Zidovudine is a thymidine analog and the prototype of Nucleoside reverse transcriptase inhibitors (NRTIs).
It is a first-line triple ARV regimen.
Mechanism of action.
- A cellular cell’s enzyme converts it to an active phosphorylated metabolite that inhibits viral reverse transcriptase and viral DNA synthesis in the body.
Indication.
- HIV in adults and children with advanced immune deficiency.
- Reduces neurological manifestation of AIDS and prevents the appearance of Kaposi lesions.
- The drug is effective against retroviruses only.
Precautions.
- Hepatic and renal insufficiency.
- Avoid lactation and pregnancy.
- Monitor hematological parameters.
Adverse effects
- Hematological disorders like neutropenia and anemia
(Dose-related)
- Nausea, insomnia, anorexia, abdominal pain, headache, and myalgia.
- Myopathy, pigmentation of nails, encephalopathy, lactic acidosis, hepatomegaly, and convulsions.
Drug interaction.
- Interaction with paracetamol increases the drug’s toxicity due to competition for glucuronidation during metabolism.
- Azole antifungals inhibit the metabolism of the drug.
- Nephrotoxic and myelosuppressive drugs increase toxicity.
Dosage.
- Dose Adults 300 mg ; Children 180 mg/m2 (max 200 mg) 6–8 hourly.
- RETROVIR, ZIDOVIR 100 mg capsules, 300 mg tablets, 50 mg/5 ml syrup.
- VIRO-Z, ZIDOMAX, ZYDOWIN 100 mg capsules, 300 mg tablets. (taken with plenty of water.)
