环丙沙星的临床药物动力学研究

研究健康志愿者口眼和静脉滴注环丙沙星的药物动力学，并比较不同剂量、空腹与进餐、单剂与多剂给药的体内过程。单剂空腹口服环丙沙星５００ｍｇ后，Ｃｍａｘ为３．４８ｍｇ·Ｌ－１、为３．０１ｈ、ＡＵＣ为１４．１４ｈ．ｍｇ·Ｌ－１，静脉滴注环丙沙星２００ｍｇ后Ｃｍａｘ为６．５６ｍｇ·Ｌ－１、为３．７３ｈ，口服环丙沙星绝对生物利用度为６８．８９％。单剂空腹口服２５０、５００和１０００ｍｇ环丙沙星后，Ｃｍａｘ为１．８２～７．７２ｍｇ·Ｌ－１，为２．４７～３．１５ｎ，ＡＵＣ与剂量呈比例增加，进餐与空腹口服环丙沙星５００ｍｇ后的体内过程显示进食可使该药的吸收轻度减少。与单剂口服５００ｍｇ相比，５００ｍｇ日２次×７ｄ多剂给药后的Ｃｍａｘ和ＡＵＣ均较单剂者略增高，草剂口服２５０、５００、１０００和５００ｍｇ多剂量后２４ｈ尿排出率为给药量的４７％～５５％，静滴２００ｍｇ者为７１．０６％，基于上述药动学资料，拟订了环丙沙星对各种感染的治疗方案。     

环丙沙星滴眼剂在家兔眼内组织分布及其药物动力学

环丙沙星（ｃｉｐｒｏｆｌｏｘａｃｉｎ，ＣＰＦＸ）滴眼液点入兔眼后，用ＨＰＬＣ法测定眼内各组织中药物浓度。结果在角膜、房水、虹膜－睫状体、晶体、玻璃体内峰浓度值分别为１９．４３μｇ／ｇ，１．５８μｇ／ｍｌ，１６．６８μｇ／ｇ，１．４２μｇ／ｇ和０．９６μｇ／ｍｌ；其半衰期分别为０．７６，０．６９，０．９２，０．６１和１．４０ｈ。结果表明ＣＰＦＸ能在眼内达到较高的抗菌浓度。     

环丙沙星滴眼液治疗急性细菌性结膜炎的临床疗效

本文对１０９例（１３０眼）临床诊断急性细菌性结膜炎，应用０．３％环丙沙星（ＣＰＬＸ）滴眼液（７０眼）和０．３％诺氟沙星（ＮＦＬＸ）滴眼液（６０眼），作了双盲随机治疗研究各１个星期。治愈率ＣＰＬＸ组６２．８６％、ＮＦＬＸ组４５％，显效ＣＰＬＸ组３２．８５％，ＮＦＬＸ组４６．６６％。治疗后细菌清除率ＣＰＬＸ组９４．７８％、ＮＦＬＸ组９２．９５％。两种抗菌素对革兰氏阳性和阴性菌的作用相似，治疗中无一例有任何副反应或局部不能耐受。ＣＰＬＸ对治疗外眼部细菌感染如急性细菌性结膜炎为一安全有效的药物，其临床疗效与对微生物作用在本组试验中与ＮＦＬＸ相似。     

Propriospinal myoclonus after treatment with ciprofloxacin.

The clinical and electrophysiological features of a truncal myoclonus in a 55-year-old man are described. The electromyographic characteristics point toward propriospinal myoclonus. It is suggested that a myoclonic generator was released after use of ciprofloxacin, by antagonising the gamma-aminobutyric acid metabolism.     

复方环丙氟哌酸鼻腔膜的研制及临床疗效观察

本文以明胶海绵为衬底,用环丙氟哌酸和氢化考的松、云南白药酊、达克罗宁制备的鼻腔消炎止血药膜,制备简便,质量稳定。临床观察结果证明,具有给药方便、疗效高、疗程短、药物作用持久,无毒副作用等优点。     

A microbiologist''s guide to travellers abroad: do as I say not as I do

Clinical microbiologists do not normally prescribe prophylactic antibiotics for travellers' diarrhoea, and when questioned at a Hospital Infection Society (HIS) meeting only 2% admitted doing so. During a HIS visit to India, 5 (28%) members took daily ciprofloxacin prophylaxis and none of them developed diarrhoea.     

