Brice J E, Moreland T A, Walker C H
Arch Dis Child. 1979 May;54(5):356-61. doi: 10.1136/adc.54.5.356.
Nalorphine and naloxone were compared as to their effectiveness as pethidine antagonists. 85 infants were divided into a control group containing 19 newborn babies whose mothers did not receive pethidine and the babies received no antagonist, and three groups in which the mothers all received pethidine and the babies had either no antagonist (24), nalorphine IV (16), or naloxone IV (26). All the babies were assessed by measuring their neurobehavioural states and respiratory functions. A further 12 newborn babies had naloxone plasma levels measured by radioimmunoassay. Although standard doses of nalorphine effectively antagonised the depressive effect on respiration induced by pethidine, there was a pronounced and undesirable excitatory agonist action. Naloxone was not observed to have any agonist activity, but the recommended IV dose (0.01 mg/kg) had only a slight and delayed antagonist action as measured by respiratory function tests. A more rapid and improved antagonism was noted after this dose was doubled (0.02 mg/kg). The plasma elimination-phase half-life of naloxone after intravenous cord injection was about 3 hours.20
对纳洛芬和纳洛酮作为哌替啶拮抗剂的有效性进行了比较。85名婴儿被分为一个对照组，其中包含19名母亲未接受哌替啶且婴儿未接受拮抗剂的新生儿，以及三个组，这三组中母亲均接受了哌替啶，婴儿分别未接受拮抗剂（24名）、接受静脉注射纳洛芬（16名）或接受静脉注射纳洛酮（26名）。通过测量所有婴儿的神经行为状态和呼吸功能进行评估。另外12名新生儿通过放射免疫分析法测量了纳洛酮的血浆水平。虽然标准剂量的纳洛芬有效地拮抗了哌替啶对呼吸的抑制作用，但存在明显且不良的激动剂兴奋作用。未观察到纳洛酮有任何激动剂活性，但通过呼吸功能测试测量，推荐的静脉注射剂量（0.01mg/kg）仅有轻微且延迟的拮抗作用。该剂量加倍（0.02mg/kg）后，拮抗作用更快且有所改善。静脉注射脐带后，纳洛酮的血浆消除相半衰期约为3小时。
