Pregabalin

Information about Pregabalin

Pregabalin is an inhibitor of neuronal activity used for therapy of neuropathy and as an anticonvulsant. 

Pregabalin Structural Formulae

Lyrica lääkepakkauksia

Liver safety of Pregabalin

Therapy with pregabalin is not associated with serum aminotransferase elevations, and clinically apparent liver injury from pregabalin has been reported but appears to be quite rare. 

Mechanism of action of Pregabalin

Pregabalin (pre gab' a lin) is a structural analogue of gamma-aminobutyric acid (GABA) but is novel in its activity, having no effects on GABA-A or GABA-B receptors.  Instead, the neuronal acitivity of pregabalin appears to be mediated by its binding to the alpha-2-delta subunit of the presynaptic voltage-gated calcium channel whcih leads to a decrease in release of neuroexcitatory neurotransmitters by hyperexcited neurons.  Pregabalin has been shown to be effective in reducing neuropathic pain from diabetic and postherpetic neuropathy and is an effective anticonvulsant. 

FDA approval information for Pregabalin

Pregabalin was approved for use in the United States in 2004.  Current indications include diabetic and post-herpetic neuropathy and as adjunctive therapy of partial onset seizures.  Pregabalin is also used for fibromyalgia and off-label for generalized anxiety disorders and migraine.

Dosage and administration for Pregabalin

Pregabalin is available in capsules in varying concentrations from 25 to 300 mg under the brand name of Lyrica.  The recommended initial dose for neuropathic pain is 50 to 75 mg two to three times daily, the maximum dose being 300 mg daily.  Higher doses are used in treating seizures. The dose should be increased and tapered gradually. 

Side effects of Pregabalin

The most common side effects of pregabalin are dose related and include peripheral edema, weight gain, dizziness, somnolence, confusion, headache, blurred vision, tremor and ataxia.

• Dailymed label info on Pregabalin
• FDA Pregabalin