左氧氟沙星治疗细菌性感染的疗效观察

目的以左氧氟沙星注射液和洛美沙星注射液随机对照治疗中、重度急慢性呼吸道、泌尿道感染，评价左氧氟沙星的疗效和安全性。方法108例病人随机分成两组，左氧氟沙星组59例（男35例，女24例）用左氧氟沙星0．2g静脉滴注bid，洛美沙星组49例（男25例，女14例），用洛美沙星0．2g静脉滴注bid，5～8d为一疗程。结果左氧氟沙星有效率为92％，不良反应率为3．3％，洛美沙星组分别为84％、6.12％。两组相比差异无显著性意义（P〉0．05）。结论左氧氟沙星治疗细菌引起的各种感染疗效显著，不良反应少。     

左氧氟沙星治疗急性呼吸道感染35例疗效观察

我院应用左氧氟沙星注射液治疗急性呼吸道感染35例,并与应用洛美沙星注射液30例作疗效比较,报告如下。     

盐酸左氧氟沙星注射液与乳酸左氧氟沙星注射液治疗下呼吸道感染的比较

目的比较盐酸左氧氟沙星注射液与乳酸左氧氟沙星注射液治疗下呼吸道感染的疗效、不良反应。方法采用回顾性调查分析的方法,将符合入选条件的下呼吸道感染患者分成两组:盐酸左氧氟沙星注射液治疗组60例,0.3 g2次/d,静脉滴注,乳酸左氧氟沙星注射液治疗组58例,0.5 g 1次/d,静脉滴注,疗程均为7～14 d。结果盐酸左氧氟沙星注射液与乳酸左氧氟沙星注射液治疗下呼吸道感染的有效率分别为83.33%和87.93%,痊愈率分别为71.67%和77.59%,不良反应发生率均为6.3%,两组相比较均无显著性差异(P>0.05)。结论左氧氟沙星是一种治疗下呼吸道感染的理想药物,盐酸左氧氟沙星注射液与乳酸左氧氟沙星注射液同样安全有效,临床疗效和不良反应相仿。     

注射用门冬氨酸洛美沙星与盐酸左氧氟沙星存在配伍禁忌

注射用门冬氨酸洛美沙星是一种广谱抗菌药,临床用于胃肠道细菌感染、呼吸道感染以及泌尿系等敏感细菌引起的感染。盐酸左氧氟沙星临床用于各种炎症所引起的重度感     

注射用门冬氨酸洛美沙星与盐酸左氧氟沙星存在配伍禁忌

注射用门冬氨酸洛美沙星是一种广谱抗菌药,临床用于胃肠道细菌感染、呼吸道感染以及泌尿系等敏感细菌引起的感染。盐酸左氧氟沙星临床用于各种炎症所引起的重度感     

乳酸左氧氟沙星治疗下呼吸道感染的临床疗效分析

目的:观察乳酸左氧氟沙星治疗下呼吸道感染的临床疗效和安全性.方法:120例患者随机分为两组,乳酸左氧氟沙星治疗组,每天0.4g;洛美沙星为对照组,每天0.4 g,疗程7～10d.结果:乳酸左氧氟沙星治疗痊愈率81.7%,总有效率,细菌清除率91.7%,其临床疗效均显著高于对照组,差别有显著性(P<0.05);乳酸左氧氟沙星不良反应发生率轻微,患者可耐受.结论:两组病例均未出现肝肾功能及造血系统功能损伤,表明乳酸左氧氟沙星是治疗呼吸道有效和安全的药物,具有较高的临床应用价值.     

顺序注射分光光度法测定左氧氟沙星、氧氟沙星和洛美沙星

本文基于左氧氟沙星、氧氟沙星和洛美沙星分别与Fe(Ⅲ)作用形成黄色络合物的现象,建立了简单、快速测定药物中左氧氟沙星、氧氟沙星和洛美沙星的顺序注射分光光度新方法。讨论了物理因素和化学因素对方法灵敏度的影响。测定左氧氟沙星、氧氟沙星和洛美沙星的工作曲线的线性范围均为10~250μg/ml。采用摩尔比法和连续变换法测定络合物的组成,Fe(Ⅲ)与药物的组成比为1∶2。将方法用于药物中左氧氟沙星、氧氟沙星和洛美沙星的测定,并与参考方法进行了对照。     

乳酸左氧氟沙星治疗下呼吸道感染120例的临床疗效分析

目的 :观察乳酸左氧氟沙星治疗下呼吸道感染的临床疗效和安全性。方法 :12 0例患者随机分为两组 ,乳酸左氧氟沙星为治疗组 ,每天 0 .4 g;洛美沙星为对照组 ,每天 0 .4 g,疗程 7～ 10 d。结果 :乳酸左氧氟沙星治疗痊愈率 81.7% ,总有效率93.3% ,细菌清除率 91.7% ,其临床疗效均显著高于对照组 ,差别有显著性 (P <0 .0 5 ) ;乳酸左氧氟沙星不良反应发生率为3.3% ,且大多轻微 ,患者可耐受。结论 :两组病例均未出现肝肾功能及造血系统功能损伤 ,表明乳酸左氧氟沙星是治疗呼吸道感染的有效和安全的药物 ,具有较高的临床应用价值。     

