Nucleoside reverse transcriptase inhibitor
Nucleoside reverse transcriptase inhibitor
Nucleoside reverse transcriptase inhibitor; obstructs RNA and DNA synthesis and inhibits viral reproduction. Used in combination with other anti-HIV drugs to reduce the viral load as low as possible and decrease the chance of further viral mutation. Thought to cross the blood–brain barrier and be effective in the treatment of HIV-related dementia. There are no long-term studies on the effectiveness of this drug.
Indications
Treatment of HIV-1 infection in combination with other antiretrovirals Contraindications and cautions
Contraindicated with life-threatening allergy or hypersensitivity to any component, moderate to severe hepatic impairment, lactation. Use cautiously with mild hepatic impairment, lactic acidosis, pregnancy. Available forms Tablets—300 mg; oral solution—20 mg/mL
Metabolism: Hepatic; T1/2: 1–2 hr
Distribution: Crosses placenta; may enter breast milk
Excretion: Urine, feces Adverse effects
CNS: Headache, weakness, malaise, fatigue, insomnia, dizziness, anxiety, depression Dermatologic: Rash GI: Diarrhea, nausea, anorexia, vomiting,dyspepsia, liver enzyme elevations, liver enlargement, risk of severe to fatal hepatomegaly Other: Severe hypersensitivity reactions (fever, malaise, nausea, vomiting, rash), severe to fatal lactic acidosis, fat redistribution, increased lipid levels, MI Interactions
Drug-drug Risk of severe toxic effects if combined with alcohol Nursing considerations
Assessment
History: Life-threatening allergy to any component, impaired hepatic or renal function, lactic acidosis, pregnancy, lactation Physical: T; affect, reflexes, peripheral sensation; R, adventitious sounds; bowel sounds, liver evaluation; LFTs, renal function tests Interventions
Administer with meals or a light snack if GI upset occurs. Black box
warning Monitor patient for signs of potentially fatal hypersensitivity reaction; give patient hypersensitivity reaction warning card provided by manufacturer. Advise patient to stop drug at first sign of reaction. Do not try the drug again if patient has a hyper- sensitivity reaction. Black box
warning Monitor patient for lactic acidosis and severe hepatomegaly; increased risk with other antivirals. Black box
warning Patients with HLA-B*5701 allele are at high risk for hypersensitivity reactions. Screening for HLA-B*5701 allele is recommended. Administer the drug concurrently with other anti-HIV drugs. Recommend the use of barrier contraceptives while on this drug.