Abacavir
sulfate
Abacavir sulfate (Ziagen)
Abacavir sulfate
(uh-BACK-ah-veer)
Pregnancy Category:
C Ziagen (Rx)
Classification: Antiviral, antiretroviral
drug
See Also: See also Antiviral
Drugs.
Action/Kinetics: Synthetic nucleoside
analog. Converted intracellularly to the active carbovir triphosphate.
Carbovir triphosphate inhibits the activity of HIV-1 reverse
transcriptase by competing with the natural substrate deoxyguanosine-5'-triphosphate
and by incorporation into viral DNA. The lack of a 3'-OH group
in the incorporated nucleoside analog prevents the formation
of the 5' to 3' phosphodiester linkage essential for DNA chain
elongation. Thus, viral DNA growth is terminated. Cross resistance
in vitro has been seen to lamivudine, didanosine, and zalcitabine.
Rapidly absorbed after PO use. Metabolized in the liver and
excreted in both the urine and feces.
Uses: In combination with other
antiretroviral drugs (e.g., lamivudine and zidovudine) to
treat HIV-1 infection. Do not add as a single agent when antiretroviral
regimens are changed due to loss of virologic response.
Special Concerns: Fatal hypersensitivity
reactions are possible (See Side Effects). Efficacy
for long-term suppression of HIV RNA or disease progression
have not been determined. Abacavir is not a cure for HIV infection;
clients may continue to show illnesses associated with HIV
infection, including opportunistic infections. The drug has
not been shown to reduce the risk of transmission of HIV to
others through sexual contact or blood. Use with caution with
liver disease.
Side Effects: Hypersensitivity:
Fever, skin rash, fatigue, N&V;, diarrhea, abdominal pain,
malaise, lethargy, myalgia, arthralgia, edema, SOB, paresthesia,
lymphadenopathy, conjunctivitis, mouth ulcerations, maculopapular
or urticarial rash life-threatening hypotension,
liver failure, renal failure, death. GI:
N&V;, diarrhea, loss of appetite, pancreatitis. Miscellaneous:
Severe hepatomegaly with steatosis (may be fatal), lactic
acidosis, pancreatitis, insomnia, other sleep disorders, headache,
fever, skin rashes.
Laboratory Test Alterations:
 LFTs,
CPK, GGT, creatinine, glucose, triglycerides. Lymphopenia,
anemia, neutropenia.
Drug Interactions: Ethanol 
excretion of abacavir 
exposure.
How Supplied: Oral Solution:
20 mg/mL; Tablets: 300 mg
Dosage
•Oral Solution, Tablets Treat HIV-1 infection.
Adults: 300 mg b.i.d. with other antiretroviral drugs.
Pediatric, 3 months to 16 years: 8 mg/kg b.i.d., not
to exceed 300 mg b.i.d., in combination with other antiretroviral
drugs. |
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