1. Supported in part by Arkansas Blue Cross and Blue Shield
and the Office of the Arkansas Drug Director and in partnership with the Arkansas Academy of Family Physicians (AAFP), the Arkansas Medical Society (AMS), the Arkansas State Medical Board (ASMB), the Arkansas Department of Health (ADH) and its Division of Substance Misuse and Injury Prevention (Prescription Drug Monitoring Program—PDMP)
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2. Gabapentin and Pregabalin: Indications and Abuse
Shona Ray-Griffith, MD
Assistant Professor
University of Arkansas for Medical Sciences

3. Disclosures I receive clinical trial support from Neuronetics.
I have received clinical trial support from Sage Therapeutics.
Neither will be discussed today.

4. Objectives Discuss pharmacology and FDA indications for gabapentin
Discuss pharmacology and FDA indications for pregabalin
Describe abuse of gabapentin and pregabalin

5. Poll Everywhere
Text shonaraygrif105 to 22333

6. https://www. polleverywhere

7. Fuentes AV, Pineda MD, Venkata KCN
Fuentes AV, Pineda MD, Venkata KCN. “Comprehension of Top 200 Prescribed Drugs in the US as a Resource for Pharmacy Teaching, Training and Practice” Pharmacy (Basel) 2018;6(2):43

8. https://www. polleverywhere

10. Pharmacology of Gabapentin
GABA analog
Does NOT bind to GABA receptor or affect GABA binding, synthesis, uptake, or degradation
Does exert a neuronal inhibitory effect by blocking presynaptic voltage-dependent calcium channels
Peak plasma concentration occurs 3 hours after oral ingestion
Renal elimination
Half-life of 5-7 hours

12. Uses of Gabapentin Alcohol use disorder Alcohol withdrawal
Chronic refractory cough
Hiccups
Chronic pruritus
Vasomotor symptoms a/w menopause
Social anxiety disorder*
Focal (partial) seizures
Postherpetic neuralgia
Fibromyalgia
Neuropathic pain
Restless legs syndrome
Postoperative pain

13. Guidelines for Neuropathic Pain
European Federation of Neurological Societies (EFNS) recommends gabapentin as first-line therapy for diabetic neuropathy, postherpetic neuralgia, and central neuropathic pain.
National Institute for Health and Care Excellence (NICE), Canadian Pain Society (CPS), and NeuPSIG (by the International Association for the Study of Pain) guidelines recommend gabapentin as first line therapy for all neuropathic pain.

14. 2014 Lawsuits

15. Pharmacology of Pregabalin
GABA analog
Does NOT bind to GABA receptor or affect GABA binding, synthesis, uptake, or degradation
Does exert a neuronal inhibitory effect by blocking presynaptic voltage-dependent calcium channels
inhibits excitatory neurotransmitter release, including glutamate, NE, serotonin, dopamine, substance P, and calcitonin gen-related peptide)
Antinociceptive and anticonvulsant activity
Peak plasma concentration occurs 3 hours after oral ingestion
Renal elimination
Half-life of 6.3 hours
Schedule V drug

17. Uses of Pregabalin Chronic refractory cough
Generalized anxiety disorder
Chronic pruritus
Focal (partial) seizures
Social anxiety disorder
Vasomotor symptoms a/w menopause
Fibromyalgia
Neuropathic pain
Diabetic neuropathy
Postherpetic neuralgia
Spinal cord injury-associated neuropathic pain
Critically ill patients
Postoperative pain
Restless legs syndrome

18. https://www. polleverywhere

19. https://www. polleverywhere

20. Abuse of Gabapentin
Smith RV, Havens JR, Walsh SL. “Gabapentin misuse, abuse and diversion: A systematic review” Addiction 2016;111:
Gabapentin misuse ranged from 15-22%
Gabapentin abuse with a prescription ranged from 40-65%
Prescriptions from a provider are main source of diversion
Used in combination with benzodiazepines, opioids, and alcohol
Cutting agent for heroin
Use for 1) recreational, 2) self-harm, and 3) self-medication

21. Abuse/Dependence of Gabapentin
Mersfelder TL and Nichols WH. “Gabapentin: Abuse, Dependence, and Withdrawal” Annals of Pharmacotherapy 2016; 50(3):
Abuse and dependence: 8 case reports
All had history of substance use disorder
Potentiates the effects of opioids
Replace effects of cocaine or the withdrawal symptoms from cocaine use
Dosages of gabapentin ranged from mg/day with average of 3000mg/day
Symptoms: euphoria, relaxation, delirium, sedation, confusion, fatigue

22. Withdrawal of Gabapentin
Mersfelder TL and Nichols WH. “Gabapentin: Abuse, Dependence, and Withdrawal” Annals of Pharmacotherapy 2016; 50(3):
Withdrawal
Onset hours after last use (doses of mg daily)
Symptoms: agitation (>50%), confusion and disorientation (45%), diaphoresis (36%), GI symptoms (23%), tremor (18%), tachycardia (18%), HTN (18%), insomnia (14%)
Isolated reports of akathisia, catatonia, and seizures
Treatment: reinstate gabapentin

23. Gabapentin/Pregabalin Abuse
Hakkinen M, Vuori E, Kalso E, Gergov M, Ojanpera I. “Profiles of pregabalin and gabapentin by postmortem toxicology” Forensic Science International 2014; 241:1-6.
: Toxicology reports on 13,766 cases out of 101,472 deaths (13.6%)
Pregabalin positive in 2.3% of toxicology investigated reports
Gabapentin positive in 0.31% of toxicology investigated reports
91% of deceased pregabalin users and 88% of deceased gabapentin users were also positive for opioids
Users were significantly younger (under 30 years)
In all cases, other drugs were found.

24. Street Rx Gabapentin Pregablin $1-2/pill for 300mg to 800mg pills
$20 for 75mg pill

25. https://www. polleverywhere

26. Questions about the Topic
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27. Case Conference and Feedback
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