Lamivudine

Aka: Lamivudine, 3TC, Epivir, Epivir-HBV

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II. Indications

  1. HIV Infection (combination therapy)
  2. Chronic Hepatitis B Infection (Coinfected with HIV)
    1. High rates of HBV resistance (14 to 32% of patients at 1 year, and 69% at 5 years)
    2. No longer recommended as a first-line agent for chronic HBV

III. Contraindications

  1. Lamivudine resistant Chronic Hepatitis B Infection

IV. Mechanism

  1. Nucleoside Reverse Transcriptase Inhibitor
  2. Lamivudine is a substituted analog of cytosine (similar to Emtricitabine)

V. Precautions

  1. High risk of resistant Chronic Hepatitis B Infection
    1. Other regimens are preferred for monotherapy of isolated Chronic Hepatitis B Infection
  2. Risk of severe HBV exacerbation on discontinuation
    1. Monitor for at least 2 months after discontinuation
  3. Risk of induced HIV resistance in undiagnosed HIV coinfection
    1. HIV Test before use
    2. Do NOT use in monotherapy in HBV/HIV infected patients

VI. Dosing: HIV Infection (combination therapy)

  1. Administer as part of a combination protocol with other Antiretrovirals
  2. Adult (or child weight >25 kg)
    1. Take 150 mg twice daily or 300 mg orally daily
  3. Child (age >=3 months)
    1. Infants and young children (weight <14 kg)
      1. Dose twice daily in infants and young children
      2. Give 5 mg/kg (up to 150 mg) orally twice daily
    2. Children >14 kg
      1. Tablets (preferred if able)
        1. Weight 14 to 20 kg: 75 mg orally twice daily (or 150 mg once daily)
        2. Weight 20 to 25 kg: 75 mg orally qAM and 150 mg qPM, or 225 mg once orally daily
        3. Weight >25 kg: 150 mg orally twice daily (or 300 mg once daily)
      2. Solution
        1. Avoid solutions if possible (contain Sorbitol that decreases Lamivudine absorption)
        2. Tablets are preferred in any child weight >14 kg able to swallow tablets
        3. Give 5 mg/kg (up to 150 mg) orally twice daily or 10 mg/kg (up to 300 mg) orally daily
  4. Renal (Adults or child weight >25 kg)
    1. eGFR 30 to 49 ml/min: Take 150 mg orally daily
    2. eGFR 15 to 29 ml/min: Take 150 mg orally for first dose, then 100 mg orally daily thereafter
    3. eGFR 5 to 14 ml/min: Take 150 mg orally for first dose, then 50 mg orally daily thereafter
    4. eGFR <5 ml/min: Take 50 mg orally for first dose, then 25 mg orally daily thereafter

VII. Dosing: Chronic Hepatitis B Infection

  1. Monotherapy for Isolated Chronic Hepatitis B Infection
    1. Precautions
      1. Low dose regimen risks HBV resistance
      2. Do NOT use this lower dose or monotherapy if coinfected with HIV
    2. Adult
      1. Epivir-HBV 100 mg orally daily
    3. Child (age >=2 years old)
      1. Epivir-HBV 3 mg/kg (up to 100 mg) orally daily
    4. Renal (Adults or child weight >25 kg)
      1. eGFR 30 to 49 ml/min: Take 100 mg orally for first dose, then 50 mg orally daily thereafter
      2. eGFR 15 to 29 ml/min: Take 100 mg orally for first dose, then 25 mg orally daily thereafter
      3. eGFR 5 to 14 ml/min: Take 35 mg orally for first dose, then 15 mg orally daily thereafter
      4. eGFR <5 ml/min: Take 35 mg orally for first dose, then 10 mg orally daily thereafter
  2. Combination therapy for Comorbid HIV Infection AND Chronic Hepatitis B Infection
    1. Avoid if Creatinine Clearance <60 ml/min
    2. Off-label use for adults (not FDA approved, and not evaluated in children)
    3. Lamivudine 300 mg orally daily AND
    4. Tenofovir disoproxil Fumarate 300 mg orally once daily

VIII. Efficacy

  1. Very effective in HIV in combination with Zidovudine (AZT)
  2. Effective in vertical transmission to newborns when given to HBV positive mothers in last 4 weeks of pregnancy

