Lamivudine – Nucleoside Reverse Transcriptase Inhibitor (NRTI)
Lamivudine is an antiretroviral and antiviral agent belonging to the nucleoside reverse transcriptase inhibitor (NRTI) class. Lamivudine is a synthetic analog of cytidine. Its mechanism of action involves the competitive inhibition of the reverse transcriptase of HIV-1 and HIV-2, as well as the DNA polymerase of the hepatitis B virus (HBV). Following intracellular phosphorylation to its active triphosphate form, lamivudine incorporates into the viral DNA chain, resulting in chain termination and premature cessation of viral genome synthesis. The drug exhibits potent antiviral activity and high selectivity for viral enzymes, having minimal impact on DNA replication processes in human cells.
The pharmacokinetic profile of lamivudine is characterized by rapid and nearly complete absorption following oral administration. Bioavailability in adults is approximately 80–87%. Peak plasma concentrations are reached in approximately 1 hour. Lamivudine has low plasma protein binding and penetrates well into the cerebrospinal fluid. Metabolism in the human body is minimal; it is excreted primarily unchanged in the urine via active tubular secretion. The elimination half-life is 5 to 7 hours. In patients with renal impairment, elimination is prolonged, necessitating dosage adjustments.
The drug is administered orally irrespective of food intake. In HIV therapy, lamivudine is always utilized as part of a combination antiretroviral regimen to prevent the development of resistance. In chronic hepatitis B, the drug is used to suppress viral replication and reduce inflammation in liver tissue.
Indications
Lamivudine is indicated for use within combination therapeutic regimens for the following viral diseases:
- HIV infection: treatment of HIV-infected adults and children (as part of a combination antiretroviral regimen).
- Chronic Hepatitis B: treatment of chronic hepatitis B in adults and children with evidence of active viral replication, elevated serum aminotransferase levels, and histological verification of active inflammatory disease or fibrosis.
Dosage and administration
The dosing regimen of lamivudine depends on the diagnosis, patient age, and renal function.
- HIV infection: the recommended dose for adults is 300 mg daily (administered once daily or 150 mg twice daily).
- Chronic Hepatitis B: the recommended dose for adults is 100 mg once daily.
- Administration Method: tablets must be swallowed with water. Administration is possible irrespective of meal times.
- Renal Impairment Adjustment: since lamivudine is renally excreted, decreased creatinine clearance requires dose reduction or extended intervals between doses under strict medical supervision.