Vertogradova T P, Kunrat I A
Antibiotiki. 1975 Jan;20(1):26-31.
Antibiotic 1719 administered intravenously to rats in a single dose of 6.0 mg/kg induced a transitory decrease in the number of myelocariocytes on the 2nd-5th day of its use mainly at the account of decreased numbers of lymphoid elements. Simultaneously momentory leucopenia (granulocytopenia) and more stable lymphopenia were observed. When the antibiotic was administered intravenously to dogs in a dose of 0.9 mg/kg 4 times and in a dose of 0.4 mg/kg 40 times, an insignificant decrease in the number of myelocarlocytes was noted. Leucopenia, lymphopenia and thrombocytopenia in the peripheral blood almost completely disappeared after discontinuation of the preparation administration. Leucocytosis (granulocytosis), lymphopenia and thrombocytopenia were registered in the dogs and rabbits treated with the antibiotic in doses of 1.5 and 3.0 mg/kg 3 and 11 times respectively. When the antibiotic was added to the rabbit blood serum in concentrations of 0.5-5 gamma/ml, 70 to 80 per cent of the preparation bound with the blood proteins. After a single intravenous administration of antibiotic 1719 to rabbits in doses of 10 and 15 mg/kg, it was detected in the blood only for 5 to 15 minutes after the administration in concentrations not exceeding 0.3 and 0.5 gamma/ml. The antibiotic penetrated into all organs in small amounts and persisted there for 1.5 to 3 hours after the administration. The antibiotic was excreted with the bile in amounts of 0.3-0.5 per cent of the dose administered for 1 to 2 hours after a single administration. The antibiotic was excreted with the urine for 3-4 hours after the administration in amounts of 3.5 per cent after a single administration and 60-72 per cent after multiple administrations.
以6.0毫克/千克的单剂量静脉注射给大鼠的抗生素1719,在使用的第2至5天导致骨髓细胞数量暂时减少,主要是由于淋巴样细胞数量减少。同时观察到短暂的白细胞减少(粒细胞减少)和更持久的淋巴细胞减少。当以0.9毫克/千克的剂量静脉注射给狗4次以及以0.4毫克/千克的剂量静脉注射40次时,发现骨髓细胞数量有不明显的减少。停药后外周血中的白细胞减少、淋巴细胞减少和血小板减少几乎完全消失。分别以1.5毫克/千克和3.0毫克/千克的剂量对狗和兔子进行3次和11次治疗后,记录到白细胞增多(粒细胞增多)、淋巴细胞减少和血小板减少。当抗生素以0.5 - 5微克/毫升的浓度添加到兔血清中时,70%至80%的制剂与血液蛋白结合。以10毫克/千克和15毫克/千克的剂量对兔子单次静脉注射抗生素1719后,给药后仅在5至15分钟内在血液中检测到,浓度不超过0.3微克/毫升和0.5微克/毫升。抗生素少量渗透到所有器官中,并在给药后在那里持续存在1.5至3小时。单次给药后1至2小时,抗生素随胆汁排出的量为给药剂量的0.3% - 0.5%。给药后3至4小时,抗生素随尿液排出,单次给药后排出量为3.5%,多次给药后为60% - 72%。