Pharmacodynamics of Pregabalin

Calcium Channel Binding

Pregabalin takes affect once it binds to the calcium channels that exist on presynaptic nerve terminals. Once bound, pregabalin has the ability to inhibit the flow of calcium ions, or calcium influx, therefore preventing the release of other neurotransmitters that are known to cause the over-excitability of the nerves. A decreased release of neurotransmitters such as norepinephrine, glutamate, and substance P., allow the symptoms of nerve pain to be temporarily relieved or controlled.

It is important to understand that Pregabalin (Lyrica) does not provide a cure or overall treatment, yet the effect is to temporarily inhibit or decrease the production of neurotransmitters that predispose pain.

(Model of Pharmacodynamic of Pregabalin. Left: Hyperexcited Neuron without Pregabalin. Right. Hyperectited Neuron with Pregabalin.)