BACKGROUND Anemia is the main concern among patients using a zidovudine (AZT)-based antiretroviral treatment (ART). Some studies suggested weight-adjusted AZT dosing as a way to reduce toxicity. We analyzed the risk factors associated with AZT-induced anemia in a cohort using AZT as substitution for stavudine (D4T). METHODS We retrospectively studied HIV-infected patients in a referral hospit...

3'-Azido-3'-deoxythymidine (AZT) is a drug of choice for the treatment of AIDS. On the basis of pharmacokinetic data, the nonhuman primate Macaca nemestrina has been shown to be a suitable animal model for use in the study of the disposition of AZT. However, since AZT is activated to its metabolite, the AZT triphosphate (AZTTP), intracellularly, we investigated the intracellular activation of A...

At present, 3'-azido-3'-deoxythymidine (AZT; zidovudine) remains the drug of choice for initiating AIDS therapy. This drug in itself is inactive; it needs to be converted intracellularly by a series of cellular kinases to AZT 5'-triphosphate (AZT-TP) to exert antiviral activity. The purpose of this study was to examine the in vivo disposition of the phosphorylated AZT anabolites in different ta...

The pharmacokinetics of two prodrugs of zidovudine (AZT), 1,4-dihydro-1-methyl-3-[(pyridylcarbonyl)oxy] ester and isoleucinyl ester (DPAZT and IAZT, respectively), were investigated in a rabbit model to determine their potential utility as drugs against human immunodeficiency virus. Drugs were administered by intravenous infusion over 5 min at doses equal to 10 mg of AZT per kg of body weight. ...

Zidovudine (azidothymidine [AZT]) inhibits human immunodeficiency virus replication and reduces the severity of acquired immunodeficiency syndrome. A limiting side effect ofAZT is a mitochondrial cardiac and skeletal myopathy in which the pharmacologically active derivative ofAZT (AZT triphosphate) plays a critical role. The present study determined biochemical mechanisms of AZT-induced mitocho...

Zidovudine (AZT) lowers the perinatal transmission of HIV but can impair mitochondrial function by depleting mitochondrial DNA (mtDNA). AZT therapy and perinatal nutritional deprivation affect the body fat distribution, which influences glucose tolerance. We sought to model intrauterine exposure to AZT in humans to determine whether it interacts with low-protein diet (LPD) to impact on birth we...

Human immunodeficiency virus type 1 (HIV-1) strains were isolated from nine patients before and after prolonged therapy with either an alternating regimen of 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (ddC) (AZT/ddC) or 2',3'-dideoxyinosine (ddI) alone. All strains obtained from four patients who received AZT/ddC for up to 41 mo were highly insensitive to AZT in vitro. Only one ...