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抗菌增效剂属于人工合成的二氨基嘧啶类药物，此类药物与抗菌药物联合使用时会以特定的机制来增强抗菌药的药物活性。近年来，由于抗生素的广泛使用甚至滥用导致细菌耐药的问题日益显现，通过加入抗菌增效剂而研制出的新制剂可以提高抗菌药在动物体内的利用率、降低药物用量、增强药物疗效、降低兽药残留及减少细菌耐药性。文章分析了近年来甲氧苄啶、二甲氧苄啶和艾地普林与各类抗生素的联合使用制备的制剂产品，发现其对疾病的治疗效果普遍优于单独使用抗生素。同时，配合中药的使用对细菌耐药的问题有显著改善，为后期抗菌增效剂的研究打开新的局面。随着对兽药制剂的研究，其不再局限于简单的剂型，通过运用新技术、新材料研制出的制剂，针对不同的给药部位和给药途径可以对病患进行更精准的治疗，减少药物达到靶部位的时间，增加患病部位的药量，此思路可为后续的研发方向提供支持和参考。文章将对抗菌药-抗菌增效剂联用制剂的研发情况进行综述。 相似文献
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阿地晋林（aditoprim,ADP）是一种新型苄氨嘧啶类药物,由瑞士Roche公司首先开始研究,华中农业大学袁宗辉课题组在国内率先开展了阿地普林中间体的合成研究工作。阿地普林与甲氧苄啶（TMP）、巴喹普林（BQP）、奥美普林（OMP）等都属于抗菌增效剂类药物,常与磺胺类药物配伍使用,以增强磺眩类药物的抗菌效力。与其它苄氨嘧啶类药物相比,阿地普林具有体内分布广泛、表观容积大、生物半衰期长、生物利用度高等优点,可作为甲氧苄啶和巴喹普林的替代药物,具有广阔的市场前景。 相似文献
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乳酸甲氧苄啶与痢菌净联用对弧菌的抑菌效果试验 总被引：4，自引：0，他引：4
由于抗菌药物的长期使用易造成细菌耐药性逐渐增加,因此,为了减缓耐药菌株的产生,提高药效,联合用药的配伍研究已受到越来越多地重视。试验采用肉汤稀释法测定了乳酸甲氧苄啶与痢菌净单用时的最小抑菌浓度（MIC）及其联用时的MIC,采用FIC指数对其联用效果进行了评价。结果表明,乳酸甲氧苄啶与痢菌净联合应用时呈现协同作用,其对鳗弧菌和副溶血弧菌的最佳配伍比为1∶1,对溶藻弧菌的最佳配伍比为1∶2。目前,通常使用的乳酸甲氧苄啶与抗菌药物的配伍比例为（1∶3）～（1∶5）,这一比例并不适用于痢菌净,建议二者的配伍比例为（1∶1）～（1∶2）。痢菌净与乳酸甲氧苄啶联用可增强抗菌活性,降低用药成本,对治疗由敏感细菌感染所致的疾病有一定的实际意义。 相似文献
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甲氧苄啶(TMP)是一种常用抗菌药,对多种革兰阳性和阴性细菌有抗菌作用,TMP一般用作抗菌增效剂和抗菌药联合使用,增强磺胺类药物及其他种类抗生素的抗菌作用。由于中药在抗菌方面效果不甚理想,因此,本文中药研究工作者对TMP与中药联合应用,增强中药抗菌效果进行了一些研究,本文就20余年来TMP对中药抗菌增效作用研究情况进行介绍。 相似文献
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主要以液体试管法和棋盘法测定3种抗菌药物和甲氧苄啶的最低抑菌浓度(MIC)，并以各药的小数抑菌浓度(nc)及小数抑菌浓度指数判断甲氧苄啶(TMP)与各药联合作用效应来评价TMP对不同抗菌药物的增效作用，确定其与抗菌药物最佳配伍比例。测定结果表明，TMP与受试药联合应用均产生协同作用，抗菌作用明显增强。TMP与不同抗菌药物配伍的最佳比例，因药物和受试菌株不同而异。 相似文献
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采用高效液相色谱-串联质谱法研究磺胺对甲氧嘧啶(SMD)和二甲氧苄啶(DVD)预混剂在白羽肉鸡体内各组织中的残留消除规律。对48只健康白羽肉鸡连续饲喂添加1 000mg/kg磺胺对甲氧嘧啶和二甲氧苄啶预混剂(含SMD 200mg,DVD 40mg)的全价饲料10d,在停药后4h,1、3、6、9、12、15d分别宰杀6只鸡,采集各组织进行药物残留测定。通过空白样品添加回收试验,所有基质中SMD和DVD的定量限分别为10μg/kg和5μg/kg,SMD和DVD分别在50、100、200μg/kg和25、50、100μg/kg 3个添加水平下的平均回收率为71.7%~102.3%,相对标准偏差为1.0%~11.9%。结果表明,磺胺对甲氧嘧啶和二甲氧苄啶预混剂在肾脏中残留量最高,肝脏其次;肌肉和皮脂中的残留量显著低于肝脏和肾脏,停药9d时,残留量低于药物残留限量。综合各组织中总残留量和最高残留限量规定,建议磺胺对甲氧嘧啶和二甲氧苄啶预混剂在鸡的休药期为7d。 相似文献
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甲氧苄啶对蒲公英体外抗菌增效作用的研究 总被引：1，自引：0，他引：1
采用微量棋盘稀释法测定了蒲公英、甲氧苄啶及两药联用对金黄色葡萄球菌、大肠杆菌和沙门氏菌的最小抑菌浓度(MIC),计算蒲公英与甲氧苄啶联用的组分抑菌浓度(FIC)指数。结果表明,蒲公英与甲氧苄啶联用对金黄色葡萄球菌、大肠杆菌和沙门氏菌的FIC指数分别为0.75、0.75和1,呈相加作用。采用平板计数的方法,测定了蒲公英与甲氧苄啶联用作用于3种细菌1、2、4和8 h后的细菌数,并计算杀菌率。利用最小二乘法对杀菌率进行拟合,计算出甲氧苄啶增强蒲公英体外抗金黄色葡萄球菌、大肠杆菌和沙门氏菌作用的最优添加剂量分别为4.0、1.8和2.0 mg/g。 相似文献
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Antibacterial synergist can enhance the antibacterial activity of the antibiotics, reduce bacterial resistance and improve treatment effect. Pharmacokinetic study is to develop dosage regimen and evaluate efficacy in clinical.Elimination of residual study can understand drug residual target tissue and residual marker to formulate appropriate withdraw time. This review briefly describes the aditoprim, trimethoprim,diaveridine of three kinds of antibacterial synergist pharmacokinetic and residue elimination rule, emphatically when contrast aditoprim to trimethoprim in the pharmacokinetic parameters of different animals. We can conclude aditoprim with longer elimination half-life and larger apparent volume of distribution, and trimethoprim elimination half-life is different in different animals, diaveridine is often used as intestinal antibacterial synergist. Recently researchers always use high performance liquid chromatography (HPLC) method or chromatographic combination method to study antibacterial synergist on pharmacokinetics and residues elimination research, it shows that the method has good specificity and high sensitivity. Currently due to the irrational use even abuse of antibiotics leading to drug failure and bacterial drug resistance problems, the presence of the antibacterial synergist for solving this problem provide a new direction, and three kinds of antibacterial synergist in different animals pharmacokinetic and residues elimination research is helpful to understand various kinds of drugs commonalities and differences in different animals, in order to find problems of this kind of drug in clinical using and continuously perfect applications of antibacterial synergist in clinical. 相似文献
