Cozanitis D A, Krieg N
Anaesthesist. 1983 Mar;32(3):93-8.
Glycopyrrolate is a quaternary ammonium compound with indications for use similar to those for atropine. Because of the quaternary nature, it is poorly absorbed when taken orally and penetrates neither placental nor blood-brain barriers. When given by the parenteral route, the cardio-vagal blocking action of glycopyrrolate is twice that of atropine while inhibition of salivation is 5-6 times greater. The use of glycopyrrolate for premedication provides a therapeutic margin 2-3 times wider than that of atropine. Glycopyrrolate administered with neostigmine to antagonise the residual neuromuscular blockade of non-depolarising relaxants has advantages over atropine because the pharmacodynamic profile is more suited to that of neostigmine. The abrupt changes in cardiac rate, therefore, become minimal. If glycopyrrolate, 5 micrograms/kg-1, is injected intravenously just before the induction of anaesthesia, severe bradycardia is inhibited when repeated doses of succinylcholine are used. Although the alkalinising effect on gastric secretions has not been substantially verified, glycopyrrolate does provide long lasting bronchodilatation from its blocking action on smooth muscle. Only a few studies with glycopyrrolate in children have yet been published. However, it appears that this drug provides no real advantages over atropine when used in paediatric anaesthesia.
格隆溴铵是一种季铵化合物,其适应证与阿托品相似。由于其季铵性质,口服时吸收较差,且不能穿透胎盘屏障和血脑屏障。经胃肠外途径给药时,格隆溴铵的心脏迷走神经阻滞作用是阿托品的两倍,而抑制唾液分泌的作用则比阿托品大5 - 6倍。用于术前用药时,格隆溴铵的治疗窗比阿托品宽2 - 3倍。与新斯的明联合使用以拮抗非去极化肌松药的残余神经肌肉阻滞时,格隆溴铵比阿托品更具优势,因为其药效学特性更适合新斯的明。因此,心率的突然变化变得最小。如果在麻醉诱导前静脉注射5微克/千克的格隆溴铵,在重复使用琥珀酰胆碱时可抑制严重心动过缓。尽管对胃酸分泌的碱化作用尚未得到充分证实,但格隆溴铵通过对平滑肌的阻滞作用确实能提供持久的支气管扩张作用。关于格隆溴铵在儿童中的研究仅有少数发表。然而,在小儿麻醉中使用时,这种药物似乎并不比阿托品有真正的优势。