Trade Names:Epivir- Tablets 150 mg- Tablets 300 mg- Solution, oral 10 mg/mL
Trade Names:Epivir-HBV- Tablets 100 mg- Solution, oral 5 mg/mLHeptovir (Canada)
Inhibits replication of HIV and hepatitis B virus (HBV).
C max is approximately 1.28 mcg/mL (single dose of 100 mg). T max is 0.5 to 2 h. Absolute bioavailability is approximately 87%.
Less than 36% protein bound. Vd is approximately 1.3 L/kg.
Metabolism of lamivudine is a minor route of elimination. The metabolite is trans-sulfoxide metabolite.
The majority is eliminated unchanged in the urine. Mean half-life is 5 to 7 h. Cl is approximately 398.5 mL/min.
AUC, C max , and half-life are increased. It is recommended that dosage be modified in these patients.Hepatic Function Impairment
Pharmacokinetics not altered by hepatic function impairment; therefore, dosage adjustment is not required.
In combination with other antiretroviral agents for the treatment of HIV infection.Epivir-HBV
Treatment of chronic hepatitis B associated with evidence of hepatitis B viral replication and active liver inflammation.
PO 150 mg twice daily or 300 mg once daily in combination with other antiretroviral agents.Children 3 mo to 16 yr of age
PO 4 mg/kg twice daily (max, 150 mg twice daily) in combination with other antiretroviral agents. Dosage adjustment needed in patients with renal function impairment.Chronic Hepatitis B ( Epivir-HBV )Adults
PO 100 mg/day. Safety and efficacy of treatment longer than 1 yr not established.Children 2 to 17 yr of age
PO 3 mg/kg/day (max, 100 mg/day). Safety and efficacy of treatment longer than 1 yr not established.Dosage Adjustments of Epivir in Renal Function ImpairmentAdults and Adolescents Epivir
Patients weighing 30 kg or more:CrCl 50 mL/min or more
PO 150 mg twice daily or 300 mg once daily.CrCl 30 to 49 mL/min
PO 150 mg once daily.CrCl 15 to 29 mL/min
PO 150 mg first dose, then 100 mg once daily.CrCl 5 to 14 mL/min
PO 150 mg first dose, then 50 mg once daily.CrCl less than 5 mL/min
PO 50 mg first dose, then 25 mg once daily.
No additional dosing is needed after routine (4-h) hemodialysis or peritoneal dialysis. There are insufficient data to recommend a specific dose adjustment in children with renal function impairment; however, a reduction in dose and/or an increase in the dosing interval should be considered.Dosage Adjustments of Epivir-HBV in Renal Function ImpairmentAdults Epivir-HBV CrCl at least 50 mL/min
PO 100 mg/day.CrCl 30 to 49 mL/min
PO 100 mg first dose, then 50 mg/day.CrCl 15 to 29 mL/min
PO 100 mg first dose, then 25 mg/day.CrCl 5 to 14 mL/min
PO 35 mg first dose, then 15 mg/day.CrCl less than 5 mL/min
PO 35 mg first dose, then 10 mg/day.
Store Epivir oral solution at 77°F and tablets at controlled room temperature (59° to 86°F). Keep oral solution tightly closed. Store Epivir-HBV tablets between 59° and 86°F and oral solution between 68° and 77°F. Keep containers tightly closed.
Lamivudine Cl may be reduced, increasing plasma concentrations.Interferon- and ribavirin-based regimens
Risk of hepatic decompensation may be increased.Zalcitabine
Lamivudine and zalcitabine may inhibit the intracellular phosphorylation of one another. Use in combination is not recommended.
None well documented.
Unless otherwise stated, the following adverse reactions were reported in patients receiving lamivudine in combination with zidovudine for HIV infection or during postmarketing.
Headache (35%); fatigue and malaise (27%); neuropathy (12%); insomnia and other sleep disorders (11%); dizziness (10%); depression (9%); paresthesia, peripheral neuropathy (postmarketing).
Skin rash (9%); alopecia, pruritus (postmarketing).Children
Ear, nose, throat infection (for HBV treatment) (25%); nasal signs and symptoms (20%); sore throat (for HBV treatment) (13%).Children
Nasal discharge or congestion (8%); ear signs or symptoms including discharge, erythema, pain, swelling (7%).
Nausea (33%); diarrhea (18%); nausea and vomiting (13%); anorexia and/or decreased appetite (10%); abdominal pain (9%); abdominal cramps (6%); dyspepsia (5%); pancreatitis, stomatitis (postmarketing).Children
Diarrhea, nausea and vomiting (8%); stomatitis (6%); splenomegaly (5%).
Anemia, lymphadenopathy, splenomegaly (postmarketing).Children
Hepatic steatosis, lactic acidosis, posttreatment exacerbation of hepatitis B (postmarketing).Children
Anaphylaxis, urticaria (postmarketing).
Decreased absolute neutrophil count (ANC), hemoglobin, and platelets; increased ALT, amylase, AST, CPK, and bilirubin.Children
Decreased ANC, hemoglobin, and platelets; increased ALT, AST, lipase, and total amylase.
Hyperglycemia, redistribution/accumulation of body fat (postmarketing).
Musculoskeletal pain (12%); myalgia (8%); arthralgia (5%; for HBV treatment, 7%); muscle weakness, rhabdomyolysis (postmarketing).
Cough (18%); abnormal breath sounds/wheezing (postmarketing).Children
Cough (15%); abnormal breath sounds/wheezing (7%).
Fever and chills (10%); weakness (postmarketing).Children
Lactic acidosis with hepatomegaly and steatosis (including fatal cases) has been reported with the use of lamivudine alone or in combination.
Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued lamivudine.
Monitor hepatic function closely with both clinical and laboratory follow-up for at least several months after stopping lamivudine. Monitor patients being treated for chronic hepatitis B for loss of therapeutic response, which may affect advisability of continuing therapy.
Category C .
Excreted in breast milk. HIV-infected mothers should not breast-feed their infants.
Safety and efficacy in children younger than 2 yr of age not established.Epivir HIV infection
Safety and efficacy in children younger than 3 mo of age not established.
Select dose with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Dosage adjustment recommended.
Lamivudine should not be used in combination with other lamivudine- or emtricitabine-containing products.
Accumulation/redistribution of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance,” has occurred in patients receiving antiretroviral therapy. A causal relationship has not been established.
Has occurred in HIV/hepatitis C virus coinfected patients receiving combination antiretroviral therapy for HIV and interferon alfa with or without ribavirin. Closely monitor patients for treatment-associated toxicities.
Epivir-HBV tablets and oral solution contain a lower dose of the same active ingredient as Epivir tablets and oral solution (and lamivudine/zidovudine tablets used to treat HIV infection). The formulation and dosage of lamivudine in Epivir-HBV are not appropriate for patients infected with HBV and HIV.
Reported in patients receiving lamivudine, particularly in HIV-infected children with prior nucleoside exposure.
In non–HIV-infected patients treated with lamivudine for chronic hepatitis B, clinical and laboratory evidence of exacerbations of hepatitis have occurred after discontinuing lamivudine.
In non–HIV-infected patients treated with lamivudine for chronic hepatitis B, emergence of lamivudine-resistant HBV has been detected and has been associated with diminished treatment response.
Data are limited. No signs or symptoms have been noted in the few cases of overdosage reported.
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