Lamivudine

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Epivir, Lamivudin, Zeffix; Belgium: Epivir, Zeffix; Bulgaria: Zeffix; Cyprus: Epivir; Czech Republic: Epivir, Lamivudine, Zeffix; Denmark: Epivir, Zeffix; Estonia: Epivir, Lamivudine, Zeffix; Finland: Epivir, Lamivudine, Zeffix; France: Epivir, Zeffix; Germany: Epivir, Lamivudin, Zeffix; Greece: Epivir, Zeffix; Hungary: Zeffix; Ireland: Epivir, Lamivudine, Zeffix; Italy: Epivir, Zeffix; Latvia: Epivir, Lamivudine, Zeffix; Lithuania: Epivir, Lamivudine, Zeffix; Luxembourg: Epivir; Malta: Epivir, Lamivudine, Zeffix; Netherlands: Epivir, Zeffix; Poland: 3TC, Epivir, Lamivudine, Zeffix; Portugal: Epivir, Lamivudina, Zeffix; Romania: Epivir, Zeffix; Slovakia: Epivir, Lamivudine, Zeffix; Slovenia: Epivir, Lamivudine, Zeffix; Spain: Epivir, Lamivudina, Zeffix; Sweden: Epivir, Lamivudine, Zeffix; UK: Epivir, Zeffix.

North America

Canada: 3TC, Heptovir; USA: Epivir.

Latin America

Argentina: 3TC, Amilitrap, Ganvirel, Heptodine, Kess, Lamibergen, Lamilea, Lamivudina, Oralmuv, Vuclodir; Brazil: Epivir, Lami, Lamivudina, Vudirax-Lamivudina; Mexico: 3TC.

Asia

Japan: Epivir, Zefix.

Drug combinations

Lamivudine and Abacavir

Lamivudine and Stavudine

Lamivudine and Tenofovir

Lamivudine and Zidovudine

Lamivudine, Abacavir, and Zidovudine

Lamivudine, Nevirapine, and Stavudine

Lamivudine, Nevirapine, and Zidovudine

Chemistry

Lamivudine: C~8~H~11~N~3~O~3~S. Mw: 229.26. (1) 2(1H)-Pyrimidinone, 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-, (2R-cis)-; (2)(-)-1-[(2R,5S)-2-(Hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine. CAS-134678-17-4 (1992).

Pharmacologic Category

Antiretrovirals; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors. (ATC-Code: J05AF05).

Mechanism of action

After lamivudine is triphosphorylated, principal mode of action is inhibition of HIV reverse transcription via viral DNA chain termination; inhibits RNA- and DNA-dependent DNA polymerase activities of reverse transcriptase. Monophosphate form of lamivudine is incorporated into viral DNA by hepatitis B virus polymerase, resulting in DNA chain termination.

Therapeutic use

Treatment of HIV infection in conjunction with other antiretrovirals. Management of chronic HBV infection associated with evidence of HBV replication and active liver inflammation.

Pregnancy and lactiation implications

Lamivudine crosses placenta. No increased risk of overall birth defects observed following 1^st^ trimester exposure. Pregnant women might be at increased risk of lactic acidosis and liver damage. HIV-infected mothers are discouraged from breast-feeding in order to decrease potential transmission of HIV.

Unlabeled use

Postexposure prophylaxis for HIV exposure as part of a multidrug regimen.

Contraindications

Hypersensitivity to lamivudine or any component of the formulation.

Warnings and precautions

Lactic acidosis and severe hepatomegaly with steatosis (sometimes fatal) reported (use with caution in known risk factors for liver disease). Concomitant use with ribavirin and interferon alpha associated with increased risk of fatal hepatic decompensation in patients coinfected with HBV and HIV. Do not use multiple lamivudine-containing preparations concomitantly. Use with caution in renal impairment. Possible redistribution or accumulation of body fat. Patients may develop immune reconstitution syndrome (inflammatory response to indolent or residual opportunistic infection). Some dosage forms may contain sucrose. Pancreatitis, sometimes fatal, reported in antiretroviral nucleoside-experienced HIV-infected pediatric patients.

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