Zidovudine

Indications
 Oral
HIV infection
Adult: 600 mg daily in divided doses, in combination with other antiretroviral agents.
Child: 6 wk - 12 yr: 160 mg/m2 every 8 hr. Max: 200 mg every 8 hr. May be used in combination with other anti-retrovirals.
Renal impairment: Haemodialysis or peritoneal dialysis: 100 mg every 6-8 hr.
CrCl (ml/min)Dosage Recommendation
<10100 mg every 6-8 hr.
Hepatic impairment: Dose reduction may be needed.
Oral
Prophylaxis of maternal-foetal HIV transmission
Adult: 100 mg 5 times daily or 200 mg tid or 300 mg bid. Start treatment after 14th wk of gestation until the start of labour.
Renal impairment: Haemodialysis or peritoneal dialysis: 100 mg every 6-8 hr.
CrCl (ml/min)Dosage Recommendation
<10100 mg every 6-8 hr.
Hepatic impairment: Dose reduction may be needed.
Oral
Prophylaxis of HIV infection in neonates
Child: Neonates: 2 mg/kg every 6 hr for 1st 6 wk of life, starting within 12 hr after birth.
Renal impairment: Dose adjustment may be needed.
Hepatic impairment: Dose adjustment may be needed.
Intravenous
HIV infection
Adult: 1-2 mg/kg every 4 hr, given as 2-4 mg/ml infusion over 1 hr.
Child: As continuous infusion: 20 mg/m2/hr. Alternatively, as intermittent infusion: 120 mg/m2 every 6 hr.
Renal impairment: Haemodialysis or peritoneal dialysis: 1 mg/kg every 6-8 hr.
CrCl (ml/min)Dosage Recommendation
<101 mg/kg every 6-8 hr.
Hepatic impairment: Dose reduction may be needed.
Intravenous
Prophylaxis of HIV infection in neonates
Child: Neonates: 1.5 mg/kg every 6 hr. Start treatment within 12 hr after birth and continue for 1st 6 wk of life. Dose to be given via IV infusion over 30 minutes.
Renal impairment: Dose adjustment may be needed.
Hepatic impairment: Dose adjustment may be needed.
Intravenous
Prophylaxis of maternal-foetal HIV transmission during labour and delivery
Adult: Loading dose: 2 mg/kg, followed by continuous infusion of 1 mg/kg/hr until umbilical cord is clamped. If caesarean section is planned, start the IV infusion 4 hr before the operation.
Renal impairment: Dose reduction may be needed.
Hepatic impairment: Dose reduction may be needed.

Special Populations: Reduce dose in patients with renal or hepatic impairment if necessary.

Reconstitution: Required dose to be removed from vial and added to 5% dextrose Inj solution to achieve a concentration <4 mg>Incompatibility: May not be compatible with meropenem and total parenteral nutrition.
Contraindications
 Lactation.
Warnings / Precautions
 Anaemia or myelosuppression, renal and hepatic impairment, elderly, pregnancy. Monitor patients with risk factors for liver disease. Blood tests should be carried out regularly, reduce dose if neutrophil or haemoglobin count is low. Monitor serum CK concentration every 3 mth in patients who have received >6 mth of treatment. Patients to contact doctor if they experience muscle weakness, shortness of breath, symptoms of hepatitis or pancreatitis.
Adverse Reactions
 Nausea, severe headache, myalgia, insomnia, vomiting, anorexia, diarrhoea, asthenia, dizziness, taste perversion, convulsions, myopathy, nail, skin and oral mucosa pigmentation, raised LFT, pancreatitis, fat redistribution.
Potentially Fatal: Lactic acidosis, severe hepatomegaly with steatosis, hepatotoxicity. Blood dyscrasias, e.g. serious anaemia (may require transfusion), neutropenia, leucopenia.
Drug Interactions
 Decreased zidovudine concentration with tipranavir. Increased risk of peripheral neuropathy with bortezomib. Increased haematological toxicity with IV pentamidine, lamivudine, dapsone, vancomycin flucytosine, amphotericin, ganciclovir, interferon alfa, cyclophosphamide and other bone marrow suppressive or cytotoxic agents Increased risk of zidovudine toxicity with atovaquone, chloramphenicol, fluconazole, valproate. Decreased absorption with clarithromycin, minimise interactions by admin at least 2 hours apart. Increased zidovudine concentration and increased potential for hypersensitivity reactions with probenecid. Increased zidovudine clearance and haematological toxicity with rifampicin. Increased bioavailability of zidovudine with nimodipine. Increased incidences of headache with benzodiazepines. Possible increase in zidovudine concentration with methadone.
Potentially Fatal: Avoid stavudine (due to inhibition of activation of stavudine), didanosine, ribavirin (antagonize effect of zidovudine), zalcitabine (inferior virological activity and a higher rate of side effects) with zidovudine. Increased risk of toxicity (e.g. hepatic decompensation, neutropenia) in patients with interferon alfa with or without ribavirin.
See Below for More zidovudine Drug Interactions
Lab Interactions
 Maternal zidovudine treatment may cause wrong results in screening tests for inborn errors of metabolism due to high urinary thymine concentrations in neonates.
Mechanism of Actions
 Zidovudine is a thymidine analogue. It is phosphorylated in the body to its active form zidovudine triphosphate which interferes in DNA synthesis of retroviruses by inhibiting DNA replication. Zidovudine inhibits the key enzyme reverse transcriptase. Human DNA polymerase is inhibited only at a conc 100 times more than that required to inhibit viral reverse transcriptase.
Absorption: Rapidly absorbed from the GI tract, delayed if taken with food (oral). Peak plasma concentrations: 1 hr. Bioavailability: 60-70%.
Distribution: Crosses the placenta and blood-brain barrier; enters breast milk and semen. Protein-binding: 34-38%
Metabolism: Intracellular; converted to the active antiviral triphosphate. Hepatic; converted to the inactive glucuronide.
Excretion: Urine (as unchanged drug and metabolites); 1 hr (elimination half-life).
Administration
 May be taken with or without food.
Storage Conditions
 Intravenous: Store at 15-25°C (59-77°F). Oral: Store at 15-25°C (59-77°F).
ATC Classification
 J05AF01 - zidovudine ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
Storage
 Intravenous: Store at 15-25°C (59-77°F). Oral: Store at 15-25°C (59-77°F).
Available As
  • Zidovudine 10 mg
  • Zidovudine 100 mg
  • Zidovudine 300 mg
  • Zidovudine 50 mg

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