Activity profile of pregabalin in rodent models of epilepsy and ataxia

The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential

“…Gabapentin and pregabalin are effective in several models of anticonvulsant action (Welty et al, 1993;Vartanian et al, 2006). By contrast, pregabalin did not reduce the incidence of spontaneous absence seizures in a genetic rat model of absence seizures (Vartanian et al, 2006). The effect of these drugs in several epilepsy models has been shown to result from binding to a 2 d-1, rather than a 2 d-2 (Lotarski et al, 2014), although there was no widespread upregulation of brain a 2 d-1 in two epilepsy models studied (Nieto-Rostro et al, 2014).…”

“…Seizure Models. Gabapentin and pregabalin are effective in several models of anticonvulsant action (Welty et al, 1993;Vartanian et al, 2006). By contrast, pregabalin did not reduce the incidence of spontaneous absence seizures in a genetic rat model of absence seizures (Vartanian et al, 2006).…”

New horizons in the development of antiepileptic drugs: Innovative strategies

“…Gabapentin and pregabalin show a similar spectrum of activity in animal models that is distinct from that of other AEDs, suggesting that they share a common mechanism of action (Vartanian et al, 2006). Recently, converging lines of evidence have pointed to the α 2 -δ proteins as critical targets for the anticonvulsant effects of both drugs.…”

Monitoring of Pregabalin in Pharmaceutical Formulations and Human Serum Using UV and RP-HPLC Techniques: Application to Dissolution Test Method

“…does not react with potassium channels, or glutamate receptors, nor does it block calcium channels rather makes amendment with calcium channels [2,4]. Its lowest effective dose is 150 mg/day.…”

“…A2δ ligands are used for the treatment of pain of diabetic neuropathy and postherpetic neuralgia [1]. In the United States it is the latest addition to the antiepileptic medication, approved by FDA in 2005 for partial epilepsy, painful diabetic polyneuropathy, postherpetic neuralgia and fibromyalgia [1][2][3][4].…”