Excretion of Cefamandole, Cefazolin, and Cephalothin into T-Tube Bile

The biliary tract excretion of cefamandole, cefazolin, and cephalothin was measured in eight patients with T-tubes inserted into their common ducts after ductal exploration for biliary tract stones. Each patient received 1.0 g intravenously of each cephalosporin on 3 separate days; T-tube bile and serum were collected at selected time intervals thereafter. In seven patients, bile and urine were collected for 6 h after the administration of each drug. Mean peak levels of cefamandole, cefazolin, and cephalothin in bile were 352, 46, and 12 μg/ml, respectively. The respective mean peak serum levels were 55.0, 92.8, and 32.4 μg/ml. Despite the fact that peak serum levels of cefazolin were 1.5 times those of cefamandole, levels in bile of cefamandole were about 8 times those of cefazolin. Over a 6-h period, almost three times as much cefamandole was excreted into bile as was cefazolin. Therefore, in those patients with biliary tract sepsis, in whom a cephalosporin is indicated for therapy, cefamandole appears to be the drug of choice.     

Pharmacology of Cephalothin in the Biliary Tract of Humans

Serum and biliary tract levels of cephalothin were determined in a large series of patients. Serum cephalothin levels in the therapeutic range were present at 1 h after a single dose of the antibiotic in only 4 of 39 (10.3%) subjects. Therapeutic bile cephalothin levels were achieved in only 2.4% of all subjects, and this occurred between 40 and 70 min after the administration of the antibiotic.     

Double-Blind Comparison of Cephacetrile with Cephalothin/Cephaloridine

Under double-blind protocol, a controlled comparison was made between a new cephalosporin, cephacetrile, and cephalothin or cephaloridine. The patient's primary physician determined the indications for treatment, and the dosage was uniform for each route of administration. Infecting strains of staphylococci and Proteus mirabilis had a lower median inhibitory concentration for cephalothin than cephacetrile; the opposite was true for Escherichia coli and Klebsiella species. The average peak serum level 1 h after a dose of 2 g intravenously was 74.9 +/- 21 and 21.5 +/- 8.7 mug/ml for cephacetrile and cephalothin, respectively; 6 h after the dose, the respective levels were 12.4 +/- 4.3 and 3.7 +/- 0.9 mug/ml. Renal clearances were similar and the plasma clearance was proportional to the serum levels. In the urine, the concentration of cephacetrile was three times higher than that of cephalothin. Based on a percentage of therapeutic potential, success in the treatment of infections with susceptible organisms was 42 and 44% for the two different drug regimens. Initial bacterial resistance was found in about one-fifth of infections, and concomitant therapy with other drugs was practiced in one-half of the treatment courses. Intravenous use of cephacetrile was discontinued prematurely more often than was use of cephalothin, suggesting less tolerance. Although there was no overt toxicity, more than 75% of patients on either regimen had some form of unwanted response to treatment, the most common being superinfection. From this limited but controlled experience, cephacetrile can be considered comparable to cephalothin in antimicrobial treatment and overall side reactions.     

Penetration of Cefazolin, Cephaloridine, and Cefamandole into Interstitial Fluid in Rabbits

We compared the penetration of three cephalosporins into interstitial fluid. Interstitial fluid was obtained in rabbits from Silastic tissue cages. Cefazolin, cephaloridine, and cefamandole were administered by the intramuscular route (30 mg/kg per injection). Peak blood levels and interstitial concentrations were studied after a single injection. Interstitial levels were also compared in a three-injection study (one injection every 12 h) and in a cumulative effect study (six injections), in which the interval between injections was established for each drug on the basis of its common therapeutic use. After a single injection, cephaloridine activity was detected more rapidly and attained higher levels than the other two drugs within the first 4 h. However, 2 h after the third injection, cefazolin levels in tissue fluid were higher than with cephaloridine. Cefamandole consistently gave the lowest interstitial levels. With all three drugs, detectable concentrations were present in interstitial fluid at a time when no detectable antibiotic was found in serum. In the six-injection study, the interstitial levels obtained with cefazolin were significantly higher than those observed with the other drugs. Our data suggest that cefazolin is a drug of choice due to its high extravascular levels.     

Comparison of Cefazolin, a New Cephalosporin Antibiotic, with Cephalothin

Resistance to cephalothin was associated in general with a lack of susceptibility to cefazolin, a new 7-amino cephalosporanic acid derivative.     

Pharmacokinetic Interpretation of Blood Levels and Urinary Excretion Data for Cefazolin and Cephalothin After Intravenous and Intramuscular Administration in Humans

Blood levels of cefazolin and cephalothin were determined in two separate crossover studies in 20 healthy male adults, each after intravenous and intramuscular administration. Pharmacokinetic parameters were calculated from the intravenous data based upon a two-compartment open model. The rate constants controlling the distribution between the central and peripheral compartments, the overall elimination rate constants, the apparent volumes of distribution, and the fraction of the dose in the central and peripheral compartments were determined. The bioavailability was calculated to be 100% for cefazolin and cephalothin.     

