STAVUDINE (D4T)

STAVUDINE (D4T)
(sta'vu-deen)
Zerit
Classifications: antiretroviral; nucleoside reverse transcriptase inhibitor (nrti);
Therapeutic: antiretroviral; nrti

Prototype: Lamivudine
Pregnancy Category: C

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 25–50 mL/min: reduce dose by 50% (also in patients with peripheral neuropathy)

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: 1–1.6 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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