Drug reference

Zidovudine

Antiretroviral · Antiviral

Also known as AZT

AntiretroviralAntiviralATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

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Mechanism

Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI). It interferes with the reverse transcriptase enzyme, which is crucial for HIV replication by preventing the transcription of viral RNA into DNA. This action inhibits viral replication in infected cells.

Indications

HIV infection (in combination with other antiretroviral drugs)HIV infection (as part of a combination product with abacavir and lamivudine, used only if patient is stabilised for 6–8 weeks on the individual components in the same proportions)HIV infectionpreventing mother-to-child transmissionProphylaxis for HIV infection (health care workers exposed to blood by needle stick injury)Prophylaxis for HIV transmission from mother to newbornHIV infected patients (in combination with at least 2 other ARV drugs)post-exposure prophylaxis of HIVmother-to-offspring transmission prophylaxis

Dosing

Adult: When used in the combination product Abacavir with lamivudine and zidovudine (Trizivir ®): 1 tablet (Lamivudine 150 mg, Abacavir 300 mg, Zidovudine 300 mg) twice daily by mouth.
Pediatric: 180 mg/m2 (max 200 mg) 6–8 hourly.
Renal adjustment: For the combination product Abacavir with lamivudine and zidovudine (Trizivir ®): Avoid if eGFR less than 50 mL/minute/1.73 m2.

Pharmacokinetics

Half-life

1.0

Bioavailability

64%

Protein binding

20–38%

Metabolism

60–80% (glucuronidation)

Excretion

Transported by OAT4 in the renal proximal tubule, which is involved in reabsorption of organic anions from tubular lumen into cell.

Contraindications

Concomitant use with ganciclovir, particularly during initial ganciclovir therapy, due to profound myelosuppression.
For the combination product Abacavir with lamivudine and zidovudine (Trizivir ®): Avoid if eGFR less than 50 mL/minute/1.73 m2.