| Antiepileptic drugs: pregabalin |
Pregabalin is an analogue of gamma-aminobutyric acid (GABA) and has anticonvulsant and analgesic properties. It is thought to act by binding to voltage-gated calcium channels in the central nervous system and possibly also by reducing release of neurotransmitters including glutamate, noradrenaline and substance P. It does not appear to interact with GABA receptors nor to interfere with GABA turnover.
Pregabalin is rapidly and well absorbed upon oral administration, with absorption being delayed but not reduced by food.
Excretion is almost completely urinary (about 98%) and dose reduction is recommended when glomerular filtration rate (GFR) is less than 60 mL/min. The dose in renal impairment should be reduced proportional to the reduction in GFR (see product information for details).
Metabolism in humans is negligible and pregabalin does not appear to have any significant drug interactions. In particular, no interaction has been observed with other anticonvulsants.
The main adverse effects observed are somnolence, dizziness, blurred vision, weight gain, peripheral oedema and elevations of creatine kinase.
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