喹诺酮类药治疗复治耐多药肺结核的成本-效果分析

目的：在环丙沙星、氧氟沙星、左氧氟沙星、司帕沙星中寻找治疗复治耐多药肺结核病的最佳方案。方法：利用已有的文献资料，采用成本-效果分析方法进行评价；同时对可能的影响因素（价格）进行考察，并作敏感性分析。结果：在痰菌转阴率比较中，左氧氟沙星与司帕沙星效果相近，优于环丙沙星和氧氟沙星（P〈0．05）；空洞关闭率、X线病灶有效率、不良反应发生率等指标各组间比较无统计学意义（P〉0．05）。各组间的医疗费用差异有统计学意义。结论：左氧氟沙星为最佳治疗方案。敏感性分析与成本-效果分析的结果一致。     

常用氟喹诺酮类药品都有哪些？

我国上市的氟喹诺酮类药品包括诺氟沙星、培氟沙星、氧氟沙星、左氧氟沙星、莫西沙星、、环丙沙星、洛美沙星、氟罗沙星、依诺沙星、司帕沙星、克林沙星、加替沙星、芦氟沙星、托氟沙星、那氟沙星、司氟沙星、吉米沙星等。     

喹诺酮类药物对离体兔软骨细胞的毒性

目的 :评价几种喹诺酮类药物对幼龄兔软骨细胞的相对毒性 ,软骨毒性与浓度、时间、年龄的关系。方法 :采用兔软骨细胞体外培养的技术 ,观察细胞形态 ,四氮甲基唑蓝 (MTT)法评价细胞的增殖 ,二甲基亚甲蓝 (DMB)法评价细胞蛋白多糖的含量。观察环丙沙星、左氧氟沙星、氟罗沙星、帕珠沙星对 1月龄兔软骨细胞的影响 ,及环丙沙星对 1,3,5月龄兔软骨细胞的影响。结果 :喹诺酮类药物使细胞形态发生改变 ;抑制细胞的增殖的作用依次为环丙沙星 >左氧氟沙星 >氟罗沙星 >帕珠沙星 ;对蛋白多糖含量的作用为环丙沙星 >左氧氟沙星 >氟罗沙星、帕珠沙星 ;环丙沙星的抑制作用随作用时间的延长和浓度的增加而增加 ,随兔年龄的增大而减少。结论 :喹诺酮类几种药物的软骨毒性存在着差异 ,且随浓度、时间、年龄不同而不同。     

司帕沙星和妥舒沙星的体内外抗菌作用研究

目的观察国产司帕沙星、妥舒沙星及其它四种氟喹诺酮类抗菌药对成都地区780株临床分离菌的体外抗菌活性，并比较司帕沙星、妥舒沙星和环丙沙星对金葡球菌、大肠埃希菌和铜绿假单胞菌感染小鼠的体内抗菌活性。方法用琼脂稀释法测定国产司帕沙星和妥舒沙星的MIC50和MIC90，并与其它四种氟喹诺酮类抗菌药进行了比较。本文还测定了抗菌药对金葡球菌、大肠埃希菌和铜绿假单胞菌感染小鼠治疗的ED50结果体外试验表明司帕沙星和妥舒沙星能有效抑制或杀灭革兰阳性、革兰阴性菌及厌氧菌，显示了广谱抗菌活性。司帕沙星和妥舒沙星对革兰阳性菌的抗菌活性是环丙沙星的2～8倍，氧氟沙星和氟罗沙星的4～16倍，是诺氟沙星的16～32倍。司帕沙星对MRSA的抗菌活性与妥舒沙星相似，但优于环丙沙星、氧氟沙星、氟罗沙星和诺氟沙星。司帕沙星对大多数革兰阴性菌的抗菌活性与环丙沙星和妥舒沙星相似，是氧氟沙星、氟罗沙星和诺氟沙星的2～8倍。两药对厌氧菌的抗菌活性也较环丙沙星强。口服或皮下注射司帕沙星对金葡球菌和大肠埃希菌所致小鼠全身性感染的保护作用优于环丙沙星和妥舒沙星。同一给药途径下司帕沙星对铜绿假单胞菌所致小鼠全身性感染的保护作用与妥舒沙星和环丙沙星相似。三种受试药对金葡球菌和大肠埃希菌所致小鼠全身性感染的保护作用优于铜绿假单胞菌所致感染。结论司帕沙星和妥舒沙星对革兰阳性菌和厌氧菌的体外抗菌活性优于环丙沙星和其它药物，对大多数革兰阴性菌的抗菌活性与环丙沙星相似，但优于其它受试药。司帕沙星对金葡球菌和大肠埃希菌所致小鼠全身性感染的体内保护作用优于环丙沙星和妥舒沙星。同一给药途径下司帕沙星对铜绿假单胞菌所致小鼠全身性感染的保护作用与妥舒沙星和环丙沙星相似。     

