Albiero L, Ongini E, Parravicini L
Eur J Pharmacol. 1978 Jul 1;50(1):1-7. doi: 10.1016/0014-2999(78)90247-9.
The neuromuscular blocking activity of netilmicin sulphate (Sch 20569), a new aminoglycoside antibiotic, was studied on the rat sciatic nerve-gastrocnemius muscle preparation. The i.v. administration of netilmicin caused a gradual fall, up to complete blockade, of the muscular contraction elicited by nerve stimulation. Conversely, the muscular response to direct stimulation was not affected. The response pattern was similar to that seen with known aminoglycoside antibiotics. The acute toxic effects (LD50 i.p. in mice) of netilmicin were antagonized by pretreatment with neostigmine; this latter partially prevented netilmicin-induced blockade, but was not able to reverse it. Calcium chloride was the only agent effective both to prevent and to reverse the neuromuscular blocking effects of netilmicin.
对新型氨基糖苷类抗生素硫酸奈替米星(Sch 20569)的神经肌肉阻断活性进行了研究,实验对象是大鼠坐骨神经-腓肠肌标本。静脉注射奈替米星会导致神经刺激引起的肌肉收缩逐渐减弱,直至完全阻断。相反,直接刺激引起的肌肉反应不受影响。这种反应模式与已知氨基糖苷类抗生素所见相似。新斯的明预处理可拮抗奈替米星的急性毒性作用(小鼠腹腔注射半数致死量);新斯的明部分预防了奈替米星诱导的阻断,但无法逆转它。氯化钙是唯一既能预防又能逆转奈替米星神经肌肉阻断作用的药物。