环丙沙星诱导耐药肺炎克雷伯菌对其他抗菌药物的耐药性研究

探讨环丙沙星诱导耐药肺炎克雷伯菌(KPn)对几类常见的抗生素的耐药性。方法 琼脂二倍稀释法测定环丙沙星对20株临床分离KPn敏感株的最低抑菌浓度(MIC),用环丙沙星对其进行体外多步诱导成耐药株。诱导前和诱导后K-B纸片扩散法进行药敏试验检测其对头孢他啶、头孢西丁、氨曲南、亚胺培南、莫西沙星、阿米卡星的敏感性。诱导后进行产超广谱β-内酰胺酶(ESBL)初筛和确证实验。结果 20株KPn有17株成功诱导成环丙沙星高度耐药株,ESBL筛选和确证实验显示17株诱导耐药株无一产ESBL。诱导耐药株对莫西沙星全部耐药,对头孢他啶、亚胺培南、氨曲南全部敏感,对阿米卡星的敏感率为88.2％(15/17),而对头孢西丁耐药率达88.2％ (15/17)、中介率12.8％(2/17)。结论 KPn在长期低剂量接触环丙沙星后可产生耐药性,且对莫西沙星和头孢西丁有交叉耐药。环丙沙星诱导耐药的KPn对头孢西丁交叉耐药的机制可能相似。     

广州地区106株淋球菌中脂蛋白分型与环丙沙星耐药相关性研究

目的:研究广州地区106株淋球菌中脂蛋白分型与环丙沙星耐药的相关性.方法:用糖琼脂稀释法测定淋球菌对环丙沙星的MIC值,PCR分别扩增淋球菌的gyrA、parC和脂蛋白基因并测序分析.结果:广州地区106株淋球菌对环丙沙星的耐药率为95 3%,共有19个脂蛋白亚型,最常见的亚型是17c,有49株(46 2%).对环丙沙星耐药的101株菌中,所有菌株在gyrA基因对应氨基酸的第91和95位点上均发生了突变,而parC基因随着MIC值的升高发生位点突变的概率呈上升趋势.在中低水平耐药组中,最常见的脂蛋白亚型是17c和14d,均有12株(28 6%).在高水平耐药组中,最常见的脂蛋白亚型是17c,有35株(59 3%),其次是14d,有11株(18 6%).结论:淋球菌脂蛋白亚型的分布存在地域性,与环丙沙星耐药程度高低无明显相关性.     

110例复发性支原体阴道炎的治疗观察

目的：研究治疗顽固性支原体阴道炎的有效方法。方法：将110例患者随机分为观察组和对照组各55例,所有患者均以阿奇霉素全身用药治疗,治疗组另给予外用盐酸环丙沙星栓剂。结果：治疗组55例患者49例治愈,占89．09％,好转5例,占9．09％,1例是无效的,占患者总数的1．82％,对照组55例,37例治愈,占67．27％,好转11例,占20％,7例无效,占12．73％,观察组疗效显著优于对照组,差异有显著性（Hc=23．73,P〈0．05）。结论：支原体阴道炎易反复发作,在治疗期间必须采取综合性的治疗,全身给药结合局部用药,可以完全治愈阴道炎反复发作。     

Ocimum basilicum: Antibacterial activity and association study with antibiotics against bacteria of clinical importance

Context: Ocimum basilicum L. (Lamiaceae), popularly known as basil, is part of a group of medicinal plants widely used in cooking and known for its beneficial health properties, possessing significant antioxidant effects, antinociceptive, and others.

Objective: The objective of this study is to determine the pharmacological effects produced on the bacterial strains Staphylococcus aureus and Pseudomonas aeruginosa when standard antibiotics and O. basilicum essential oil are combined.

Materials and methods: The extraction of O. basilicum (leaves) components was done by steam distillation. The Minimum inhibitory concentration (MIC) was calculated using microdilution technique, where the oil concentrations varied from 2 to 1024?μg/mL. The combinations of O. basilicum oil with ciprofloxacin or imipenem were analyzed by the checkerboard method where fractional inhibitory concentration (FIC) indices were calculated.

