Pregabalin: a new neuromodulator with broad therapeutic indications.
OBJECTIVE
To review pregabalin's pharmacology, pharmacokinetics, efficacy, and adverse effects in the treatment of neuropathic pain, epilepsy, and anxiety.


METHODS
A MEDLINE search (1993-October 2005) for peer-reviewed English-language publications was performed. Abstracts from professional meetings were also included. Key terms were anxiety, diabetic neuropathy, epilepsy, neuropathic pain, postherpetic neuralgia, pregabalin, and seizures.


METHODS
Basic pharmacology data were extracted from animal studies; pharmacokinetic data were extracted from human studies. Multicenter, double-blind, placebo-controlled, parallel-group studies were included to describe the efficacy and adverse effects of pregabalin.


RESULTS
Pregabalin is a new agent that exerts its pharmacodynamic effect by modulating voltage-gated calcium channels. Pregabalin has a linear pharmacokinetic profile. It is completely absorbed, not bound to plasma proteins, not metabolized, and eliminated unchanged through the kidneys. Doses must be adjusted in patients with renal insufficiency. Clinical trials showed that pregabalin is effective in neuropathic pain associated with postherpetic neuralgia, diabetic peripheral neuropathy, in partial epilepsy as adjunctive therapy, and in generalized and social anxiety disorders. The most common adverse effects were dizziness and somnolence. Few serious adverse effects were reported. Pregabalin should not be discontinued rapidly.


CONCLUSIONS
Pregabalin is an effective and safe analgesic, antiepileptic, and anxiolytic medicine. It will provide a new treatment option for patients with neuropathic pain and partial epilepsy.
Shneker
Bassel F
BF
Department of Neurology, College of Medicine, Ohio State University, Columbus, 43210, USA.
McAuley
James W
JW
D000379:Agoraphobia / Q000188:drug therapy / Q000523:psychology; D001007:Anxiety / Q000188:drug therapy*; D003929:Diabetic Neuropathies / Q000188:drug therapy / Q000473:pathology; D004827:Epilepsy / Q000188:drug therapy*; D006566:Herpesviridae Infections / Q000150:complications; D006801:Humans; D015337:Multicenter Studies as Topic; D009437:Neuralgia / Q000150:complications; D018377:Neurotransmitter Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010146:Pain / Q000188:drug therapy* / Q000209:etiology; D010523:Peripheral Nervous System Diseases / Q000150:complications*; D000069583:Pregabalin; D016032:Randomized Controlled Trials as Topic; D012640:Seizures / Q000188:drug therapy / Q000209:etiology; D005680:gamma-Aminobutyric Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use
D018377:Neurotransmitter Agents; D000069583:Pregabalin; D005680:gamma-Aminobutyric Acid