Comparative Stability of Cephalothin and Cefazolin in Buffer or Human Serum

A marked loss in potency was observed when cephalothin was incubated for 5 h in human serum at 37 degrees C. Cefazolin was stable under these conditions.     

蛋白质组学技术在胆道疾病临床研究中的应用

由于蛋白质组学研究高通量的特点,它成为早期诊断各种疾病（尤其是肿瘤）、寻找疾病新的标志物、指导分型的重要研究手段。胆道恶性肿瘤往往恶性程度高,不易早期诊断,术后5年生存率较低,在治疗上暂时无有效办法,寻求早期诊断、早期治疗无疑是相当重要的,因此蛋白质组学已成为胆道疾病研究的前沿领域和热点。     

Double-Blind Comparison of Phlebitis Produced by Cefazolin Versus Cephalothin

In a double-blind study with each patient as his own control, 1 g of cefazolin and 2 g of cephalothin were administered intravenously every 6 h to 20 patients in opposite arms for a period of 48 h each. The degree of phlebitis was significantly more severe with cephalothin than with cefazolin (P < 0.05); however, neither the incidence of phlebitis nor the time of onset of phlebitis was significantly different between the two drugs.     

Treatment of Experimental Staphylococcus aureus Endocarditis: Comparison of Cephalothin, Cefazolin, and Methicillin

The effectiveness of cefazolin in Staphylococcus aureus endocarditis has been questioned because of in vitro inactivation by staphylococcal beta-lactamase. Cefazolin, although inactivated in vitro by S. aureus beta-lactamase, was as effective as cephalothin in the treatment of left-sided S. aureus endocarditis in rabbits. Cefazolin (20 mg/kg every 6 or 8 h), cephalothin (40 mg/kg every 6 h), and methicillin (40 mg/kg every 6 h), administered intramuscularly, were compared in the treatment of left-sided endocarditis caused in rabbits by a highly penicillin-resistant strain of S. aureus. The three antibiotics were all effective in reducing titers in vegetations. However, at the dose used, methicillin reduced the titers more rapidly than cephalothin or cefazolin. Cefazolin concentrations in serum were about double those achieved with cephalothin or methicillin. However, cefazolin was only half as active as methicillin and one-eighth as active as cephalothin in vitro in a serum assay. The half life in serum of cefazolin, cephalothin, and methicillin were each about 30 min. Serum bactericidal activities of the three antibiotics were very similar.     

Treatment of Experimental Staphylococcus aureus Abscesses: Comparison of Cefazolin, Cephalothin, Cefoxitin, and Cefamandole

Cefazolin (CZ), cephalothin (CF), cefoxitin (CX), and cefamandole (CM) were evaluated in therapy of Staphylococcus aureus infection produced in perforated table tennis balls placed intraperitoneally in rabbits. Four weeks after placement of two balls in each rabbit, a beta-lactamase producing strain of S. aureus was injected into one of the balls. Twenty-four hours later therapy was initiated with 40 mg of CZ or 80 mg of CF, CX, or CM per kg intramuscularly every 6 h. After 24 h of treatment, the mean log(10) colony-forming units per ml were 7.1 for CZ, 6.7 for CF, 6.5 for CX, and 7.2 for CM. After 72 h the mean log(10) colony-forming units per ml were 5.0 for CZ, 4.1 for CF, 3.6 for CX, and 5.6 for CM. After 8 days, the titers were 1.6/ml for CZ, 1.0 for CF, 1.9 for CX, and 3.6 for CM. CZ serum levels were about double CF and CX levels and about two-thirds of CM levels. In sterile ball fluid CZ and CM levels were more than double CF or CX concentrations. Concentrations of all four antibiotics were lower in infected balls.     

Antibacterial Activity of Cefuroxime, a New Cephalosporin Antibiotic, Compared with That of Cephaloridine, Cephalothin, and Cefamandole

The in vitro activity of cefuroxime, a new cephalosporin derivative, was compared with that of cephaloridine, cephalothin, and cefamandole against strains of gram-positive and gram-negative bacteria recently isolated from clinical sources. Cefuroxime showed very similar activity to cefamandole against Staphylococcus aureus, Haemophilus influenzae, and most members of the Enterobacteriaceae. It was more active than cefamandole against gonococci, pneumococci, and most streptococci. Increasing the inoculum size appeared to have less effect on the minimum inhibitory concentrations of cefuroxime for gram-negative bacilli than has been found with the other cephalosporin derivatives, and minimum bactericidal concentrations of cefuroxime were only marginally greater than minimum inhibitory concentrations.     

