Literature DB >> 17535044

Multiple-Dose Pharmacokinetics of Delavirdine Mesylate and Didanosine in HIV-Infected Patients.

Gene D Morse1, Susan E Cohn, Mark J Shelton, Carol Greisberger, Steven R Cox, Andrew A Della-Coletta, William W Freimuth, Richard C Reichman.   

Abstract

BACKGROUND: Delavirdine is a non-nucleoside reverse transcriptase inhibitor with pH-dependent absorption characteristics that has received accelerated approval for the treatment of patients with HIV-1 infection. In a prior single-dose study concurrent administration of delavirdine mesylate and didanosine (buffered formulation) resulted in up to a 31% decrease in the area under the plasma delavirdine concentration versus time curve (AUC) compared with when both drugs were taken separately.
OBJECTIVE: To evaluate the interaction of these two agents at steady state. STUDY DESIGN AND PATIENTS: A total of 11 HIV-infected subjects who were previously stabilised on didanosine were enrolled into a randomised, open-labelled crossover study. Nine subjects continued to receive their prescribed dose and schedule of didanosine, with each dose of didanosine taken either together with or 1 hour after delavirdine mesylate (400mg every 8 hours). Pharmacokinetic studies at baseline, day 14 and day 28 were conducted and the plasma concentrations of delavirdine and didanosine were determined.
RESULTS: A lower delavirdine maximum plasma concentration (C(max)) [22.4 +/- 11 vs 35.5 +/- 17muM; p = 0.045] was noted when delavirdine and didanosine were taken together. However, no significant difference was noted for delavirdine AUC (114 +/- 56 muM.h compared with 153 +/- 79 muM.h [p = 0.181]). In addition, no differences were noted for didanosine pharmacokinetic parameters between treatments.
CONCLUSION: These data indicate that patients receiving didanosine and delavirdine as part of a combination regimen during long-term therapy can be instructed to take them together in an attempt to enhance adherence to treatment with both antiretroviral agents.

Entities:  

Year:  2003        PMID: 17535044     DOI: 10.2165/00044011-200323050-00002

Source DB:  PubMed          Journal:  Clin Drug Investig        ISSN: 1173-2563            Impact factor:   2.859


  16 in total

Review 1.  Delavirdine: clinical pharmacokinetics and drug interactions.

Authors:  J Q Tran; J G Gerber; B M Kerr
Journal:  Clin Pharmacokinet       Date:  2001       Impact factor: 6.447

2.  Competing drug-drug interactions among multidrug antiretroviral regimens used in the treatment of HIV- infected subjects: ACTG 884.

Authors:  C V Fletcher; E P Acosta; H Cheng; R Haubrich; M Fischl; R Raasch; C Mills; X J Hu; D Katzenstein; R P Remmel; R M Gulick
Journal:  AIDS       Date:  2000-11-10       Impact factor: 4.177

3.  In vitro protein-binding characteristics of delavirdine and its N-dealkylated metabolite.

Authors:  A J Chaput; R D'Ambrosio; G D Morse
Journal:  Antiviral Res       Date:  1996-10       Impact factor: 5.970

Review 4.  Clinical pharmacokinetics of non-nucleoside reverse transcriptase inhibitors.

Authors:  P F Smith; R DiCenzo; G D Morse
Journal:  Clin Pharmacokinet       Date:  2001       Impact factor: 6.447

5.  Efficacy and safety of delavirdine mesylate with zidovudine and didanosine compared with two-drug combinations of these agents in persons with HIV disease with CD4 counts of 100 to 500 cells/mm3 (ACTG 261). ACTG 261 Team.

Authors:  G H Friedland; R Pollard; B Griffith; M Hughes; G Morse; R Bassett; W Freimuth; L Demeter; E Connick; T Nevin; M Hirsch; M Fischl
Journal:  J Acquir Immune Defic Syndr       Date:  1999-08-01       Impact factor: 3.731

6.  ACTG 260: a randomized, phase I-II, dose-ranging trial of the anti-human immunodeficiency virus activity of delavirdine monotherapy. The AIDS Clinical Trials Group Protocol 260 Team.

Authors:  M F Para; P Meehan; J Holden-Wiltse; M Fischl; G Morse; R Shafer; L M Demeter; K Wood; T Nevin; N Virani-Ketter; W W Freimuth
Journal:  Antimicrob Agents Chemother       Date:  1999-06       Impact factor: 5.191

7.  Didanosine measurement by radioimmunoassay.

Authors:  M DeRemer; R D'Ambrosio; G D Morse
Journal:  Antimicrob Agents Chemother       Date:  1996-06       Impact factor: 5.191

8.  U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication.

Authors:  T J Dueweke; S M Poppe; D L Romero; S M Swaney; A G So; K M Downey; I W Althaus; F Reusser; M Busso; L Resnick
Journal:  Antimicrob Agents Chemother       Date:  1993-05       Impact factor: 5.191

9.  Simple, rapid and sensitive high-performance liquid chromatographic determination of delavirdine and its N-desisopropyl metabolite in human plasma.

Authors:  B A Staton; M G Johnson; J M Friis; W J Adams
Journal:  J Chromatogr B Biomed Appl       Date:  1995-06-09

10.  The binding of a novel bisheteroarylpiperazine mediates inhibition of human immunodeficiency virus type 1 reverse transcriptase.

Authors:  T J Dueweke; F J Kézdy; G A Waszak; M R Deibel; W G Tarpley
Journal:  J Biol Chem       Date:  1992-01-05       Impact factor: 5.157

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  1 in total

1.  Effect of Food on the Steady-State Pharmacokinetics of Delavirdine in Patients with HIV Infection.

Authors:  Gene D Morse; Margaret A Fischl; Mark J Shelton; Steve R Cox; Leslie Thompson; Andrew A Della-Coletta; William W Freimuth
Journal:  Clin Drug Investig       Date:  2003       Impact factor: 2.859

  1 in total

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