左氧氟沙星治疗呼吸道感染的临床疗效

左氧氟沙星(levofloxacin)为新一代喹诺酮类抗菌药,具有比氧氟沙星更强及更广谱的抗菌作用。为观察左氧氟沙星治疗呼吸道感染的临床疗效和安全性,我院于1999年1月～2001年12月采用左氧氟沙星治疗30例呼吸道感染病例,取得了较好的疗效,现将结果报道如下。     

左氧氟沙星治疗下呼吸道感染临床观察

目的评价左氧氟沙星治疗下呼吸道感染的效果和安全性。方法收集左氧氟沙星治疗下呼吸道感染病例110例,采用随机对照的方法,分实验组55例,对照组55例。实验组给予左氧氟沙星0．2g,2次／d;对照组给予罗红霉素0．15g,2次／d;疗程均为12d。结果左氧氟沙星和罗红霉素的有效率分别为92．73％和90．90％,不良反应发生率分别为3．64％和5．45％。结论左氧氟沙星与治疗下呼吸道感染疗效确切的罗红霉素比较,无明显差异,左氧氟沙星可作为治疗下呼吸道感染的一线药物。     

3种喹诺酮类药物治疗老年性肺炎的药物经济学评价

目的 :评价3种喹诺酮类药物治疗老年性肺炎的疗效及经济效果。方法 :选择186例老年性肺炎患者 ,随机分为3组 ,分别给予氧氟沙星、左氧氟沙星、洛美沙星治疗 ,观察各组疗效并运用药物经济学方法进行分析。结果 :3组治疗有效率分别为80 65 %、87 1 %、72 58 % ;不良反应发生率分别为7 65 %、6 35 %、13 81 %。平均成本 -效果比分别为2176、3464、3732。结论 :药物经济学分析结果为氧氟沙星优于左氧氟沙星 ,优于洛美沙星。     

Permeability classification of representative fluoroquinolones by a cell culture method

This study was undertaken to categorize representative fluoroquinolone drug substance permeability based on the methods outlined in the Food and Drug Administration's biopharmaceutic classification system (BCS) Guidance for Industry. The permeability of ciprofloxacin, levofloxacin, lomefloxacin, and ofloxacin was measured in an in vitro Caco-2 assay with previously demonstrated method suitability. The permeability class and efflux potential were ascertained by comparing test drug results with standard compounds (metoprolol, atenolol, labetalol, and rhodamine-123). All 4 quinolones drugs demonstrated concentration-dependent permeability, indicating active drug transport. In comparing absorptive versus secretive in vitro transport, the tested fluoroquinolones were found to be subject to efflux in varying degrees (ciprofloxacin > lomefloxacin > rhodamine 123 > levofloxacin > ofloxacin). Based on comparison to labetalol, the high permeability internal standard, ciprofloxacin was classified as a low permeability drug, whereas lomefloxacin, levofloxacin, and ofloxacin were classified as high permeability drugs. The in vitro permeability results matched human in vivo data based on absolute bioavailabilities. This laboratory exercise demonstrated the applicability of an in vitro permeability method for classifying drugs as outlined in the BCS Guidance.     

3种抗菌药治疗老年性肺炎的药物经济学评价

目的：评价3种抗菌药治疗老年性肺炎的疗效及经济效果。方法：选择372例老年性肺炎患者，随机分为3组，分别给予头孢曲松钠、左氧氟沙星、洛关沙星治疗，观察各组疗效并运用药物经济学方法进行分析。结果：3组治疗有效率分别为80．65％、87．1％、72．58％；不良反应发生率分别为7．65％、6．35％、13．81％。平均成本一效果比分别为6528、10392、11196。结论：药物经济学分析结果为头孢曲松钠优于左氧氟沙星，优于洛关沙星。     

3种喹诺酮类药物治疗呼吸道感染的成本-效果比较

目的比较氧氟沙星、左氧氟沙星及洛美沙星治疗呼吸道感染的成本-效果,促进临床合理用药。方法回顾性分析医院2011年6月至12月收治的134例呼吸道感染患者的临床资料,根据不同治疗方法分为氧氟沙星组、左氧氟沙星组和洛美沙星组,采用药物经济学方法进行分析。结果氧氟沙星、左氧氟沙星及洛美沙星的有效率分别为80.43%,88.64%,77.27%,成本-效果比值分别为6.27,6.16,6.88。结论左氧氟沙星注射液是治疗呼吸道感染最安全有效、经济合理的药物。     

