头孢维星研究进展

头孢维星是一种新型的动物专用第3代头孢菌素类广谱抗菌药。头孢维星现主要用于犬和猫,具有吸收迅速、消除缓慢、生物利用度高、药效维持时间长、治疗指数高等特点,可作为犬、猫的长效抗生素使用。论文对头孢维星的作用机制、药动学、药效学及临床应用方面进行综述,以期为头孢维星在兽医临床应用提供参考依据。     

头孢维星研究概况

头孢维星是一种新型的动物专用第3代头孢菌素类广谱抗菌药。头孢维星现主要用于犬和猫,具有吸收迅速、消除缓慢、生物利用度高、药效维持时间长、治疗指数高等特点,可作为犬、猫的长效抗生素使用。论文对头孢维星的作用机制、药动学、药效学及临床应用方面进行综述,以期为头孢维星在兽医临床应用提供参考。     

头孢维星的药动学研究

头孢维星作为犬、猫的临床常用药,具有吸收快、消除半衰期长、生物利用度高、药效持久、安全性好、治疗指数高等特点,单剂量给药后可在体内维持14 d的有效血药浓度。其常被用于治疗由伪中间型葡萄球菌、艰难梭菌、大肠埃希菌、多杀性巴氏杆菌等引起的犬、猫疾病。同时也常作为预防用药,防治术后感染。本文拟对头孢维星的药动学研究进展做以综述,以期为头孢维星的临床用药提供科学指导。     

头孢维星在犬体内的药动学及生物利用度研究

建立了一种头孢维星在犬血浆中的高效液相色谱检测法,并研究了头孢维星在犬体内的药动学特征及生物利用度。选用健康家犬12只,按单剂量(8 mg/kg b.w.)分别静脉注射或皮下注射头孢维星,利用建立的方法对头孢维星在犬血浆中的浓度进行测定,采用Win Nonlin5.2.1程序的非房室模型处理药时数据。结果显示,静脉注射组的主要药动学参数为t1/2β=129.15±35.79 h;MRT=152.56±44.95 h;λz=0.0059±0.0023 h-1;Cl=1.24±0.56 m L/(h·kg);AUC=6942.88±2462.48μg獉h/m L;V=170.20±28.09 m L/kg。皮下注射组的主要药动学参数为t1/2β=136.94±20.96 h;MRT=167.77±28.15 h;Tmax=0.83±0.26 h;Cmax=59.51±7.99μg/m L;λz=0.0052±0.0009 h-1;Cl=1.05±0.21 m L/(h·kg);AUC=7332.58±1118.30μg·h/m L;V=203.81±30.09 m L/kg;F=105.61%。结果表明,头孢维星在家犬体内表现出吸收迅速、消除缓慢、表观分布容积大、生物利用度高等药动学特点。     

头孢维星钠对皮肤病患犬血液生理生化指标的影响研究

正犬皮肤病是临床常见的疾病之一,约占临床病例的20%,皮肤病一般不会导致死亡,但治疗却有一定难度,复发率高,治疗周期长,有的甚或久治不愈。患有皮肤病的犬猫主要表现为剧痒,疼痛和极度不安,动物啃挠患部导致皮肤破溃,细菌侵入而引发炎症反应。头孢维星钠是新型动物专用第三代广谱长效抗生素,具有消除缓慢、生物利用度高、外周组织浓度高于血浆浓度等特点,     

动物专用头孢噻呋

头孢噻呋是第1个动物专用的第3代头孢菌素类抗生素,具有抗茵谱广,抗茵活性强,给药后吸收迅速,生物利用度高,半衰期长,药效持久等特点.近年来,在兽医临床上的应用日趋广泛.论文从头孢噻呋的理化性质、抗茵活性、抗生素后效应、药代动力学特征、临床应用、不良反应和头孢噻呋在动物性食品中的残留检测等方面进行了综述.为该药在兽医临床应用提供参考.     

