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stavudine (Zerit, d4T)
Tradename: Zerit.
Indications:
- treatment of HIV1/AIDS
a) intolerant to approved therapies
b) significant clinical deterioration while receiving approved therapies
c) approved therapies contraindicated
Dosage:
1) 40 mg PO BID, or
2) 30 mg PO BID if < 60 kg
Tabs: 15, 20, 30, 40 mg. Powder for oral solution (flavored): 1 mg/mL (200 mL). Dose adjustment in renal failure:
creatinine clearance dose (>60kg) dose (<60kg)
> 50 mL/min 40 mg every 12 hours 30 mg every 12 hours
26-49 mL/min 20 mg every 12 hours 15 mg every 12 hours
10-25 mL/min 20 mg 1st every 24 hours 15 mg every 24 hours
Pharmacokinetics:
- elimination 1/2life 1-1.4 hours (5-8 hours ESRD)
Adverse effects:
1) common (> 10%)
- peripheral neuropathy*
2) less common (1-10%)
- headache, fever/chills, abdominal pain, back pain, malaise, asthenia, nausea/vomiting, diarrhea, myalgia, insomnia, anxiety, depression, pancreatitis
3) other
- elevated transaminases
- rash
- syndrome of hepatic steatosis & lactic acidosis [5]
- lipodystrophy [6]
- dyslipidemia [6]
* peripheral neuropathy may be dose-limiting
Drug interactions:
- do not use with zidovudine (AZT) [6]
Laboratory:
- stavudine in serum/plasma
Mechanism of action:
1) a thymidine analog.
2) inhibits HIV reverse transcriptase
3) d4T penetrates the blood brain barrier into the CSF
Interactions
drug interactions
drug adverse effects of antiretroviral agents
General
nucleoside reverse transcriptase inhibitor (NRTI)
Properties
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category C
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Journal Watch 20(17):137, 2000
Miller et al Ann Intern Med 133:192, 2000
- Medical Knowledge Self Assessment Program (MKSAP) 14, 17.
American College of Physicians, Philadelphia 2006, 2014