ZIDOVUDINE

Structure/Class
  1. nucleoside analog reverse-transcriptase inhibitor
Pharmacodynamics
  1. It acts by inhibiting viral reverse transcriptase, therefore preventing formation of ds-DNA (the pro-virus).
    • It is a drug that is usually prescribed in combination therapy because this lowers the possibility of resistance developing.
  2. Indications as follows:
    • HIV affected individuals.
    • Reduce progression to AIDS dementia
    • Reduce rate of vertical transmission.
  3. Adverse effects
    • Myelosuppression – either macrocytic anaemia or neutropenia
Pharmacokinetics
  1. Administered PO
  2. Serum T ½ only 1 hour, but it has an intracellular T ½ of 3-4 hours allowing BD dosing.
  3. It undergoes hepatic glucuronidation and is excreted by the kidney.
  4. Enzyme inhibitors will increase zidovudine levels.
  5. Zidovudine may decrease phenytoin levels.