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Abacavir
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DRUG INFO
Abacavir
Drug Name:
Abacavir
Indication: For the treatment of HIV-1 infection, in combination with other antiretroviral agents
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.
Drug Category: Anti-HIV Agents; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors; ATC:J05AF06
Brand Names/Synonyms: 1592U89; ABC; Abacavir; Abacavir [Inn]; Ziagen
Dosage Forms: SOLUTION; TABLET
Absorption: Rapid and extensive after oral administration (83% bioavailability)
Interactions:
DrugBank: Interactions for Abacavir
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.
Chemical IUPAC Name: [4-(2-amino-6-cyclopropylamino-9H-purin-9-yl)-1-cyclopent-2-enyl]methanol
Chemical Formula: C14H18N6O
Half Life: 1.5 hours
Drug Type: Approved Drug
# Accession No: APRD00216
CAS Registry Number: 136470-78-5
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Abacavir News
(When available)
AHF Asks Medi-Cal to Place Restrictions on Glaxo AIDS Drug ... 05 Jan 2006
Yahoo! News (press release) ...the NIH suspended part of a three-arm, two-year government sponsored AIDS Clinical Trials Group Study (ACTG 5095) comparing AZT+3TC+abacavir (the components of ...
Tenofovir and Abacavir Similarly Beneficial for Treatment-Related ... Dec 19, 2005
DG News WASHINGTON, DC -- December 19, 2005 -- Switching from a thymidine analog to either tenofovir disoproxil fumarate (Viread) or abacavir (Ziagen) will equally ...
Limb gat gains lower when switching from AZT to abacavir or ... Dec 15, 2005
Aidsmap, People switching from AZT- (zidovudine, Retrovir) containing anti-HIV regimens to either tenofovir- (Viread) or abacavir- (Ziagen) containing regimens are ...
Co-Administration of Combination Tablet and Tenofovir Elucidates ... Dec 22, 2005
DG News DC -- December 22, 2005 -- When HIV develops resistance to the combination antiretroviral drug Trizivir (zidovudine + lamivudine + abacavir) and tenofovir ...
Combination HIV Drug Trizivir, Along with Tenofovir, Well ... Dec 22, 2005
DG News The combination tablet contains 300 mg of abacavir (Ziagen), 300 mg of zidovudine (Retrovir), and 150 mg of lamivudine (Epivir). ...
Kivexa available on PBS Dec 7, 2005
NAPWA, Kivexa, a new single-pill combination of the antiviral drugs abacavir (Ziagen) and lamivudine (3TC) became available for S100 prescription from 1 December. ...
Government drags its feet on patents for AIDS drugs Dec 26, 2005
Newindpress, ...any objections. The ARVs whose patents are awaiting include Abacavir, Combivir, Trizivir, Kaletra, Lexiva and Efavirenz. Combivir ...
Neurological side-effects of efavirenz mild and transient, study ... Dec 12, 2005
Aidsmap, A5095, a three-arm randomised, controlled study that was designed to compare the effects of first-line HIV treatment with efavirenz, abacavir (Ziagen) and ...
Unaffordable AIDS Drug Prices... Again Dec 11, 2005
Doctors Without Borders, For example, GlaxoSmithKline's price for abacavir in the poorest countries is about $ 890 per patient/year — this single drug costs four times more than the ...
ICAAC: Early trials involving new GSK protease inhibitor have ... Dec 19, 2005
Aidsmap, ...were treated with 300mg of 640385, boosted by 100mg of ritonavir twice daily in combination with two nucleoside analogues (excluding tenofovir and abacavir). ...
ICAAC: Switch from AZT or d4T to tenofovir may improve blood fat ... Jan 13, 2006
Aidsmap, Zerit) may show better improvements in blood fat levels when they switch to tenofovir (Viread) than when they switch to abacavir (Ziagen), according to the ...
Switching from AZT results in only slight reversal of lipoatrophy Dec 30, 2005
The Advocate, ...adults experiencing fat loss from their limbs experience a slight reversal of lipoatrophy when switching from AZT to either Viread or Ziagen, according to a ...
ICAAC: HCV only factor associated with liver problems in patients ... Jan 8, 2006
Aidsmap, ...copies/ml. The most frequently prescribed drugs were Kaletra (39%), efavirenz (Sustiva)(43%), and abacavir (Ziagen) (31%). A total ...
Co-Administration of Combination Tablet and Tenofovir Elucidates ... Dec 22, 2005
DG News The combination tablet Trizivir contains 300 mg of abacavir (Ziagen), 300 mg of zidovudine (Retrovir), and 150 mg of lamivudine (Epivir). ...
Tenofovir and Abacavir Similarly Beneficial for Treatment-Related ... Dec 19, 2005
DG News WASHINGTON, DC -- December 19, 2005 -- Switching from a thymidine analog to either tenofovir disoproxil fumarate (Viread) or abacavir (Ziagen) will equally ...
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