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

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.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Acarbose
Acarbose may decrease the excretion rate of Abacavir which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Abacavir which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Acetaminophen
Acetaminophen may decrease the excretion rate of Abacavir which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Aclidinium
Abacavir may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine
Abacavir may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Abacavir which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Abacavir which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Abacavir which could result in a higher serum level.
Adenine
The metabolism of Abacavir can be decreased when combined with Adenine.
Adenovirus type 7 vaccine live
The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Abacavir.
Albutrepenonacog alfa
Abacavir may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
Alclofenac
Alclofenac may decrease the excretion rate of Abacavir which could result in a higher serum level.
Aldesleukin
Aldesleukin may decrease the excretion rate of Abacavir which could result in a higher serum level.
Allopurinol
Allopurinol may decrease the excretion rate of Abacavir which could result in a higher serum level.
Allylestrenol
Abacavir may decrease the excretion rate of Allylestrenol which could result in a higher serum level.
Almasilate
Abacavir may decrease the excretion rate of Almasilate which could result in a higher serum level.
Alminoprofen
Alminoprofen may decrease the excretion rate of Abacavir which could result in a higher serum level.
2 References
  1. 1 . Zucman D, Truchis Pd, Majerholc C, Stegman S, Caillat-Zucman S: Prospective screening for human leukocyte antigen-B*5701 avoids abacavir hypersensitivity reaction in the ethnically mixed French HIV population. J Acquir Immune Defic Syndr. 2007 May 1;45(1):1-3.PubMed: 17356469
  2. 2 . Link Link