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# Zidovudine

The first antiretroviral (AZT). Little used in adults today because of bone marrow toxicity, but still part of newborn prophylaxis.

Updated 2026-11-01

- Class: [Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs)](https://durgical.com/en/pharmacology/classes/nucleoside-nucleotide-reverse-transcriptase-inhibitors/)
- Enzyme: HIV-1 reverse transcriptase
- ATC code: J05AF01
- WHO Model List of Essential Medicines

Also called: AZT, azidotimidina, ZDV

✂**HIV-1 reverse transcriptase**Zidovudine

ⓘ The figure shows zidovudine triphosphate (AZT-TP), the active form, in the polymerase site of HIV-1 reverse transcriptase with DNA.

**Target in 3D:** HIV-1 reverse transcriptase. PDB structure 3V4I (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/3V4I) · Drag to rotate · pinch to zoom

## Mechanism of action

A thymidine analogue with an azido group instead of the 3'-hydroxyl. It is phosphorylated to zidovudine triphosphate, which competes with dTTP; incorporated into viral DNA, it ends the chain. It also partly inhibits human polymerases, especially the mitochondrial one, which explains myopathy and marrow toxicity.

- It is phosphorylated to zidovudine triphosphate
- It competes with dTTP at reverse transcriptase
- The azido group blocks DNA chain extension

## Pharmacokinetics

**Metabolism**
Glucuronidation in the liver to an inactive metabolite

**Elimination**
Zidovudine and its glucuronide leave in urine; they build up in severe kidney failure

## Indications

- HIV-1 infection, combined with other antiretrovirals [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)
- Prevention of mother-to-child HIV transmission [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)

## Adverse effects

### Common

- Nausea, headache, malaise
- Macrocytosis
- Changes in skin and nail pigmentation

### Serious (rare, important)

- Severe anaemia and neutropenia
- Symptomatic myopathy with long-term use
- Lactic acidosis and hepatomegaly with steatosis

## Contraindications

- Previous severe hypersensitivity (anaphylaxis, Stevens-Johnson) to zidovudine

## Key interactions

**Ganciclovir, interferon alfa and other myelosuppressive or cytotoxic drugs**
Additive bone marrow toxicity

**Ribavirin**
Worsens anaemia in HIV-hepatitis C co-infection; the combination is not advised

**Stavudine**
Antagonism between these two thymidine analogues has been shown: the combination is avoided

## What is monitored

- Complete blood count (haemoglobin and neutrophils) regularly
- Muscle symptoms and CK if myopathy is suspected
- Lactate if acidosis symptoms appear
- Viral load and CD4

## Administration and safety

- Available as capsules, syrup and intravenous injection (the latter mainly during labour)
- In newborns, the liquid form needs careful checking of the ordered volume
- Do not confuse zidovudine with similar-sounding drugs; check the abbreviation AZT on orders

## Nursing care

- Check blood count before and during treatment
- Watch for pallor, fatigue, fever or infections (anaemia, neutropenia)
- Ask about muscle pain or weakness
- In exposed newborns, coordinate prophylaxis as the team orders

## Pregnancy and breastfeeding

It is approved to prevent mother-to-child HIV transmission and is now part of regimens for exposed newborns.

## Memory aid

'AZT = Anaemia, Zapped muscles (myopathy), Transmission to the baby prevented'.

## Test yourself

Think of the answer, then tap the question to see it.

## What is zidovudine's most typical toxicity?

Bone marrow suppression: anaemia (often macrocytic) and neutropenia.

## Why is zidovudine not combined with ganciclovir without close monitoring?

Both are myelotoxic and their marrow effects add up.

## Which use of zidovudine is still relevant today?

Preventing mother-to-child HIV transmission, mainly in newborn prophylaxis.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/zidovudine/)

## Related drugs

- [Lamivudine](https://durgical.com/en/pharmacology/lamivudine/)
- [Nevirapine](https://durgical.com/en/pharmacology/nevirapine/)

## Related conditions

- [HIV infection and AIDS](https://durgical.com/en/conditions/hiv-infection-and-aids/)

[← Back to the class: Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs)](https://durgical.com/en/pharmacology/classes/nucleoside-nucleotide-reverse-transcriptase-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - ZIDOVUDINE capsule](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9907acb2-e4a0-46f9-93c0-a8d7b7ce98cf) (DailyMed (U.S. National Library of Medicine), 2025); [Zidovudine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a687007.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=J05AF01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/) (World Health Organization, 2025).

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Representative model, for educational purposes only.

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/zidovudine/
