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Monday, November 28, 2011

STAVUDINE (d4T)

Antiviral Activity

Used in the treatment of HIV-1 infection in combination with at least two additional antiretroviral agents
Active against susceptible HIV strains

Pregnancy Risk Factor

Category C

Contraindication/Precaution

Hypersensitivity to stavudine or to any of its components
HIV-infected mothers should not breast-feed in order to avoid transmission to a non-infected newborn
Do not use in the presence of bone marrow depression
Use caution in the presence of impaired liver/renal function
Use caution in the presence of peripheral Neuropathy, lactic acidosis/severe hepatomegaly with Steatosis

Mechanism of Action

Inhibits viral DNA synthesis by causing DNA chain termination because stavudine lacks the 3'-hydroxyl group necessary for DNA elongation
Also inhibits cellular DNA polymerase beta and gamma, and markedly reduces the synthesis of mitochondrial DNA

Pharmacodynamics/Kinetics

Metabolism: 
Not elucidated yet in humans
Half-life: 
1.25 hours
Elimination: 
Renal (40%)

Dosage

Children : 

< 30 kg of body weight: 1 mg/kg PO q12h 30-60 kg of body weight:  30 mg PO bid Adults:   < 60 kg of body weight: 30 mg PO bid   ³ 60 kg of body weight: 40 mg PO bid Dosage In Renal Failure Creatinine clearance (ml/min): 10-25: 20 mg PO q24h (15 mg if less then 60 kg) 26-50: 20 mg PO q12h (15 mg if less then 60 kg) >50: unchanged
Dialysis
Hemo: 20 mg q24h (³60 kg) or 15 mg q24h (<60 kg)
CAPD: N/A

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