Levofloxacin for prophylaxis in breast cancer surgery compared with ofloxacin

BACKGROUND: We found that once-daily use of ofloxacin is beneficial from the standpoints of economy and patient compliance. Levofloxacin, has twice the antimicrobial activity and same toxicity of ofloxacin. We investigated the clinical usefulness of levofloxacin compared with ofloxacin in breast surgery. METHOD: Between July, 1996 and April, 1999, 199 consecutive patients hospitalized in our department for treatment of breast cancer were enrolled in this study with their informed consent and 181 patients were evaluated. RESULTS: Four (4%) of the 99 patients in the levofloxacin group had wound infections, as did 5 (6%) of the 82 patients in the ofloxacin group. The median times needed for wound care, with 25th and 75th percentiles, were 13 [9, 16] days in the levofloxacin group and 11 [9, 16] days in the ofloxacin group. From infected wound three strains of Staphylococcus aureus were detected from the levofloxacin group and two strains were from ofloxacin group, but no methicillin-resistant strains were isolated. Multiple regression analysis showed that only wound dehiscence was a significant factor in the occurrence of wound infection and the period of wound care. No signs or symptoms suggesting levofloxacin or ofloxacin toxicity were observed. Laboratory test changes before and after treatment were similar in the two groups. CONCLUSION: It appears that levofloxacin is not superior to ofloxacin in prophylactic efficacy for postoperative wound infection after breast surgery.     

Binding characteristics of fluoroquinolones to synthetic levodopa melanin

To define the binding characteristics of fluoroquinolones to synthetic levodopa melanin, the binding of various drugs, including levofloxacin and ofloxacin, and positive controls (timolol and chloroquine), was investigated in-vitro. The affinity and capacity of the drug binding were calculated by Langmuir's adsorption isotherm. The affinity constant (K) and the binding capacity (r(max)) of levofloxacin were similar to those of timolol and much lower than those of chloroquine. Racemic ofloxacin and its enantiomers showed similar K and r(max), suggesting that the binding lacked stereoselectivity. The binding experiment with levofloxacin derivatives indicated that the basic nitrogen atom at position 7 of the quinolone ring, but not carboxyl group at position 3, would play a critical role in the interaction of fluoroquinolones with melanin. The melanin-drug complexes of levofloxacin and chloroquine were washed with neutral phosphate buffer, ethanol and 1 M HCl solution to explain the nature of the interaction of melanin with the drugs. Electrostatic forces mainly participate in the formation of the chloroquine-melanin complex, whereas van der Waals' and hydrophobic interactions are involved in the levofloxacin-melanin complex in addition to electrostatic forces. The interactions of various fluoroquinolones such as norfloxacin, enoxacin, sparfloxacin, ciprofloxacin and lomefloxacin with melanin were also studied. The results showed that the relative K value was: chloroquine approximately ciprofloxacin, sparfloxacin >/= lomefloxacin > timolol, levofloxacin approximately enoxacin, norfloxacin, and that the relative r(max) value was: norfloxacin, enoxacin >/= chloroquine, sparfloxacin > levofloxacin, ciprofloxacin, timolol, lomefloxacin. The fluoroquinolones vary in their affinity and capacity to bind with melanin, and ciprofloxacin and sparfloxacin showed a stronger interaction with melanin than the other fluoroquinolones studied.     

Levofloxacin

Levofloxacin (DR-3355, Daiichi) is a new fluoroquinolone antibiotic which is the active isomer of ofloxacin (DL-8280, Daiichi). By removing the inactive isomer, the in vitro activity of levofloxacin is 8-128 times higher than that of ofloxacin. This means that bacterial species, which have borderline susceptibility to ofloxacin and other first generation fluoroquinolones (e.g., pneumococci and organisms causing atypical pneumonia), are considerably more sensitive to levofloxacin. The pharmacokinetics of levofloxacin, which is available for both oral and i.v. administration, are characterised by a very high bioavailability, low (30-40%) protein binding, high tissue concentrations and elimination via the kidneys with minimal liver metabolism. As a consequence of the low degree of metabolism, levofloxacin does not interact with other drugs to any major extent. The safety and efficacy of levofloxacin are well documented in lower respiratory tract infections, skin and soft tissue infections, and urinary tract infections. The safety profile seems advantageous and the risks of phototoxicity, CNS toxicity and cardiac reactions (prolongation of QT-time) are low. Serious liver toxicity, leading to the recent withdrawal of trovafloxacin, has not been a problem in levofloxacin studies. Levofloxacin is a valuable addition to the group of fluoroquinolone antibiotics.     