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J A Lohuis H M Sutter T Graser B Ludwig A S van Miert W F Rehm E Rohde B Schneider M Wanner T van Werven 《American journal of veterinary research》1992,53(12):2311-2314
Plasma disposition of aditoprim, a new dihydrofolate reductase inhibitor, was studied in healthy cows and cows with endotoxin-induced mastitis. A single dose of 5 mg of aditoprim/kg of body weight was administered IV to 5 healthy cows and to the same cows 3 weeks later at 2 hours after intramammary infusion of 0.1 mg of endotoxin into the rear quarters. Mastitis developed in all endotoxin-infused quarters and cows had systemic signs of disease (fever, tachycardia, depression) from 2 to 10 hours after infusion of endotoxin. Pharmacokinetic characteristics of aditoprim in healthy cows were a large volume of distribution (6.28 L/kg), a systemic clearance of 0.82 L/h/kg, and an elimination half-life of 7.26 hours. In cows with mastitis, plasma concentrations of aditoprim were lower between 5 and 26 hours after injection. The systemic clearance (1.00 L/h/kg) and the volume of distribution (12.25 L/kg) were significantly higher in cows with mastitis, but elimination half-life was not significantly different. The lower plasma concentrations of aditoprim between 5 and 26 hours after injection in cows with mastitis are explained by fluid compartment shifts and/or blood flow changes induced by mastitis, although increased elimination of aditoprim in cows with mastitis cannot completely be ruled out. The antibacterial activity of aditoprim is nearly the same as that of trimethoprim. The longer elimination half-life time of aditoprim, however, indicates that it may have a practical pharmacotherapeutic advantage over trimethoprim. 相似文献
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Some pharmacokinetic parameters of aditoprim were determined in 3- and 6-month-old pigs. After intravenous administration of 5 mg/kg body weight, the mean total body clearance of the older pigs was smaller than that of the younger pigs. This difference was not reflected in the elimination half-life. After oral administration of 5 mg/kg body weight, the mean absorption rate constant was smaller and the mean absorption half-life was longer in the older pigs. The age-related changes in the pharmacokinetics of aditoprim were not sufficiently pronounced to suggest the necessity of modifying the oral dosage regimen in pigs of this age range. The favourable pharmacokinetics of aditoprim in pigs (large apparent volume of distribution, long elimination half-life and high bioavailability) may permit introduction of this drug into swine practice, after safety and residue depletion studies. 相似文献
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1. The pharmacokinetic and residue elimination patterns of sulphachloropyridazine appear to be modified by disease, even without affecting key organs essential for drug metabolism. 2. Drug kinetics and residue elimination data of a sulphachloropyridazine-trimethoprim preparation were compared using infectious coryza-affected (IC) fowl and healthy chickens. 3. The plasma concentrations of sulphachloropyridazine and trimethoprim were higher in affected animals, hence a reduced volume of distribution was obtained. 4. The half-life of sulphachloropyridazine and trimethoprim was reduced in IC-affected fowl and body clearance values were decreased. 5. The rate of drug residue elimination was noticeably slower in the IC-affected group. 6. These results indicate that drug elimination patterns in healthy and diseased animals are not the same. 相似文献
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头孢喹肟在猪呼吸道感染中应用的研究进展 总被引：1，自引：1，他引：0