头孢噻呋钠在毛皮动物疾病防治上的应用

<正>头孢噻呋钠(头孢畜健)是全球第一个畜禽专用的第3代头孢菌素,头孢噻呋钠以其优良的抗菌活性、体内动力学过程、极低的药物残留以及动物专用的属性,成为新一代兽药的代表,在兽医临床中具有广阔的应用前景。日照市药械站在门诊中应用齐鲁动物保健品有限公司生产的头孢畜健收到了非常好的效果,现把临床部分病例介绍如下。     

临床兽用抗菌药有哪些种类?

正临床常用的抗菌药包括抗生素和合成抗菌药。抗生素有:⑴青霉素类:如青霉素、苄星青霉素、氨苄西林、阿莫西林、海他西林。⑵头孢菌素类:如头孢氨苄、头孢噻呋、头孢喹肟等。⑶氨基糖苷类:如链霉素、庆大霉素、卡那霉素、新霉素、大观霉素和安普霉素等。⑷四环素类:如金霉素、土霉素、四环素和多西环素等。⑸酰胺醇类:如氟苯     

黄杨宁中主要生物碱分离纯化方法

综述了目前黄杨宁中环维黄杨星D的分离纯化和质量控制的几种方法,并对其进行了比较.通过对HPLC法和薄层色谱法在环维黄杨星D分离纯化中的应用及影响.探索进一步的优化条件,以期为黄杨宁药品生产过程中提高有效成分和杂质控制的检测提供帮助.     

盐酸头孢噻呋注射液治疗奶牛急性产后子宫炎的研究进展

盐酸头孢噻呋注射液在国外已广泛用于治疗奶牛急性产后子宫炎,本文结合国内外研究进展,阐述了盐酸头孢噻呋注射液的作用机制、抗菌活性、药代动力学、临床应用以及残留消除等内容,为盐酸头孢噻呋注射液在治疗奶牛急性产后子宫炎上的研究及应用提供相关参考。     

Pharmacokinetics of intravenous and subcutaneous cefovecin in alpacas

The purpose of this study was to determine the pharmacokinetics of cefovecin after intravenous and subcutaneous dose of 8 mg/kg to alpacas. Bacterial infections requiring long‐term antibiotic therapy such as neonatal bacteremia, pneumonia, peritonitis, dental, and uterine infections are a significant cause of morbidity and mortality in this species. However, few antimicrobials have been evaluated and proven to have favorable pharmacokinetics for therapeutic use. Most antimicrobials that are currently used require daily injections for many days. Cefovecin is a long‐acting cephalosporin that is formulated for subcutaneous administration, and its long‐elimination half‐life allows for 14‐day dosing intervals in dogs and cats. The properties of cefovecin may be advantageous for medical treatment of camelids due to its broad spectrum, route of administration, and long duration of activity. Pharmacokinetic evaluation of antimicrobial drugs in camelids is essential for the proper treatment and prevention of bacterial disease, and to minimize development of antibiotic resistant bacterial strains due to inadequate antibiotic concentrations. Cefovecin mean half‐life, volume of distribution at steady‐state, and clearance after intravenous administration were 10.3 h, 86 mL/kg, and 7.07 mL·h/kg. The bioavailability was 143%, while half‐life, C_max, and T_max were 16.9 h, 108 μg/mL, and 2.8 h following subcutaneous administration. In the absence of additional microbial susceptibility data for alpaca pathogens, the current cefovecin dosage regimen prescribed for dogs (8 mg/kg SC every 14 days) may need to be optimized for the treatment of infections in this species.     

Clinical efficacy and safety of cefovecin in the treatment of canine pyoderma and wound infections

OBJECTIVES: To determine the efficacy and safety of cefovecin in the treatment of bacterial skin infections in dogs. METHOD: Dogs with superficial or deep pyoderma or wounds/abscesses were enrolled in three separate studies. Dogs (354) were randomised to treatment and received either cefovecin administered by subcutaneous injection at 14 day intervals, as clinically necessary, or amoxicillin/clavulanic acid as oral tablets twice daily for 14 days. Courses of treatment were repeated at 14 day intervals up to a total of four courses. Clinicians responsible for assessing lesions were masked to treatment allocation. Only animals where the presence of a pretreatment bacterial pathogen was confirmed were included in the analysis of efficacy. Cases were evaluated for clinical efficacy at 28 days after initiation of the final course of treatment. Clinical efficacy was assessed by scoring the clinical signs typical of skin infections. RESULTS: Cefovecin demonstrated statistical non-inferiority compared with amoxicillin/clavulanic acid for all three clinical diagnoses; for cefovecin, up to 96.9 per cent efficacy was observed versus 92.5 per cent for amoxicillin/clavulanic acid. CLINICAL SIGNIFICANCE: Cefovecin was shown to be as effective as amoxicillin/clavulanic acid administered orally in the treatment of bacterial skin infections in dogs. Cefovecin offers the additional benefit of eliminating owner non-compliance.     

