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Abacavir
See also Nucleoside analogue reverse transcriptase inhibitors (NRTIs)
General information
Abacavir is a guanidine analogue that inhibits HIV reverse transcriptase. In vitro, its potency is similar to that of zidovudine, protease inhibitors, and dual nucleoside combinations. It reduces viral load and increases the CD4 count in HIV-infected patients. Viral resistance is not rapidly selected for, but cross-resistance has been shown to other analogues of cytosine and guanidine (didanosine, lamivudine, and zalcitabine).
Abacavir has good oral systemic availability and penetrates the nervous system. It does not interfere with drugs that are metabolized by liver microsomal cytochrome P450 [ ]. It has no other significant drug interactions and can be administered without food restrictions.
General adverse effects and adverse reactions
The adverse effects of abacavir that have been most often observed in clinical trials are fatigue, nausea and vomiting, abdominal pain, diarrhea, headache, rash, and dyspepsia [ , ]. Allergic reactions lead to withdrawal of therapy in about 3% of patients [ ]. These can be severe, and anaphylaxis has been reported after rechallenge in a patient with an apparent allergic reaction to abacavir [ ]. It is wise to avoid rechallenge when allergy is suspected [ ]. In one study nausea and vomiting occurred in 38–57% of patients, headache in 27–41%, malaise and fatigue in 28%, diarrhea in 18–23%, and weakness in 29% [ ]. There was also one case of agranulocytosis accompanied by a skin rash.
Drug studies
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