Zidovudine (AZT)

Products

Zidovudine is commercially available as film-coated tablets, capsules, and syrup (Retrovir AZT, combination products). It was approved in 1987 as the first AIDS drug.

Structure and properties

Zidovudine (C10H13N5O4, Mr = 267.2 g/mol) or 3-azido-3-deoxythymidine (AZT) is an analog of thymidine. It exists as an odorless, white to beige, crystalline substance that is soluble in water. Zidovudine is a prodrug that is biotransformed intracellularly to the active metabolite zidovudine triphosphate. See also under the article Nucleic Acids.

Effects

Zidovudine (ATC J05AF01) has antiviral properties against HIV. The effects are due to inhibition of the viral enzyme reverse transcriptase, which transcribes viral RNA into DNA and is important in viral replication. The activated agent is incorporated into DNA and leads to chain termination.

Indications

For treatment of infection with HIV as part of combination antiretroviral therapy.

Dosage

According to the SmPC. Medicines are usually taken twice daily, independent of meals.

Contraindications

  • Hypersensitivity
  • Granulocytopenia
  • Anemia

Full details of precautions and interactions can be found in the drug label.

Adverse effects

The most common possible adverse effects include headache, feeling sick, nausea, poor appetite, and vomiting. Severe adverse effects include neutropenia, anemia, myopathy, lactic acidosis, and liver toxicity.