Pregabalin

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Abstract
▴ Pregabalin, the pharmacologically active S-enantiomerof 3-aminomethyl-5-methyl-hexanoic acid, has a similar pharmacological profile to that of its developmental predecessor gabapentin, but showed greater analgesic activity in rodent models of neuropathic pain. ▴ The exact mechanism of action of pregabalin is unclear, although it may reduce excitatory neuro-transmitter release by binding to the α2-δ protein subunit of voltage-gated calcium channels. ▴ Oral pregabalin at fixed dosages of 300 and 600 mg/day, administered three times daily, was superior to placebo in relieving pain and improving pain-related sleep interference in three randomised, double-blind, multicentre studies of 5–8 weeks' duration in a total of 724 evaluable patients with painful diabetic peripheral neuropathy (DPN). ▴ Significant reductions in weekly mean pain scores (primary endpoint) and sleep interference scores were observed at 1 week and sustained thereafter. A significant reduction in pain was apparent on the first day of treatment with pregabalin 300 mg/day. ▴ Twice daily fixed (600 mg/day) or flexible (150–600 mg/day) pregabalin was also effective in reducing pain and sleep interference in two 12-week placebo-controlled trials in a total of 733 randomised DPN patients. ▴ Pregabalin was well tolerated in DPN patients; mild-to-moderate dizziness, somnolence and peripheral oedema were the most common adverse events.