STAVUDINE (D4T) (sta'vu-deen)
Zerit Classifications: antiretroviral; nucleoside reverse transcriptase inhibitor (nrti); Therapeutic: antiretroviral; nrti Prototype: Lamivudine Pregnancy Category: C
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Availability
15 mg, 20 mg, 30 mg, 40 mg capsules; 1 mg/mL solution
Action
Synthetic analog of thymidine (a major nucleoside in DNA) with antiviral action against HIV, the causative agent of AIDS.
Phosphorylated to stavudine triphosphate by endogenous thymidine kinase. Appears to act by being incorporated into the growing
DNa chains by viral transcriptase, thus terminating viral replication.
Therapeutic Effect
Inhibits the replication of HIV in human cells and decreases the viral load.
Uses
Treatment of adults with advanced HIV infection who are intolerant of other antiretroviral agents (zidovudine, didanosine,
zalcitabine) or who have deteriorated on the other agents.
Contraindications
Hypersensitivity to stavudine; pregnancy (category C), lactation.
Cautious Use
Previous hypersensitivity to zidovudine, didanosine, or zalcitabine; folic acid or B12 deficiency; liver and renal insufficiency; alcoholism; peripheral neuropathy; history of pancreatitis.
Route & Dosage
Advanced HIV Infection Adult: PO <60 kg, 30 mg q12h; ≥60 kg, 40 mg q12h Child: PO <30 kg, give 2 mg/kg/d in 2 divided doses; ≥30 kg, same as adult
Renal Impairment Clcr 2550 mL/min: reduce dose by 50% (also in patients with peripheral neuropathy)
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Administration
Oral
- Adhere strictly to 12-h interval between doses.
- Reconstitute powder by adding 202 mL of water to the container. Shake vigorously. Yields 200 mL of 1 mg/mL solution.
- Store at room temperature, 15°30° C (59°86° F).
Adverse Effects (≥1%)
CNS: Peripheral neuropathy, paresthesias.
GI: Anorexia, nausea, vomiting, diarrhea, cramping, pancreatitis, abdominal pain, elevated liver function tests, abdominal pain.
Body as a Whole: Headache, chills/fever,
myalgia. Hematologic: Anemia, neutropenia.
Skin: Rash. Metabolic: Lactic acidosis in pregnant women.
Interactions
Drug: Didanosine may increase risk of pancreatitis and hepatotoxicity;
probenecid can decrease elimination.
Pharmacokinetics
Absorption: Readily absorbed from GI tract; 82% reaches systemic circulation.
Peak: Effect 6 wk.
Distribution: Distributes into CSF; excreted in breast milk of animals.
Metabolism: Metabolized in liver; in addition to hepatic metabolism, some investigators suggest that degradation and salvage by other
pyrimidine pathways may contribute to elimination; intracellularly, stavudine is phosphorylated by cellular enzymes to its
active triphosphate form.
Elimination: Primarily in urine.
Half-Life: 11.6 h.
Nursing Implications
Assessment & Drug Effects
- Monitor for peripheral neuropathy and report numbness, tingling, or pain, which may indicate a need to interrupt stavudine.
- Lab tests: Monitor liver enzymes, CBC with differential, PT and INR, and kidney function periodically.
- Monitor for development of opportunistic infection.
Patient & Family Education
- Take drug exactly as prescribed.
- Report to physician any adverse drug effects that are bothersome.
- Report symptoms of peripheral neuropathy to physician immediately.