pregabalin
Meaning of pregabalin: Designed around the shape of a calming brain chemical, yet it works nowhere near that chemical's receptors.
Definition of pregabalin
Pregabalin is a medicine used for nerve-related pain, as an add-on treatment for certain seizures, and for fibromyalgia and, in some countries, generalized anxiety disorder. It is built on the chemical skeleton of GABA, a natural calming messenger in the nervous system, but it does not act at GABA receptors and works by a separate route.
How does it work?
Nerve cells release their chemical messengers when calcium flows in through channels in the cell membrane. Pregabalin attaches to a particular part of those channels, the alpha-2-delta subunit, and reduces how much calcium enters when the nerve fires. Less calcium means less release of the messengers that carry pain and excitation signals onward, among them glutamate and substance P. The effect is largest where nerves are already firing excessively, which is why the drug damps down abnormal signaling more than normal traffic. This mechanism explains the shared name with gabapentin, a close relative acting at the same site.
What is it used for?
| Use | What is being treated |
|---|---|
| Neuropathic pain | Burning or shooting pain from damaged nerves, as in diabetes or shingles |
| Partial seizures | Added to other antiseizure treatment rather than used alone |
| Fibromyalgia | Widespread pain with disturbed sleep and sensitivity to touch |
| Generalized anxiety disorder | Approved for this in some countries and not in others |
Ordinary pain from injury or inflammation responds differently, since the drug acts on nerve signaling rather than on the tissue damage producing it.
What accompanies its use?
Because it acts across the nervous system rather than at one site, drowsiness, dizziness, unsteadiness, blurred vision, swelling of the ankles and weight gain are the effects reported most often, and they are more pronounced early and at higher doses. The drug is cleared almost entirely by the kidneys, so impaired kidney function raises the level in the body considerably. Pregabalin also carries a potential for misuse and dependence that was not recognized when it was introduced, and it has since been placed under legal control as a scheduled medication in a number of countries. Stopping it abruptly after regular use can produce withdrawal symptoms including insomnia, sweating, nausea and anxiety.
Used in a sentence
Pregabalin was prescribed for management of the patient's neuropathic pain.
Good to know
Pregabalin is built on the structure of GABA but does not act at GABA receptors, and it is now recognized to carry a potential for misuse and dependence, which led to legal controls on its supply in several countries.