LAMIVUDINE (lam-i-vu'deen) Epivir, Epivir-HBV, Heptovir Classifications: antiretroviral agent; nucleoside reverse transcriptase inhibitor (nrti); Therapeutic: antiretroviral; nrti Pregnancy Category: C
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Availability
100 mg, 150 tablets; 5 mg/mL, 10 mg/mL oral solution
Action
Lamivudine is a synthetic nucleoside analog reverse transcriptase inhibitor. It inhibits the transcription of the HIV viral
RNA chain, as well as the hepatitis B viral RNA chain.
Therapeutic Effect
Antiviral action is effective against HIV viruses and hepatitis B (HBV) viral infections.
Uses
HIV infection in combination with zidovudine; treatment of chronic hepatitis B.
Contraindications
Hypersensitivity to lamivudine, pregnancy (category C), lactation.
Cautious Use
Renal impairment, renal failure; diabetes mellitus, diabetes mellitus; obesity; children.
Route & Dosage
HIV Infection Adult: PO 150 mg b.i.d. Child (3 mo16 y): PO 4 mg/kg b.i.d. (max: of 150 mg b.i.d.)
Renal Impairment Clcr 3049 mL/min: 150 mg q.d.; 1529 mL/min: 150 mg first dose, then 100 mg q.d.; 514 mL/min: 150 mg first
dose, then 50 mg q.d.; <5 mL/min: 50 mg first dose, then 25 mg q.d.
Chronic Hepatitis B Adult: PO 100 mg q.d.
Renal Impairment Clcr 3049 mL/min: 100 mg first dose, then 50 mg q.d.; 1529 mL/min: 100 mg first dose, then 25 mg q.d.; 514
mL/min: 35 mg first dose, then 15 mg q.d.; <5 mL/min: 35 mg first dose, then 10 mg q.d.
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Administration
Oral
- Give Epivir b.i.d. in combination with AZT. The recommended dose for adults who weigh <50 kg (110 lb) is 2 mg/kg. Give Epivir-HBV
qd; do NOT give in combination with AZT.
- Store solution at 2°25° C (36°77° F) tightly closed.
Adverse Effects (≥1%)
CNS: Neuropathy, insomnia, sleep disorders,
dizziness, depression,
headache, fatigue,
fever, chills. GI: Nausea, diarrhea, vomiting, anorexia, abdominal pain, cramps, dyspepsia, increased LFTs (ALT, amylase),
hepatomegaly with steatosis. Hematologic: Neutropenia, anemia, thrombocytopenia.
Musculoskeletal: Myalgia, arthralgia, malaise, pain.
Skin: Rash.
Respiratory: Nasal symptoms, cough.
Metabolic: Lactic acidosis.
Interactions
Drug: Increases the C
max of
zidovudine. Trimethoprim-sulfamethoxazole increases serum levels of lamivudine. Increased risk of lactic acidosis in combination with other
reverse transcriptase inhibitors and
antiretroviral agents.
Pharmacokinetics
Absorption: Rapidly absorbed from GI tract (86% reaches systemic circulation).
Distribution: Low binding to plasma proteins.
Metabolism: Minimal.
Elimination: Excreted primarily unchanged in urine.
Half-Life: 24 h.
Nursing Implications
Assessment & Drug Effects
- Monitor children closely for S&S of pancreatitis; if they occur, immediately stop drug and notify physician.
- Lab tests: Monitor CBC with differential, kidney & liver function, and serum amylase throughout therapy.
- Monitor for and report all significant adverse reactions.
Patient & Family Education
- Report any of the following immediately: nausea, vomiting, anorexia, abdominal pain, jaundice.
- Note: The long-term effects of lamivudine are unknown.