Hartley R, Green M, Quinn M, Levene M I
Department of Clinical Medicine, University of Leeds.
Arch Dis Child. 1993 Jul;69(1 Spec No):55-8. doi: 10.1136/adc.69.1_spec_no.55.
Morphine pharmacokinetics were studied in 17 premature neonates (26-34 weeks' gestation) after intravenous infusion during the first 24 hours of life. Infants received either standard dose morphine that comprised of a 100 micrograms/kg/hour loading infusion for 2 hours followed by a maintenance infusion of 12.5 micrograms/kg/hour, or a high dose of 200 micrograms/kg/hour for 2 hours followed by 50 micrograms/kg/hour. Mean plasma concentrations of morphine (SD) after 2 and 24 hours were 99 (12.9) and 96.4 (3.2) ng/ml, and 184.2 (37.7) and 319 (71.2) ng/ml for the standard and high dose regimens, respectively. Morphine-3-glucuronide plasma concentrations achieved about 20% and 80% of morphine values at 2 and 24 hours respectively. Morphine-6-glucuronide could not be detected at 2 hours, but attained 20-25% of morphine plasma concentrations by 24 hours. The population mean morphine clearance was 2.4 ml/min/kg, the elimination half life was 8.75 hours and the volume of distribution was 1.82 1/kg. High plasma concentrations of morphine appeared to be well tolerated. Although mean arterial blood pressure decreased during the first six hours of treatment, this was not statistically significant; two infants experienced transient muscle rigidity, but no evidence of seizures was noted. There appears to be no clinical advantage in using the high dose regimen.
对17名早产新生儿(孕周26 - 34周)在出生后24小时内静脉输注吗啡后的药代动力学进行了研究。婴儿接受标准剂量吗啡,即先以100微克/千克/小时的负荷输注2小时,随后以12.5微克/千克/小时的维持输注;或高剂量吗啡,即先以200微克/千克/小时输注2小时,随后以50微克/千克/小时输注。标准剂量和高剂量方案在2小时和24小时后的吗啡平均血浆浓度(标准差)分别为99(12.9)和96.4(3.2)纳克/毫升,以及184.2(37.7)和319(71.2)纳克/毫升。吗啡-3-葡萄糖醛酸苷的血浆浓度在2小时和24小时分别达到吗啡值的约20%和80%。吗啡-6-葡萄糖醛酸苷在2小时时未检测到,但到24小时时达到吗啡血浆浓度的20 - 25%。群体平均吗啡清除率为2.4毫升/分钟/千克,消除半衰期为8.75小时,分布容积为1.82升/千克。高血浆浓度的吗啡似乎耐受性良好。虽然在治疗的前六个小时平均动脉血压有所下降,但无统计学意义;两名婴儿出现短暂的肌肉强直,但未观察到癫痫发作的证据。使用高剂量方案似乎没有临床优势。