What is "pregabalin"

n. An anticonvulsant drug used for neuropathic pain and as an adjunct therapy for seizures.

Pregabalin (PGN) marketed under the brand name Lyrica among others, is a medication used to treat epilepsy, neuropathic pain, fibromyalgia, and generalized anxiety disorder. Its use for epilepsy is as an add-on therapy for partial seizures with or without secondary generalization in adults. Some off-label uses of pregabalin include restless leg syndrome, prevention of migraines, social anxiety disorder, and alcohol withdrawal.

Common side effects include: sleepiness, confusion, trouble with memory, poor coordination, dry mouth, problem with vision, and weight gain. Potentially serious side effects include angioedema, drug misuse, and an increased suicide risk. Taken at high doses or for a long period of time, pregabalin is known to be moderately addictive. It may induce a state of both physical and psychological dependence, but taken at therapeutic doses the liability of addiction is low.

Pregabalin is a derivative of the inhibitory neurotransmitter GABA, also known as gamma-Aminobutyric acid. Pregabalin is a potent gabapentinoid and a close structural analogue of GABA. Pregabalin binds with high affinity to the αδ subunit-containing voltage-gated calcium channels (VDCC) and neural GABA concentrations increase because of the activity of the L-Glutamic acid decarboxylase (GAD) enzyme; which converts glutamate into GABA. In addition to its effects on GABA-AT substrate behavior, pregabalin blocks glutamate release. GABA is potentiated, but through a different mechanism. Continued application of pregabalin increases the density of GABA transporter proteins and increases the rate of functional GABA transport. This binding site has been referred to as the gabapentin receptor or gabapentin site ( αδ subunit), as it is the target of the related drug gabapentin.

Parke-Davis developed pregabalin as a successor to gabapentin and was brought to market by Pfizer after the company acquired Warner-Lambert. There is to be no generic version available in the United States until 2018. A generic version is available in Canada and the United Kingdom. In the US it costs about 300-400 USD per month.