左氧氟沙星、氟罗沙星、司帕沙星口服治疗泌尿系统感染的成本-效果分析

目的比较左氧氟沙星、氟罗沙星、司帕沙星口服治疗泌尿系统感染的经济效果。方法采用药物经济学原理对3种治疗方案进行成本一效果分析。结果左氧氟沙星,氟罗沙星、司帕沙星口服治疗泌尿系统感染的有效率分别为80％、90％、86．6％（P〉0．05）;成本一效果比（C／E）分别为1．04、1、665、2．40。与左氧氟沙星比,每增加1个单位效果氟罗沙星需多花费6．67元,司帕沙星需多花费18．89元。结论左氧氟沙星口服治疗泌尿系统感染比氟罗沙星、司帕沙星更具成本一效果优势。     

氟喹诺酮类药物应用情况分析

目的　了解氟喹诺酮类药物在广东地区医院的应用情况及其变化趋势。方法　对广东地区有代表性的43家医院2001-2003年氟喹诺酮类药物的用药金额、用药频度(DDDs)、日均费用等进行统计和分析。结果与结论　2002年氟喹诺酮类药物用药金额比2001年稍微下降, 2003年比2002年增长13. 49%。用药金额居前四位的分别是左氧氟沙星,环丙沙星,氟罗沙星,氧氟沙星。左氧氟沙星约占总金额的三分之一。DDDs居前四位的分别是左氧氟沙星,环丙沙星,司帕沙星,氧氟沙星。日均费用居前四位的分别是依诺沙星、加替沙星,氟罗沙星、莫西沙星。     

司帕沙星与其他5种抗菌药体外抗菌活性比较研究

测定了司帕沙星对临床分离的１９９ 株致病菌的体外抗菌活性并与氧氟沙星、环丙沙星、头孢唑啉、头孢噻肟、阿米卡星的抗菌活性进行比较。司帕沙星对革兰阳性菌的ＭＩＣ９０为０．１２５～０．５ｍ ｇ／Ｌ,对金葡球菌、化脓链球菌的抑菌率均为１００％ ,强于氧氟沙星、环丙沙星;对革兰阴性菌也具有良好的体外抗菌活性,与氧氟沙星、环丙沙星相似。不同细菌接种量和不同浓度血清对其抗菌活性无明显影响,仅在ｐＨ５．０ 时抗菌活性略有下降     

氟喹诺酮类药物应用情况分析

目的了解氟喹诺酮类药物在广东地区医院的应用情况及其变化趋势.方法对广东地区有代表性的43家医院2001-2003年氟喹诺酮类药物的用药金额、用药频度(DDDs)、日均费用等进行统计和分析.结果与结论 2002年氟喹诺酮类药物用药金额比2001年稍微下降,2003年比2002年增长13.49%.用药金额居前四位的分别是左氧氟沙星,环丙沙星,氟罗沙星,氧氟沙星.左氧氟沙星约占总金额的三分之一.DDDs居前四位的分别是左氧氟沙星,环丙沙星,司帕沙星,氧氟沙星.日均费用居前四位的分别是依诺沙星、加替沙星,氟罗沙星、莫西沙星.     

司帕沙星与左氧氟沙星治疗男性导尿患者泌尿道感染的临效果研究

目的:探讨司帕沙星与左氧氟沙星治疗男性留置导管时的泌尿道感染的作用.方法:选取2016年3月～2017年3月我院接诊的男性导尿患者60例,按照随机抽签法分为对照组和观察组各30例.对照组只使用左氧氟沙星胶囊治疗,观察组只给予司帕沙星治疗,比较两组临床治疗总有效率和细菌学清除率及药物不良反应发生率.结果:观察组泌尿道感染治疗总有效率96.7％与对照组的90.0％比较无显著差异(P>0.05),且药物不良反应及细菌学清除率比较均无显著差异(P>0.05).结论:司帕沙星与左氧氟沙星治疗男性留置尿管泌尿道感染的疗效比较无显著差异,均能取得理想效果,且用药安全性好,具有推广意义.     

