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RETROVIR: profile and news
Treatment simplification appears clinically safe in children with ... May 11, 2006 Starting treatment with Kaletra involves greater risk of increased ... Apr 24, 2006 Aurobindo Pharma CB uses rare premium structure Apr 23, 2006 Long-term study plays down risk of brain problems in HIV-positive ... Apr 26, 2006 GSK turns to RFID to protect its AIDS drug Apr 21, 2006 Other information Indication For the treatment of Human immunovirus (HIV) infections Pharmacology Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Zidovudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. Mechanism Of Action Zidovudine, a structural analog of thymidine, inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Drug Category Anti-HIV Agents; Antimetabolites; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors; ATC:J05AF01 Brand Names/Synonyms AZT; Apo-Zidovudine; Azidothymidine; Aztec; Combivir; Compound S; Novo-Azt; Retrovir; Trizivir; ZIDOVUDINE EP III; Zidovudine Dosage Forms CAPSULE; LIQUID; SYRUP; TABLET Absorption Rapid and alomost complete absorption from the gastrointestinal tract. Interactions Interactions for Zidovudine: Antiretroviral Agents: Concomitant use of zidovudine with stavudine should be avoided since an antagonistic relationship has been demonstrated in vitro. Some nucleoside analogues affecting DNA replication, such as ribavirin, antagonize the in vitro antiviral activity of Zidovudine against HIV; concomitant use of such drugs should be avoided. Doxorubicin: Concomitant use of zidovudine with doxorubicin should be avoided since an antagonistic relationship has been demonstrated in vitro. Phenytoin: Phenytoin plasma levels have been reported to be low in some patients receiving Zidovudine, while in one case a high level was documented. However, in a pharmacokinetic interaction study in which 12 HIV-positive volunteers received a single 300-mg phenytoin dose alone and during steady-state zidovudine conditions (200 mg every 4 hours), no change in phenytoin kinetics was observed. Although not designed to optimally assess the effect of phenytoin on zidovudine kinetics, a 30% decrease in oral zidovudine clearance was observed with phenytoin. Overlapping Toxicities: Coadministration of ganciclovir, interferon-alpha, and other bone marrow suppressive or cytotoxic agents may increase the hematologic toxicity of zidovudine. Chemical IUPAC Name 1-[4-azido-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-methyl-1H-pyrimidine-2,4-dione Chemical Formula C10H13N5O4 Half Life 0.5-3 hours Drug Type Approved Drug # Accession No APRD00449 CAS Registry Number 30516-87-1 |
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