Products
Abacavir is commercially available as film-coated tablets and as an oral solution (Ziagen, combination products). It has been approved in many countries since 1999. Generic versions are approved.
Structure and properties
Abacavir (C14H18N6O, Mr = 286.3 g/mol) is present in drugs, among other forms, as abacavir sulfate, a white crystalline powder that is soluble in water. It is a prodrug that is metabolized in cells to carbovir triphosphate, an analog of deoxyguanosine-5′-triphosphate (dGTP).
Effects
Abacavir (ATC J05AF06) has antiviral properties. The effects are due to inhibition of HIV reverse transcriptase, which transcribes viral RNA into DNA and has a central role in viral replication. Abacavir prevents the integration of viral DNA into the host cell genome.
Indications
For the treatment of HIV infection as part of combination antiretroviral therapy.
Dosage
According to the SmPC. Medicines are taken once or twice daily and independently of meals.
Contraindications
- Hypersensitivity
- Moderate to severe hepatic insufficiency
Full precautions can be found in the drug label.
Interactions
Abacavir is metabolized primarily by alcohol dehydrogenase and by glucuronidation and, unlike other HIV medications, does not interact with CYP450.
Adverse effects
The most common potential adverse effects include nausea, headache, feeling sick, fatigue, vomiting, and sleep disturbances. Abacavir can cause a life-threatening hypersensitivity reaction that affects multiple organs and is accompanied by fever and a rash.
