新肌松药溴化双托品铵的药理学研究

溴化双托品铵是以阿托品为原料,合成而得的一种双季铵化合物。实验表明,家兔垂头量为0.134±0.016mg/kg;麻醉猫坐骨神经胫前肌阻断量为0.16±0.029mg/kg,作用持续21±3.9min。经典与电生理方法研究表明,它是一种非去极化型肌松药。家兔连续多次给药时有一定蓄积作用。麻醉猫快速静注给药,可使血压下降。若以缓慢静滴给药,降压作用显著减轻。对ECG则无明显影响。

PHARMACOLOGICAL STUD IES OF BISATROPINIUM BROMIDE, A NEW MUSCLE RELAXANT

Bisatropinium bromide(BA), 1, 4-diethoxybenzene-bis-atropinium dibromide, is a new muscle relaxant synthesized with atropine. This paper reports the results of pharmacological studies.In rabbits, the head-drop dose of BA was found to be 0.13±0.029 mg/kg(ⅳ). In sciatic-tibialis anterior preparations of anesthetized cats, the neuromuscular blocking dose of BA was 0.16±0.029 (?)g/kg(ⅳ), with a duration of 21±3.9 min. The evidences obtained by classical and electrophysiological methods indicate that BA is a non-depolarzing muscle relaxant.When BA(1.4 x head-drop dose) was administered repeatedly to conscious rabbits for 9 times within 2.5 h, certain accumulative effect was observed. Nevertheless, all animals recovered without deleterious effect. Bolus intravenous injection of BA at a neuromuscular blocking dose produced a trancient hypotension in anesthetized cats, but seldom in rabbits. The hypotensive effect of BA could be nullified to a slight degree by administering the drug through slow intravenous drip. Further experiments showed that the hypotensive effect in cats was chiefly mediated by its sympathetic ganglion blocking action. In anesthetized cats, doses of BA sufficient to produce a complete muscle paralysis provoked no marked ECG changes. BA retained feeble antimuscarinic activity.On account of its high potency, suitable duration of action and relative safety shown in animal experiments, we think that BA may be a new muscle relaxant of potential clinical value.