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Lamivudine


ACCESSION NB: DB00709 (APRD00681)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
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 Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV).

CATEGORIES:
Anti-HIV Agents Nucleoside and Nucleotide Reverse Transcriptase Inhibitors Reverse Transcriptase Inhibitors

ABSORPTION: Lamivudine was rapidly absorbed after oral administration in HIV-infected patients. Absolute bioavailability in adults is 86% ± 16% for the tablet and 87% ± 13% for the oral solution.

INDICATION:
For the treatment of HIV infection and chronic hepatitis B (HBV).

PHARMACODYNAMICS:
Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV). Lamivudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.

MECHANISM OF ACTION:
Lamivudine is a synthetic nucleoside analogue and is phosphorylated intracellularly to its active 5'-triphosphate metabolite, lamivudine triphosphate (L-TP). This nucleoside analogue is incorporated into viral DNA by HIV reverse transcriptase and HBV polymerase, resulting in DNA chain termination.

PROTEIN BINDING:
36%

METABOLISM:
The only detected metabolite of lamivudine is trans-sulfoxide.

AFECTED ORGANISMS:
Human Immunodeficiency Virus Hepatitis B virus