Results: Ocimum basilicum essential oil, imipenem, and ciprofloxacin showed respective MIC antibacterial activities of 1024, 4, and 2?μg/mL, against S. aureus. In S. aureus, the oil with imipenem association showed synergistic effect (FIC?=?0.0625), while the oil with ciprofloxacin showed antagonism (FIC value?=?4.25). In P. aeruginosa, the imipenem/oil association showed additive effect for ATCC strains, and synergism for the clinical strain (FIC values?=?0.75 and 0.0625). The association of O. basilicum essential oil with ciprofloxacin showed synergism for clinical strains (FIC value?=?0.09).

Conclusion: Ocimum basilicum essential oil associated with existing standard antibiotics may increase their antibacterial activity, resulting in a synergistic activity against bacterial strains of clinical importance. The antibacterial activity of O. basilicum essential oil may be associated with linalool.     

Efficacy and pharmacodynamics of gemifloxacin versus levofloxacin in guinea pig pneumococcal pneumonia induced by strains with decreased ciprofloxacin susceptibility

Quinolone in vivo bactericidal activity was investigated in a guinea pig pneumonia model using three Streptococcus pneumoniae strains with decreasing susceptibility to ciprofloxacin. Treatment regimens resulted in values of AUC_{0–24 h} and C_{30 min} similar to those of standard oral regimens in human serum. Efficacy was defined as a significant difference in number of viable bacteria in the lungs compared with the control. Ciprofloxacin, levofloxacin and gemifloxacin were effective against the levofloxacin-susceptible strain. Only gemifloxacin achieved a ≥99.9% reduction versus control against the levofloxacin intermediate-resistant strain. Gemifloxacin achieved a 99.69% reduction and was the only quinolone significantly different from the control (P<0.05) against the levofloxacin-resistant strain. Gemifloxacin offers in vivo activity against ciprofloxacin- to levofloxacin-resistant pneumococci.     

Evaluation of the efficacy and safety of intravenous ciprofloxacin versus meropenem in the treatment of postoperative infection

Therapeutic options for postoperative infection in gastrointestinal surgery are limited. To identify new treatment alternatives, the Japan Society for Surgical Infection conducted a multicenter prospective, randomized, controlled clinical trial comparing the efficacy of intravenous ciprofloxacin (CIP IV) and intravenous meropenem (MEM IV). Between July 2005 and May 2008, the trial recruited patients who developed postoperative infection or had suspected infectious systemic inflammatory response syndrome after elective clean-contaminated gastrointestinal surgery. All patients had received prophylactic postoperative antibiotic treatment. Patients received either intravenous CIP IV 300 mg b.i.d. or MEM IV 500 mg b.i.d. A total of 205 patients from 31 institutions were enrolled. Of these, 101 were randomized to CIP IV and 104 to MEM IV. There were 100 and 102 in the intent-to-treat (ITT)/safety population and 75 and 77 in the per-protocol (PP) population. There was no significant difference between CIP IV and MEM IV in terms of clinical efficacy, bacteriological efficacy, incidence of adverse drug reactions, duration of antimicrobial treatment, or relapse/reactivation. Overall clinical success PP population) was high in both treatment groups: 85.3% (64/75) for CIP IV and 89.6% (69/77) for MEM IV, although the non-inferiority of CIP IV was not demonstrated (difference −4.3%, 95% CI −14.8, 6.2). In patients who had undergone upper gastrointestinal surgery, success was 88.5% (23/26) for CIP IV and 85.2% (23/27) for MEM IV. Intravenous ciprofloxacin is as effective as intravenous meropenem in the empiric therapy of postoperative infection after gastrointestinal surgery.     

Comparison of an ELISA and a HPLC for Determination of Ciprofloxacin Residues in Pork

To determine ciprofloxacin (CPFX) residues in pork, an ELISA and a high-performance liquid chromatography (HPLC) procedure were developed and compared on sensitivity, precision and accuracy. For ELISA, CPFX was converted by an active ester method into CFPX-human serum albumin (CPFX-HSA) and CFPX-bovine serum albumin (CPFX-BSA), and the latter allowed the production of CPFX-specific rabbit antisera for the development of an indirect competitive ELISA procedure. For HPLC, an ODS reverse phase column was used with ultraviolet detection, and triethylamine and acetonitrile (87:13) were employed as mobile phase. The limits of detection (LODs) were 0.32 ng ml -1 for ELISA and 10 ng ml -1 for HPLC. The linear detection ranges were 0.32-5000 ng ml -1 for ELISA and 10-5120 ng ml -1 for HPLC. The coefficients of variation were 4.51-11.50% for ELISA and 0.70-9.10% for HPLC over the range of CPFX concentrations of each method. The mean recovery of HPLC (80.58%) was higher than that of ELISA (66.18%). The results suggested that the ELISA, with its high detection throughput and excellent sensitivity and specificity, could be used as a screening method for CPFX residues in pork. The HPLC, for its great precision and accuracy, was an effective confirmatory method for CPFX residues in pork.     

