Description

Simple

An antiviral medication used to treat HIV.

Clinical

An antiviral nucleoside reverse transcriptase inhibitor used in combination with other antiretrovirals for the treatment of HIV.

Overview

Abacavir (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. Chemically, it is a synthetic carbocyclic nucleoside and is the enantiomer with 1S, 4R absolute configuration on the cyclopentene ring. In vivo, abacavir sulfate dissociates to its free base, abacavir.

Pharmacology

Indication

For the treatment of HIV-1 infection, in combination with other antiretroviral agents.

Pharmacodynamic

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 a... Read more

Mechanism of action

Abacavir is a carbocyclic synthetic nucleoside analogue and an antiviral agent. 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 revers... Read more

Absorption

Rapid and extensive after oral administration (83% bioavailability, tablet). When a 300 mg tablet is given twice daily to subjects, the peak plasma concentration (Cmax) was 3.0 ± 0.89 mcg/mL and the area under the curve (AUC 0-12 hours) was 6.02 ± 1.73 mcg•hr/mL.

Protein binding

Moderate (approximately 50%). Binding of abacavir to plasma protein was independent of concentration.

Volume of distribution

0.86 ± 0.15 L/kg [IV administration]

Clearance

0.80 ± 0.24 L/hr/kg [asymptomatic, HIV-1-infected adult patients receiving single (IV dose of 150 mg]

Half life

1.54 ± 0.63 hours

Route of elimination

Elimination of abacavir was quantified in a mass balance study following administration of a 600-mg dose of 14C-abacavir: 99% of the radioactivity was recovered, 1.2% was excreted in the urine as abacavir, 30% as the 5′-carboxylic acid metabolite, 36% as the 5′-glucuronide metabolite, and 15% as uni... Read more

Toxicity

Some myocardial degeneration has been noticed in rats and mice. The most commonly reported adverse reactions of at least moderate intensity (incidence ≥10%) in adult HIV-1 clinical trials were nausea, headache, malaise and fatigue, nausea and vomiting, and dreams/sleep disorders. Serious hypersensit... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • adult
  • Kind: experimental
    • Percent: 19%
  • Kind: comparator
    • Percent: 17%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 13%
  • Kind: comparator
    • Percent: 9%
  • Clinical Trial
    Malaise US
    • adult
  • Kind: experimental
    • Percent: 12%
  • Kind: comparator
    • Percent: 12%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: 12%
  • Kind: comparator
    • Percent: 12%
  • Clinical Trial
    Rashes US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 12%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 11%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 11%
  • Clinical Trial
    Migraine US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 11%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Sleep Disorders US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Dreams US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Malaise US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: 2%
  • Kind: comparator
    • Percent: 9%
  • Clinical Trial
    Drug Hypersensitivity US
    • adult
  • Kind: experimental
    • Percent: 9%
  • Kind: comparator
    • Percent: <1%
  • Clinical Trial
    Chills US
    • pediatric
  • Kind: experimental
    • Percent: 9%
  • Kind: comparator
    • Percent: 7%
  • Clinical Trial
    Fever US
    • pediatric
  • Kind: experimental
    • Percent: 9%
  • Kind: comparator
    • Percent: 7%
  • Clinical Trial
    Vomiting US
    • pediatric
  • Kind: experimental
    • Percent: 9%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Nausea US
    • pediatric
  • Kind: experimental
    • Percent: 9%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Gastrointestinal signs and symptoms US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 8%
  • Clinical Trial
    Hypersensitivity Reaction US
    • adult
  • Kind: experimental
    • Percent: 8%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Gastritis US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 8%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 8%
  • Clinical Trial
    Severe drug hypersensitivity reaction US
    • adult
  • Kind: experimental
    • Percent: 8%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Musculoskeletal Pain US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: comparator
    • Percent: 7%
  • Clinical Trial
    Skin rashes US
    • pediatric
  • Kind: experimental
    • Percent: 7%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Depressive Disorders US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Vertigo US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Musculoskeletal Pain US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Fever US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Chills US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Depressive Disorders US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Bronchitis US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Pyrexia US
    • adult
  • Kind: experimental
    • Percent: 3-5%
  • Clinical Trial
    Anxiety US
    • adult
  • Kind: experimental
    • Percent: 3-5%
  • Clinical Trial
    Throat infection US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Viral respiratory infections US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Anxiety US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Renal signs US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Renal symptoms US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Nonspecific pain US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Skin rashes US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Ear Infection US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Nose infection US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Headache US
    • pediatric
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Pneumonia US
    • pediatric
  • Kind: experimental
    • Percent: 4%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Presence of HLA-B*5701 allele
        • Drugbank Id: DBCOND0108169
    • Regions: US
    • Patient Conditions:
        • Name: Severe Hepatic Impairment
        • Drugbank Id: DBCOND0070791
        • Modification Of:
          • Base:
            • Name: Heptic Impairment
            • Drugbank Id: DBCOND0072269
          • Severity:
            • Includes:
              • severe
    • Regions: US
    • Patient Conditions:
        • Name: Moderate Hepatic Impairment
        • Drugbank Id: DBCOND0045420
        • Modification Of:
          • Base:
            • Name: Hepatic Impairment
            • Drugbank Id: DBCOND0031585
          • Severity:
            • Includes:
              • moderate

    Food Interactions

    Avoid alcohol. Alcohol increases the systemic exposure to the drug.

    Take with or without food. The absorption is unaffected by food.