Prasugrel pharmacokinetics and pharmacodynamics in subjects with moderate renal impairment and end-stage renal disease.

Objective: The pharmacokinetic (PK) and pharmacodynamic (PD) responses to prasugrel were compared in three studies of healthy subjects vs. those with moderate or end-stage renal impairment. Methods: Two of the three protocols were parallel-design, open-label, single dose (60-mg prasugrel) studies in...

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Published in:Journal of Clinical Pharmacy & Therapeutics Vol. 34; no. 5; pp. 585 - 595
Main Authors: Small DS, Wrishko RE, Ernest CS II, Ni L, Winters KJ, Farid NA, Li YG, Brandt JT, Salazar DE, Borel AG, Kles KA, Payne CD
Format: pictorial research tables/charts Journal Article
Published: Wiley-Blackwell Oct2009
Online Access:View this record in EBSCOhost
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      dt: Oct2009
      vid: 34
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      pub: Wiley-Blackwell
      place: Malden, Massachusetts
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        10.1111/j.1365-2710.2009.01068.x
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        atl: Prasugrel pharmacokinetics and pharmacodynamics in subjects with moderate renal impairment and end-stage renal disease.
      aug:
        au:
          Small DS
          Wrishko RE
          Ernest CS II
          Ni L
          Winters KJ
          Farid NA
          Li YG
          Brandt JT
          Salazar DE
          Borel AG
          Kles KA
          Payne CD
        affil: Eli Lilly and Company, Indianapolis, IN, USA.
      sug:
        subj:
          Kidney Diseases
          Kidney Failure, Chronic
          Platelet Aggregation Inhibitors Pharmacodynamics
          Platelet Aggregation Inhibitors Pharmacokinetics
          Adult
          Confidence Intervals
          Data Analysis Software
          Descriptive Statistics
          Female
          Funding Source
          Male
          Middle Age
          Human
          Adult: 19-44 years
          Middle Aged: 45-64 years
          Female
          Male
      ab: Objective: The pharmacokinetic (PK) and pharmacodynamic (PD) responses to prasugrel were compared in three studies of healthy subjects vs. those with moderate or end-stage renal impairment. Methods: Two of the three protocols were parallel-design, open-label, single dose (60-mg prasugrel) studies in subjects with end-stage renal disease (ESRD; n = 12) or moderate renal impairment ( n = 10) and matched healthy subjects with normal renal function ( n = 10). The third protocol was an open-label, single-dose escalation (5, 10, 30 and 60 mg prasugrel) study in subjects with ESRD ( n = 16) and matched healthy subjects with normal renal function ( n = 16). Plasma concentrations of prasugrel's active metabolite were determined and pharmacokinetic parameter estimates were derived. Maximum platelet aggregation (MPA) was measured by light transmission aggregometry using 20 [mu]m adenosine diphosphate as agonist. Results: Across all studies, prasugrel's Cmax and AUC0- t were 51% and 42% lower in subjects with ESRD than in healthy subjects. AUC0- t did not differ between healthy subjects and subjects with moderate renal impairment. The magnitude of change and time-course profiles of MPA was similar for healthy subjects compared with subjects with moderate renal impairment and those with ESRD. Prasugrel was well-tolerated in all subjects. Conclusion: There was no difference in pharmacokinetics or PD responses between subjects with moderate renal impairment and healthy subjects. Despite significantly lower exposure to prasugrel's active metabolite in subjects with ESRD, MPA did not differ between healthy subjects and those with ESRD.
      pubtype: Academic Journal
      doctype:
        pictorial
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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