Ciprofloxacin sensitizes hormone-refractory prostate cancer cell lines to doxorubicin and docetaxel treatment on a schedule-dependent manner

Purpose  Combination therapy has generated a significant interest in the clinical setting since certain agents, with known mechanisms of action and non-overlapping toxicities may increase the therapeutic potential of anticancer drugs by decreasing systemic toxicity and overcoming drug resistance. Doxorubicin and docetaxel, two standard antineoplastic agents in hormone-refractory prostate cancer (HRPC) therapy and ciprofloxacin were evaluated singly and in several simultaneous and sequential drug combination schemes, against PC-3 and LNCaP cell lines. Methods  Cellular viability was determined by the resazurin assay and the assessment of synergism, additivity or antagonism was carried out by the median effect analysis. The importance of dose, exposure time and type of administration were investigated and compared. Results  Ciprofloxacin–doxorubicin or docetaxel combinations resulted in prominent additive or synergistic effects in both cell lines, when the cells were pre-treated with ciprofloxacin. These results suggest a rationale for dose reduction of doxorubicin and docetaxel in prostate cancer therapy, since the doses needed to achieve 50% cell death may be decreased by approximately 4- to 15-fold or 3- to 8-fold, respectively, after a pre-treatment with ciprofloxacin. In contrast, the referred combinations yielded moderate antagonistic effects when used concurrently in this in vitro system. Conclusions  Ciprofloxacin sensitized HRPC cells to doxorubicin or docetaxel-induced growth inhibition and, therefore, may play a role as chemosensitizing agent in prostate cancer treatment.     

Pharmacokinetics of CIPRODEX otic in pediatric and adolescent patients

OBJECTIVE: Describe the pharmacokinetics of ciprofloxacin and dexamethasone after administration of CIPRODEX Otic Suspension (CIP/DEX) into the middle ears of children. DESIGN: Open-label, single-dose, pharmacokinetic studies, administering four drops of CIP/DEX instilled into each middle ear through the tympanostomy tubes immediately following tube placement. Blood was collected for 6h and analyzed for ciprofloxacin and dexamethasone concentrations using a validated liquid chromatography and tandem mass spectrometry (LC/MS/MS) method. SETTING: The study was conducted through a referral pediatric otolaryngology practice with actual surgical procedures performed in an ambulatory care center. PATIENTS: Twenty-five randomly selected patients, 1-14 years of age (mean age, 5 years), receiving tympanostomy tubes. RESULTS: Peak ciprofloxacin plasma levels were observed at about 1h, with a mean C(max) of 1.33+/-0.96 ng/mL (range <0.5-3.45 ng/mL) and an estimated half-life of 3.0+/-1.2h. Peak dexamethasone plasma levels were observed within 2h with a mean C(max) of 0.90+/-1.04 ng/mL (range <0.05-5.10 ng/mL) and an estimated half-life of 3.9+/-2.9h. CONCLUSION: These results demonstrated low systemic exposure of ciprofloxacin and dexamethasone following topical otic administration in pediatric patients.     

氧氟沙星、环丙沙星抗胆道感染作用的实验研究

目的观察喹诺酮类抗生素(环丙沙星、氧氟沙星)在胆汁中的代谢过程,为临床医师提供胆道感染时合理选用有效抗生素的理论依据。方法犬为实验动物,行胆总管造瘘,以备留取胆汁标本。静脉滴注氧氟沙星(Ofloxacin)、环丙沙星(Ciprofloxacin)后,留取静脉及胆汁标本,用微生物法测定药物浓度,3P87软件数据处理,得出药物动力学参数。结果静脉滴注氧氟沙星、环丙沙星后,胆汁中主要的代谢参数峰值时间(Tpeakmin)分别为58、72;峰值浓度(Cmaxμg/ml)分别为8.02、8.81;半衰期(T