What is zidovudine? How does it work (mechanism of action)?

Zidovudine (formerly called azidothymidine [AZT]), a pyrimidine nucleoside analogue active against HIV. RETROVIR IV Infusion is a sterile solution
for intravenous infusion only. Each mL contains 10 mg zidovudine in Water for Injection. Hydrochloric acid and/or sodium hydroxide may have been added to adjust the pH to approximately 5.5. RETROVIR IV Infusion contains no preservatives. The chemical name of zidovudine is 3′-azido-3′-deoxythymidine.

What are the uses for zidovudine?

Zidovudine is used for the treatment of HIV and the prevention of HIV transmission from an infected mother to her fetus.

What are the side effects of zidovudine?

The most severe side effects of ziovudine are

  • a decrease in blood cells,
  • muscle pain (myopathy),
  • enlarged liver,
  • (hepatomegaly),
  • and metabolic disturbance (lactic acidosis).

Other side effects are

WARNING

Warning Retrovir (zidovudine) has been associated with hematologic toxicity, including neutropenia and severe anemia, particularly in patients with advanced human immunodeficiency virus (HIV) disease (see warnings). Prolonged use of Retrovir has been associated with symptomatic myopathy. Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues alone or in combination, including Retrovir and other antiretrovirals.

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What is the dosage for zidovudine?

  • For the treatment of HIV infection the recommended oral dose for adults is 100 mg every 4 hours. The intravenous dose is 1 to 2 mg/kg every 4 hours.
  • For children 3 months to 12 years old, the oral starting dose is 180 mg/m2 every 6 hours not to exceed 200 mg every 6 hours.
  • Infants should be given 2 mg/kg orally every 6 hours within 12 hours of birth and for 6 weeks or 1.5 mg/kg intravenously every 6 hours.
  • To prevent HIV transmission from mother to fetus, the dose is 100 mg five times daily or 200 mg three times daily.
  • Treatment should be initiated between the 14th and 34th weeks of pregnancy and continued until the time of labor.
  • During labor and delivery, 2mg/kg should be administered intravenously over 1 hr followed by 1 mg/kg/hr until the umbilical cord is clamped.

Which drugs or supplements interact with zidovudine?

  • Fluconazole (Diflucan), probenecid and trimethoprim (Trimpex) reduce the elimination of zidovudine and therefore increase the blood concentration of zidovudine. This can lead to increased side effects from zidovudine.

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Is zidovudine safe to take if you are pregnant or breastfeeding?

  • Zidovudine is used for preventing transmission of the HIV virus from mother to fetus.
  • Although it is not known whether zidovudine is excreted in breast milk, HIV infected mothers should not breast feed because of the potential risk of transmitting HIV to an infant that is not infected.

What else should you know about zidovudine?

What preparations of zidovudine are available?
  • Capsules: 100 mg
  • Tablet: 300 mg
  • Syrup 50 mg/5 ml
  • Injections 10mg/ml
How should I keep zidovudine stored?

Store at room temperature, 15-30 C (59-86 F). Keep capsules and syrup away from light.

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Medically Reviewed on 11/22/2019

References

FDA Prescribing Information.