P - Contraindicated in pregnancy
L - Contraindicated in lactation
Abacavir is the most powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.
Rapidly absorbed after oral administration with an oral bioavailability of about 80%.
50% bound to plasma proteins. Crosses the blood brain barrier.
Undergoes intracellular metabolism to carbovir triphosphate which is the active metabolite.
Elimination half-life: About 1.5 hours after a single oral dose. Elimination by hepatic metabolism mainly by alcohol dehydrogenase and glucuronidation. The metabolites are excreted mainly in the urine.
Abacavir is converted to the active form carbovir triphosphate intracellularly. It competitively inhibits the reverse transcriptase of retroviruses interfering with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.
Anorexia, headache, nausea, vomiting, diarrhoea, rash, fever, cough, dyspnoea, fatigue, malaise, lethargy, abdominal pain. Pancreatitis and elevated blood glucose and TG concentrations.
Potentially Fatal: Severe hypersensitivity reactions.
May result in acute renal failure with rhabdomyolysis, coma and seizures.
Recovery after MI, elderly, CVS disease, liver impairment, epilepsy, psychosis, increased intraocular pressure, history of urinary retention, alcohol, pregnancy and lactation; avoid abrupt withdrawal.
Alcohol may cause decreased elimination of abacavir. Lactic acidosis with nucleoside analogues concomitantly. Decreased serum concentrations of methadone.
Drinking alcoholic beverages increases the level of abacavir in the blood, perhaps increasing the risk of side effects.
Adult: Combined with other antiretrovirals: 300 mg bid or 600 mg once daily.
Child: Combined with other antiretrovirals: >3 months: 8 mg/kg bid. Max: 600 mg daily.
Renal impairment: Avoid in end stage renal disease.
Hepatic impairment: Child pugh category A: 200 mg bid. Avoid in moderate-severe impairment.
May be taken with or without food.
Contraindicated in pregnancy.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
It is not known whether abacavir passes into breast milk. However, because of the possibility that this medicine could cause unwanted effects in nursing babies and the risk of passing HIV on to the infant, breast-feeding is not recommended.
This medicine has been tested in children of 3 months of age and older and, in effective doses, has not been shown to cause different side effects or problems than it does in adults.
There is no specific information comparing use of abacavir in the elderly with use in other age groups.
Moderate to severe renal and hepatic impairment; end stage renal disease; history of hypersensitivity reactions. Pregnancy and lactation.
Store at 20-25°C.
Store at 20-25°C.