Pregabalin

doi:10.2165/00003495-200464240-00006

Paper

Pregabalin

Published 2012 · J. Frampton, L. Scott

Drugs

Q1 SJR score

108

Citations

1

Influential Citations

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Abstract

Pregabalin, the pharmacologically active S-enantiomer of 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 neurotransmitter release by binding to the alpha2-delta 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.

RCT

Large Human Trial

Highly Cited

Study Snapshot

Pregabalin effectively reduces pain and sleep interference in diabetic peripheral neuropathy patients, with mild-to-moderate side effects.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Pregabalin

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References

The Biology and Pharmacology of Calcium Channel α2-δ Proteins Pfizer satellite symposium to the 2003 Society for Neuroscience Meeting Sheraton New Orleans Hotel New Orleans, LA November 10, 2003

Pregabalin and gabapentin, novel analgesic and anticonvulsant compounds, bind to calcium channel alpha2-delta proteins, offering potential benefits in pain and seizure management.

Pregabalin relieves symptoms of painful diabetic neuropathy

Pregabalin effectively reduces pain and improves sleep in patients with diabetic peripheral neuropathy, with well-tolerated effects at all doses.

Pregabalin for the treatment of painful diabetic peripheral neuropathy: a double-blind, placebo-controlled trial

Pregabalin is a safe and effective treatment for decreasing pain associated with diabetic peripheral neuropathy, improving mood, sleep disturbance, and quality of life.

Advances in neuropathic pain: diagnosis, mechanisms, and treatment recommendations.

Neurological pain can be effectively treated with medications like gabapentin, 5% lidocaine patch, opioid analgesics, tramadol hydrochloride, and tricyclic antidepressants.

Pregabalin and gabapentin reduce release of substance P and CGRP from rat spinal tissues only after inflammation or activation of protein kinase C

Gabapentin and pregabalin reduce the release of sensory neuropeptides in the spinal cord only after significant inflammation or protein kinase C activation.

Citations

Pharmacological Effects of Paeonia lactiflora Focusing on Painful Diabetic Neuropathy.

Paeonia lactiflora shows potential as a novel therapeutic approach for treating painful diabetic neuropathy due to its antinociceptive, anti-inflammatory, antioxidant, and antiapoptotic properties.

The landscape of global research on diabetic neuropathy

Diabetic neuropathy research faces geographical imbalances and urgent need for standardized diagnostic criteria, reliable biomarkers, and innovative treatment approaches to address the global impact of this debilitating condition.

Pregabalin induced balance disorder, asthenia, edema, and constipation in an elderly adult: A case report

Elderly patients should be prescribed lower initial doses of pregabalin and titrated to the maximum tolerable dose to avoid dose-limiting adverse drug reactions.

Effects of single preoperative oral pregabalin administration on postoperative hyperalgesia and opioid consumption after total abdominal hysterectomy

Preoperative oral pregabalin 150 mg effectively reduces postoperative pain intensity, hyperalgesia, and opioid consumption after total abdominal hysterectomy, but may increase postoperative side effects like dizziness and somnolence.

Drug repurposing - A search for novel therapy for the treatment of diabetic neuropathy.

Drug repurposing offers a promising approach for discovering novel therapies for diabetic neuropathy, overcoming barriers and accelerating the translation of existing drugs to patients.