Limbert M, Isert D, Klesel N, Markus A, Seeger K, Seibert G, Schrinner E
Hoechst AG, Pharma Research, Frankfurt/Main, Federal Republic of Germany.
Antimicrob Agents Chemother. 1991 Jan;35(1):14-9. doi: 10.1128/AAC.35.1.14.
Cefquinome is a new injectable aminothiazolyl cephalosporin derivative. It is stable against chromosomally and plasmid-encoded beta-lactamases and has a broad antibacterial spectrum. Staphylococcus aureus, streptococci, Pseudomonas aeruginosa, and members of the family Enterobacteriaceae (Escherichia coli, Salmonella spp., Klebsiella spp., Enterobacter spp., Citrobacter spp., and Serratia marcescens) are inhibited at low concentrations. Cefquinome is also active against many strains of methicillin-resistant staphylococci and enterococci. Its in vitro activity against gram-negative anaerobes is very limited. The high in vitro activity of cefquinome is reflected by its high in vivo efficacy against experimental septicemia due to different gram-positive and gram-negative bacteria. We studied the pharmacokinetic properties of cefquinome in mice, dogs, pigs, and calves. After single parenteral administrations, cefquinome displayed high peak levels, declining with half-lives of about 0.5, 0.9, 1.2, and 1.3 h, respectively. The areas under the concentration-time curve determined for dogs and mice showed linear correlations to the given doses. In dogs the urinary recovery was more than 70% within 24 h of dosing.
头孢喹肟是一种新型的注射用氨噻唑基头孢菌素衍生物。它对染色体介导和质粒介导的β-内酰胺酶均稳定，抗菌谱广。金黄色葡萄球菌、链球菌、铜绿假单胞菌以及肠杆菌科成员（大肠杆菌、沙门氏菌属、克雷伯菌属、肠杆菌属、柠檬酸杆菌属和粘质沙雷氏菌）在低浓度下即被抑制。头孢喹肟对许多耐甲氧西林葡萄球菌和肠球菌菌株也有活性。其对革兰氏阴性厌氧菌的体外活性非常有限。头孢喹肟的高体外活性反映在其对由不同革兰氏阳性和革兰氏阴性细菌引起的实验性败血症具有高体内疗效。我们研究了头孢喹肟在小鼠、犬、猪和犊牛体内的药代动力学特性。单次非肠道给药后，头孢喹肟呈现出较高的峰值水平，其半衰期分别约为0.5、0.9、1.2和1.3小时，随后下降。对犬和小鼠测定的浓度-时间曲线下面积与给药剂量呈线性相关。在犬中，给药后24小时内尿液回收率超过70%。
