Abacavir and Lamivudine

Table of contents

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

Brand Names

Europe

Austria: Kivexa; Belgium: Kivexa; Bulgaria: Kivexa; Cyprus: Kivexa; Czech Republic: Kivexa; Denmark: Kivexa; Estonia: Kivexa; Finland: Kivexa; France: Kivexa; Germany: Kivexa; Greece: Kivexa; Hungary: Kivexa; Ireland: Kivexa; Italy: Kivexa; Latvia: Kivexa; Lithuania: Kivexa; Luxembourg: Kivexa; Malta: Kivexa; Netherlands: Kivexa; Poland: Kivexa; Portugal: Kivexa; Romania: Kivexa; Slovakia: Kivexa; Slovenia: Kivexa; Spain: Kivexa; Sweden: Kivexa; UK: Kivexa.

North America

Canada: Kivexa; USA: Epzicom.

Latin America

Argentina: Kivexa; Brazil: Kivexa; Mexico: Kivexa.

Asia

Japan: Epzicom.

Drug combinations

Abacavir, Lamivudine, and Zidovudine

Chemistry

Abacavir Sulfate: (C~14~H~18~N~6~O)~2~ H~2~SO~4~. Mw: 670.74. (1S,4R)-4-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol sulfate (2:1). CAS-188062-50-2 (1997).

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

Anti-infective Agents, Antiretrovirals, Nucleoside and Nucleotide Reverse Transcriptase Inhibitors. (ATC-Code: J05AR02).

Mechanism of action

Abacavir phosphorylated to carbovir triphosphate interferes with HIV viral RNA-dependent DNA polymerase, inhibiting viral replication. Triphosphorylated lamivudine inhibits HIV reverse transcription via viral DNA chain termination. Inhibits RNA-dependent DNA polymerase activities of reverse transcriptase.

Therapeutic use

Treatment of HIV infections in combination with other antiretroviral agents.

Pregnancy and lactiation implications

Unlabeled use

Contraindications

Hypersensitivity to abacavir, lamivudine, or any component of the formulation. Renal (CrCl <50 mL/minute) and hepatic impairment.

Warnings and precautions

May cause redistribution of fat. Hypersensitivity reactions have occurred (increased risk in patients with HLA-B*5701 allele). Immune reconstitution syndrome might be developed. Lactic acidosis and hepatomegaly with steatosis have been reported. Clinical exacerbations after discontinuing therapy for chronic hepatitis B in HIV patients have occurred. Caution in combination with interferon alfa with or without ribavirin in HIV/HBV-coinfected patients. Caution in renal dysfunction (contraindicated in CrCl <50 mL/minute or in risk factors for coronary heart disease). Avoid use in children.

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