Infecton: a 99mTc–ciprofloxacin radiopharmaceutical for the detection of bone infection

Objective   To evaluate Infecton scintigraphy, with technetium-99m-radiolabeled ciprofloxacin, as a means to detect bone infection, in comparison with other conventional scintigraphic and radiologic methods.
Methods   Forty-five patients with known or suspected bone infection underwent 50 scans with Infecton. Almost all were also subjected to a three-phase ^99mTc-methylene diphosphonate bone scan and most of them to a ^99mTc-human polyclonal immunoglobulin scan as well as to a gallium-67-citrate scan, plus computerized tomography or magnetic resonance imaging or both. Clinical laboratory criteria for the presence of osteomyelitis were based on the definitions of the Centers for Disease Control and Prevention.
Results   Staphylococcus aureus and Pseudomonas aeruginosa were the most frequently isolated pathogens. Based on the CDC clinical laboratory criteria as well as on conventional scan results, Infecton was characterized in 35 studies as 'true positive', in eight as 'true negative', in two as 'false positive', in one as 'false negative', and in four as 'indeterminate'. The sensitivity and specificity of Infecton scintigraphy were found to be 97.2% and 80%, respectively, with positive and negative predictive values of 94.6% and 88.9%.
Conclusions   It is concluded that Infecton is a very sensitive and quite specific marker of bone infection, but care must be taken in cases of excessive new bone formation and primary bone tumors, where false-positive results may be obtained.     

Clonality among ampicillin-resistant Enterococcus faecium isolates in Sweden and relationship with ciprofloxacin resistance

Objective  To investigate clonal relationships in a nationwide sample of human Enterococcus faecium isolates.
Methods  Biochemical fingerprinting (PhP (PhenePlate) typing) was used to compare 180 fecal ampicillin-resistant E. faecium (ARE) isolates with 169 matched fecal ampicillin-susceptible E. faecium (ASE) isolates from patients in 23 hospitals, collected in 1998, and to study 39 fecal ARE isolates from non-hospitalized individuals collected in 1998, and five ARE and 29 ASE isolates from the early 1990s. Representative ARE and ASE isolates were subjected to pulsed-field gel electrophoresis (PFGE) analysis of genomic DNA and sequencing of the regions encoding the fluoroquinolone targets of the enzymes GyrA and ParC.
Results  Both PhP and PFGE results showed a higher homogeneity among ARE than among ASE isolates ( P  < 0.001). One PhP type (FMSE1) comprised 73% of the hospital ARE isolates (53% of ARE isolates from non-hospitalized individuals, and four of five ARE isolates from the early 1990s), but only 1% of the ASE isolates. PFGE of the hospital E. faecium isolates revealed that 23 of the 25 ARE isolates and one of the 22 ASE isolates were of one dominating type. High-level resistance to ciprofloxacin (MIC > 16 mg/L) was present in 91% of ARE isolates, whereas only low-level resistance (MIC 4–16 mg/L; 35% of isolates) was found among ASE isolates. One mutation in parC (codon 80) and one of two mutations in gyrA (codons 83 or 87) were detected in all ARE isolates tested with high-level ciprofloxacin resistance, but were lacking in ARE and ASE isolates with low-level ciprofloxacin resistance.
Conclusion  Most ARE isolates in Sweden were clonally related. High-level ciprofloxacin resistance was found in ARE isolates of PhP type FMSE1 as well as in other PhP types, but never in ASE isolates.     

国产环丙沙星注射液临床疗效的观察

目的 :评价国产环丙沙星注射液治疗下呼吸道、泌尿系及伤寒等细菌性感染的临床疗效、细菌学疗效和安全性。方法 :采用随机对照开放试验的方法 ,对国产环丙沙星注射液的临床疗效和细菌清除率进行了观察。结果 :国产环丙沙星注射液临床疗效有效率 84.0 % ,痊愈率 56.0 % ,与对照组头孢氨噻肟疗效一致 ,无显著性差异 ( P>0 .0 5)。国产环丙沙星注射液细菌清除率 76.9% ,与头孢氨噻肟比较疗效接近 ( P>0 .0 5) ,对肺炎克雷伯杆菌、大肠杆菌、变形杆菌、枸橼酸杆菌、伤寒杆菌及不动杆菌具有良好的清除作用 ,对铜绿假单胞菌亦有满意的抗菌活性。不良反应轻微 ,用药安全。结论 :国产环丙沙星注射液为广谱、高效、安全的抗菌药物 ,对不能耐受口服制剂者可避免胃肠道的直接刺激作用 ,对重症不能口服者提供了很好的给药途径     

口服氢氧化铝对静脉给予环丙沙星的体内药动学影响

目的：探讨临床常见的静脉给予环丙沙星同时经口给予含铝抗酸剂是否合理。方法：采用紫外分光光度法测定家兔血清中的环丙沙星浓度，对静脉给予环丙沙星在口服含铝抗酸剂前后的体内药动学的情况进行了比较。结果：各取血时间点的环丙沙星平均血药浓度数值相近，同时口服含铝抗酸剂不影响经静脉给予环丙沙星的AUC。结论：静脉给予环丙沙星与经口给予含铝抗酸剂是合理的。