Abacavir (Ziagen)
Carbocyclic nucleoside reverse transcriptase inhibitor (NRTI) used as part of combination antiretroviral therapy for HIV-1. Typical dose 600 mg PO once daily or 300 mg twice daily. Plasma half-life is short (~1.5h), but the active intracellular anabolite carbovir-triphosphate has a prolonged intracellular half-life (~21h) permitting once-daily dosing. Oral bioavailability ~83%. Metabolized by alcohol dehydrogenase and glucuronidation (not CYP). CRITICAL: HLA-B*5701 genotyping is mandatory prior to initiation due to a potentially fatal hypersensitivity reaction in carriers.
Projected serum levels — 600 mg, once daily
Maintenance schedule: 600 mg once daily (oral).
Modeled steady state after ~1 days: peak ≈ 56.5 mg, trough ≈ 0.001 mg body load. Population-based estimate over 15 days for a 600 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Antiretroviral
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 1.5 h
- Common dose
- 600 mg
- Suggested maximum
- 600 mg/day
- Reference dose range
- 300–600 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 300 mg oral — Cmax 3 mg/L at 0.70 h
Documented interactions
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moderate
Carbamazepine (Tegretol) + Abacavir (Ziagen)
Carbamazepine (Tegretol) inducer of UGT predicted to change Abacavir (Ziagen) AUC by ~0.69x
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moderate
Phenytoin (Dilantin) + Abacavir (Ziagen)
Phenytoin (Dilantin) inducer of UGT predicted to change Abacavir (Ziagen) AUC by ~0.64x
-
moderate
Valproic Acid / Divalproex (Depakote) + Abacavir (Ziagen)
Valproic Acid / Divalproex (Depakote) reversible_inhibitor of UGT predicted to change Abacavir (Ziagen) AUC by ~1.65x
Serum checks 3 modeled interaction pairings for abacavir (ziagen) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Pharmacokinetics of abacavir and its unique metabolite, carbovir triphosphate, in HIV-infected adults
Clinical PK study defining abacavir plasma half-life (~1.5h) and long intracellular carbovir-TP half-life (~21h) supporting once-daily dosing.
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Pharmacokinetics, metabolism, and excretion of the antiretroviral agent abacavir (1592U89) in healthy volunteers
Mass-balance and metabolism study characterizing non-CYP metabolism (ADH/UGT), oral bioavailability ~83%, and principal metabolite profile.
2 published studies referenced in the app, each with a plain-language summary.