Serum lamivudine levels in the presence of a lamivudine-resistant HBV mutant

Dig Liver Dis. 2004 Oct;36(10):677-81. doi: 10.1016/j.dld.2004.03.020.

Abstract

Background/aims: Lamivudine efficiently inhibits hepatitis B virus replication and has been used to treat hepatitis B virus recurrence after orthotopic liver transplantation. Although effective, its use is hampered by viral breakthrough due to the appearance of hepatitis B virus drug-resistant strains. Aims of this work were to evaluate the inter- and intra-individual variations of lamivudine serum levels and the effects on the drug levels of the lamivudine-resistant hepatitis B virus mutant infection.

Methods: Serum lamivudine concentration was measured by high-performance liquid chromatography. Polymerase chain reaction analysis and sequencing analysis of the reverse transcriptase area of the polymerase was performed on each sample using specific primers. A polymerase chain reaction-enzyme-linked immunosorbent assay was used to differentiate between wild-type hepatitis B virus and lamivudine-resistant hepatitis B virus strain.

Results: Lamivudine serum levels presented minor inter- and intra-individual fluctuations along time, with an important increase at the time of the hepatitis flare-up due to the hepatitis B virus mutant presence. When the wild-type hepatitis B virus briefly reappeared as a mixed population, the titre of lamivudine dropped to below the detection level.

Conclusions: While lamivudine serum levels appears stable when the anti-viral efficacy is fully achieved, important fluctuations are present according to the type of viral population, with a considerable decrease possibly due to the presence of the wild-type virus.

MeSH terms

  • Anti-HIV Agents / blood
  • Anti-HIV Agents / therapeutic use
  • Chromatography, High Pressure Liquid
  • Drug Resistance, Viral / genetics
  • Enzyme-Linked Immunosorbent Assay
  • Hepatitis B / drug therapy*
  • Hepatitis B virus / drug effects*
  • Hepatitis B virus / genetics
  • Hepatitis B virus / isolation & purification
  • Humans
  • Lamivudine / blood
  • Lamivudine / therapeutic use*
  • Male
  • Middle Aged
  • Mutation
  • Polymerase Chain Reaction
  • Recurrence

Substances

  • Anti-HIV Agents
  • Lamivudine