Drug Detail

Lamivudine

Last Updated June 10, 2016

Trade Names

  • Lamivudine: 3TC, Aspen Lamivudine, Legram, Cipla-Lamivudine, Adco-Lamivudine, Sonke Lamivudine, Lazena, Lamivudine Winthrop, Pharma-Q Lamivudine;
  • Lamivudine/zidovudine: Combivir, Aspen Lamzid, Adco-Lamivudine + Zidovudine, Cipla-Duovir, Divuwin, Lodiz, Sonke Lamivudine+Zidovudine, Zovilam;
  • Lamivudine/stavudine/nevirapine: Sonke-LamNevStav, Virtrium (Aspen);
  • Lamivudine/abacavir: Kivexa, Dumiva (Mylan);
  • Lamivudine/abacavir/zidovudine: Trizivar, Sonke Abaclamizid;
  • Lamivudine/zidovudine plus efavirenz: Cipla-Duovir/Cipla Efavirenz copack;
  • Tenofovir/lamivudine/efavirenz: Tenarenz (Aspen), Eflaten;
  • Zidovudine/lamivudine/nevirapine: Mivirdo (Mylan), Triplavar

Drug Classification

Nucleoside reverse transcriptase inhibitor antiretroviral

Formulations

  • Lamivudine: 150 mg, 300 mg tablets; 10 mg/mL oral solution, 10 mg/mL syrup
  • Lamivudine/zidovudine: 150/300 mg tablets
  • Lamivudine/stavudine/nevirapine: 150/30/200 mg tablets
  • Lamivudine/abacavir: 300/600 mg tablets
  • Lamivudine/abacavir/zidovudine: 300/300/150 mg tablets
  • Lamivudine/zidovudine plus efavirenz: 150/300 mg tablets copackaged with efavirenz 600 mg tablets
  • Tenofovir/lamivudine/efavirenz: 300/300/600 mg tablets
  • Zidovudine/lamivudine/nevirapine: 300/150/200 mg tablets

Indications and Pharmacology

Indication: treatment of HIV infection in combination with other antiretrovirals; reduction of perinatal transmission of HIV, postexposure prophylaxis, in combination with other antiretrovirals. SA Formulary lists an unregistered use in HIV/hepatitis B coinfection.

Mechanism of action*: a cytosine analogue that is phosphorylated intracellularly to lamivudine 5’-triphosphate, which interferes with HIV viral RNA–dependent DNA polymerase inhibiting viral replication.

Pharmacokinetics*: renal excretion 70%. Half-life: serum = 2-4 hours; intracellular = 16-19 hours. Detectable levels found in cerebrospinal fluid after oral administration.

Dosage

Adult Dose: 150 mg twice daily or 300 mg once daily.

Take without regard to meals.*

Use in Renal or Hepatic Insufficiency:
Dosage for patients with chronic kidney disease or end-stage renal disease:

  • Creatinine clearance ≥ 50 mL/min: Normal dose.
  • Creatinine clearance 30-49 mL/min: 150 mg daily orally.
  • Creatinine clearance 15-29 mL/min: 150 mg orally first dose, then 100 mg daily orally.
  • Creatinine clearance 5-14 mL/min: 150 mg orally first dose, then 50 mg/day orally.
  • Creatinine clearance < 5 mL/min: 50 mg orally first dose, then 25 mg daily orally.
  • Receiving haemodialysis: 50 mg orally first dose, then 25 mg daily orally (Dose lamivudine after dialysis).
  • Receiving peritoneal dialysis: 50 mg orally first dose, then 25 mg daily orally.

Zidovudine/lamivudine should be administered as separate component medications in patients with creatinine clearance < 50 mL/min.

Chronic hepatitis B infection: 100-150 mg daily.

  • In patients with HIV/hepatitis B coinfection, use dose for HIV treatment.

Use in Pregnancy and Breastfeeding: Category C. Excreted in high concentrations in breast milk.

Use in Children:

  • Neonates < 30 days old: 2 mg/kg twice daily.
  • 3 months to 12 years: 4 mg/kg (maximum 150 mg) twice daily.

Children with renal impairment:

  • Glomerular filtration rate 30-50 mL/min/1.73 m²: 4 mg/kg once daily.
  • Glomerular filtration rate 10-29 mL/min/1.73 m²: 2 mg/kg once daily.
  • Glomerular filtration rate < 10 mL/min/1.73 m²: 1 mg/kg once daily.

Warnings

Contraindicated in severe anaemia or neutropenia.

US Prescribing Information Boxed Warning*: hepatitis B virus testing should be done prior to initiation of lamivudine and caution used in coinfected patients.

Patients receiving lamivudine and other antiretroviral agents may continue to develop opportunistic infections and other complications of HIV infection. Patients should therefore remain under close supervision by medical practitioners experienced in the treatment of patients with HIV-associated diseases.*

Use with caution in patients with hepatitis B infection; rebound hepatitis may occur following therapy withdrawal.

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues and other antiretrovirals.*

Drug–Drug Interactions

Contraindicated: none.

Precautions: none.

Considerations for Special Populations

See above for pregnancy and lactation and paediatric dosing. Dosing adjustments in renal impairment and with hepatitis B monoinfection.

Adverse Effects

Minimal toxicity; adverse effects occur infrequently.

*Information from US prescribing information.
Recommendation from South African Renal Society, 2008.