(Lyrica) Pregabalin: An antiepileptic agent useful for neuropathic pain.

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Am J Health Syst Pharm. 2007 Jul 15;64(14):1475-82.

Pregabalin: An antiepileptic agent useful for neuropathic pain.

Blommel ML, Blommel AL.

West Virginia Center for Drug and Health Information, town.

PURPOSE: The pharmacology, pharmacokinetics, clinical efficacy,

adverse effects, and dosage and administration of pregabalin are

reviewed.

SUMMARY: Pregabalin is the first drug to receive approved labeling

from the Food and Drug Administration (FDA) for the treatment of

painful diabetic neuropathy and postherpetic neuralgia and is the

first antiepileptic agent to receive FDA-approved labeling since

1999. Pregabalin is the pharmacologically active S-enantiomer of

racemic 3-isobutyl gamma-aminobutyric acid. Pregabalin has

demonstrated efficacy in the management of neuropathic pain

associated with diabetic peripheral neuropathy, postherpetic

neuralgia, and as adjunctive therapy for adult patients with partial

onset seizures. Its exact mechanism of action is unknown.

Pregabalin is rapidly absorbed and exhibits linear pharmacokinetics

after oral administration. The lack of hepatic metabolism and lack

of interaction with cytochrome P-450 isoenzymes explain the absence

of drug interactions with pregabalin. Several clinical studies have

demonstrated pregabalin's efficacy for each of the FDA-approved

indications, with dizziness and somnolence reported as the most

common adverse events.

Pregabalin has been designated as a Schedule V controlled substance

because of its potential for abuse and dependence. The starting

dosage for patients with neuropathic pain associated with diabetic

peripheral neuropathy is 50 mg three times daily and may be

increased to 300 mg daily within one week based on efficacy and

tolerability. The starting dosage for patients with partial-onset

seizures is 75 mg twice daily or 50 mg three times daily and may be

increased to 600 mg daily based on individual response and

tolerability.

CONCLUSION: Pregabalin may be beneficial for the treatment of

neuropathic pain or partial-onset seizures in patients who do not

respond to conventional treatments or cannot tolerate their adverse

effects.