PHARMACOLOGY AND CHEMOTHERAPY OF AMPICILLIN - A NEW BROAD-SPECTRUM PENICILLIN

PHARMACOLOGY AND CHEMOTHERAPY OF AMPICILLIN - A NEW BROAD-SPECTRUM PENICILLIN
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DOI:
10.1111/j.1476-5381.1962.tb01416.x
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发表时间:
1962-01-01
期刊:
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY
影响因子:
--
通讯作者:
BROWN, DM
BROWN, DM
中科院分区:
其他
文献类型:
--
作者:
ACRED, P;TURNER, DH;BROWN, DM

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本文报道了一种新的青霉素--6[D(长划线)-[α]-氨基苯基-乙酰氨基]青霉酸的药理和化学性质。它无毒,可被口服吸收,并以类似于其他青霉素的方式在全身分布。它在胆汁和尿液中浓度较高时被原封不动地从体内消除。几乎所有的抗生素都可以在肌肉注射后2小时的尿液和肠道内容物中找到,但在口服后就不能了。结论是,抗生素在体内不会代谢。对感染动物的研究表明,它与现有的口服青霉素对化脓性葡萄球菌史密斯(青霉素敏感)、A组化脓性链球菌和肺炎双球菌同样有效。它对青霉素耐药葡萄球菌无效。当在感染了革兰氏阴性菌、鼠伤寒沙门氏菌和肺炎克雷伯氏菌的小鼠身上进行测试时,它的活性比四环素和氯霉素强得多。
The pharma-cology and chemotherapy of a new penicillin, 6[D([long dash])-[alpha]-aminophenyl-acetamido] penicillanic acid, are described. It is non-toxic, is absorbed orally and is distributed throughout the body in a manner similar to other penicillins. It is eliminated unchanged from the body in high concentrations in the bile and urine. Almost all of the antibiotic can be accounted for in the urine and intestinal contents 2 hr after intramuscular administration but not after oral administration. It is concluded that the antibiotic is not metabolized within the body. Studies with infected animals show that it is as effective as the existing oral penicillins against Staphylococcus pyogenes Smith (penicillin sensitive), Streptococcus pyogenes Group A and Diplococcus pneumoniae. It is ineffective against penicillin-resistant Staphylococci. When tested in mice infected with the gram-negative organisms, Salmonella typhimurium and Klebsiella pneumoniae, it was considerably more active than tetracycline and chloramphenicol.