Drug Index

Abacavir

 
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Mechanism :

Abacavir is a carbocyclic synthetic nucleoside analogue. Abacavir is converted by cellular enzymes to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5’-triphosphate (dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Abacavir is also a weak inhibitor of cellular DNA polymerases (alpha, beta, and gamma).


Indication :

• HIV infection


Contraindications :

Contraindicated in patients with previously demonstrated hypersensitivity to abacavir or any other component of the products. Patients testing positive for the presence of the HLA-B*5701 allele are at a significantly increased risk for hypersensitivity reactions. Fatal rechallenge reactions have been associated with re-administration of abacavir to patients with a prior history of a hypersensitivity reaction to abacavir. Contraindicated in patients with moderate or severe hepatic impairment.


Dosing :

>3 months-18 years: 8 mg/kg BDS OR 16 mg/kg per day. Max: 300 mg BDS.


Adverse Effect :

Fever/chills, redistribution/accumulation of body fat, lactic acidosis, hepatic steatosis, rash, Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), erythema multiforme, insomnia, headache, malaise, fatigue, anxiety, depression, hyperglycemia, hypertriglyceridemia, nausea, vomiting, diarrhea, anorexia; pancreatitis (rare), asthenia, musculoskeletal pain, cough, thrombocytopenia, hypersensitivity reaction.


Interaction :

Ethanol: Decreases the elimination of abacavir causing an increase in overall exposure.
Ganciclovir-Valganciclovir: May enhance the adverse/toxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Hematologic toxicity is of specific concern.
Protease Inhibitors: May decrease the serum concentration of Abacavir.
Ribavirin: May enhance the hepatotoxic effect of Reverse Transcriptase Inhibitors (Nucleoside). Lactic acidosis may occur.


07/18/2019 12:05:09 Abacavir
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