Drug Detail

Stavudine

Last Updated June 10, 2016

Trade Names

  • Stavudine: Zerit, Aspen Stavudine, Sonke Stavudine;
  • Lamivudine/stavudine/nevirapine: Sonke-LamNevStav, Virtrium (Aspen)

Drug Classification

Nucleoside reverse transcriptase inhibitor antiretroviral

Formulations

  • Stavudine: 15 mg, 20 mg, 30 mg, 40 mg capsules;
  • Lamivudine/stavudine/Nevirapine: 150/30/200 mg tablets

Indications and Pharmacology

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.

Dosage

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

  • Creatinine clearance > 50 mL/min: no adjustment.
  • Creatinine clearance 26-50 mL/min: 20 mg orally twice daily.
  • Creatinine clearance ≤ 25 mL/min: 20 mg daily orally.
  • Receiving haemodialysis: 20 mg daily orally (administer stavudine after haemodialysis).
  • Receiving peritoneal dialysis: unknown, use with caution.

< 60 kg

  • Creatinine clearance > 50 mL/min: no adjustment.
  • Creatinine clearance 26-50 mL/min: 15 mg orally twice daily.
  • Creatinine clearance ≤ 25 ml/min: 15 mg orally twice daily.
  • Receiving haemodialysis: 15 mg daily orally (administer stavudine after haemodialysis).
  • Receiving peritoneal dialysis: unknown, use with caution.

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:

  • > 3 months and ≤ 30 kg (off label): 1 mg/kg twice daily.
  • > 30 kg: same as adults.

Warnings

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.

Drug–Drug Interactions

  • Didanosine: coadministration should be avoided.*
  • Intracellular concentration of stavudine is inhibited with use of zidovudine; avoid concomitant use.
  • Concurrent use of drugs that cause peripheral neuropathy increases risk of neuropathy.
  • Caution required with drugs known to cause pancreatitis.

Considerations for Special Populations

See above for pregnancy and lactation and paediatric dosing.

Adverse Effects

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.