NURIKA Hard capsule Ref.[50571] Active ingredients: Pregabalin

Absorption

Pregabalin is absorbed after oral administration in the fasted state. Peak plasma concentrations are achieved within 1 hour and is independent of dose. Pregabalin oral bioavailability is estimated to be ≥90% and is independent of dose. After repeated administration, steady state is achieved within 24 to 48 hours.

Distribution

The apparent volume of distribution of pregabalin following oral administration is approximately 0,56 l/kg. Pregabalin is not bound to plasma proteins.

Metabolism

Pregabalin undergoes negligible metabolism. About 98% of the unchanged pregabalin is recovered in the urine.

Elimination

Pregabalin is eliminated primarily unchanged by renal excretion. Pregabalin has a mean elimination half-life of 6,3 hours. Pregabalin plasma clearance and renal clearance are directly proportional to creatinine clearance (see section 5.2 – Pharmacokinetics in Special Patient Groups – Renal impairment). Dosage adjustment in patients with reduced renal function or undergoing haemodialysis is necessary (see section 4.2 – Table 1).

Linearity / non-linearity

Pregabalin pharmacokinetics are linear over the recommended daily dose range. Inter-subject pharmacokinetic variability for pregabalin is low (<20%). Multiple dose pharmacokinetics are predictable from single-dose data. Therefore routine monitoring of plasma concentrations of pregabalin is not necessary.

Pharmacokinetics in special patient groups

Renal impairment

Pregabalin clearance is directly proportional to creatinine clearance. Pregabalin is effectively removed from plasma by haemodialysis (following a 4 hour haemodialysis treatment, plasma pregabalin concentrations are reduced by approximately 50%). Because renal elimination is the major elimination pathway, a dosage reduction in patients with renal impairment and dosage supplementation following haemodialysis is necessary (see section 4.2 – Table 1).

Hepatic impairment

Since pregabalin does not undergo significant metabolism and is excreted unchanged in the urine, impaired liver function would not be expected to significantly alter pregabalin plasma concentrations.

Elderly (over 65 years of age)

Pregabalin clearance tends to decrease as age increases. This decrease in pregabalin oral clearance is consistent with decreases in creatinine clearance associated with increasing age. Reduction of the dose of pregabalin may be required in patients who have age related compromised renal function (see section 4.2 – Table 1).