Page Banner
Mayo Clinic Laboratories > Therapeutics > Drug class testing > Gabapentinoids

Gabapentinoids

Support individualized care with gabapentinoid testing

Gabapentin and pregabalin are used across multiple clinical settings, including for neuropathic pain and seizure disorders. As efforts to minimize opioid and benzodiazepine exposure have continued, gabapentinoid use has increased substantially.¹,²

Adverse effects related to gabapentinoid use are predominantly related to the central nervous system CNS, with respiratory depression becoming an important safety concern when these medications are used with opioids or other CNS depressants.¹ Misuse is also clinically relevant in higher-risk populations, including patients with substance use disorder or psychiatric conditions. Recent evidence shows that gabapentinoids are often misused with opioids or other substances and that concurrent use with opioids or benzodiazepines increases overdose risk.3

Individualized gabapentinoid testing, guided by the clinical question and patient-specific needs, can provide objective information about recent medication exposure to help inform clinical assessment.4

Additional information

Mayo Clinic Laboratories offers serum and urine testing options for gabapentin and pregabalin to support patient-specific testing needs. Serum testing provides quantitative drug concentrations for therapeutic drug monitoring, while urine testing can provide evidence of recent exposure as part of a targeted or broader drug monitoring strategy.

~150%

~150% increase in annual gabapentin prescriptions from 2010–20255

~50%

~50% of U.S. jurisdictions enacted policies related to gabapentin scheduling or required prescription reporting from 2016–20246

~9%

~9% of U.S. treatment-seeking individuals with opioid use disorder reported past-month nonmedical gabapentin use7,8

Gabapentinoid test menu

Serum testing Serum testing
Targeted mass spectrometry urine screening Targeted mass spectrometry urine screening
Comprehensive urine monitoring Comprehensive urine monitoring
Pain management Pain management

Serum testing

Serum testing is useful when quantitative drug concentrations may help assess medication exposure, investigate suspected toxicity, or guide individualized dosing, including in patients with altered renal function.4,8,9

Key testing

Learn more Explore precision epilepsy therapeutics

Targeted mass spectrometry urine screening

Targeted urine testing is useful when recent exposure to gabapentin, pregabalin, selected prescription, nonprescription, illicit stimulants, and PCP is the primary clinical question and broader controlled substance monitoring is not needed.

Key testing

Comprehensive urine monitoring  

Comprehensive urine drug monitoring is useful when monitoring needs extend across multiple drug classes or biomarkers. Our comprehensive controlled substance monitoring profile incorporates specimen validity testing, with testing for gabapentinoids, opioids, benzodiazepines, stimulants, PCP, and cocaine metabolites for a broad look at a patient’s drug use.

Key testing

Pain management

Our comprehensive pain management monitoring profile incorporates specimen validity testing and testing for gabapentinoids, opioids, benzodiazepines, stimulants, barbiturates, cocaine metabolites, THC, PCP, and ethanol biomarkers.10

Key testing

References
  1. Chincholkar M. Gabapentinoids: pharmacokinetics, pharmacodynamics and considerations for clinical practice. Br J Pain. 2020;14(2):104-114. doi:10.1177/2049463720912496.
  2. Drug Enforcement Administration, Diversion Control Division, Drug & Chemical Evaluation Section. Gabapentin. April 2026. Accessed September 14, 2026. https://www.deadiversion.usdoj.gov/drug_chem_info/gabapentin.pdf.
  3. Evoy KE, Drain D, Pedigo J, Covvey JR, Ramey O. Misuse of pregabalin and gabapentin: a second systematic review update. Drugs. 2026;86(8):1365-1378. doi:10.1007/s40265-026-02342-w.
  4. Hart XM, Gründer G, Hiemke C, et al. Consensus Guidelines for Therapeutic Drug Monitoring in Neuropsychopharmacology: Update 2026 - Pharmacokinetic, pharmacogenetic and clinical aspects. Pharmacopsychiatry. 2026;59(4):166-295. doi:10.1055/a-2860-7861
  5. Drug Enforcement Administration, Diversion Control Division, Drug & Chemical Evaluation Section. Gabapentin. Published April 2026. Accessed August 31, 2026. https://www.deadiversion.usdoj.gov/drug_chem_info/gabapentin.pdf
  6. Combs KG, Vickers-Smith R, Stewart C, Wacker D, Hincapie-Castillo JM. A comprehensive analysis of jurisdiction-specific laws related to scheduling or required prescription drug monitoring of gabapentin in the United States, 2016-2024. Int J Drug Policy. 2026;147:105064. doi:10.1016/j.drugpo.2025.105064
  7. Ellis MS, Buttram ME, Kasper ZA, Cicero TJ. Nonmedical use of gabapentin and opioid agonist medications in treatment-seeking individuals with opioid use disorder. Drug Alcohol Depend. 2022;234:109400. doi:10.1016/j.drugalcdep.2022.109400
  8. Evoy KE, Drain D, Pedigo J, Covvey JR, Ramey O. Misuse of pregabalin and gabapentin: a second systematic review update. Drugs. 2026;86(8):1365-1378. doi:10.1007/s40265-026-02342-w
  9. Mayo Clinic Laboratories. Gabapentin, Serum (GABA). Mayo Clinic Laboratories Test Catalog. Accessed August 31, 2026. https://www.mayocliniclabs.com/test-catalog/overview/80826.
  10. Mayo Clinic Laboratories. Pregabalin, Serum (PGN). Mayo Clinic Laboratories Test Catalog. Accessed August 31, 2026. https://www.mayocliniclabs.com/test-catalog/Overview/65119.
  11. Jannetto PJ, Bratanow NC, Clark WA, et al. Executive summary: American Association of Clinical Chemistry Laboratory Medicine Practice Guideline-using clinical laboratory tests to monitor drug therapy in pain management patients. J Appl Lab Med. 2018;2(4):489-526.