Pharmacokinetics of prostaglandins
Pharmacokinetics of prostaglandins
复制标题
DOI：
10.1016/s1521-6934(03)00043-9
复制
发表时间：
2003-10-01
影响因子：
5.5
通讯作者：
Bygdeman, M
中科院分区：
文献类型：
--
作者：
Bygdeman, M
天然存在的前列腺素 (PG) 在人体循环中快速代谢。因此，为了临床使用，已经开发了许多能够抵抗快速失活的PG类似物。其中包括卡前列素、吉美前列素和米索前列醇。肌肉注射卡前列素后，血浆水平在 20 分钟后达到峰值，此后缓慢下降。在羊水中，半衰期为 31 至 37 小时。吉美前列素经阴道给药，2-3小时后达到最高血浆水平，至少68小时内可检测到水平。口服、阴道和舌下给药后可以获得米索前列醇的药代动力学数据。口服治疗后，血浆水平在约30分钟达到峰值，而阴道给药后，血浆水平逐渐升高，并在70-80分钟后达到最高水平，但在更长的时间内仍可检测到。舌下给药后，峰值浓度与口服治疗相同，但下降速度明显更慢。 PGE(2) 宫颈内给药可能被视为局部治疗，而阴道给药后通常会发现血浆代谢物水平升高。等离子体轮廓随所使用的车辆而变化。
Naturally occurring prostaglandins (PGs) are rapidly metabolized in the human circulation. For clinical use a number of PG analogues have therefore been developed which are resistant to rapid inactivation. Among these are carboprost, gemeprost and misoprostol. Following intramuscular injection of carboprost, plasma levels peaked after 20 minutes and declined slowly thereafter. In amniotic fluid the half-life was between 31 and 37 hours. Gemeprost is administered vaginally, and maximum plasma levels were reached after 2-3 hours, with detectable levels for at least 68 hours. Pharmacokinetic data on misoprostol are available following oral, vaginal and sublingual administration. Following oral treatment, plasma levels peaked at about 30 minutes, while after vaginal administration of the tablets the levels increased gradually and reached maximum levels after 70-80 minutes, but remained detectable for a significantly longer time. After sublingual administration the peak concentration was the same as for oral treatment but declined significantly more slowly. Endocervical administration of PGE(2) might be regarded as a local therapy, while following vaginal administration increased plasma levels of metabolites can generally be found. The plasma profile varies with the vehicle used.