Products
Stavudine is commercially available in capsule form (Zerit). It has been approved in many countries since 1996.
Structure and properties
Stavudine (C10H12N2O4, Mr = 224.2 g/mol) is a thymidine analog with a missing 3′-hydroxy group. It is a prodrug that is biotransformed intracellularly to the active metabolite stavudine triphosphate. Stavudine exists as a white powder that is soluble in water.
Effects
Stavudine (ATC J05AF04) has antiviral properties against HIV. The effects are due to inhibition of the viral enzyme reverse transcriptase, which transcribes viral RNA into DNA and is important in viral replication. The activated agent is incorporated into DNA and leads to chain termination.
Indications
For treatment of infection with HIV as part of combination antiretroviral therapy.
Dosage
According to the SmPC. The drug is usually taken twice daily and preferably fasting, one hour before meals.
Contraindications
Stavudine is contraindicated in case of hypersensitivity. For complete precautions, see the drug label.
Interactions
Drug-drug interactions are possible with drugs that are also tubular secreted and with zidovudine, doxorubicin, and ribavirin. In combination with hydroxyurea and didanosine, inflammation of the pancreas (pancreatitis) may occur. Therefore, concomitant treatment is not recommended.
Adverse effects
The most common possible adverse effects include headache, diarrhea, neuropathy, rash, nausea, and vomiting. Stavudine may rarely cause dangerous lactic acidosis and liver enlargement.
