- only drug shown to reduce mortality in late-stage AIDS, reduce
opportunistic infection and progression to AIDS
Mechanism of Action
- ZDV enters cell by diffusion undergoes anabolic phosphorylation to the
triphosphate ZDV-TP
- This is a competitive inhibitor of HIV-1 RT, therefore when incorporated
causes chain termination as incoming nucleotide triphosphate cannot make a
triphosphate bond
- Human DNA polymerases are much less sensitive to inhibition therefore
selective viral effect
Adverse Effects
- Bone marrow suppression causing anaemia
- Nausea+ vomiting
- Fatigue/headache
- Melanonychia (blue-grey nail discolouration)
- Mitochondrial myopathy (rare)
- Mutagenic and carcinogenic (used in pregnant women as reduces HIV
maternal-foetal transmission)
Pharmacokinetics
- Almost totally absorbed from gut >90% (Orally, 200mg 3X daily)
- Short half life 1-2hrs
- Resistance develops slowly
- Several drug interactions
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