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Zerit

Clinical Pharmacology
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Clinical Pharmacology

Zerit

Binding of stavudine to serum proteins was negligible over the concentration range of 0.01 to 11.4 µg/mL. Stavudine distributes equally between red blood cells and plasma. Volume of distribution is shown in Table 2.

Metabolism

The metabolism of stavudine has not been elucidated in humans.

Elimination

In humans, renal elimination accounts for about 40% of the overall clearance regardless of the route of administration (Table 2). The mean renal clearance was about twice the average endogenous creatinine clearance, indicating active tubular secretion in addition to glomerular filtration. The remaining 60% of the drug is presumably eliminated by endogenous pathways.

Table 2: Pharmacokinetic Parameters of Stavudine in HIV-Infected Adults: Bioavailability, Distribution, and Clearance

Parameter Mean ±SD n
Oral bioavailability (%) 86.4 ± 18.2 25
Volume of distribution (L)a 46 ±21 44
Total body clearance (mL/min)a 594 ± 164 44
Apparent oral clearance (mL/min)b 560 ± 182c 113
Renal clearance (mL/min)a 237 ± 98 39
Elimination half-life, IV dose (h)a 1.15 ± 0.35 44
Elimination half-life, oral dose (h)b 1.6 ±0.23 8
Urinary recovery of stavudine (% of dose)a,d 42 ± 14 39
a following 1-hour IV infusion.
b following single oral dose.
c assuming a body weight of 70 kg.
d over 12-24 hours.

Special Populations

Pediatric

For pharmacokinetic properties of stavudine in pediatric patients see Table 3.

Table 3: Pharmacokinetic Parameters (Mean ± SD) of Stavudine in HIV-Exposed or -Infected Pediatric Patients

Parameter Ages 5 weeks to 15 years n Ages 14 to 28 days n Day of Birth n
Oral bioavailability (%) 76.9 ±31.7 20 ND   ND  
Volume of distribution (L/kg)a 0.73 ±0.32 21 ND   ND  
Ratio of CSF: plasma concentrations (as %)b 59 ±35 8 ND   ND  
Total body clearance(mL/min/kg)a 9.75 ±3.76 21 ND   ND  
Apparent oral clearance(mL/min/kg)c 13.75 ±4.29 20 11.52 ±5.93 30 5.08 ± 2.80 17
Elimination half-life, IV dose (h)a 1.11 ±0.28 21 ND   ND  
Elimination half-life, oral dose (h)c 0.96 ±0.26 20 1.59 ±0.29 30 5.27 ± 2.01 17
Urinary recovery of stavudine(% of dose)c,d 34 ±16 19 ND   ND  
a following 1-hour IV infusion.
b at median time of 2.5 hours (range 2-3 hours) following multiple oral doses.
c following single oral dose.
d over 8 hours.ND = not determined.

Renal Impairment
Brand Name: Zerit
Generic Name: Stavudine
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