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Lamivudine
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Lamivudine is an oral medication that is used for the treatment of infections with the human immunodeficiency (HIV) and hepatitis B viruses. It is in a class of drugs called reverse transcriptase inhibitors which ... includes zalcitabine (Hivid), zidovudine (Retrovir), didanosine (Videx), and stavudine (Zerit). During infection with HIV, the HIV virus multiplies within the body's cells. The viruses then are released from the cells and spread throughout the body where they infect other cells. In this manner, HIV infection spreads to new, uninfected cells that the body is continually producing, and HIV infection is perpetuated. When producing new viruses, the HIV virus must manufacture new DNA for each virus.
Lamivudine is a potent reverse transcriptase inhibitor of the class nucleoside analog reverse transcriptase inhibitor (NARTI). Lamivudine has been used for treatment of chronic hepatitis B at a lower dose than for treatment of HIV. Lamivudine was approved by the Food and Drug Administration in 1995 for use with Zidovudine (AZT). When HIV infects a cell, reverse transcriptase copies the viral single stranded RNA genome into a double-stranded viral DNA. The viral DNA is then integrated into the host chromosomal DNA which then allows host cellular processes, such as transcription and translation to reproduce the virus. RTIs block reverse transcriptase's enzymatic function and prevent completion of synthesis of the double-stranded viral DNA ... preventing HIV from multiplying.
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Lamivudine should not be taken together with Combivir, a medication that contains a combination of lamivudine and zidovudine. Lamivudine may cause lactic acidosis (the build up of lactic acid in the body). Lactic acidosis symptoms can start slowly and gradually get worse. Symptoms include unusual muscle pain and weakness, trouble breathing, fast or uneven heart rate, nausea, vomiting, stomach pain, and numbness or cold feeling in your arms or legs. Call your doctor at once if you have any of these symptoms, even if they are only mild. Early signs of lactic acidosis generally get worse over time and this condition can be fatal.
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J. Reichen M.D. Lamivudine ([(-)2'-deoxy-3'-thiacytidine, 3TCâ, Zeffixâ] is well introduced as a treatment for HIV infection but has ... activity [I]n vitro against the replication of the hepatitis B virus by inhibiting HBV DNA polymerase. In addition to this effect it also restores T-cell responsiveness (1). Dose-finding studies (25, 100, 300 mg/d) determined 100 mg/d to be the lowest dose making HBV-DNA undetectable in all patients (2-4). This is the dose used thereafter in most trials. Liver disease does not affect disposition of lamivudine and therefore, no dose adjustment is necessary (5).
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Resistance: Lamivudine-resistant variants of HIV-1 have been selected in vitro. Genotypic analysis showed that the resistance was due to a specific amino acid substitution in the HIV-1 reverse transcriptase at codon 184 changing the methionine residue to either isoleucine or valine. HIV-1 strains resistant to both lamivudine and zidovudine have been isolated from patients. Susceptibility of clinical isolates to lamivudine and zidovudine was monitored in controlled clinical trials. In patients receiving lamivudine monotherapy or combination therapy with lamivudine plus zidovudine, HIV-1 isolates from most patients became phenotypically and genotypically resistant to lamivudine within 12 weeks. In some patients harboring zidovudine-resistant virus at baseline, phenotypic sensitivity to zidovudine was restored by 12 weeks of treatment with lamivudine and zidovudine.
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Lamivudine was approved as an antiretroviral drug (ARV) for people with HIV infection. It has been studied in adults and children over 3 months old.There are no absolute rules about when to start ART. You and your health care provider should consider your CD4 cell count, your viral load, any symptoms you are having, and your attitude about taking ART. Fact Sheet 404 has more information about guidelines for the use of ART.
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