BACKGROUND Lipoatrophy is known to be associated with stavudine as part of the treatment for HIV infection, but it is less clear if this serious side effect is also related to other nucleoside reverse transcriptase inhibitors like zidovudine. We aimed to determine whether zidovudine-sparing first-line antiretroviral therapy would lead to less lipoatrophy and other metabolic changes than zidovud...

Zidovudine was the first agent approved for treatment of HIV disease, and since its widespread availability in 1987, the pharmacokinetic disposition and clinical effects of ZDV have been extensively evaluated. In addition to its utility as a component of a multidrug combination regimen for the treatment of adult and pediatric HIV-1 infection, it is the only agent approved by the FDA for the pre...

Clinical benefit of zidovudine alone in the treatment of HIV infection wanes after several years, with decreasing CD4 1 cell numbers and increasing HIV RNA in plasma. To develop treatment strategies following prolonged zidovudine treatment, 92 subjects from the AIDS Clinical Trials Group (ACTG) 175 study after a median of 3.6 years of zidovudine monotherapy were randomized to treatment with sta...

Literature data on the properties of zidovudine relevant to waiver of in vivo bioequivalence (BE) testing requirements for the approval of immediate-release (IR) solid oral dosage forms containing zidovudine alone or in combination with other active pharmaceutical ingredients (APIs) are reviewed. Solubility, dissolution, and permeability data for zidovudine, along with its dosing schedule, ther...

Zidovudine is phosphorylated in both infected and uninfected cells to the monophosphate (MP) derivative by cellular thymidine kinase. Subsequent phosphorylation of zidovudine-MP to the diphosphate (DP), and then the triphosphate (TP) derivative is catalysed by cellular thymidylate kinase and non-specific kinases respectively. Zidovudine-TP acts as an inhibitor of and substrate for the viral rev...

The effect of zidovudine on plasma and genital human immunodeficiency virus type 1 (HIV-1) was determined in 42 antiretroviral-naive HIV-1-seropositive women in Nairobi. After 7 days of zidovudine treatment, HIV-1 RNA levels decreased by 0.5 to 1.1 log(10) in plasma and genital secretions. HIV-1 RNA half-life following zidovudine treatment was 4.7, 1.3, and 0.9 days in plasma, cervix, and vagin...

Prolonged, continuous, high-dose zidovudine administration to adult rodents is associated with the development of nonmetastasizing vaginal squamous tumors in 13 percent of female rodents (at estimated drug concentrations three and 24 times that of human therapeutic exposure in mice and rats, respectively) (1). In rodents, unmetabolized zidovudine is concentrated in urine with reflux into the va...

The development and validation of a simple and accurate method based on HPLC with ultraviolet detection for the quantification of zidovudine in rat plasma and its application to a pharmacokinetic study following a single intranasal dose zidovudine is described. Zidovudine was extracted from the plasma using a single-step deproteinization. Chromatographic separation of zidovudine from interferin...

OBJECTIVE To evaluate the effects of zidovudine therapy in patients with mildly symptomatic HIV infection using Q-TWiST (quality-adjusted: Time Without Symptoms and Toxicity). DESIGN Analysis of a previously reported multicenter, randomized, placebo-controlled clinical trial. SETTING Thirty-two AIDS Clinical Trial units. PATIENTS A total of 351 patients with mildly symptomatic HIV infecti...