Dosing and uses of Epivir, Epivir HBV (lamivudine)
Adult dosage forms and strengths
tablet
- 100mg (Epivir HBV)
- 150mg (Epivir)
- 300mg (Epivir)
oral solution
- 5mg/mL (Epivir HBV)
- 10mg/mL (Epivir)
HIV Infection
Epivir: 300 mg PO qDay or 150 mg PO q12hr
Chronic Hepatitis B
Epivir HBV: 100 mg PO qDay
Renal Impairment
CrCl ≥ 50 mL/min: 150 mg PO q12hr or 300 mg PO qDay
CrCl 30-49 mL/min: 150 mg PO qDay
CrCl 15-29 mL/min: 150 mg first dose, then 100 mg qDay
CrCl 5-14 mL/min: 150 mg first dose, then 50 mg qDay
CrCl <5 mL/min: 50 mg first dose, then 25 mg qDay
See Also Combos
with zidovudine (Combivir)
with abacavir (Epzicom)
with abacavir/zidovudine
Dosing Considerations
Monitor amylase q4-8week
Pediatric dosage forms and strengths
tablet
- 100mg (Epivir HBV)
- 150mg (Epivir)
- 300mg (Epivir)
oral solution
- 5mg/mL (Epivir HBV)
- 10mg/mL (Epivir)
HIV Infection
Epivir
- Neonates (aged <4 weeks): 2 mg/kg PO q12hr (for prevention of transmission or treatment)
- Infants 1-3 months: 4 mg/kg PO q12hr
- 3 months -16 years: 4 mg/kg PO q12hr or 8 mg/kg PO qDay; not to exceed 300 mg/day
Chronic Hepatitis B
Use Epivir HBV
<2 years: Safety and efficacy not established
≥2 years: 3 mg/kg PO qDay; not to exceed 100 mg/day
Dosing Considerations
Monitor amylase q4-8week
Lamiduvine (Epivir) scored tablet is the preferred formulation for HIV-1-infected pediatric patients who weigh at least 14 kg and for whom a solid dosage form is appropriate; consider more frequent monitoring of HIV-1 viral load when treating with lamiduvine (Epivir) oral solution; see also warnings and precautions section
Epivir, Epivir HBV (lamivudine) adverse (side) effects
>10%
Cough
Diarrhea
Fatigue & malaise
Fever (peds)
Headache
Musculoskeletal pain
Nausea
Nervous system neuropathy
Pancreatitis
Peripheral neuropathy
Nasal S/s
Vomiting
1-10%
Abdominal cramps, abdominal pain
Anorexia &/or decr appetite
Arthralgia
Chills
Depression
Dizziness
Dyspepsia
Insomnia
Myalgia
Rash
Thrombocytopenia
Creatine phosphokinase increased
Frequency not defined
Body fat redistribution
Elevated amylase
Neutropenia
Hepatitis B exacerbation
Postmarketing reports
Immune reconstitution
Warnings
Black box warnings
Lactic acidosis and severe hepatomegaly with steatosis (including fatal cases) reported with use of nucleoside analogues alone or in combination with other antiretrovirals
Not FDA approved for treatment of chronic hepatitis B virus (HBV) infection, and the safety and efficacy of this drug have not been established in patients co-infected with HBV and HIV
Tablets and oral solution formulations used to treat HIV infection contain a higher dose of lamivudine than formulations indicated for chronic hepatitis B infection; patients with HIV should receive only formulation specific for HIV
Contraindications
Hypersensitivity
Cautions
(All NRTIs): risk of potentially fatal lactic acidosis & severe hepatomegaly with steatosis when used alone or in combination with other antiretrovirals
Exacerbation of hepatitis B in HBV/HIV coinfected patients may occur on discontinuation
Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs
Discontinue immediately if signs or symptoms of pancreatitis occur in patients with history of pancreatitis
Patients with HIV-1 infection should receive only dosage forms of lamivudine appropriate for treatment of HIV-1
Emergence of lamivudine-resistant HBV variants associated with lamivudine-containing antiretroviral regimens reported
Concomitant administration of emtricitabine with lamivudine-containing products not recommended
Hepatic decompensation (some fatal) reported in HIV-1/HCV co-infected patients receiving interferon and ribavirin-based regimens; monitor for treatment-associated toxicities; discontinue therapy as medically appropriate and consider dose reduction or discontinuation of interferon alfa, ribavirin, or both
Use with caution in pediatric patients with a history of pancreatitis or other significant risk factors for pancreatitis; discontinue treatment as clinically appropriate
Lower Virologic Suppression Rates and Increased Risk of Viral Resistance with Oral Solution
- Pediatric subjects who received lamivudine (Epivir) oral solution concomitantly with other antiretroviral oral solutions at any time in the ARROW trial had lower rates of virologic suppression, lower plasma lamivudine exposure, and developed viral resistance more frequently than those receiving lamivudine (Epivir) tablets; lamivudine (Epivir) scored tablet is the preferred formulation for HIV-1-infected pediatric patients who weigh at least 14 kg and for whom a solid dosage form is appropriate; consider more frequent monitoring of HIV-1 viral load when treating with lamivudine (EPIVIR) oral solution.
Pregnancy and lactation
Pregnancy category: C; A pregnancy registry has been established to monitor maternal-fetal outcomes of women exposed to lamivudine: 1-800-258-4263
Lactation: HIV+ women are advised not to breastfeed
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Epivir, Epivir HBV (lamivudine)
Mechanism of action
Nucleoside Reverse Transcriptase Inhibitor (NRTI); following phosphorylation, inhibits HIV reverse transcriptase by viral DNA chain termination; cytosine analog
Useful in combination with ZDV
ZDV-induced codon mutations result in viral sensitivity to drug
Pharmacokinetics
Absorption: Rapid
Vd: 1.3 L/kg
Protein Bound: <36%
Metabolism: 5.6% to trans-sulfoxide metabolite
Bioavailability: Absolute; Cp max decreased with food although AUC not significantly affected, 66% (children); 87% (adults)
Half-life elimination: 2 hr (children); 5-7 hr (adults)
Excretion: Primarily urine
