Pregabalin Abuse Potential

Pregabalin, also known by its brand name Lyrica, is a medication primarily prescribed for neuropathic pain, epilepsy, and generalized anxiety disorder (GAD). While it is highly effective for these conditions, there is increasing evidence highlighting Pregabalin abuse potential worldwide.

What is Pregabalin?

Pregabalin is a gabapentinoid that works by binding to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system. This action reduces the release of excitatory neurotransmitters, such as glutamate, noradrenaline, and substance P, which are involved in pain transmission and neuronal excitability[1].

Initially developed as an anticonvulsant, pregabalin has also proven effective in treating neuropathic pain, fibromyalgia, and GAD. However, its ability to induce relaxation and euphoria has led to its misuse in certain populations[2].

Why is Pregabalin Abused?

Several factors contribute to pregabalin abuse:

1. Euphoric Effects – When taken in high doses, pregabalin produces a sense of well-being and euphoria, making it attractive to recreational users[3].
2. Relaxation and Sedation – Pregabalin has anxiolytic and sedative effects, which can make it appealing to individuals suffering from anxiety or insomnia[4].
3. Polydrug Use – Pregabalin is often misused alongside opioids, benzodiazepines, or alcohol to enhance its sedative effects, which increases the risk of overdose and death[5].
4. Availability – Pregabalin is widely prescribed for neuropathic pain and anxiety disorders, making it easily accessible[6].

Who is at Risk of Abusing Pregabalin?

Certain populations are more likely to abuse pregabalin, including:

• Individuals with a history of substance use disorders – Research indicates that those who have abused opioids, benzodiazepines, or alcohol are at a higher risk of misusing pregabalin[1].
• Patients with psychiatric conditions – Individuals with depression, anxiety, or post-traumatic stress disorder (PTSD) may misuse pregabalin for self-medication[3].
• Incarcerated individuals – Pregabalin abuse has been reported in prison populations, where it is sought for its psychoactive effects[6].

Dangers of Pregabalin Abuse

Short-Term Effects of Pregabalin Abuse

When misused, pregabalin can cause a range of adverse effects, including:

• Drowsiness and dizziness – These side effects can impair cognitive and motor functions, increasing the risk of accidents and injuries[2].
• Blurred vision and confusion – High doses can cause perceptual distortions and impair judgment[4].
• Euphoria and relaxation – While these effects contribute to its abuse potential, they can also lead to psychological dependence[5].

Long-Term Effects of Pregabalin Abuse

Prolonged misuse of pregabalin can lead to severe consequences, such as:

• Tolerance and Dependence – Chronic use can lead to the development of tolerance, requiring higher doses to achieve the same effects. This can result in physical and psychological dependence[3].
• Withdrawal Symptoms – Stopping pregabalin suddenly can cause withdrawal symptoms, including insomnia, nausea, sweating, anxiety, and seizures[2].
• Increased Overdose Risk – When combined with other central nervous system (CNS) depressants like opioids, pregabalin significantly increases the risk of respiratory depression and fatal overdose[5].

Pregabalin and Overdose Risks

While pregabalin has a relatively wide safety margin when taken as prescribed, overdoses have been reported, particularly in cases of polydrug use. Symptoms of a pregabalin overdose may include:

• Severe drowsiness and sedation
• Respiratory depression
• Coma
• Cardiovascular instability

In recent years, pregabalin-related deaths have increased, especially among individuals combining it with opioids or benzodiazepines. One study found that pregabalin was implicated in 22% of opioid-related overdose deaths in the UK[6].

Regulatory Responses and Prescription Monitoring

Changes in Drug Scheduling

Due to the increasing rates of misuse, several countries have reclassified pregabalin as a controlled substance:

• United Kingdom – In 2019, pregabalin was reclassified as a Class C controlled substance, requiring stricter prescription monitoring[6].
• European Union – Some countries have imposed restrictions on pregabalin prescribing due to its high abuse potential[4].
• United States – While not classified as a federally controlled substance, some states have implemented stricter monitoring requirements[3].

Prescription Monitoring Programs (PMPs)

To prevent misuse, many healthcare systems have implemented PMPs that track prescribing patterns and identify high-risk patients. Physicians are advised to:

• Conduct regular patient assessments to monitor for signs of misuse.
• Educate patients about the risks of pregabalin dependence.
• Consider alternative treatments for individuals with a history of substance abuse.

Alternatives to Pregabalin for Pain and Anxiety Management

For individuals at high risk of pregabalin misuse, alternative medications and non-pharmacological treatments should be considered:

• For Neuropathic Pain:
  • Gabapentin (lower abuse potential than pregabalin)
  • Tricyclic antidepressants (e.g., amitriptyline)
  • Serotonin-norepinephrine reuptake inhibitors (SNRIs) (e.g., duloxetine)
• For Anxiety Disorders:
  • Selective serotonin reuptake inhibitors (SSRIs)
  • Cognitive-behavioral therapy (CBT)
  • Lifestyle modifications (e.g., meditation, exercise)

Conclusion

Pregabalin remains a highly effective medication for treating neuropathic pain, epilepsy, and anxiety disorders. However, its growing potential for abuse and dependence has led to increased regulatory scrutiny. Healthcare professionals must balance its therapeutic benefits with the risks of abuse by closely monitoring patients, educating them about its dangers, and considering alternative treatments when necessary.

References

1. Schjerning, O., Rosenzweig, M., Pottegård, A., Damkier, P., & Nielsen, J. (2016). Abuse Potential of Pregabalin: A Systematic Review. CNS Drugs, 30(1), 9–25. Retrieved from: https://pubmed.ncbi.nlm.nih.gov/26767525/
2. Grosshans, M., Mutschler, J., Hermann, D., Klein, O., Dressing, H., Kiefer, F., & Mann, K. (2010). Pregabalin Abuse, Dependence, and Withdrawal: A Case Report. American Journal of Psychiatry, 167(7), 869. Retrieved from: https://pubmed.ncbi.nlm.nih.gov/20595436/
3. Evoy, K. E., Morrison, M. D., & Saklad, S. R. (2017). Abuse and Misuse of Pregabalin and Gabapentin. Drugs, 77(4), 403–426. Retrieved from: https://pubmed.ncbi.nlm.nih.gov/28144823/
4. Schifano, F. (2014). Misuse and Abuse of Pregabalin and Gabapentin: Cause for Concern? CNS Drugs, 28(6), 491–496. Retrieved from: https://pubmed.ncbi.nlm.nih.gov/24760436/
5. Gahr, M., Franke, B., Freudenmann, R. W., & Hiemke, C. (2013). Pregabalin Abuse and Dependence in Germany: A Growing Concern? European Journal of Clinical Pharmacology. Retrieved from: https://pubmed.ncbi.nlm.nih.gov/23455538/
6. Montastruc, F., Palmaro, A., Bagheri, H., Schmitt, L., & Montastruc, J. L. (2018). Pregabalin Misuse in the European Union: A Nationwide Analysis Using the EudraVigilance Database. British Journal of Clinical Pharmacology, 84(11), 2456–2463. Retrieved from: https://pubmed.ncbi.nlm.nih.gov/30152078/