Selgas R, Martinez M E, Miranda B, Bajo M A, Romero J R, Ausejo M, Sanchez-Cabezudo M J, Lopez-Revuelta K, Sanchez-Sicilia L
Servicio de Nefrologia, Hospital La Paz, Madrid, Spain.
Perit Dial Int. 1993;13(2):122-5.
To evaluate the kinetics of calcitriol (1,25(OH)2D3) administered subcutaneously.
Calcitriol kinetics and efficacy after subcutaneous administration were studied in 13 CAPD patients with varying degrees of increased plasma levels of parathyroid hormone (i-PTH). A single dose of 2 micrograms of calcitriol was administered subcutaneously, and its serum levels at baseline and after 1, 2, 6, 12, and 24 hours were determined. Plasma ionized calcium and i-PTH were also determined at these periods.
Serum calcitriol levels reached peak levels of 60 and 70 pg/mL at 1 and 2 hours after administration, respectively. These levels decreased thereafter, but remained above baseline values during 24 hours. The mean value of the area under the curve (AUC) was 809 +/- 226 pg/mL/hour. Plasma i-PTH levels showed a slight decrease after 1 and 2 hours, returning to baseline levels after this period. Plasma ionized calcium did not show significant changes during the study. A slight pain at the site of injection was mentioned by some patients.
The subcutaneous route for calcitriol administration achieves theoretically adequate plasma levels in continuous ambulatory peritoneal dialysis (CAPD) patients. This is important when parenteral administration of calcitriol is considered in the treatment of secondary hyperparathyroidism.
评估皮下注射骨化三醇(1,25(OH)₂D₃)的药代动力学。
对13例甲状旁腺激素(i-PTH)血浆水平不同程度升高的持续性非卧床腹膜透析(CAPD)患者,研究皮下注射骨化三醇后的药代动力学及疗效。皮下注射单剂量2微克骨化三醇,并测定基线时以及注射后1、2、6、12和24小时的血清水平。在这些时间段还测定了血浆离子钙和i-PTH。
给药后1小时和2小时血清骨化三醇水平分别达到峰值60和70 pg/mL。此后这些水平下降,但在24小时内仍高于基线值。曲线下面积(AUC)的平均值为809±226 pg/mL/小时。血浆i-PTH水平在1小时和2小时后略有下降,此后恢复到基线水平。研究期间血浆离子钙未显示出显著变化。一些患者提到注射部位有轻微疼痛。
在持续性非卧床腹膜透析(CAPD)患者中,皮下注射骨化三醇的途径理论上可达到足够的血浆水平。在考虑采用胃肠外途径给予骨化三醇治疗继发性甲状旁腺功能亢进时,这一点很重要。