Pregabalin--a neuromodulator for the treatment of neuropathic pain, generalized

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Med Monatsschr Pharm. 2007 Nov;30(11):396-400.

Pregabalin--a neuromodulator for the treatment of neuropathic pain,

generalized anxiety disorders and fibromyalgia syndrome

Nymdelger S, Nieber K.

Universität Leipzig, Institut für Phamazie, Leipzig.

Synthesized in 1990 as an anticonvulsant agent, pregabalin was

designed as a lipophilic gamma-aminobutyric acid (GABA) analog

substituted at the 3'-position in order to facilitate diffusion

across the blood-brain barrier. It is an alpha2delta1 ligand that

binds to, and modulates, voltage-gated calcium channels. This

modulation is characterized by a reduction of the excessive

neurotransmitter release that is observed in certain neurologic and

psychotic disorders.

Pregabalin has analgetic, anticonvulsant, and anxiolytic activity

and has demonstrated efficacy in the management of neuropathic pain

associated with diabetic peripheral neuropathy, postherpetic

neuralgia, and as adjuvant therapy for adult patients with partial

onset seizures. Pregabalin was significantly more effective than

placebo for the treatment of generalized anxiety disorder as well as

of fibromyalgia and was well tolerated by most of the patients.