Professional Information

Stavudine

Pronunciation: (STAV-yoo-deen)
Class: Nucleoside reverse transcriptase inhibitor

Trade Names:
Zerit
- Capsules 15 mg
- Capsules 20 mg
- Capsules 30 mg
- Capsules 40 mg
- Powder for oral solution 1 mg/mL solution after reconstitution (200 mL bottle)

Pharmacology

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Inhibits replication of HIV.

Pharmacokinetics

Absorption

Stavudine is rapidly absorbed. C _max and AUC range from 0.03 to 4 mg/kg. T _max occurs 1 h after dosing.

Distribution

Stavudine distributes equally between RBCs and plasma. Protein binding ranges from 0.01 to 11.4 mcg/mL.

Elimination

Renal elimination accounts for approximately 40% of overall clearance regardless of the route of administration. Stavudine undergoes active tubular secretion as well as glomerular filtration.

Special Populations

Renal Function Impairment

Oral Cl and CrCl decreases in patients with renal insufficiency. Adjust dosage in patients with reduced CrCl and patients receiving maintenance hemodialysis.

Indications and Usage

For the treatment of HIV-1 infection in combination with other antiretroviral agents.

Contraindications

Standard considerations.

Dosage and Administration

Adults

PO 40 mg every 12 h for patients weighing at least 60 kg; 30 mg every 12 h for patients weighing under 60 kg. May be taken without regard to food.

Children

PO 1 mg/kg/dose every 12 h for patients weighing under 30 kg; give those weighing at least 30 kg the adult dosage.

Renal Function Impairment

Use drug cautiously in patients with renal function impairment. Dosage adjustment based on renal function may be required (see table).

Renal Function Impairment Dosage CrCl (mL/min) ≥ 60 kg < 60 kg > 50 40 mg every 12 h 30 mg every 12 h 26 to 50 20 mg every 12 h 15 mg every 12 h 10 to 25 20 mg every 24 h 15 mg every 24 h

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F) in a tightly closed container protected from moisture. Store solution in refrigerator. Keep bottle tightly closed. Discard any unused solution after 30 days.

Drug Interactions

Didanosine

Pancreatitis has occurred when in combination with stavudine (with or without hydroxyurea).

Zidovudine

May competitively inhibit the phosphorylation of stavudine; this combination is not recommended.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Peripheral neuropathy; headache; insomnia.

Dermatologic

Rash.

GI

Pancreatitis (may be fatal); diarrhea; nausea and vomiting; abdominal pain; anorexia.

Hematologic

Anemia; leukopenia; thrombocytopenia.

Hepatic

Lactic acidosis; hepatomegaly with hepatic steatosis.

Metabolic

AST greater than 5 times the ULN; ALT greater than 5 times ULN; amylase at least 1.4 times the ULN.

Miscellaneous

Allergic reaction; chills/fever; myalgia.

Precautions

Warnings

Pancreatitis

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.

Pregnancy

Category C .

Lactation

Undetermined; do not breast-feed.

Children

Safety and efficacy of extended-release dosage form not established.

Fat redistribution

Accumulation/redistribution of body fat including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have occurred in patients receiving antiretroviral therapy. A causal relationship has not been established.

Hemodialysis

20 mg every 24 h (patients at least 60 kg) or 15 mg every 24 h (patients less than 60 kg) administered after the completion of hemodialysis and at the same time of the day on nondialysis days.

Peripheral neuropathy

Symptoms may worsen temporarily following therapy discontinuation. If symptoms of peripheral neuropathy develop, then interrupt therapy. Symptoms may resolve if therapy is withdrawn promptly. If symptoms resolve completely, then resume therapy at 50% of the recommended dose. If neuropathy recurs after resumption of stavudine, consider permanent discontinuation. Manage clinically significant elevations of hepatic transaminases in the same way.

Patient Information

Warn patient that this drug is not to be used by itself but is combined with other antiviral agents.
Advise patient to take drug twice daily every 12 h without regard to meals.
Remind patient using solution to use measuring cup provided with drug and to shake bottle vigorously before measuring each dose.
Instruct patient to report the following symptoms immediately to the health care provider: abdominal pain; nausea; vomiting; numbness, tingling, burning, or pain in hands or feet; profound weakness or tiredness; unexpected stomach discomfort; feeling cold, dizzy, or lightheaded; slow or irregular heartbeat.
Inform patient that drug does not completely eliminate HIV virus and therefore does not reduce risk of transmitting HIV. Appropriate precautions must be followed.
Advise patient that drug is not a cure for HIV infection and that the patient may continue to acquire illnesses associated with HIV infection, including opportunistic infections and to remain under a health care provider's care.