Trandolapril: A Clinical Profile

Leeuw, Peter W. de

doi:10.1016/0895-7061(95)00192-1

Cited by 4 publications

(2 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…1,2 Being a prodrug, it is hydrolyzed in the liver to the active diacid metabolite trandolaprilat. [3][4][5][6] Published data of the elimination half-lives of trandolapril and trandolaprilat are in the range of 0.6-6 and 22.5-33.5 hours, respectively, at steady state. Therefore, trandolapril has the longest duration of action among the antihypertensive drugs developed so far.…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, trandolapril has the longest duration of action among the antihypertensive drugs developed so far. [3][4][5][6] Published data of the elimination half-lives of trandolapril and trandolaprilat are in the range of 0.6-6 and 22.5-33.5 hours, respectively, at steady state. 7,8 Excretion of trandolapril and its metabolites is about 33% renal and 66% in feces.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Comparative pharmacokinetics of trandolapril, its active metabolite, and verapamil in human plasma of Egyptian population using HPLC–MS/MS

Magdy

El‐Khatib

Hemdan

et al. 2018

Drug Testing and Analysis

View full text Add to dashboard Cite

Trandolapril and verapamil are commonly used antihypertensive drugs. However, there is a lack of available data on the change of their pharmacokinetics in patients with liver or kidney impairment and hence the need for dose adjustment. In this article, a high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and validated for the monitoring of trandolapril, its active metabolite trandolaprilat, and verapamil in human plasma of patients with renal impairment and/or liver insufficiency. The chromatographic separation was achieved on a Gemini C reversed phase column using a gradient elution mode with a run time of 10 minutes. The mobile phase consisted of a mixture of methanol and 2% acetic acid. The electrospray ionization MS/MS analysis was performed in multiple reaction monitoring (MRM) mode. The assay was validated as per Food and Drug Administration (FDA) guidelines for bioanalytical method validation and proved to be suitable for the determination of therapeutic drug levels in plasma. The inter-group changes in pharmacokinetic data were compared to that of healthy volunteers. The comparison showed a significant difference in the pharmacokinetic parameters between the studied groups. The presented results exhibit the benefits of the proposed assay as a validated analytical tool for the continuous drug monitoring.

show abstract

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Comparative pharmacokinetics of trandolapril, its active metabolite, and verapamil in human plasma of Egyptian population using HPLC–MS/MS

Magdy

El‐Khatib

Hemdan

et al. 2018

Drug Testing and Analysis

View full text Add to dashboard Cite

show abstract

T

Bruchhausen

Ebel

Hackenthal³

et al. 1999

Hagers Handbuch Der Pharmazeutischen Praxis

View full text Add to dashboard Cite

Pharmacokinetics, Pharmacodynamics, and Tolerability of Single and Multiple Doses of Trandolapril, an Effective Angiotensin-Converting Enzyme Inhibitor, in Healthy Chinese Subjects

Liu

et al. 2015

Eur J Drug Metab Pharmacokinet

View full text Add to dashboard Cite

Trandolapril is the pro-drug of trandolaprilat, a non-sulfhydryl angiotensin-converting enzyme inhibitor. This study was designed to assess the pharmacokinetics (PK), pharmacodynamics (PD), and tolerability of single and multiple doses of trandolapril in healthy Chinese subjects. Healthy subjects (six men and six women) were randomized into a single-dose, 3 × 3 crossover study (1-2-4 mg, 2-4-1 mg, and 4-1-2 mg), and a multiple-dose study (2 mg/day, 6 days). Serial blood and urine samples were collected after drug administration and analyzed using a validated LC-MS/MS method, and the trandolapril and trandolaprilat PK parameters were obtained. PD was evaluated by the changes in blood pressure and heart rates after dosing. Tolerability was assessed by monitoring adverse events, vital signs, ECGs, and changes in laboratory tests. In the single-dose study, trandolapril was absorbed rapidly, and peak plasma levels (C max, 1.57, 3.77, and 7.99 ng/mL) and AUCs (1.89, 3.46, and 6.47 ng/mL) were dose-dependent. The AUC0-∞ of trandolaprilat was dose-dependent, but in a non-linear fashion. The cumulative urine excretion of trandolapril and trandolaprilat was 5.51, 6.20, and 7.41 % for three doses, respectively. In the multiple-dose study, steady-state pharmacokinetics was observed; there was no trandolapril accumulation, but there was mild trandolaprilat accumulation (R = 1.67). Trandolapril was well tolerated. The most pronounced reductions in blood pressure were observed at 8 h after administration, which was later than T max. No orthostatic hypotension occurred. The pharmacokinetics and pharmacodynamics following single and multiple oral doses trandolapril in healthy Chinese subjects are similar to those observed in non-Chinese healthy subjects.

show abstract

Trandolapril: A Clinical Profile

Cited by 4 publications

References 15 publications

Comparative pharmacokinetics of trandolapril, its active metabolite, and verapamil in human plasma of Egyptian population using HPLC–MS/MS

Comparative pharmacokinetics of trandolapril, its active metabolite, and verapamil in human plasma of Egyptian population using HPLC–MS/MS

T

Pharmacokinetics, Pharmacodynamics, and Tolerability of Single and Multiple Doses of Trandolapril, an Effective Angiotensin-Converting Enzyme Inhibitor, in Healthy Chinese Subjects

Contact Info

Product

Resources

About