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Zidovudine
drug data and news
Zidovudine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Zidovudine | ||
| Brand Names/Synonyms | AZT; Apo-Zidovudine; Azidothymidine; Aztec; Combivir; Compound S; Novo-Azt; Retrovir; Trizivir; ZIDOVUDINE EP III; Zidovudine | ||
| Indication | For the treatment of Human immunovirus (HIV) infections | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Zidovudine News (When available) |
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| Dosage Forms | CAPSULE; LIQUID; SYRUP; TABLET | ||
| Drug_Category | Anti-HIV Agents; Antimetabolites; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors; ATC:J05AF01 | ||
| 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. | ||
| Toxicity | LD50=3084 mg/kg (orally in mice) | ||
| Organisms Affected | Human immunodeficiency virus | ||
| Chemical IUPAC Name | 1-[4-azido-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-methyl-1H-pyrimidine-2,4-dione | ||
| Chemical Formula | C10H13N5O4 | ||
| Molecular Weight | 267.242 g/mol | ||
| Smiles String | CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-] | ||
| Melting Point | 106-112 oC | ||
| Water Solubility | 1-5 g/100 mL at 17 C | ||
| State | Solid | ||
| LogP/Hphobicity | 0.05 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 0.5-3 hours | ||
| Protein Binding [%] | 30-38% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ret1375.shtml http://www.drugs.com/cons/Zidovudine.html http://www.rxlist.com/cgi/generic3/zidovud.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00449 | ||
| CAS Registry Number | 30516-87-1 | ||
| KEGG Compound ID | C07210 | ||
| PubChem ID | SID:332180 | ||
| PharmGKB ID | Not Available | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 1946323 |
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