Abstract

Flupirtine is a non-opioid, centrally acting analgesic which is marketed for oral and per rectal use. It has been used in managing acute post-operative pain, musculoskeletal pain and muscle spasm. NMDA (N-methyl-D-aspartate receptor) antagonism leading to opening of potassium channel opening at the neuronal membrane appears to be the mechanism of pain relief of this unique drug. It has membrane stabilization properties and ability to modulate GABA-A receptor at the neuronal level. The pain relief offered by flupirtine is comparable to NSAIDs or COX-2 inhibitors. Flupirtine doesn’t lead to drowsiness, constipation, nausea ,vomiting and tolerance which is seen with opioids. Unlike NSAIDs, it does not lead to gastric acidity, renal dysfunction, thrombotic events and bleeding due to anti-platelet action. The rise in serum creatinine and liver enzymes are transient and negligible. In few studies, the drug has been found to have cyprotective and anti-oxidant properties. It has been used in chronic headaches, migraine and parkinsonism in a small group of patients. The drug has been approved for use in European countries but the US-FDA approval is still pending.

Highlights

  • Post-operative pain is a distressing experience which can have deleterious consequences on the patients psychology if not handled effectively

  • For e.g., nonsteroidal anti-inflammatory drugs (NSAIDs) and COX-2 inhibitors which provide adequate pain relief cannot be offered to elderly patients or patients having cardiac or cerebrovascular disease or risk factors

  • The trial involving flupirtine in fibromyalgia was started by Adeona Pharmaceuticals which later became known as Synthetic Biologics

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Summary

INTRODUCTION

Post-operative pain is a distressing experience which can have deleterious consequences on the patients psychology if not handled effectively. This affects overall recovery and can end up in hospital phobia which can affect the family, social and personal life[1]. An indwelling epidural catheter with continuous local anesthesia infusion with or without opioid provides adequate pain relief in the post-operative period. Acetaminophen is a safe drug which can be used in patients of all age groups safely, except in patients with hepatic impairment It can not be used as the sole analgesic because it is effective in mild to moderate pain only

Why Flupirtine?
Acute and chronic pain indications
The history of Flupirtine
Pharmacokinetics of flupirtine
ADVANTAGE OF FLUPIRTINE
ADVERSE EFFECTS
CONCLUSION
Findings
17. European Medical Agency

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