Yancey R J, Kinney M L, Ford C W
J Antimicrob Chemother. 1985 Feb;15(2):219-32. doi: 10.1093/jac/15.2.219.
Staphylococcus aureus is a frequent cause of bovine mastitis worldwide. A model that may predict the efficacy of antimicrobial agents in the treatment of bovine mastitis induced by Staph. aureus was developed in lactating mice. Infection was established by the inoculation of lactating CF1 mice with Staph. aureus into the mammary gland via the teat duct. At the dose of bacteria used, 85-90% of the inoculated, untreated animals developed a nonlethal, acute mastitis within 48 h. Antibiotic treatment was administered subcutaneously or by the intramammary route. Lincosaminide antibiotics including lincomycin, clindamycin, and pirlimycin were evaluated in this system. Other compounds which have been used in therapy of bovine mastitis including novobiocin, penicillin G, ampicillin, cloxacillin and rifamycin-SV were used as reference antibiotics. Pirlimycin was the most effective of the antibiotics tested in this standardized system. Depending upon the route of administration, this novel lincosaminide was 15 to 95-fold more effective than clindamycin, three- to six-fold better than lincomycin, two- to ten-fold more effective than novobiocin, 13- to 17-times more effective than cloxacillin and 8- to 22-times better than rifamycin-SV on a weight-dose comparison. Penicillin G and ampicillin were the least effective drugs tested against mastitis induced by the beta-lactamase producing strain of Staph. aureus used in these assays. Pharmacokinetic experiments suggested that the greater effectiveness of pirlimycin compared to clindamycin and lincomycin was due to increased affinity for and prolonged retention in the mammary gland.
金黄色葡萄球菌是全球范围内引起奶牛乳腺炎的常见病因。在泌乳小鼠中建立了一个模型,用于预测抗菌药物治疗由金黄色葡萄球菌引起的奶牛乳腺炎的疗效。通过经乳头导管将金黄色葡萄球菌接种到泌乳的CF1小鼠乳腺中来建立感染。在所使用的细菌剂量下,85 - 90%接种但未治疗的动物在48小时内发生非致死性急性乳腺炎。抗生素治疗通过皮下或乳腺内途径给药。在该系统中评估了包括林可霉素、克林霉素和吡利霉素在内的林可酰胺类抗生素。其他已用于奶牛乳腺炎治疗的化合物,包括新生霉素、青霉素G、氨苄青霉素、氯唑西林和利福霉素 - SV用作参考抗生素。在这个标准化系统中,吡利霉素是测试的抗生素中最有效的。根据给药途径,在重量剂量比较中,这种新型林可酰胺类药物比克林霉素有效15至95倍,比林可霉素好3至6倍,比新生霉素有效2至10倍,比氯唑西林有效13至17倍,比利福霉素 - SV好8至22倍。青霉素G和氨苄青霉素是针对这些试验中使用的产生β - 内酰胺酶的金黄色葡萄球菌菌株诱导的乳腺炎测试中最无效的药物。药代动力学实验表明,吡利霉素比克林霉素和林可霉素更有效的原因是对乳腺的亲和力增加和在乳腺中的滞留时间延长。