Antibacterial Activity of Cefamandole, a New Cephalosporin Antibiotic, Compared with that of Cephaloridine, Cephalothin, and Cephalexin

The in vitro antibacterial activity of cefamandole, a new cephalosporin antibiotic, was compared with that of cephaloridine, cephalothin, and cephalexin against 1,213 strains of gram-positive and gram-negative bacteria recently isolated from clinical sources. The decreasing order of activity of the four agents against gram-positive cocci was cephaloridine, cephalothin, cefamandole, and cephalexin. However, cefamandole was the most active of the four against Haemophilus species and gram-negative bacilli susceptible to cephalosporins. It was also active against many strains resistant to the other cephalosporins, such as Enterobacter species and indole-positive Proteus species, but there was a marked inoculum effect with all of these organisms, and minimal bactericidal concentrations were usually considerably higher than minimal inhibitory concentrations. Cefamandole, like other cephalosporins, had no useful activity against Pseudomonas species.     

Effect of Diuretics on Urinary Excretion of Cephalothin in Humans

Diuretics and antibiotics are frequently used concomitantly. The possibility of drug interactions led us to study the effects of several diuretics on the renal elimination of cephalothin. Five healthy volunteers received a constant infusion of 500 mg of sodium cephalothin per h for 9 h on 4 consecutive days. Each day, after the third hour of infusion, the subjects were given one of the following in varying order: (i) furosemide (1 mg/kg, intravenous), (ii) mercaptomerin (250 mg, intramuscular), (iii) mannitol (25 g, intravenous), or (iv) no diuretic (control day). Fluid losses were replaced hourly. Serum and complete urine collections were obtained each hour and assayed for creatinine and cephalothin (bioassay). Clearances (milliliter per minute) and urinary excretions (milligram per hour) of cephalothin did not differ either when the diuretic day values were compared with control day, or when pre- and postdiuretic results on the same day were compared. Creatinine clearances were not affected by diuretics except for a transient rise after furosemide.     

高龄胆道病人263例围手术期处理

目的：总结高龄胆道疾病患者的治疗经验。方法：对1998年1月至2000年5月我科收治的60岁以上因胆道疾病入院患者的临床资料进行回顾性分析。结果：263例中合并内科疾病者169例,占64．26％,其中以心血管疾病最多,78例（46．15％）,其次为呼吸系统疾病,62例（36．64％）,行非手术治疗28周,发生并发症14例（505）,主要为肺部感染,死亡4例（14．295）。入院24小时内行急诊手术78例,发生并发症18例（23．1％）,死亡1例（1．28％）;24小时后行择期手术167例,发生并发症36例（21．6％）,死亡6例（3．595）。手术组术后并发症主要是肺部感染。结论：高龄胆道疾病患者合并病多,手术风险性增加,术后并发症发生率也较高,需加强围手术期处理;只要有手术指征,应尽早行手术治疗。     

自然组织谐波成像在胆道疾患中的应用价值

目的：通过与常规超声即基波成像的对比观察,探讨自然组织谐波成像在胆道疾患中的应用价值。方法：采用数字式超声诊断仪基波成像和自然组织谐波成像分别对60例各种胆道疾患患者和60例正常人进行胆道系统超声检查对比分析。结果：1、自然组织谐波成像的60例各种胆道疾患中胆囊隆起性病变、胆囊结石、胆总管结石、胆总管下端占位清晰显示率分别为100％、100％、93％、80％;而基波成像清晰显示率则分别为80％、90％、60％、40％,二者呈显著差异（P＜0．05）。总显示率自然组织谐波成像均在100％,而基波成像分别为100％、100％、87％、60％,后二者也呈显性差异;2、在超声检查的60例正常人对照组中,自然组织谐波成像的胆囊轮廓、胆囊壁层次显示清晰者为99％胆总管显示率为98％;而基波成像者则分别为90％和93％。二者有一定差异,但无统计学意义（P＞0．05）。结论：自然组织谐波成像对胆道系统疾患的超声图像能明显地改善信噪比和分辨率,提高二维图像质量。尤其是对胆总管疾患的声像图改善更为突出。自然组织谐波成像在检查胆道疾患中有极高的应用价值。     

纤维胆道镜治疗胆道残余结石的观察及护理

纤维胆道镜治疗胆道残余结石是临床治疗胆道残余结石的新途径。本文总结了我科２５０例纤维胆道镜取石术后护理经验。介绍了术后并发症：Ｔ管瘘管穿孔、胆道出血、术后发热、恶心、呕吐、导管脱出、十二指肠穿孔的临床观察及护理。