理．粉液混合装袋醋浸后外敷在肾区皮肤上，用药物导入仪肾区靶点式导人人体。并用一般西医常规治疗。结果：平均治疗3周血肌酐下降23％，BUN下降26％，24h蛋白尿下降23％，尿量增加16％，收缩压下降9％，舒张压下降7％。结论：中药的肾区皮肤外敷渗透加西医常规治疗效果明显高于一般常规治疗。     

后腹腔镜下肾肿瘤剜除术的临床疗效观察(附5例报告)

目的：探讨后腹腔镜下肾肿瘤剜除术的操作要点及临床价值。方法：采用后腹腔镜下肾肿瘤剜除术治疗肾肿瘤5例，其中肾癌3例，肾错钩瘤2例，瘤体直径1．5～4．0cm。具体方法是：①暴露瘤体和肾动脉；②采用硅胶管牵拉肾动脉，必要时可暂时阻断肾动脉；③于瘤体1cm正常肾组织处用电钩切除瘤体；④采用生物蛋白胶、止血纱布缝合加压处理创面出血。结果：手术均获成功。手术时间150～210min，术中出血80～350ml。术后1～2天肠道功能恢复并可床上活动，1～4天可下床活动。术后住院5～9天，平均7天。结论：后腹腔镜下肾肿瘤剜除术具有创伤小、康复快、安全、住院时间短等优点；对外生性生长、直径小于4cm瘤体，该法可作为首选手术方法。     

低能级体外冲击波碎石治疗肾鹿角形结石

目的探讨低能级体外冲击波碎石(extracorporeal shock wave lithortripsy,ESWL)治疗肾鹿角形结石的效果. 方法对18例鹿角形结石进行体外冲击波治疗.碎石能级1～3级,冲击次数1 800～3 000次,脉冲间隔60 ～80次/min,工作电压10～12.75 kV. 若结石直径>3 cm,在碎石前预先插入双J管,防止石街形成.对直径>4 mm的残余结石,再次行ESWL,直至结石完全消失. 结果所有病人耐受良好,治疗结束能自行回家.除1例碎石失败外,余17例经ESWL治疗成功.治疗3～9次,至完全排除结石.66例次(66/77,85.7%)术后有1～2次肉眼血尿.5例出现石街,长1.9～5.2 cm,4例石街经再次碎石成功,1例输尿管镜取石. 结论低能级ESWL治疗肾鹿角形结石是一种安全、有效的方法.