Trandolapril: pharmacokinetics of single oral doses in healthy male volunteers.

Abstract:

:The pharmacokinetics and dose proportionality of trandolapril, a new angiotensin-converting enzyme (ACE) inhibitor, were investigated in 12 healthy male volunteers in a four-way randomized crossover study over the therapeutic dose range, 0.5-4 mg. Trandolapril is rapidly absorbed, with a single elimination half-life (t1/2) of 0.72 h, irrespective of dose. Peak plasma levels (Cmax) occurred at 0.5 h and were proportional to the dose, as was the area under the plasma concentration-time curve (AUC). Concentration of the active metabolite (trandolaprilat) increased with increasing doses but in a nonlinear fashion, probably owing to saturable plasma ACE binding. However, the Cmax and AUC values for trandolaprilat were directly proportional to the highest doses, 2 and 4 mg, suggesting linear kinetics for the trandolaprilat, which is not bound to ACE. Trandolapril showed linear kinetics but trandolaprilat showed some features of nonlinear kinetics, particularly at low doses.

journal_name

J Cardiovasc Pharmacol

authors

Lenfant B,Mouren M,Bryce T,De Lauture D,Strauch G

subject

Has Abstract

pub_date

1994-01-01 00:00:00

pages

S38-43

eissn

0160-2446

issn

1533-4023

journal_volume

23 Suppl 4

pub_type

临床试验,杂志文章,随机对照试验
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  • Pentoxifylline Ameliorates Cardiac Fibrosis, Pathological Hypertrophy, and Cardiac Dysfunction in Angiotensin II-induced Hypertensive Rats.

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    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

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    doi:

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    更新日期:1994-06-01 00:00:00

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    pub_type: 杂志文章,评审

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  • Late INa Inhibition as an Antiarrhythmic Strategy.

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    pub_type: 杂志文章,评审

    doi:10.1097/FJC.0000000000000510

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  • Pharmacologic Prevention of Myocardial Ischemia-Reperfusion Injury in Patients with Acute Coronary Syndrome Undergoing Percutaneous Coronary Intervention.

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    doi:

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    更新日期:1995-01-01 00:00:00

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    pub_type: 临床试验,杂志文章,随机对照试验

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    pub_type: 临床试验,杂志文章,评审

    doi:

    authors: Seibold JR

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