Zidovudine-also known as azidothymidine (AZT), is an antiretroviral medication used to prevent and treat HIV/AIDS.

Zidovudine (ZDV), also known as azidothymidine (AZT), is an antiretroviral medication used to prevent and treat HIV/AIDS.

Zidovudine-also known as azidothymidine (AZT), is an antiretroviral medication used to prevent and treat HIV/AIDS.

Azidothymidine; Retrovir; 3'-Azido-3'-deoxythymidine; AZT

Retrovir, Viro-Z, Zidine, Zidine 100, Zidine 300, Zido- H, Zidomax, Zidovir, Zilion, ZVD, ZVD Plus, Zydowin

1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methyl-1,2,3,4-tetrahydropyrimidine-2,4-dione

 It is a structural analog of thymidine, a prodrug that must be phosphorylated to its active 5′-triphosphate metabolite, zidovudine triphosphate (ZDV-TP). It inhibits the activity of HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleotide analogue. It is also a weak inhibitor of cellular DNA polymerase α and γ. It competes with the natural substrate dGTP and incorporates itself into viral DNA.

The recommended dose is 600 mg/day in divided doses as PO

Treatment of HIV (human immunovirus)/AIDS

Lactic acidosis, severe hepatomegaly with steatosis, hepatotoxicity. Nausea, severe headache, myalgia, insomnia, vomiting, anorexia, diarrhoea, asthenia, dizziness, taste perversion, convulsions, myopathy, nail, skin and oral mucosa pigmentation, raised LFT, pancreatitis, fat redistribution, neutropenia, leucopenia.

• Decreased zidovudine concentration with tipranavir.
• Avoid didanosine, ribavirin (antagonize effect of zidovudine), stavudine (due to inhibition of activation of stavudine), zalcitabine (inferior virological activity and a higher rate of side effects) with zidovudine.
• Increased risk of peripheral neuropathy with bortezomib.
• Increased haematological toxicity with IV pentamidine, lamivudine, dapsone, vancomycin flucytosine, amphotericin, ganciclovir, interferon alfa, cyclophosphamide and other bone marrow suppressive or cytotoxic agents Increased risk of zidovudine toxicity with atovaquone, chloramphenicol, fluconazole, valproate.
• Decreased absorption with clarithromycin, minimise interactions by admin at least 2 hours apart.
• Increased zidovudine concentration and increased potential for hypersensitivity reactions with probenecid.
• With rifampicin, clearance and haematological toxicity ogf zidovudine will be increased.
• Increased bioavailability of zidovudine with nimodipine.
•  Increased incidences of headache with benzodiazepines.
• Possible increase in zidovudine concentration with methadone.
• Increased risk of toxicity (e.g. hepatic decompensation, neutropenia) in patients with interferon alfa with or without ribavirin.

Reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy Dose selection in elder patients should be cautious.

Store at 15-25°C (59-77°F). 

Molecular weight

267.2413

Molecular formula

C10H13N5O4

CAS number

30516-87-1

Precautions

• Anaemia or myelosuppression, renal and hepatic impairment, elderly, pregnancy.
• Monitor patients with risk factors for liver disease.
• Diagnose blood regularly, reduce dose if haemoglobin or neutrophil count is low.
• Monitor serum CK concentration every 3 months in patients who have received >6 months of treatment.
• Contact physician if shortness of breath, muscle weakness, symptoms of hepatitis or pancreatitis experiences.