Pregabalin's Non-Renal Excretion Percentage
Less than 2% of pregabalin is excreted non-renally, as it undergoes negligible metabolism in humans and is predominantly excreted unchanged in the urine. 1
Pharmacokinetic Profile of Pregabalin
- Pregabalin exhibits highly predictable and linear pharmacokinetics with minimal metabolism, making it easy to use in clinical practice 2
- Approximately 90% of pregabalin is excreted unchanged in the urine through glomerular filtration and tubular secretion 3
- Less than 2% of pregabalin undergoes metabolism, with these metabolites being recovered in the urine 1, 2
- Pregabalin does not bind to plasma proteins and is not subject to hepatic metabolism 2
- The drug does not induce or inhibit liver enzymes such as the cytochrome P450 system 2
Clinical Implications of Pregabalin's Excretion Profile
- Due to its predominantly renal elimination, pregabalin clearance is directly proportional to creatinine clearance 3
- Dosage adjustment is necessary in patients with renal impairment (creatinine clearance <60 mL/min) 3, 2
- A 50% reduction in pregabalin daily dose is recommended for patients with creatinine clearance between 30-60 mL/min compared to those with normal renal function 3
- Further dose reductions (approximately 50%) are needed for each additional 50% decrease in creatinine clearance 3
- Pregabalin is highly cleared by hemodialysis, potentially requiring supplemental doses after dialysis sessions 3
Pharmacokinetic Parameters
- Pregabalin is rapidly absorbed following oral administration, with peak plasma concentrations occurring between 0.7 and 1.3 hours 4
- The drug has high oral bioavailability of approximately 90%, which is independent of dose 4
- Elimination half-life is approximately 6.3 hours in subjects with normal renal function 2
- Steady state is achieved within 24-48 hours of repeated administration 2, 4
- Food reduces the rate but not the extent of pregabalin absorption, allowing administration without regard to meals 4
Drug Interaction Potential
- Due to its minimal metabolism and lack of protein binding, pregabalin has a low potential for pharmacokinetic drug-drug interactions 1, 2
- In vitro and in vivo studies have confirmed that pregabalin is unlikely to be involved in significant pharmacokinetic interactions with other medications 1
- No pharmacokinetic interactions have been observed between pregabalin and commonly used antiepileptic drugs including carbamazepine, valproic acid, lamotrigine, phenytoin, phenobarbital, and topiramate 1