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abacavir (Ziagen, ABC)

Indications: - HIV therapy, used in combination with Combivir - acceptable alternative for use during pregnancy [9] Contraindications: - HLA-B*5701 positive patients should not be prescribed abacavir due to risk of hypersensitivity Dosage: 300 mg PO BID Tabs: 300 mg. Adverse effects: 1) hypersensitivity (5%): a) fever, rash, lymphadenopathy, fatigue, GI symptoms b) generally observed within 1st 6 weeks of therapy c) may be fatal [2] 2) rash (less severe allergic reaction) - 30% 3) lactic acidosis [3] 4) serious, sometimes fatal hypersensitivity reactions [6] 5) associated with more cardiovascular deaths than tenofovir [7,8] Laboratory: - HLA-B*5701 allele testing [5] prior to administration - abacavir is not recommended for individuals with the HLA-B*5701 variant allele [10] - abacavir in body fluid - abacavir in amniotic fluid - abacavir in CSF - abacavir in cord blood - abacavir in serum/plasma Mechanism of action: 1) in vitro synergy with zidovudine (AZT), nevirapine (NVP), & amprenavir 2) in vitro additive or synergistic effect with didanosine (DDI), lamivudine (3TC), ritonavir (RTV), stavudine (d4T), zalcitabine (ddC)

Interactions

drug interactions drug adverse effects of antiretroviral agents

Related

Acquired Immuno-Deficiency Syndrome (HIV infection stage 3, AIDS)

General

nucleoside reverse transcriptase inhibitor (NRTI)

Properties

Database Correlations

PUBCHEM correlations

References

  1. Kaiser Permanente Northern California Regional Drug Formulary, Update 9/99
  2. Prescriber's Letter 7(12):68 2000
  3. Prescriber's Letter 9(8):47 2002
  4. Department of Veterans Affairs, VA National Formulary
  5. Guidelines for the use of Antiretroviral agents in HIV-1 infected adults and adolescents. DHHS Panel of Antiretriviral Guidelines for Adults and Adolescents - A Working Group of the Office of AIDS Research Advisory Council (ORAC) http://aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf (corresponding NGC guideline withdrawn March 2016)
  6. FDA MedWatch http://www.fda.gov/medwatch/safety/2008/safety08.htm#abacavir
  7. Martin A et al Simplification of antiretroviral therapy with tenofovir- emtricitabine or abacavir-lamivudine: A randomized, 96-week trial. Clin Infect Dis 2009 Nov 15; 49:1591. PMID: 19842973
  8. FDA MedWatch, 03/01/2011 Abacavir - Ongoing Safety Review: Possible Increased Risk of Heart Attack including Ziagen, Trizivir, and Epzicom http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm245190.htm
  9. Zuger A Use of Antiretroviral Drugs in Pregnancy. Physician's First Watch, April 22, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. 2014. AIDSinfo. Clinical Guidelines Portal. March 28, 2014. http://aidsinfo.nih.gov/Guidelines/HTML/3/perinatal-guidelines/0 (corresponding NGC guideline withdrawn March 2016)
  10. Clinical Pharmacogenetics Implementation Consortium (CPIC) guideline information for abacavir and HLA-B. https://www.pharmgkb.org/guideline/PA166104997

Component-of

abacavir/dolutegravir/lamivudine abacavir/lamivudine (Epzicom) abacavir/lamivudine/zidovudine (Trizivir)