从药物动力学观点看喹诺酮类药物的不良反应

评述氟喹诺酮类药物最新的药物动力学、相互作用和特殊的耐受性。左氧氟沙星的口服吸收最高(99%～ 10 0 % ) ,口服 5 0 0mg后比司帕沙星 (4 0 0mg)或环丙沙星 (5 0 0mg ,每日 2次 )达到更高的初始浓度 ,2 4h后下降缓慢。口服 2 5 0mg后的Cmax范围从环丙沙星、加替沙星和莫西沙星的 1.2、1.71和 2 .17mg/L ,到左氧氟沙星的2 48mg/L(P <0 .0 1)。环丙沙星的AUC最低为 4.6h·mg/L ,加替沙星、左氧氟沙星和莫西沙星分别为 15、17.9和19 7h·mg/L(P <0 .0 1)。所有氟喹诺酮类药物与含有多价阳离子的物质具有相互作用 ,并且当与含铁化合物共同使用时 ,生物利用度降低 5 0 % (环丙沙星和莫西沙星所受的影响比左氧氟沙星或gemifloxacin更大 )。在氟喹诺酮类药物中 ,与茶碱相互作用最明显的是依诺沙星、培氟沙星和环丙沙星 ,而左氧氟沙星无此相互作用的报道。司帕沙星与心脏的QT间期延长有关 ,并有高光毒性。正在观察莫西沙星的QT间期作用。左氧氟沙星无QT间期延长 ,且光毒性非常低 ,使其成为最安全的氟喹诺酮类药物     

Febrile neutropenia in a bone marrow transplantation unit

A total of 119 strains of coagulase-negative staphylococci isolated from clinical specimens were speciated and tested for sensitivity to methicillin and four fluoroquinolones (ciprofloxacin, sparfloxacin, levofloxacin and ofloxacin). Resistance to fluoroquinolones was significantly more common in Staphylococcus haemolyticus (43%) than in Staphylococcus epidermidis (11%). Methicillin-resistant strains of S. haemolyticus were more often resistant to ciprofloxacin than were methicillin-resistant strains of S. epidermidis (P < 0.05). Sparfloxacin was the most active against fluoroquinolone-sensitive strains, and levofloxacin was twice as active as ofloxacin. There was cross-resistance between the four fluoroquinolones. Levofloxacin was the most active against resistant strains, but MICs obtained for all the compounds seemed to be outside the clinically useful range for the treatment of systemic infections.     

盐酸左氧氟沙星治疗呼吸系统细菌感染的临床比较研究

目的观察盐酸左氧氟沙星对呼吸系统细菌感染效果。方法选取呼吸系统细菌感染患者150例,分为左氧氟沙星组和环丙沙星组,分别静点左氧氟沙星和环丙沙星,比较两组患者的症状缓解时间和细菌清除率。结果左氧氟沙星组的细菌清除率为90.27%,症状缓解时间为(3.5±1.2)d,环丙沙星组的细菌清除率为73.97%,症状缓解时间为(6.8±1.4)d,统计学分析,P<0.05,有统计学意义。结论盐酸左氧氟沙星治疗呼吸系统细菌感染起效快、细菌清除率高。     

Characterization of histamine release induced by fluoroquinolone antibacterial agents in-vivo and in-vitro

Characterization of histamine release induced by fluoroquinolone antibacterial agents, levofloxacin and ciprofloxacin, was investigated in-vivo and in-vitro. Intravenous injection of levofloxacin and ciprofloxacin at 1-10 mg kg(-1) produced dose-related elevations in plasma histamine level in anaesthetized dogs. In contrast, levofloxacin was devoid of plasma histamine increment in anaesthetized rats at 100 mg kg(-1), whereas ciprofloxacin at the same dose caused endogenous histamine release. Levofloxacin and ciprofloxacin induced non-cytotoxic secretion of histamine from all mast cells tested in a concentration-dependent manner, whereas rat skin and peritoneal mast cells were thirty- to one-hundred-times less sensitive to the effect of fluoroquinolones as compared with the canine skin mast cells. These results suggest that the functional heterogeneity of mast cells from different species in histamine releasing activity of fluoroquinolones may exist, and that mast cells from the dog appear to be particularly sensitive to the effect of the fluoroquinolones.     

