Dosing & Uses
Dosage Forms & 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
Dosage Forms & Strengths
tablet
- 100mg (Epivir HBV)
- 150mg (Epivir)
- 300mg (Epivir)
oral solution
- 5mg/mL (Epivir HBV)
- 10mg/mL (Epivir)
HIV Infection
Indicated for treatment of HIV infection in combination with other antiretroviral agents
Epivir oral solution
- Neonates (aged <4 weeks): 2 mg/kg PO q12hr (for prevention of transmission or treatment)
- ≥1 month: 4 mg/kg PO q12hr
- ≥3 months: 5 mg/kg PO q12hr or 10 mg/kg PO qDay; not to exceed 300 mg/day
- May switch to once daily dosing after age 3 yr in clinically stable patients with undetectable viral load and stable CD4 count (NIH HIV guidelines)
- Also see Dosing Considerations
Epivir tablet
- Weight-based dosing
- 14 to <20 kg: 75 mg PO q12hr, OR 150 mg qDay
- ≥20 to <25 kg: 75 mg AM and 150 mg PM PO, OR 220 mg qDay
- ≥25 kg: 150 mg PO q12hr, OR 300 mg PO qDay
- The NIH pediatric HIV treatment guideline (March, 2016) does not recommend initiating once-daily lamivudine liquid formulation for HIV-infected infants and young children
Chronic Hepatitis B
Use Epivir HBV
<2 years: Safety and efficacy not established
Dosing Considerations
Monitor amylase q4-8week
Lamiduvine 150-mg scored tablet is the preferred formulation for HIV-1 infected children and adolescents ≥14kg and whom a solid dosage form is appropriate
Tablet regimens are recommended when possible to avoid potential interactions with sorbitol
Consider more frequent monitoring of HIV-1 viral load when treating with lamiduvine (Epivir) oral solution; see also warnings and precautions section
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse 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
Blood and lymphatic system disorders
Anemia (including pure red cell aplasia and severe anemias progressing on therapy), lymphadenopathy, splenomegaly, thrombocytopenia
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; discontinue therapy if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur
Epivir-HBV is not FDA approved for treatment of HIV-1 infection; lamivudine dosage in EPIVIR-HBV is subtherapeutic and monotherapy is inappropriate for the treatment of HIV-1 infection and the safety and efficacy of this drug have not been established in patients co-infected with HBV and HIV; severe acute exacerbations of hepatitis B reported in patients who have discontinued anti-hepatitis B therapy (including HBV formulation); hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who discontinue anti-hepatitis B therapy; if appropriate, initiation of anti-hepatitis B therapy may be warranted
Tablets and oral solution formulations used to treat HIV infection contain a higher dose of lamivudine than formulations indicated for chronic hepatitis B infection; HBV is not approved for treatment of HIV-1 infection because lamivudine dosage in HBV formulation is subtherapeutic and monotherapy is inappropriate for treatment of HIV-1 infection; patients with HIV should receive only formulation specific for HIV
Contraindications
Hypersensitivity
Cautions
Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, reported with use of nucleoside analogues, including lamivudine; a majority of these cases have been in women; female sex and obesity may be risk factors for development of lactic acidosis and severe hepatomegaly with steatosis in patients treated with antiretroviral nucleoside analogues; suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity, which may include hepatomegaly and steatosis even in the absence of marked transaminase elevations
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
EPIVIR-HBV is not appropriate for patients co-infected with HBV and HIV-1; if patient with unrecognized or untreated HIV-1 infection is prescribed EPIVIR-HBV for treatment of HBV, rapid emergence of HIV-1 resistance is likely to result because of subtherapeutic dose and inappropriate use of monotherapy for HIV-1 treatment
In order to reduce risk of resistance in patients receiving monotherapy, consider a switch to alternative regimen if serum HBV DNA remains detectable after 24 weeks of treatment; optimal therapy should be guided by resistance testing
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 & Lactation
Pregnancy
A pregnancy registry has been established to monitor maternal-fetal outcomes of women exposed to lamivudine: 1-800-258-4263
Available data from the APR show no difference in the overall risk of birth defects for lamivudine or zidovudine compared with background rate for birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population; APR uses the MACDP as the U.S. reference population for birth defects in the general population; MACDP evaluates women and infants from a limited geographic area and does not include outcomes for births that occurred at less than 20 weeks gestation; rate of miscarriage is not reported in the APR
Lactation
The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in the United States not breastfeed infants to avoid risking postnatal transmission of HIV-1 infection; lamivudine is present in human milk; there is no information on effects of lamivudine or zidovudine on breastfed infant or effects of drugs on milk production; because of potential for (1) HIV-1 transmission (in HIV-negative infants), (2)developing viral resistance (in HIV-positive infants), and (3) serious adverse reactions in a breastfed infant, instruct mothers not to breastfeed if they are receiving therapy
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
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
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Formulary
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