Single subcutaneous dosing of cefovecin in rhesus monkeys (Macaca mulatta): a pharmacokinetic study

Bakker, J., Thuesen, L. R., Braskamp, G., Skaanild, M. T., Ouwerling, B., Langermans, J. A. M., Bertelsen, M. F. Single subcutaneous dosing of cefovecin in rhesus monkeys (Macaca mulatta): a pharmacokinetic study. J. vet. Pharmacol. Therap. 34 , 464–468. Cefovecin is a third‐generation cephalosporin approved for antibacterial treatment with a 14‐day dosing interval in dogs and cats. This antibiotic may also be useful for zoo and wildlife veterinary medicine, because of its broad spectrum and long duration of activity. The aim of the study was to determine whether cefovecin is a suitable antibiotic to prevent skin wound infection in rhesus monkeys. Therefore, the pharmacokinetics (PK) of cefovecin after a single subcutaneous injection at 8 mg/kg bodyweight in four rhesus monkeys (Macaca mulatta) and sensitivity of bacterial isolates from fresh skin wounds were determined. After administration, blood, urine, and feces were collected, and concentrations of cefovecin were determined. Further, the minimum inhibitory concentrations (MIC) for bacteria isolated from fresh skin wounds of monkeys during a health control program were determined. The mean maximum plasma concentration (C_max) of cefovecin was 78 μg/mL and was achieved after 57 min. The mean apparent long elimination half‐life (t½) was 6.6 h and excretion occurred mainly via urine. The MIC for the majority of the bacteria examined was >100 μg/mL. The PK of cefovecin in rhesus monkeys is substantially different than for dogs and cats. Cefovecin rapidly reached C_max which however was lower than most of the MIC levels and with a very short t½. Therefore, cefovecin is not recommended for treating skin wounds in rhesus monkeys.     

The efficacy and safety of cefovecin in the treatment of feline abscesses and infected wounds

OBJECTIVES: To determine the efficacy and safety of cefovecin for the treatment of bacterial abscesses and wounds in cats at clinics in Germany, France, Spain and the UK. METHOD: Cats with abscesses or wounds were enrolled. Cats (217) were randomised to treatment with either cefovecin administered by subcutaneous injection at 14 day intervals or amoxicillin/clavulanic acid as twice-daily oral tablets for 14 days. Treatment courses were repeated at 14 day intervals, when deemed necessary. Clinicians assessing lesions were masked to treatment allocation. Only animals with a confirmed pretreatment bacterial pathogen were included in the efficacy analysis. Cases were evaluated 28 days after initiation of the final course of treatment. RESULTS: Cefovecin was as efficacious as amoxicillin/clavulanic acid, and efficacy was 100 per cent for both treatments. CLINICAL SIGNIFICANCE: Cefovecin, administered as a single subcutaneous injection repeated at 14 day intervals as required, was shown to be as efficacious as oral amoxicillin/clavulanic acid in the treatment of abscesses/wounds in cats.     

