Trade Names:Ziagen- Tablets 300 mg- Solution, oral 20 mg/mL
Converted by cellular enzymes to carbovir triphosphate, which inhibits HIV-1 reverse transcriptase and interferes with DNA synthesis.
Rapidly and extensively absorbed. Bioavailability is 83% (tablets). C max is approximately 3 mcg/mL and AUC 0-12 is approximately 6.02 mcg•h/mL.
Vd after IV administration is approximately 0.86 L/kg. Plasma protein binding is approximately 50%.
Metabolized to inactive metabolites by alcohol dehydrogenase and glucuronyl transferase.
1.2% is excreted in the urine as abacavir; 81% as inactive metabolites; 16% is excreted in the feces. The half-life is approximately 1.54 h and Cl is approximately 0.8 L/h/kg (after IV administration).
No data.Hepatic Function Impairment
In mild hepatic function impairment (Child-Pugh score 5 to 6), AUC increased 89%, and half-life increased 58%.Children
Steady-state C max is 3.71 mcg/mL with a dosage of 8 mg/kg twice daily.
Treatment of HIV-1 in combination with other antiretroviral agents.
Moderate or severe hepatic function impairment; hypersensitivity to any component of the product.
PO 600 mg once daily or 300 mg twice daily in combination with other antiretroviral agents.Adolescents and Children 3 mo to 16 yr of age
PO 8 mg/kg twice daily (max, 300 mg twice daily) in combination with other antiretroviral agents.Hepatic Function Impairment
PO 200 mg twice daily in patients with mild hepatic function impairment (Child-Pugh score 5 to 6).
Store at controlled room temperature (68° to 77°F). Solution may be refrigerated, but do not freeze.
Increases exposure to abacavir by decreasing the elimination and prolonging the half-life.Methadone
Plasma levels of methadone may be decreased in some patients, reducing the therapeutic effect.
None well documented.
The following adverse reactions have been reported with use of abacavir in combination with 1 or more antiretroviral agent.
Headache (13%); fatigue/malaise (12%); dreams/sleep disorders (10%); headache/migraine (7%); depressive disorders, dizziness (6%); anxiety (5%).
Rashes (7%); erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).
Ear/nose/throat infection (5%).
Nausea (19%); nausea and vomiting (10%); diarrhea (7%); abdominal pain/gastritis/GI signs and symptoms (6%); vomiting (2%).
Hepatic steatosis, lactic acidosis (postmarketing).
Neutropenia (5%); thrombocytopenia (1%).
Drug hypersensitivity (9%); hypersensitivity reaction (8%).
Elevated CPK (8%); elevated ALT, elevated AST, hypertriglyceridemia (6%); hyperamylasemia (4%).
Redistribution/accumulation of body fat (postmarketing).
Musculoskeletal pain (6%).
Viral respiratory infection (5%); bronchitis, pneumonia (4%).
Fever and/or chills (9%).
WarningsFatal hypersensitivity reaction
Serious and sometimes fatal hypersensitivity reactions have been associated with abacavir. The hypersensitivity is a multi-organ syndrome. Discontinue abacavir as soon as a hypersensitivity reaction is suspected. Persons carrying the HLA-B*5701 allele are at increased risk of experiencing abacavir hypersensitivity. Prior to starting therapy, screening for the allele is recommended. Regardless of HLA-B*5701 status, permanently discontinue abacavir if hypersensitivity cannot be ruled out. Never restart abacavir or any other form of abacavir-containing product because more severe symptoms can occur within hours and may include life-threatening hypertension and death.Lactic acidosis and hepatomegaly
Lactic acidosis and severe hepatomegaly with steatosis, including death, have been reported with use of nucleoside analogues alone or in combination, including abacavir.
Category C .
Undetermined; however, HIV-infected mothers should not breast-feed.
Safety and efficacy not established in children younger than 3 mo of age.
Select dose with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function and comorbidity.
Redistribution/accumulation of body fat have been observed (eg, buffalo hump, peripheral/facial wasting, central obesity).
Has been reported.
Abacavir administration has been associated with an increased risk of MI.
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