Pharmacokinetics of intravenous and oral isosorbide - 5 - mononitrate.

Abstract:

:The pharmacokinetics of isosorbide-5-mononitrate (IS-5-MN) has been studied in two groups of healthy volunteers after oral (n = 20) and intravenous (n = 11) administration of 20 mg, which had previously been proved to be as effective as 20 mg sustained-release isosorbide dinitrate (ISDN). IS-5-MN in serum was measured by gas chromatography using capillary columns. The kinetic calculations were carried out with a newly developed model, which assumes a virtual volume of distribution dependent on time. IS-5-MN is rapidly (invasion half-life 4.1 min) and completely absorbed from the gastro-intestinal tract without any first pass metabolism. The maximum concentration of 480 micrograms/l was reached 1.2 h after oral administration of 20 mg. The substance was distributed throughout the total body water (distribution coefficient: 0.62), and was eliminated with a terminal t1/2 of 4.1 and 4.6 h after oral and intravenous administration, respectively. Total body clearance was 115ml/min. Thus, IS-5-MN is unlike ISDN with respect to the absence of first-pass metabolism and an 8-times longer half-life. The consequences for therapy are discussed.

journal_name

Eur J Clin Pharmacol

authors

Abshagen U,Betzien G,Endele R,Kaufmann B

doi

10.1007/BF00618777

subject

Has Abstract

pub_date

1981-01-01 00:00:00

pages

269-75

issue

4

eissn

0031-6970

issn

1432-1041

journal_volume

20

pub_type

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