The bactericidal activity of levofloxacin against ampicillin-resistant and ampicillin-susceptible Haemophilus influenzae in comparison with ofloxacin, ciprofloxacin and sparfloxacin

The bactericidal activity of levofloxacin against four Haemophilus influenzae clinical isolates (two ampicillin-resistant and two susceptible) was compared with that of ofloxacin, ciprofloxacin and sparfloxacin at concentrations simulating the peak serum concentrations obtained with the recommended oral doses. Bactericidal activity was assessed using time-kill curves and minimum kill-time values. Both concentrations of levofloxacin rapidly killed all the study strains, with mean kill times of 4 h and no viable bacteria remaining after 18-h exposure. The bactericidal activities of levofloxacin, ofloxacin and sparfloxacin were similar. The minimum kill-times for both concentrations of ciprofloxacin were 28-35% longer than those of levofloxacin. These results support the use of levofloxacin for H. influenzae infections, including ampicillin-resistant strains.     

A critical review of the fluoroquinolones: focus on respiratory infections.

The new fluoroquinolones (clinafloxacin, gatifloxacin, gemifloxacin, grepafloxacin, levofloxacin, moxifloxacin, sitafloxacin, sparfloxacin and trovafloxacin) offer excellent activity against Gram-negative bacilli and improved Gram-positive activity (e.g. against Streptococcus pneumoniae and Staphylococcus aureus) over ciprofloxacin. Ciprofloxacin still maintains the best in vitro activity against Pseudomonas aeruginosa. Clinafloxacin, gatifloxacin, moxifloxacin, sitafloxacin, sparfloxacin and trovafloxacin display improved activity against anaerobes (e.g. Bacteroides fragilis) versus ciprofloxacin. All of the new fluoroquinolones display excellent bioavailability and have longer serum half-lives than ciprofloxacin allowing for once daily dose administration. Clinical trials comparing the new fluoroquinolones to each other or to standard therapy have demonstrated good efficacy in a variety of community-acquired respiratory infections (e.g. pneumonia, acute exacerbations of chronic bronchitis and acute sinusitis). Limited data suggest that the new fluoroquinolones as a class may lead to better outcomes in community-acquired pneumonia and acute exacerbations of chronic bronchitis versus comparators. Several of these agents have either been withdrawn from the market, had their use severely restricted because of adverse effects (clinafloxacin because of phototoxicity and hypoglycaemia; grepafloxacin because of prolongation of the QTc and resultant torsades de pointes; sparfloxacin because of phototoxicity; and trovafloxacin because of hepatotoxicity), or were discontinued during developmental phases. The remaining fluoroquinolones such as gatifloxacin, gemifloxacin, levofloxacin and moxifloxacin have adverse effect profiles similar to ciprofloxacin. Extensive post-marketing safety surveillance data (as are available with ciprofloxacin and levofloxacin) are required for all new fluoroquinolones before safety can be definitively established. Drug interactions are limited; however, all fluoroquinolones interact with metal ion containing drugs (eg. antacids). The new fluoroquinolones (gatifloxacin, gemifloxacin, levofloxacin and moxifloxacin) offer several advantages over ciprofloxacin and are emerging as important therapeutic agents in the treatment of community-acquired respiratory infections. Their broad spectrum of activity which includes respiratory pathogens such as penicillin and macrolide resistant S. pneumoniae, favourable pharmacokinetic parameters, good bacteriological and clinical efficacy will lead to growing use of these agents in the treatment of community-acquired pneumonia, acute exacerbations of chronic bronchitis and acute sinusitis. These agents may result in cost savings especially in situations where, because of their potent broad-spectrum activity and excellent bioavailability, they may be used orally in place of intravenous antibacterials. Prudent use of the new fluoroquinolones will be required to minimise the development of resistance to these agents.     

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.     

