Stavudine information from DrugsUpdate
L - Contraindicated in lactation
Stavudine (2'-3'-didehydro-2'-3'-dideoxythymidine, d4T, brand name Zerit) is a nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV.
Stavudine is converted intracellularly to the active metabolite stavudine 5'-triphosphate which is then incorporated into the viral DNA by reverse transcriptase resulting in premature ending of the DNA chain elongation.
Rapidly absorbed from the GI tract after oral admin, food may delay its absorption; peak plasma concentrations within 1 hour.
Crosses the blood-brain barrier and negligible plasma protein binding.
Intracellular; converted to the active antiviral triphosphate.
Urine (about 40%); 1.5 hours (elimination half-life).
Headache, nausea, vomiting, asthenia, chest pain, influenza-like syndrome, insomnia, abdominal pain, anorexia, neutropenia, thrombocytopenia, arthralgia, myalgia, mood changes, dyspnoea, pharyngitis, skin rashes, pruritus.
Fatal and nonfatal cases have occurred in combination with didanosine with or without hydroxyurea.
Lactic Acidosis and Hepatomegaly
Reported with steatosis (including fatal cases) with the use of nucleoside analogues alone or in combination. Reported in pregnant women who have received didanosine and stavudine with other antiretroviral agents. Use the combination with caution in pregnant women.
Chronic overdosage may lead to peripheral neuropathy and hepatic toxicity.
Hepatomegaly or other risk factors for liver disease. History of peripheral neuropathy and renal impairment. Pregnancy. Discontinue treatment if peripheral neuropathy develops; may resume treatment at half the previous dose if symptoms resolve upon drug withdrawal. Monitor for signs of pancreatitis. Discontinue treatment if there is a rapid increase in aminotransferase concentrations, progressive hepatomegaly or steatosis, or metabolic or lactic acidosis. Increased risk of severe and fatal hepatic adverse events in patients with chronic hepatitis B or C treated with combination antiretroviral therapy.
Antiviral effect inhibited by zidovudine, doxorubicin and ribavirin. Avoid concurrent admin with drugs that cause pancreatitis (e.g. IV pentamidine) or peripheral neuropathy (e.g. metronidazole, isoniazid and vincristine). Increased risk of adverse effects such as hepatoxicity, peripheral neuropathy and pancreatitis if used with hydroxycarbamide and didanosine.
Adult: <60: 30 mg; ≥60 kg: 40 mg. Doses to be taken every 12 hours.
Child: From birth-13 days old: 500 mcg/kg; ≥14 days old and weighing <30 kg: 1 mg/kg; 30 kg-<60 kg: 30 mg; ≥60 kg: 40 mg. Doses to be taken every 12 hours.
CrCl (ml/min) Dosage Recommendation
26-50 <60 kg: 15 mg; ≥60 kg: 20 mg. Doses to be taken every 12 hours.
<25 <60 kg: 15 mg; ≥60 kg: 20 mg. Doses to be taken every 24 hours.
May be taken with or without food
List of Contraindications
Caution when used during pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindicated in lactation
Safety and efficacy of extended-release dosage form not established
Clinical studies of stavudine did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently than younger patients. Greater sensitivity of some older individuals to the effects of stavudine cannot be ruled out.
Store at 25°C