Goto A, Amano M, Sakai A, Hara M, Takahashi N
Preclinical Research Laboratories, Bristol-Myers Research Institute, Ltd.
Jpn J Antibiot. 1990 Jul;43(7):1289-309.
General pharmacological properties of BMY-28100, a new semisynthetic oral cephalosporin, were studied in experimental animals. The obtained results are summarized as follows: 1. BMY-28100 had no effect on gross behavior and the central nervous system in mice and rats nor on EEG activities in rabbits. 2. BMY-28100 did not affect the smooth muscle isolated from rats, guinea pigs or rabbits nor did it influence ganglionic transmission in cats. 3. Effects of BMY-28100 on the atrium and heart isolated from guinea pigs were not obvious. Several parameters of the cardiovascular system were examined and found unchanged by administration of BMY-28100 to rabbits. 4. In the digestive system, BMY-28100 had no effect on charcoal meal transport in the small intestine of mice. In rats, however, gastric secretion was reduced at a dose level of 125 mg/kg or higher and bile secretion was enhanced at a dose level of 500 mg/kg. 5. BMY-28100 had no effect on neuromuscular transmission in rabbits and showed no local anesthetic activity in guinea pigs. 6. BMY-28100 decreased urine volume and urinary excretion of electrolytes in dose-dependent manners in rats. Sulfobromophthalein excretion in rats was inhibited only at the highest dose tested. BMY-28100 had no effect on blood coagulation and red blood cell resistance in rats or rabbits. BMY-28100 revealed no antiinflammatory activity in rats. 7. BMY-28167, a trans-isomer of BMY-28100, had no or weak effects on some of above test systems when compared with BMY-28100. These results suggest that BMY-28100 has hardly any pharmacological properties leading to severe adverse reactions in clinical use.
对新型半合成口服头孢菌素BMY - 28100的一般药理学特性在实验动物中进行了研究。所得结果总结如下：1. BMY - 28100对小鼠和大鼠的总体行为及中枢神经系统无影响，对兔的脑电图活动也无影响。2. BMY - 28100对从大鼠、豚鼠或兔分离的平滑肌无影响，对猫的神经节传递也无影响。3. BMY - 28100对从豚鼠分离的心房和心脏的作用不明显。对兔的心血管系统的几个参数进行了检查，发现给予BMY - 28100后这些参数未发生变化。4. 在消化系统中，BMY - 28100对小鼠小肠内炭末推进无影响。然而，在大鼠中，剂量为125mg/kg或更高时胃分泌减少，剂量为500mg/kg时胆汁分泌增加。5. BMY - 28100对兔的神经肌肉传递无影响，在豚鼠中无局部麻醉活性。6. BMY - 28100以剂量依赖性方式减少大鼠的尿量和电解质尿排泄。仅在测试的最高剂量下，大鼠的磺溴酞排泄受到抑制。BMY - 28100对大鼠或兔的血液凝固和红细胞抵抗力无影响。BMY - 28100在大鼠中未显示出抗炎活性。7. BMY - 28167是BMY - 28100的反式异构体，与BMY - 28100相比，对上述某些测试系统无影响或作用较弱。这些结果表明BMY - 28100在临床使用中几乎没有导致严重不良反应的药理学特性。
