Pharmacokinetics and safety of concentration-controlled oral zidovudine therapy

Edward P. Acosta, Keith Henry, Linda M. Page, Alejo Erice, Henry H. Balfour, Courtney V Fletcher

Research output: Contribution to journalArticle

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Abstract

Study Objective. To evaluate the pharmacokinetics, safety, and feasibility of concentration-controlled oral zidovudine therapy. Design. Randomized, crossover, open-label study. Setting. University-affiliated general clinical research center. Patients. Eight individuals infected with the human immunodeficiency virus with CD4+ lymphocyte counts of 100 cells/μl or greater. Intervention. During the 24-week study, patients received oral zidovudine regimens that consisted of a standard fixed dose of 500 mg/day and a concentration-controlled regimen designed to maintain a steady-state plasma concentration (C(ss)) of 0.187 ± 0.04 mg/L (0.7 ± 0.14 μM). Measurements and Main Results. The mean C(ss) during standard therapy was 0.170 ± 0.024 mg/L versus 0.205 ± 0.021 mg/L with the concentration-controlled regimen (p=0.025). Respective mean changes in hemoglobin were -0.02 g/dl (range - 0.9-0.9 g/dl) and -0.30 g/dl (range -1.5-0.4 g/dl, p=0.67). The absolute neutrophil count decreased 0.90 x 109/L during standard therapy and increased 0.40 x 109/L during concentration-controlled therapy (p=0.07). The regimens did not differ in toxicity. Conclusion. Concentration-controlled oral antiretroviral therapy with zidovudine is feasible and safe, and provides pharmacologic data to determine the regimen's virologic and immunologic benefits.

Original languageEnglish (US)
Pages (from-to)424-430
Number of pages7
JournalPharmacotherapy
Volume17
Issue number3
StatePublished - May 1 1997

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Zidovudine
Pharmacokinetics
Safety
Therapeutics
CD4 Lymphocyte Count
Hemoglobins
Neutrophils
HIV
Research

ASJC Scopus subject areas

  • Pharmacology (medical)

Cite this

Acosta, E. P., Henry, K., Page, L. M., Erice, A., Balfour, H. H., & Fletcher, C. V. (1997). Pharmacokinetics and safety of concentration-controlled oral zidovudine therapy. Pharmacotherapy, 17(3), 424-430.

Pharmacokinetics and safety of concentration-controlled oral zidovudine therapy. / Acosta, Edward P.; Henry, Keith; Page, Linda M.; Erice, Alejo; Balfour, Henry H.; Fletcher, Courtney V.

In: Pharmacotherapy, Vol. 17, No. 3, 01.05.1997, p. 424-430.

Research output: Contribution to journalArticle

Acosta, EP, Henry, K, Page, LM, Erice, A, Balfour, HH & Fletcher, CV 1997, 'Pharmacokinetics and safety of concentration-controlled oral zidovudine therapy', Pharmacotherapy, vol. 17, no. 3, pp. 424-430.
Acosta EP, Henry K, Page LM, Erice A, Balfour HH, Fletcher CV. Pharmacokinetics and safety of concentration-controlled oral zidovudine therapy. Pharmacotherapy. 1997 May 1;17(3):424-430.
Acosta, Edward P. ; Henry, Keith ; Page, Linda M. ; Erice, Alejo ; Balfour, Henry H. ; Fletcher, Courtney V. / Pharmacokinetics and safety of concentration-controlled oral zidovudine therapy. In: Pharmacotherapy. 1997 ; Vol. 17, No. 3. pp. 424-430.
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