Lahera V, Cachofeiro V, Cañizo F J, Durán F, Parada J, Rodriguez F J, Tresguerres A F
Prostaglandins Leukot Med. 1986 Jun;22(3):265-73. doi: 10.1016/0262-1746(86)90137-x.
ZK 36 374 is a chemically stable prostacyclin analogue which has been demonstrated to be a potent vasodilator. The effects of the drug on blood pressure, plasma renin activity, diuresis and urinary excretion of prostaglandin E2 and sodium, were studied on the 1st and 7th days of treatment and a week after the end of the administration to rats submitted to the following experimental situations: Goldblatt 2k-1c, Goldblatt 2k-1c + 5% NaCl loading, 5% NaCl loading, and controls. ZK 36 374 was continuously administered during one week by an osmotic pump subcutaneously implanted and connected to the right jugular vein. Twenty four hours after the pump implantation, blood pressure decreased in the three experimental groups. At the 7th day, pressure remained at similar levels except in NaCl loaded rats where an increase was observed. At the 15th day pressure levels returned to pretreatment values. On the 7th day of treatment urinary PGE2 showed higher values than pretreatment ones, to return to pretreatment at the 15 day. Sodium excretion showed an increase on the 7th day and was even higher on the 15th day. Plasma renin activity levels remained unchanged during the treatment except in the Goldblatt 2k-1c group which showed a significant fall at the 7th day. All the changes described on the 1st day of treatment might be related to counteraction of the blood pressure decrease on the same day.
ZK 36 374是一种化学性质稳定的前列环素类似物，已被证明是一种强效血管扩张剂。在以下实验情况下，对大鼠进行治疗的第1天和第7天以及给药结束后一周，研究了该药物对血压、血浆肾素活性、利尿以及前列腺素E2和钠的尿排泄的影响：Goldblatt 2k-1c、Goldblatt 2k-1c + 5%氯化钠负荷、5%氯化钠负荷以及对照组。ZK 36 374通过皮下植入并连接到右颈静脉的渗透泵持续给药一周。泵植入24小时后，三个实验组的血压均下降。在第7天，除了氯化钠负荷的大鼠血压升高外，其他组血压维持在相似水平。在第15天，血压水平恢复到治疗前的值。治疗第7天，尿中前列腺素E2的值高于治疗前，在第15天恢复到治疗前水平。钠排泄在第7天增加，在第15天更高。治疗期间血浆肾素活性水平保持不变，除了Goldblatt 2k-1c组在第7天出现显著下降。治疗第1天所描述的所有变化可能与当天血压下降的对抗作用有关。