国产盐酸洛美沙星体内外抗菌作用实验研究

盐酸洛美沙星对革兰阴性菌具有强的抗菌活性，其ＭＩＣ５０多数为０．２５ｍｇ·Ｌ－１；对金葡球菌ＭＩＣ５０为０．５ｍｇ·Ｌ－１；对绿脓假单胞菌ＭＩＣ５０为１ｍｇ·Ｌ－１。盐酸洛美沙星体外抗菌活性与诺氟沙星、氧氟沙星相近而略逊于环丙沙星。盐酸洛美沙星对金葡球菌、大肠杆菌和绿脓假单胞菌感染小鼠ｉｖ的ＥＤ５０分别是４．４７、１．６２和１７．１３ｍｇ·ｋｇ－１，体内抗菌作用较环丙沙星弱但强于诺氟沙星和／或氧氟沙星。     

Levofloxacin: a review of its use in the treatment of bacterial infections in the United States

Levofloxacin (Levaquin) is a fluoroquinolone antibacterial agent with a broad spectrum of activity against Gram-positive and Gram-negative bacteria and atypical respiratory pathogens. It is active against both penicillin-susceptible and penicillin-resistant Streptococcus pneumoniae. The prevalence of S. pneumoniae resistance to levofloxacin is <1% overall in the US.A number of randomised comparative trials in the US have demonstrated the efficacy of levofloxacin in the treatment of infections of the respiratory tract, genitourinary tract, skin and skin structures. Sequential intravenous to oral levofloxacin 750mg once daily for 7-14 days was as effective in the treatment of nosocomial pneumonia as intravenous imipenem/cilastatin 500-1000mg every 6-8 hours followed by oral ciprofloxacin 750mg twice daily in one study. In patients with mild to severe community-acquired pneumonia (CAP), intravenous and/or oral levofloxacin 500mg once daily for 7-14 days achieved clinical and bacteriological response rates similar to those with comparator agents, including amoxicillin/clavulanic acid, clarithromycin, azithromycin, ceftriaxone and/or cefuroxime axetil and gatifloxacin. A recent study indicates that intravenous or oral levofloxacin 750mg once daily for 5 days is as effective as 500mg once daily for 10 days, in the treatment of mild to severe CAP. Exacerbations of chronic bronchitis and acute maxillary sinusitis respond well to treatment with oral levofloxacin 500mg once daily for 7 and 10-14 days, respectively.Oral levofloxacin was as effective as ofloxacin in uncomplicated urinary tract infections and ciprofloxacin or lomefloxacin in complicated urinary tract infections. In men with chronic bacterial prostatitis treated for 28 days, oral levofloxacin 500mg once daily achieved similar clinical and bacteriological response rates to oral ciprofloxacin 500mg twice daily. Uncomplicated skin infections responded well to oral levofloxacin 500mg once daily for 7-10 days, while in complicated skin infections intravenous and/or oral levofloxacin 750mg for 7-14 days was at least as effective as intravenous ticarcillin/clavulanic acid (+/- switch to oral amoxicillin/clavulanic acid) administered for the same duration.Levofloxacin is generally well tolerated, with the most frequently reported adverse events being nausea and diarrhoea; in comparison with some other quinolones it has a low photosensitising potential and clinically significant cardiac and hepatic adverse events are rare. CONCLUSION: Levofloxacin is a broad-spectrum antibacterial agent with activity against a range of Gram-positive and Gram-negative bacteria and atypical organisms. It provides clinical and bacteriological efficacy in a range of infections, including those caused by both penicillin-susceptible and -resistant strains of S. pneumoniae. Levofloxacin is well tolerated, and is associated with few of the phototoxic, cardiac or hepatic adverse events seen with some other quinolones. It also has a pharmacokinetic profile that is compatible with once-daily administration and allows for sequential intravenous to oral therapy. The recent approvals in the US for use in the treatment of nosocomial pneumonia and chronic bacterial prostatitis, and the introduction of a short-course, high-dose regimen for use in CAP, further extend the role of levofloxacin in treating bacterial infections.     

Chemotherapeutic efficacy of ofloxacin against experimental pneumonia with Pseudomonas aeruginosa in guinea pigs

The chemotherapeutic efficacy of ofloxacin against experimental pneumonia was investigated with special reference to its treatment regimen. A pneumonia model was successfully produced by inhalation of a virulent strain of Pseudomonas aeruginosa in guinea pigs immunosuppressed with cortisone acetate. One or 4 days after infection, the animals were treated orally with the fixed daily doses of ofloxacin either once a day or thrice a day for 3 consecutive days. Ofloxacin given thrice a day eliminated the organisms from the lung more efficiently than the equivalent total doses injected once a day in both series of treatment, starting 1 or 4 days after infection. The superiority of the triple dosing in chemotherapeutic efficacy of ofloxacin was found to be attributable at least to the longer retention of its pulmonary levels exceeding the antibiotic concentrations.