A comparative study of the fluoroquinolone antibacterial agents on the action potential duration in guinea pig ventricular myocardia

We examined the effects of ten fluoroquinolone antibacterial agents, levofloxacin, sitafloxacin, trovafloxacin, ciprofloxacin, gemifloxacin, tosufloxacin, gatifloxacin, grepafloxacin, moxifloxacin and sparfloxacin, on action potentials recorded from guinea pig ventricular myocardia. Sparfloxacin prolonged action potential duration (APD) by about 8% at 10 microM and 41% at 100 microM. Gatifloxacin, grepafloxacin and moxifloxacin also prolonged APD at 100 microM by about 13%, 24% and 25%, respectively. In contrast, levofloxacin, sitafloxacin, trovafloxacin, ciprofloxacin, gemifloxacin and tosufloxacin had little or no APD-prolonging effect at concentrations as high as 100 microM. These findings suggest that there are differences in potency to prolong QT interval among the fluoroquinolones.     

Inhibitory and bactericidal activities of gemifloxacin and other antimicrobials against Mycoplasma pneumoniae

The MIC of gemifloxacin was compared with that of sparfloxacin, levofloxacin, moxifloxacin, gatifloxacin, ciprofloxacin, doxycycline, erythromycin, azithromycin and clarithromycin using 97 clinical isolates of Mycoplasma pneumoniae. MBCs of fluoroquinolones were determined for a subgroup of 12 isolates. Macrolides were the most potent agents with MIC₉₀s for all drugs 0.001 mg/l. The doxycycline MIC₉₀ was 0.5 mg/l. Gemifloxacin MICs ranged from 0.001 to 0.25 mg/l. The gemifloxacin MIC₉₀ (0.125 mg/l) was equivalent to moxifloxacin and gatifloxacin, was 2-fold lower than sparfloxacin, 8-fold lower than levofloxacin and 32-fold lower than ciprofloxacin. MBCs for gemifloxacin were predominantly within 2–4 times the corresponding MIC values, indicating a bactericidal effect.     

甲磺酸加替沙星与其他4种氟喹诺酮类药物对临床分离菌的体外抗菌活性比较

目的 :比较甲磺酸加替沙星与氧氟沙星、左氧沙星、环丙沙星、司帕沙星对 182株临床分离菌的体外抗菌活性。方法 :采用琼脂平板二倍稀释法测定加替沙星等 5种氟喹诺酮类药物对 182株临床试验分离菌株的最低抑菌浓度 (MIC)。结果 :加替沙星对葡萄球菌属的MIC90 比其他 4种氟喹诺酮类药物低。葡萄球菌属对加替沙星的敏感率显著高于其他4种氟喹诺酮类药物 ;对其他G 球菌的MICR 也较其他氟喹诺酮类药物低。G-杆菌中埃希菌属、肠杆菌属对加替沙星的敏感率明显高于其他 4种氟喹诺酮类药物 ,加替沙星对埃希菌属、肠杆菌属的MIC90比左氧沙星低 2倍 ,比其他 3种抗菌药物低 8倍 ;假单胞菌属、克雷伯菌属和其他G-杆菌对加替沙星的敏感率与左氧沙星的差异无统计学意义 ,与其他 3种氟喹诺酮类药物的差异有统计学意义。结论 :甲磺酸加替沙星具有广谱而强大的体外抗菌活性。     

Fluoroquinolone-induced renal failure.

Fluoroquinolones are generally well tolerated, clinically useful antimicrobials. This paper highlights rare, but potentially serious, adverse effects involving the kidney. Other antimicrobials have long been known to cause various forms of nephrotoxicity occurring as allergic interstitial nephritis, granulomatous interstitial nephritis, necrotising vasculitis, allergic tubular nephritis or a tubular necrosis. A Medline search (1985 to May 1999) of ciprofloxacin, norfloxacin, levofloxacin, ofloxacin, trovafloxacin, enoxacin, sparfloxacin, grepafloxacin, gatifloxacin, clinafloxacin and moxifloxacin was conducted to ascertain the incidence and features of fluoroquinolone nephrotoxicity. Unfortunately, the data primarily consist of case reports and temporally related events. The incidence of these adverse effects is hard to estimate, and the cause may be multifactorial. While the use of ciprofloxacin appears to increase the risk, this may be due to its longer and more widespread use when compared with the newer agents.