Is gabapentin (GABA analog) a scheduled medication?

Gabapentin's Controlled Substance Status

Gabapentin is not a federally scheduled controlled substance, though some individual states have reclassified it as a Schedule V controlled substance due to its potential for misuse. 1

Federal Classification Status

• According to the FDA drug label, gabapentin is explicitly classified as "not a scheduled drug" 1
• Gabapentin does not exhibit affinity for benzodiazepine, opiate, or cannabinoid receptor sites, which differentiates it from many traditional controlled substances 1
• Unlike pregabalin (which has a similar mechanism of action), gabapentin remains unscheduled at the federal level 2

State-Level Regulations

• Since 2016, multiple states have implemented their own regulations for gabapentin due to concerns about misuse 3
• Approximately 14 US states and jurisdictions have either:
  • Implemented legislative mandates requiring pharmacovigilance programs
  • Amended rules and regulations
  • Begun crafting policy
  • Started gathering additional data for decision making 3
• Some states have specifically reclassified gabapentin as a Schedule V controlled substance at the state level 4

Abuse Potential Considerations

• There are documented reports of gabapentin misuse and abuse, particularly among individuals with:
  • History of opioid abuse
  • Mental illness
  • Previous prescription drug abuse 4
• Postmarketing reports indicate gabapentin misuse typically involves:
  • Taking higher than recommended doses
  • Using for unapproved purposes
  • Seeking euphoria or potentiation of opioid effects 1, 4
• The risk of gabapentin misuse is generally considered small and not comparable to the much higher risks associated with alcohol, benzodiazepines, opioids, stimulants, or illicit drugs 5

Clinical Implications

• Healthcare providers should carefully evaluate patients for history of drug abuse before prescribing gabapentin 1
• Monitoring for signs of gabapentin misuse or abuse is recommended, including:
  • Development of tolerance
  • Self-dose escalation
  • Drug-seeking behavior 1
• Abrupt discontinuation of gabapentin (particularly at higher than recommended doses) has been associated with withdrawal symptoms including agitation, disorientation, and confusion 1
• When prescribing gabapentin to patients with polysubstance abuse history, increased caution and surveillance are warranted 6

Pharmacological Context

• Gabapentin and pregabalin both bind to voltage-gated calcium channels at the α2δ subunit to inhibit neurotransmitter release 7
• Despite similar mechanisms, pregabalin is federally classified as a Schedule V controlled substance while gabapentin remains unscheduled at the federal level 2