What is the half-life of Lyrica (pregabalin)?

Half-Life of Lyrica (Pregabalin)

The half-life of Lyrica (pregabalin) is approximately 6.3 hours in adults with normal renal function. 1

Pharmacokinetic Profile of Pregabalin

Pregabalin has a predictable and linear pharmacokinetic profile that makes it relatively straightforward to use in clinical practice:

• Absorption: Pregabalin is rapidly absorbed following oral administration

  • Peak plasma concentrations occur within 1.5 hours after administration 1
  • Oral bioavailability is ≥90% and is independent of dose 1
  • Food decreases Cmax by 25-30% and increases time to peak concentration to approximately 3 hours, but does not affect the total absorption 1

• Distribution:

  • Does not bind to plasma proteins 1
  • Apparent volume of distribution is approximately 0.5 L/kg 1

• Metabolism and Elimination:

  • Undergoes negligible metabolism in humans 1
  • Approximately 90% of the administered dose is recovered in urine as unchanged pregabalin 1
  • Mean elimination half-life is 6.3 hours in subjects with normal renal function 1
  • Elimination is nearly proportional to creatinine clearance 1

Important Clinical Considerations

Population-Specific Variations in Half-Life

1. Renal Impairment:

   • Pregabalin clearance is nearly proportional to creatinine clearance
   • Dosage reduction is necessary in patients with renal dysfunction 1
   • Hemodialysis effectively removes pregabalin from plasma (approximately 50% reduction after 4-hour treatment) 1

2. Age-Related Differences:

   • Elderly: Pregabalin oral clearance tends to decrease with increasing age, consistent with age-related decreases in creatinine clearance 1
   • Pediatric patients: Half-life is shorter in children
     • 3-4 hours in pediatric subjects up to 6 years of age
     • 4-6 hours in those 7 years and older 1

3. Other Factors:

   • No significant differences in pharmacokinetics based on race or gender 1

Clinical Implications of Pregabalin's Half-Life

• The 6.3-hour half-life allows for twice or three times daily dosing regimens
• Steady state is achieved within 24-48 hours after starting treatment 1
• Multiple-dose pharmacokinetics can be predicted from single-dose data 1

Potential Pitfalls in Clinical Practice

1. Renal Function Assessment: Always assess renal function before prescribing pregabalin, as dosage adjustments are necessary in patients with impaired renal function.

2. Drug Accumulation: Despite its relatively short half-life, pregabalin can accumulate in patients with renal impairment if not properly dose-adjusted.

3. Withdrawal Symptoms: The relatively short half-life means that abrupt discontinuation may lead to withdrawal symptoms. Always taper pregabalin gradually when discontinuing.

4. Pediatric Dosing: Remember that children have faster clearance and shorter half-life, requiring weight-based dosing to achieve similar exposures to adults 1.

Pregabalin's predictable pharmacokinetics with minimal metabolism, lack of protein binding, and primarily renal elimination make it a medication with relatively few pharmacokinetic drug interactions, though its dosing must be carefully adjusted in patients with renal impairment.