Gabapentinoid Benefit and Risk Stratification: Mechanisms Over Myth

Area of Science:

• Pharmacology and Pain Management
• Neuroscience

Background:

• Gabapentinoids (gabapentin and pregabalin) are increasingly prescribed off-label for pain management.
• Concerns regarding misuse and addiction potential have been raised, but evidence is limited.
• This review addresses myths and facts surrounding gabapentinoid medications.

Purpose of the Study:

• To provide a balanced perspective on the efficacy and safety of gabapentinoids.
• To clarify the neurobiological mechanisms underlying gabapentinoid action.
• To address allegations of misuse and addiction potential.

Main Methods:

• Narrative review of existing literature.
• Analysis of neurobiological mechanisms.
• Examination of clinical and epidemiological addiction studies.

Main Results:

• Gabapentinoids modulate voltage-gated calcium channels and NMDA receptors, reducing central sensitization and aiding sleep.
• They have a favorable safety profile with a low risk of misuse, abuse, and dependence.
• Misuse is primarily observed in individuals with opioid use disorder, often to alleviate withdrawal symptoms.

Conclusions:

• Gabapentinoids are valuable in pain management, particularly for central sensitization and sleep disturbances.
• They have low intrinsic addictive potential but require cautious use in patients with opioid use disorder.
• Risk-benefit assessment is crucial, especially when co-prescribing with opioids.