Selected pharmacokinetic parameters for Cefovecin in hens and green iguanas

The third generation cephalosporin cefovecin has been shown to have an exceptionally long elimination half-life in dogs and cats, making it suitable for antibacterial treatment with a 14-day dosing interval in these species. Pharmacokinetic parameters for cefovecin were investigated in juvenile hens and green iguanas, following subcutaneous injections with 10 mg cefovecin/kg bodyweight. Preliminary studies in eight additional species of birds and reptiles were performed and results were compared with the parameters found in hens and green iguanas. The kinetics were characterized by rapid absorption with peak plasma concentration of 6 ± 2 μg/mL in hens and 35 ± 12 μg/mL in green iguanas. The mean plasma half-life for cefovecin was 0.9 ± 0.3 h for hens and 3.9 h in green iguanas. Volume of distribution was 1.6 ± 0.5 L/kg for hens and 0.3 L/kg for green iguanas and clearance was 1252 ± 185 mL·h/kg for hens and 53 mL·h/kg for green iguanas. Results from preliminary studies did not differ notably from those seen in hens and green iguanas. Cefovecin is not suitable for the treatment of bacterial infections with a 14-day dosing interval in hens or green iguanas and seems not to be in a number of other bird and retile species either.     

Efficacy and safety of cefovecin for the treatment of urinary tract infections in cats

OBJECTIVES: To determine the efficacy and safety of cefovecin (Convenia); Pfizer Animal Health) in the treatment of urinary tract infections in cats. METHOD: A multi-centre, masked, randomised study was conducted in cats presenting with clinical signs indicative of urinary tract infections. Cephalexin (Rilexine); Virbac) administered orally twice daily at 15 mg/kg bodyweight for 14 days was compared with a single subcutaneous injection of cefovecin in cats. The primary efficacy parameter assessed was bacterial elimination of the pretreatment uropathogen. RESULTS: Four hundred and thirty-four cats were screened for urinary tract infections. One hundred and eighty-five cats were treated with either cefovecin (n=124) or cephalexin (n=61). Ninety-seven cats (22.2 per cent) had confirmed bacteriuria and 82 cats were included in efficacy analysis. Escherichia coli was eliminated in 76.7 per cent (23 of 30) of cefovecin-treated cats compared with 62.5 per cent (10 of 16) of cephalexin-treated cats. Cefovecin demonstrated statistical non-inferiority compared with cephalexin for bacterial elimination. There were no suspected adverse drug reactions attributable to treatment with cefovecin or cephalexin. CLINICAL SIGNIFICANCE: Cefovecin was demonstrated to be an effective and safe treatment for urinary tract infections.     

育成波尔山羊胚胎移植研究

利用进口FSH超排12月龄的波尔母山羊6只，获卵83枚 ，只均13.8枚，获可用胚74枚，最高一只19枚，只均12.33枚。共移植奶山羊受体37只，两 个情期不返情27只，情期不返情率72.97%。35～40 d用B超探测仪检查怀孕结果(以观 察到胎儿为准)，实际怀孕22只，移植妊娠率59.46%，其中移植双胚的妊娠率66.67%，单胚 的妊娠率50.00%。     

细胞培养过程中白色念珠菌污染的防控

为探讨大扶康防控细胞培养过程中白色念球菌污染的可行性,采用不同浓度的大扶康共同培养,观察其抑制白色念珠菌的效果,及对小鼠成肌细胞C2C12生长情况的影响。结果：采用300 μg/ml大扶康防控效果最佳,毒性作用小,对C2C12细胞的生存率无明显影响。采用30 μg/ml大扶康与20 μg/ml硫酸阿米卡星＋50 μg/ml头孢他啶配伍的方法可有效预防细胞培养过程中的真菌污染。结论：采用大扶康可有效控制细胞培养中白色念珠菌的污染。采用大扶康与硫酸阿米卡星＋头孢他啶配伍的方法可有效预防细胞培养过程中的真菌污染。     

鹿花盘蛋白质的提取与生物活性测定

采用盐提、热变性处理及凝胶过滤法从鹿花盘中提取 鹿花盘蛋白质(PSAB)。PSAB经SDS-PAGE电泳呈现5条谱带，测定其分子量分别为65.57KD、2 8.179KD、21.265KD、16.758KD、13.79KD；氨基酸分析表明，鹿花盘蛋白质含有17种氨基酸 。动物实验表明，鹿花盘蛋白质能显著地增强机体的抗疲劳作用和提高肾上腺功能；对油漆 应激小鼠有明显保护作用，能显著增加小鼠红细胞数和血红蛋白的含量。表明PSAB具有滋补 强壮、养气补血的作用，是鹿花盘的活性成分之一。