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Abacavir
drug data and news
Abacavir 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 | Abacavir | ||
| Brand Names/Synonyms | 1592U89; ABC; Abacavir; Abacavir [Inn]; Ziagen | ||
| Indication | For the treatment of HIV-1 infection, in combination with other antiretroviral agents | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Abacavir is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Abacavir 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 | Abacavir is a carbocyclic synthetic nucleoside analogue. Intracellularly, Abacavir is converted by cellular enzymes to the active metabolite carbovir triphosphate, an analogue of deoxyguanosine-5'-triphosphate (dGTP). Carbovir triphosphate inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. | ||
| Abacavir News (When available) |
Research Needs State, Corporate Support 06 Mar 2006 CROI: abacavir may be safer than nevirapine in Africans Feb 8, 2006 CROI: abacavir gene testing reveals high levels of ... Feb 14, 2006 CROI: early vs delayed Trizivir in TB/HIV coinfected - no ... Mar 2, 2006 Advances in First-Line and "Switch" Antiretroviral Strategies for ... Feb 2, 2006 AIDS: Help the victims Feb 25, 2006 Global Challenges | Clinton Foundation To Help Train Nurses in ... Feb 22, 2006 CROI: Risk of new illnesses declines sharply after first 2 months ... Feb 10, 2006 CROI: Lipodystrophy stable in children on HIV treatment and does ... Feb 23, 2006 CROI: AZT, 3TC and FTC achieve good concentrations in the female ... Feb 17, 2006 AHF Applauds Idaho Medicaid for Placing Restrictions on Glaxo AIDS ... Feb 23, 2006 Add new comment Feb 15, 2006 Simplified treatment regimens show promise in HIV-infected ... Feb 6, 2006 CROI: Tenofovir and kidney toxicity - low rates seen, but some ... Feb 9, 2006 CROI News Feature: Experts divided over the future of treatment ... Feb 9, 2006 4-Day-A-Week Treatment Plan for HIV Infected Adolescents Feb 18, 2006 | ||
| Dosage Forms | SOLUTION; TABLET | ||
| Drug_Category | Anti-HIV Agents; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors; ATC:J05AF06 | ||
| Absorption | Rapid and extensive after oral administration (83% bioavailability) | ||
| Interactions |
-->Interactions for Abacavir: Pharmacokinetic properties of abacavir were not altered by the addition of either lamivudine or zidovudine or the combination of lamivudine and zidovudine. No clinically significant changes to lamivudine or zidovudine pharmacokinetics were observed following concomitant administration of abacavir. Abacavir has no effect on the pharmacokinetic properties of ethanol. Ethanol decreases the elimination of abacavir causing an increase in overall exposure . The addition of methadone has no clinically significant effect on the pharmacokinetic properties of abacavir. In a study of 11 HIV-infected patients receiving methadone-maintenance therapy (40 mg and 90 mg daily) with 600 mg of ZIAGEN twice daily (twice the currently recommended dose), oral methadone clearance increased 22% (90% CI 6% to 42%). This alteration will not result in a methadone dose modification in the majority of patients; however, an increased methadone dose may be required in a small number of patients. | ||
| Toxicity | Some myocardial degeneration has been noticed in rats and mice | ||
| Organisms Affected | Human immunodeficiency virus | ||
| Chemical IUPAC Name | [4-(2-amino-6-cyclopropylamino-9H-purin-9-yl)-1-cyclopent-2-enyl]methanol | ||
| Chemical Formula | C14H18N6O | ||
| Molecular Weight | 286.333 g/mol | ||
| Smiles String | C1CC1NC2=NC(=NC3=C2N=CN3C4CC(C=C4)CO)N | ||
| Melting Point | 165 °C | ||
| Water Solubility | 77 mg/mL (sulfate salt) | ||
| State | Solid | ||
| LogP/Hphobicity | 0.389 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic, by alcohol dehydrogenase and glucuronosyltransferase | ||
| Half Life | 1.5 hours | ||
| Protein Binding [%] | 49% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Abacavir.html http://www.rxlist.com/cgi/generic2/abavir.htm http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1527.shtml http://www.drugs.com/pdr/ABACAVIR_SULFATE.html | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00216 | ||
| CAS Registry Number | 136470-78-5 | ||
| KEGG Compound ID | C07624 | ||
| PubChem ID | SID:208126 | ||
| PharmGKB ID | PA448004 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2240358 |
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