The Chemical Structure Of Pregabalin

1996 Words Apr 15th, 2015 8 Pages
Introduction Pregabalin, trade name Lyrica, approved for its anticonvulsant properties and to relieve pain in those who suffer from diabetic neuropathy. The chemical structure of pregabalin is structurally analogous to γ-aminobutyric acid (GABA), an inhibitory neurotransmitter found in the central nervous system and functions by binding to α2δ voltage-gated calcium ion channel in presynaptic, inhibiting the release of neurotransmitters, most notably GABA. By decreasing the amount of the inhibitory neurotransmitter GABA in synaptic terminals, epileptic seizures can be controlled and prevented.1
Each drug displays its own properties when introduced to the body and all traits must be evaluated to observe effectiveness and side effects that may occur. Pregabalin, although structurally and functionally similar to gabapentin (trade name Neurontin), has been shown to be more potent and exhibits linear kinetic properties, unlike gabapentin. Some factors that contribute to its success are that it has a bioavailability of 90%, 98% is excreted in urine unchanged, thus no or few side reactions occur, and it is able to pass through the blood-brain barrier. Beneficial effects of taking pregabalin can be observed in as little as 2 days of administration, unlike most other central nervous system drugs, which typically take effect.1
Pregabalin is prescribed to treat conditions such as epilepsy and diabetic neuropathy. In addition, pregabalin has been approved for the treatment of…
Open Document