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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Nucleoside and nucleotide reverse transcriptase inhibitors
abacavir
J05AF06
Forms & Strengths
- Oral solution: 20 mg/mL
- Tablet: 300 mg
Adult Dosing
- 300 mg orally twice daily or 600 mg orally once daily
- Can be taken with or without food
Pediatric Dosing
- Pediatric patients 3 months to <16 years: 8 mg/kg orally twice daily (maximum 300 mg twice daily)
- Alternatively, weight-based once-daily dosing up to 600 mg daily may be used
Indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents
Mechanism of Action
- Nucleoside reverse transcriptase inhibitor (NRTI)
- Competes with natural triphosphate substrates to inhibit HIV-1 reverse transcriptase, causing chain termination and halting viral DNA synthesis
Contraindications
- Presence of HLA-B*5701 allele
- Prior hypersensitivity reaction to abacavir
- Moderate to severe hepatic impairment (Child-Pugh Class B or C)
Adverse Reactions
- Hypersensitivity reaction (potentially fatal)
- Lactic acidosis and severe hepatomegaly with steatosis
- Nausea, headache, fatigue, insomnia, vomiting
- Elevated liver enzymes
Drug Interactions
- Alcohol: increases abacavir AUC by 41% and prolongs elimination half-life
- Methadone: minor decrease in methadone levels, may require dosage adjustment for methadone
- Riociguat: potential increased exposure of riociguat via CYP3A/P-gp inhibition
Curated Content: Needs Vetting Before Put to Clinical Use