Liashenko Iu I
Antibiotiki. 1979 Apr;24(4):303-6.
The levels of benzylpenicillin on its intramuscular administration in doses of 100000 or 200000 units, as well as the renal and hepatic functions and the antibiotic binding by the host protein components were studied in 44 angina patients and 29 healthy persons. The benzylpenicillin levels were always markedly higher in the angina cases than those in the healthy persons. The ratio of the free and protein bound fractions of the antibiotic in the above groups was practically the same. At the same time the amount of benzylpenicillin excreted with the urine was higher in the angina patients than in the healthy persons approximately by 2 times. The study of the function of the internal organs revealed a marked decrease in the daily diuresis in all the angina patients and microhematuria in the 1/4 of the cases. The impairment of the renal function was determined by the laboratory methods practically in all the patients. On the basis of the data obtained it was concluded that the increased benzylpenicillin levels in the angina cases were connected with a decreased capacity for inactivating this substance by the liver enzymatic systems due to the changed function of this organ. The fact of the increased antibiotics levels in the host is considered as a positive phenomenon providing inhibition of the disease causative agents resistant to usual concentrations of the drug.
对44例心绞痛患者和29名健康人研究了肌内注射100000或200000单位剂量苄青霉素后的血药浓度，以及肾功能、肝功能和宿主蛋白质成分对抗生素的结合情况。心绞痛患者的苄青霉素血药浓度始终明显高于健康人。上述两组中抗生素游离部分与蛋白结合部分的比例基本相同。同时，心绞痛患者尿液中苄青霉素的排泄量比健康人高出约2倍。对内脏器官功能的研究发现，所有心绞痛患者的每日尿量均显著减少，四分之一的病例出现微血尿。几乎所有患者通过实验室方法均确定存在肾功能损害。根据所获数据得出结论，心绞痛患者苄青霉素血药浓度升高与肝脏酶系统使该物质失活的能力下降有关，这是由于肝脏功能改变所致。宿主中抗生素水平升高这一事实被视为一种积极现象，可抑制对常规药物浓度耐药的病原体。
