Abacavir Sulfate information from DrugsUpdate
P - Contraindicated in pregnancy
L - Caution when used during lactation
Abacavir is a nucleoside analog which inhibits reverse transcriptase enzyme and interferes with DNA synthesis mainly used to treat HIV and AIDS.
Pharmacokinetics
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.
Absorption
Rapidly and extensively absorbed. Bioavailability is 83% (tablets).
Distribution:
50% bound to plasma proteins.
Metabolism
Metabolized to inactive metabolites by alcohol dehydrogenase and glucuronyl transferase.
Elimination
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 hour.
Abacavir Sulfate Indications / Abacavir Sulfate Uses
Information not available.
Abacavir Sulfate Adverse Reactions / Abacavir Sulfate Side Effects
Mainly hypersensitivity reactions symptoms include fever, skin rash, fatigue; gastrointestinal symptoms such as nausea, vomiting, diarrhea or abdominal pain and respiratory symptoms such as pharyngitis, dyspnea or cough.
Precautions
Overdosage
May result in acute renal failure with rhabdomyolysis, coma and seizures.
Special Precautions
Special Precautions
Recovery after MI, elderly, CVS disease, liver impairment, epilepsy, psychosis, increased intraocular pressure, history of urinary retention, alcohol, pregnancy and lactation; avoid abrupt withdrawal.
Other Drug Interactions
Alcohol may cause decreased elimination of abacavir. Lactic acidosis with nucleoside analogues concomitantly. Decreased serum concentrations of methadone.
Other Interactions
Drinking alcoholic beverages increases the level of abacavir in the blood, perhaps increasing the risk of side effects.
Dosage
Adults
PO 600 mg once daily or 300 mg twice daily in combination with other antiretroviral agents.
Adolescents and Children
PO 8 mg/kg twice daily (max, 300 mg twice daily) in combination with other antiretroviral agent
Hepatic Impairment
PO 200 mg twice daily in patients with mild hepatic function impairment.
Food(before/after)
May be taken with or without food.
List of Contraindications
Abacavir Sulfate and Pregnancy
Contraindicated in pregnancy.
Abacavir Sulfate and Lactation
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.
Abacavir Sulfate and Children
Safety and efficacy not established in children younger than 3 months of age.
Abacavir Sulfate and Geriatic
There is no specific information comparing use of abacavir in the elderly with use in other age groups.
Abacavir Sulfate and Other Contraindications
Moderate or severe hepatic function impairment; hypersensitivity to any component of the product.
Storage
Store at 20-25°C. Solution may be refrigerated, but do not freeze.
Lab interference
Store at 20-25°C. Solution may be refrigerated, but do not freeze.
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