呼吸道疾病严重威胁畜禽养殖业的发展,导致动物生长缓慢,使发病率和死亡率大幅升高,造成巨大的经济损失。胸膜肺炎放线杆菌、多杀性巴氏杆菌、链球菌、副猪嗜血杆菌等是诱发猪呼吸道感染的常见病原菌。头孢喹肟为第4代头孢菌素类动物专用抗生素,具有抗菌谱广、吸收速度快、达峰时间短、生物利用度高、对哺乳动物毒性低及对β-内酰胺酶稳定的特点,能有效治疗猪呼吸道类疾病,防止耐药性的产生。文章阐述了头孢喹肟的理化特性、杀菌机理、药动学特征等,并通过比较头孢喹肟在不同动物体内的药学参数表明头孢喹肟在猪体内达峰时间短,达峰浓度高,消除半衰期较长,能迅速发挥高效的抗菌作用,且能维持一定时间的抗菌效果;系统地介绍了头孢喹肟对猪呼吸道主要致病菌的体外抗菌活性及临床治疗效果,发现呼吸道临床病原菌对头孢喹肟敏感性高,临床应用前景广。目前头孢喹肟在临床应用存在一些问题,不合理使用会导致其出现耐药性,通过PK-PD同步模型的研究及耐药判定标准的建立,可为该药的合理应用提供科学依据。 相似文献
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Butch KuKanich Mark Papich David Huff Michael Stoskopf 《Journal of zoo and wildlife medicine》2004,35(2):179-184
Amikacin, an aminoglycoside antimicrobial, was administered to a killer whale (Orcinus orca) and a beluga whale (Delphinapterus leucas) for the treatment of clinical signs consistent with gram-negative aerobic bacterial infections. Dosage regimens were designed to target a maximal plasma concentration 8-10 times the minimum inhibitory concentrations of the pathogen and to reduce the risk of aminoglycoside toxicity. Allometric analysis of published pharmacokinetic parameters in mature animals yielded a relationship for amikacin's volume of distribution, in milliliters, given by the equation Vd = 151.058(BW)1.043. An initial dose for amikacin was estimated by calculating the volume of distribution and targeted maximal concentration. With this information, dosage regimens for i.m. administration were designed for a killer whale and a beluga whale. Therapeutic drug monitoring was performed on each whale to assess the individual pharmacokinetic parameters. The elimination half-life (5.99 hr), volume of distribution per bioavailability (319 ml/kg). and clearance per bioavailability (0.61 ml/min/kg) were calculated for the killer whale. The elimination half-life (5.03 hr), volume of distribution per bioavailability (229 ml/kg). and clearance per bioavailability (0.53 ml/min/kg) were calculated for the beluga whale. The volume of distribution predicted from the allometric equation for both whales was similar to the calculated pharmacokinetic parameter. Both whales exhibited a prolonged elimination half-life and decreased clearance when compared with other animal species despite normal renal parameters on biochemistry panels. Allometric principles and therapeutic drug monitoring were used to accurately determine the doses in these cases and to avoid toxicity. 相似文献
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N. E. Søli T. Framstad E. Skjerve S. Sohlberg S. A. Ødegaard 《Veterinary research communications》1990,14(5):403-410
Three sulphadiazine/trimethoprim preparations were administered orally during feeding to pigs. Six male and six female pigs were used. Clinically important pharmacokinetic parameters of the two drugs in the three preparations were determined and compared.The plasma concentrations of sulphadiazine and trimethoprim increased rapidly in the pigs followed by a quite rapid decrease from 4 to 12 h after oral administration. The mean values of the absorption half-lives of sulphadiazine and trimethoprim were 0.9–1.6 h and 0.5–0.8 h, respectively. The corresponding values for the elimination half-lives of sulphadiazine and trimethoprim were 3.1–4.3 h and 3.4–6.0 h, respectively. There were no significant differences between the pharmacokinetic parameters of the two compounds in the three preparations with the exception of Tmax for sulphadiazine and t1/2 for trimethoprim. Comparative bioavailability calculations showed no statistically significant differences between sulphadiazine and trimethoprim in the three preparations.The weight increase of the pigs during the experimental period (mean = 37.3–64.9 kg) did not cause differences in the kinetics of the two drugs which could have consequences for the use of the three combined preparations in clinical practice.No unacceptable or antibacterial residues of sulphadiazine or trimethoprim were found in the kidneys of pigs slaughtered at 5, 7 and 10 days after administration. 相似文献