Pregabalin is widely used as a analgesic compound for the treatment of neuropathic pain. In this study using a animal model researchers studied pregabalin's antipain mechanisms and assessed the effectiveness of pregabalin in a model using mechanical and cold hypersensitivity.  In general the idea about its mechanism of action is, that both gabapentin and pregabalin inhibit Ca(2+) currents via high-voltage-activated channels containing the alpha2delta1 subunit, thus reducing neurotransmitter release and attenuating the postsynaptic excitability.

Mechanism of action of pregabalin broadend 

This mechanism of action can be broadend due to the following.

The researchers administered systemic or intrathecal pregabalin  and found that pregabalin successfully decreased mechanical as well as cold hypersensitivity, as a pretreatment, not post treatment. The administration of pregabalin was also effective in reducing the behavioral hypersensitivity,

Furthertmore pregabalin's effects at inhibiting hind paw formalin-induced nociception in rats and formalin-induced release of excitatory amino acids (EAAs) in the spinal cord dorsal horn (SCDH) both in  rats as well as in rats with neuropathic pain.

Pregabalin dose-dependently reduced nociceptive scores and pregabalin reduces the formalin-induced release of the neurotransmittor glutamate in SCDH.

These models show that pregabalin might also reduce neuropathic pain by inhibiting the release of glutamate in the SCDH. That would be an additional mechanism of action. ^[1]

Centre for the study and treatment of neuropathic pain and neuropathy in Soest, the Nertherlands

This site helps patients and treating physicians, neurologists, anesthesiologists and other pain specialists to find the best and most up to date research findings related to neuropathy and neuropathic pain and the treatment thereof.

In our centre we are specialised in treating patients suffering from neuropathic pain and neuropathy following an Integrated Medicine concept. Part of our activities are within the field of consultation. We assist pharmaceutical companies in R&D strategies related to finding new drugs to treat neuropathic pain and neuropathy.

February 2010, Jan M. Keppel Hesselink, MD, PhD.

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