Emtricitabine

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
  • Genes that may be involved
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Belgium: Emtriva; Czech Republic: Emtriva; Denmark: Emtriva; Estonia: Emtriva; Finland: Emtriva; France: Emtriva; Germany: Emtriva; Greece: Emtriva; Hungary: Emtriva; Ireland: Emtriva; Italy: Emtriva; Latvia: Emtriva; Lithuania: Emtriva; Netherlands: Emtriva; Poland: Emtriva; Portugal: Emtriva; Romania: Emtriva; Slovakia: Emtriva; Spain: Emtriva; Sweden: Emtriva; UK: Emtriva.

North America

Canada: Emtriva; USA: Emtriva.

Latin America

Argentina: Emtriva; Mexico: Emtriva.

Asia

Japan: Emtriva.

Drug combinations

Emtricitabine and Tenofovir

Emtricitabine, Efavirenz, and Tenofovir

Chemistry

Emtricitabine: C~8~H~10~FN~3~O~3~S. Mw: 247.25. (1)(2R-cis)-4-Amino-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone; (2) 5-Fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine. CAS-143491-57-0.(1998).

Pharmacologic Category

Antiretrovirals, Nucleoside and Nucleotide Reverse Transcriptase Inhibitors. (ATC-Code: J05AF09).

Mechanism of action

Emtricitabine, a synthetic antiretroviral agent, is a nucleoside reverse transcriptase inhibitor. The antiviral activity of emtricitabine depends on intracellular conversion of the drug to a 5′-triphosphate metabolite. Following conversion to a pharmacologically active metabolite, emtricitabine apparently inhibits replication of human retroviruses type 1 (HIV-1) and type 2 (HIV-2) by interfering with viral RNA-directed DNA polymerase (reverse transcriptase). Emtricitabine exerts a virustatic effect against retroviruses by acting as a reverse transcriptase inhibitor. Also has some activity against hepatitis B virus (HBV).

Therapeutic use

Used in conjunction with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults, adolescents, and pediatric patients.

Pregnancy and lactiation implications

There are no studies of emtricitabine during human pregnancy. Pregnant women may be at increased risk of lactic acidosis and liver damage. HIV-infected women are discouraged from breast-feeding in order to decrease the potential transmission of HIV.

Unlabeled use

Hepatitis B (with HIV coinfection).

Contraindications

Hypersensitivity to emtricitabine or any component of the formulation.

Warnings and precautions

May cause fat redistribution. Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection. Lactic acidosis and severe hepatomegaly with steatosis reported with nucleoside analogs, including fatal cases (use with caution in risk factors for liver disease). Use with caution in renal impairment. Prior to initiation of emtricitabine therapy for the treatment of HIV-1 infection, patients should be tested for chronic hepatitis B virus (HBV). Not indicated for treatment of chronic hepatitis B. Severe acute exacerbations of HBV infection reported in HIV-infected patients following discontinuance of emtricitabine.

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