IX. Adverse Effects

  1. See nRTI for adverse effects attributed to the class
  2. Generally well tolerated
  3. Similar adverse effects to Zidovudine (AZT) but much less severe
  4. Hepatitis B infection flares on Medication Withdrawal
  5. Gastrointestinal upset (Nausea, Vomiting, Diarrhea)
  6. Headache
  7. Dizziness
  8. Myalgia
  9. Malaise
  10. Neutropenia
  11. Pancreatitis
    1. More common in children with HIV Infection or if coinfected with HBV and HIV

X. Safety

  1. Avoid in Lactation
  2. Pregnancy Category C (pregnancy registry exists)
    1. Among the preferred nRTI agents in pregnancy

XI. Drug Interactions

  1. Sorbitol
    1. Decreases Lamivudine absorption

XII. Resources

  1. Lamivudine (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=89226149-47fa-4f7d-bb1f-1aa7034486b8

XIII. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (1998) Med Lett Drugs Ther 40(1041):115 [PubMed]
  3. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  4. (2013) Med Lett Drugs Ther 11(127): 19-30 [PubMed]
  5. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]

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Related Studies

Cost: Medications

lamivudine (on 11/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
LAMIVUDINE 150 MG TABLET Generic $0.85 each
LAMIVUDINE 300 MG TABLET Generic $1.29 each
LAMIVUDINE HBV 100 MG TABLET Generic $1.64 each
LAMIVUDINE-ZIDOVUDINE TABLET Generic $0.75 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Ontology: Lamivudine (C0209738)

Definition (NCI) A synthetic nucleoside analogue with activity against hepatitis B virus (HBV) and HIV. Intracellularly, lamivudine is phosphorylated to its active metabolites, lamiduvine triphosphate (L-TP) and lamiduvine monophosphate (L-MP). In HIV, L-TP inhibits HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleoside analogue into viral DNA. In HBV, incorporation of L-MP into viral DNA by HBV polymerase results in DNA chain termination. L-TP is a weak inhibitor of mammalian DNA polymerases alpha and beta, and mitochondrial DNA polymerase. (NCI04)
Definition (NCI_NCI-GLOSS) A drug used to treat infection caused by viruses.
Definition (CSP) zalcitabine analog
Definition (MSH) A reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.
Definition (PDQ) A synthetic nucleoside analogue with activity against hepatitis B virus (HBV) and HIV. Intracellularly, lamivudine is phosphorylated to its active metabolites, lamiduvine triphosphate (L-TP) and lamiduvine monophosphate (L-MP). In HIV, L-TP inhibits HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleoside analogue into viral DNA. In HBV, incorporation of L-MP into viral DNA by HBV polymerase results in DNA chain termination. L-TP is a weak inhibitor of mammalian DNA polymerases alpha and beta, and mitochondrial DNA polymerase. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42593&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42593&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1471" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D019259
SnomedCT 108698001, 386897000
LNC LP21312-1, MTHU013847
English 3TC, 2',3' Dideoxy 3' thiacytidine, 2',3'-Dideoxy-3'-thiacytidine, 2(1H)-Pyrimidinone, 4-amino-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)-, (2R-cis)-, Lamivudine, THREE TC, DIDEOXYTHIACYTIDINE 002 003 003, 2'3' dideoxy 3' thiacytidine, lamivudine (medication), LAMIVUDINE, Lamivudine [Chemical/Ingredient], 3tc, lamiVUDine, LamiVUDine, 3'-Thia-2',3'-dideoxycytidine, 4-Amino-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)-2(1H)-pyrimidinone, lamivudine, Lamivudine (product), Lamivudine (substance)
Swedish Lamivudin
Czech lamivudin
Finnish Lamivudiini
Russian 2',3'-DIDEZOKSI-3'-TIATSITIDIN, LAMIVUDIN, 2',3'-ДИДЕЗОКСИ-3'-ТИАЦИТИДИН, 3TC, ЛАМИВУДИН
German DREI TC, DIDESOXYTHIACYTIDIN 002 003 003, 3TC, 2'3'-Didesoxy-3'-thiacytidin, Lamivudin
Polish Lamiwudyna
Japanese 2',3'-ジデオキシ-3'-チアシチジン, ラミブジン
Spanish lamivudina (producto), lamivudina (sustancia), lamivudina, 3TC, 2',3'-Didesoxi-3'-tiacitidina, Lamivudine
French 3TC, Didésoxy-2',3' thiacytidine-3', Lamivudine
Italian Lamivudina
Portuguese 3TC, 2',3'-Didesoxi-3'-tiacitidina, Lamivudina
Derived from the NIH UMLS (Unified Medical Language System)

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