Pregabalin pharmacokinetics

Oxycodone/Lorazepam/Ethanol Multiple oral doses of pregabalin were coadministered with oxycodone, lorazepam, or ethanol. Although no pharmacokinetic interactions were seen, additive effects on cognitive and gross motor functioning were seen when pregabalin was coadministered with those drugs. 

There appears to be no pharmacokinetic interaction between pregabalin and carbamazepine, gabapentin, lamotrigine, phenobarbital, phenytoin, topiramate, valproate, alcohol, lorazepam, or oxycodone. However, the impairment of cognitive and gross motor function caused by oxycodone was additive with pregabalin, and pregabalin may potentiate the effects of alcohol and lorazepam. 

The manufacturer notes that there was no clinically relevant pharmacokinetic interaction between pregabalin and lorazepam or alcohol, and that concurrent use caused no clinically important effect on respiration. However, they note that pregabalin may potentiate the effects of lorazepam and alcohol. ... 

Brodie MJ, Wilson EA, Wesche DL, Alvey CW, F dinitis EJ, Posvar EL, Hounslow NJ, Bron NJ, Gibson GL, Bockbrader HN Pregabalin drug intemction studies lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and val M oate in patients with p ial epilepsy. Epilepsia (2005) 46, 1407-13. 

Pregabalin does not appear to affect the pharmacokinetics or contraceptive efficacy of ethinyiestradioi or norethisterone. In addition, the pharmacokinetics of pregabaiin were not affected by the contraceptive steroids. 

A study in 16 subjects found that pregabalin 200 mg every 8 hours had no effect on the pharmacokinetics of ethinylestradiol or norethisterone taken as a combined oral contraceptive (Orthonovum) and did not reduce the contraceptive effect as measured by progesterone levels. Neither contraceptive steroid had an effect on the pharmacokinetics of pregabalin. No special contraceptive precautions therefore appear to be required during concurrent use. 

The bio availability of gabapentin is approximately 60%, 47%, 34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day given in three divided doses, respectively. The bioavailability is not dose-proportional (as the dose is increased, bioavailability decreases). In contrast, pregabalin offers a more linear pharmacokinetic profile over gabapentin and a consistent >90% bioavailability. Pregabalin may result in a shorter course of titration and quicker response in clinical application. 

Pregabalin displays linear pharmacokinetics across its therapeutic range and has high bioavailabihty resulting in predictable dose-dependent responses. 

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