基本氨苯蝶啶类似物二甲基氨基羟基丙氧基氨苯蝶啶的药效学和药代动力学。

Pharmacodynamics and pharmacokinetics of the basic triamterene analogue dimethylaminohydroxypropoxytriamterene.

作者信息

Priewer H, Kraft H, Mutschler E

出版信息

Arzneimittelforschung. 1985;35(11):1688-91.

Abstract

The diuretic, natriuretic and potassium retaining effects of dimethylaminohydroxypropoxytriamterene (RPH 2823), a basic triamterene derivative, were studied in male Wistar rats. Compared to triamterene (TA) RPH 2823 has a pronounced effect on urine volume and on the excretion of sodium; in addition it possesses a higher antikaliuretic potency than TA. In combination with furosemide, 2.5 mumol/kg RPH 2823 can avoid the kaliuresis of 25 mumol/kg furosemide. The pharmacokinetics of RPH 2823 after i.v. application of 1 mg/kg and 5 mg/kg were studied in female rats. The substance is not metabolized. RPH 2823 has a terminal elimination half-life of 3 h. About 47% of the given dose are excreted unchanged with urine. Furthermore, the volume of distribution VD beta and the total body clearance were calculated.

摘要

对一种碱性氨苯蝶啶衍生物二甲氨基羟基丙氧基氨苯蝶啶（RPH 2823）在雄性Wistar大鼠体内的利尿、利钠和保钾作用进行了研究。与氨苯蝶啶（TA）相比，RPH 2823对尿量和钠排泄有显著作用；此外，它的抗利尿作用比TA更强。与呋塞米联合使用时，2.5 μmol/kg的RPH 2823可避免25 μmol/kg呋塞米引起的利尿作用。在雌性大鼠中研究了静脉注射1 mg/kg和5 mg/kg剂量的RPH 2823后的药代动力学。该物质未被代谢。RPH 2823的终末消除半衰期为3小时。约47%的给药剂量以原形经尿液排泄。此外，还计算了分布容积VDβ和全身清除率。