Document Detail


The effects of age and gender on the pharmacokinetics and pharmacodynamics in healthy subjects of the plasminogen activator, lanoteplase.
MedLine Citation:
PMID:  21545481     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
AIMS: To investigate the influence of age and gender on the intravenous pharmacokinetics and pharmacodynamics of the plasminogen activator, lanoteplase.
METHODS: Forty healthy subjects (10 each of young males, elderly males, young females and elderly females) received a single bolus 10 kU kg(-1) intravenous dose of lanoteplase. Plasma from blood serially collected for 24 h post-dose was analyzed for lanoteplase (antigen), fibrinogen, plasminogen and α2-antiplasmin concentrations, plasma plasminogen activation activity (PPAA) and rapid plasminogen activator inhibitor (PAI-1).
RESULTS: Lanoteplase mean total systemic clearance (CL(t)) values ranged from 1.9 to 2.8 l h(-1) and mean steady-state volume of distribution (V(ss)) values ranged from 12.3 to 15.6 l. Age-by-gender interactions were observed for lanoteplase CL(t) (P= 0.04), but no differences were observed for V(ss) or elimination half-life. Elderly females had a 27% lower mean CL(t) than young females (95% CI for the difference 0.17, 1.27 l h(-1)) and 32% lower CL(t) than elderly males (95% CI for the difference 0.15, 1.65 l h(-1)). PPAA AUC/dose values did not show an age-by-gender interaction. Haemostasis parameters indicated only a slight degree of systemic plasminogen activation.
CONCLUSIONS: Elderly females had a lower mean lanoteplase CL(t) than elderly males and young females. However, no difference was observed between young and elderly females for the AUC/dose of PPAA. In addition, there were no age-related or gender-related differences observed in the other pharmacodynamic parameters measured.
Authors:
Nimish N Vachharajani; Ralph H Raymond; Wen-Chyi Shyu; Bruce C Stouffer; David W Boulton
Publication Detail:
Type:  Clinical Trial; Journal Article    
Journal Detail:
Title:  British journal of clinical pharmacology     Volume:  72     ISSN:  1365-2125     ISO Abbreviation:  Br J Clin Pharmacol     Publication Date:  2011 Nov 
Date Detail:
Created Date:  2011-10-12     Completed Date:  2012-02-09     Revised Date:  2013-05-24    
Medline Journal Info:
Nlm Unique ID:  7503323     Medline TA:  Br J Clin Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  775-86     Citation Subset:  IM    
Copyright Information:
© 2011 Bristol-Myers Squibb, Co. British Journal of Clinical Pharmacology © 2011 The British Pharmacological Society.
Affiliation:
Bristol-Myers Squibb Research and Development, Princeton, New Jersey 08543-4000, USA.
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MeSH Terms
Descriptor/Qualifier:
Adult
Age Factors
Aged
Analysis of Variance
Area Under Curve
Blood Coagulation / drug effects*
Dose-Response Relationship, Drug
Female
Humans
Male
Middle Aged
Plasminogen Activators / pharmacokinetics*,  pharmacology
Sex Factors
Tissue Plasminogen Activator / pharmacokinetics*,  pharmacology
Young Adult
Chemical
Reg. No./Substance:
153484-31-2/SUN 9216; EC 3.4.21.-/Plasminogen Activators; EC 3.4.21.68/Tissue Plasminogen Activator
Comments/Corrections

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