Half-Life of Pregabalin in Normal Renal Function
The half-life of pregabalin in individuals with normal renal function is approximately 6.3 hours. 1, 2
Pharmacokinetic Properties of Pregabalin
- Pregabalin is well absorbed after oral administration with bioavailability greater than or equal to 90% that is independent of dose 1
- Following oral administration, peak plasma concentrations occur within 1.5 hours in fasting conditions 1
- When taken with food, the rate of absorption decreases (Cmax reduced by 25-30%), but the total absorption remains clinically unaffected 1, 2
- Steady state plasma concentrations are achieved within 24-48 hours of repeated administration 1, 3
- Pregabalin demonstrates highly predictable and linear pharmacokinetics across its dosing range 2, 3
Metabolism and Elimination
- Pregabalin undergoes negligible metabolism in humans with approximately 90% of the administered dose recovered in urine as unchanged drug 1
- The N-methylated derivative of pregabalin, the major metabolite found in urine, accounts for only 0.9% of the dose 1
- Pregabalin is eliminated primarily by renal excretion as unchanged drug 1, 2
- Mean renal clearance is estimated to be 67.0 to 80.9 mL/min in young healthy subjects 1
- Pregabalin clearance is nearly proportional to creatinine clearance, indicating that renal tubular reabsorption is involved in its elimination 1, 4
Clinical Implications
- The predictable pharmacokinetics and 6.3-hour half-life allow for effective twice-daily dosing in clinical practice 2, 3
- In subjects with normal renal function, urinary specimens would typically be negative for pregabalin within 5-6 days after intake 5
- The elimination half-life based on creatinine-normalized concentrations in urine is approximately 5.7-5.9 hours, consistent with plasma half-life 5
- For extended-release formulations of pregabalin, the pharmacokinetic profile maintains similar elimination characteristics with the same half-life 6
Special Considerations
- Renal function significantly impacts pregabalin clearance, with decreased clearance in patients with impaired renal function 1, 4
- Dosage adjustments are necessary for patients with creatinine clearance <60 mL/min 4
- Pregabalin is effectively removed by hemodialysis, with plasma concentrations reduced by approximately 50% following a 4-hour hemodialysis treatment 1
- Age-related decreases in renal function may necessitate dose adjustments in elderly patients 1
The consistent 6.3-hour half-life in normal renal function provides a reliable basis for dosing strategies and therapeutic monitoring in clinical practice.