Last Updated June 10, 2016
Nucleoside reverse transcriptase inhibitor antiretroviral
Indication: treatment of HIV infection in combination with other antiretrovirals, postexposure prophylaxis in combination with other antiretrovirals.
Mechanism of action*: a thymidine analogue that is phosphorylated intracellularly to stavudine triphosphate, which interferes with HIV viral RNA–dependent DNA polymerase inhibiting viral replication.
Pharmacokinetics: renal excretion 40%. Half-life: serum = 1.0-1.5 hours; intracellular = 7.5 hours. Food delays but does not decrease absorption. Penetrates the cerebrospinal fluid.
Adult Dose: 30 mg twice daily (World Health Organisation recommendation of higher dose of 40 mg twice daily no longer recommended due to toxicity).
Take without regard to meals.
Use in Renal or Hepatic Insufficiency: Use with caution in hepatic or renal disease.
Dosage for patients with chronic kidney disease or end-stage renal disease†:
≥ 60 kg
< 60 kg
Use in Pregnancy and Breastfeeding: Category C. Excreted in breast milk is unknown. Avoid concurrent use with didanosine in pregnancy to avoid risk of lactic acidosis.
Use in Children:
US Prescribing Information Boxed Warning*: fatal and nonfatal pancreatitis has occurred and should be discontinued in anyone with suspected pancreatitis.
US Prescribing Information Boxed Warning*: lactic acidosis/hepatomegaly with steatosis has been reported with nucleoside analogues with fatal cases reported. Use with caution in patients with risk factors for liver disease and suspend treatment if a patient develops signs and symptoms. Patients should be informed of signs and symptoms of hyperlactemia and advised to consult doctor as soon as possible if they occur.
See above for pregnancy and lactation and paediatric dosing.
Peripheral neuropathy (may be reversible upon discontinuation), lipoatrophy, hyperlipidaemia, insulin resistance/diabetes mellitus, rapidly progressing ascending neuromuscular weakness (rare).
*Information from US prescribing information.
†Recommendation from South African Renal Society, 2008.