Is There a Recreational Misuse Potential for Pregabalin Analysis of Anecdotal Online Reports in Comparison with Related Gabapentin and Clonazepam Data

Schifano, Fabrizio; D’Offizi, Stefano; Piccione, Michele; Corazza, Ornella; Deluca, Paolo; Davey, Zoe; Melchiorre, Giuditta Di; Furia, Lucia Di; Farré, Mercè; Flesland, Liv; Mannonen, Miia; Majava, Aino; Pagani, Stefania; Peltoniemi, Teuvo; Siemann, Holger; Skutle, Arvid; Torrens, Marta; Pezzolesi, Cinzia; Kreeft, P van der; Scherbaum, Norbert

doi:10.1159/000321079

Cited by 174 publications

(150 citation statements)

References 24 publications

Supporting

Mentioning

136

Contrasting

Unclassified

Order By: Relevance

“…At dosages exceeding the therapeutic dosages, gabapentinoids, different from clonazepam (e.g. a powerful benzodiazepine compound that may be misused; [25]), seem to anecdotally possess both sedative as well as dissociative/psychedelic effects [10]. This may be considered an observation that is in apparent contrast with gabapentinoids, similar to benzodiazepines, being GABA analogues only [26].…”

Section: Methods/literature Search Strategymentioning

confidence: 99%

“…Indeed, the absolute bioavailability of gabapentin drops from 60 to 33 % as the dosage increases from 900 to 3,600 mg/day, while the absolute bioavailability of pregabalin remains at C90 % irrespective of the dosage [15]. One could conclude from here that distinct pharmacokinetic advantages of pregabalin over gabapentin may translate into an improved therapeutic effect [5], but may explain as well why pregabalin is anecdotally perceived as more 'powerful' by drug misusers [10,28].…”

Section: Pregabalin Vs Gabapentinmentioning

confidence: 99%

“…In Norway, Persheim et al [9] analysed changes for the period 2008-2011 in the drug reimbursement system relating to expenditures for potentially addictive drugs in patients with severe/non-malignant chronic pain, and found that about one-third of the approved applications were for pregabalin. In parallel with this, there is an anecdotally growing black market, with gabapentinoids being allegedly available without prescriptions through online pharmacies [10]. In line with this, pregabalin and gabapentin first emerged in the UK mortality databases in 2006 and have shown an increasing trend since then in respect of being implicated in death.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Misuse and Abuse of Pregabalin and Gabapentin: Cause for Concern?

2014

Self Cite

View full text Add to dashboard Cite

Gabapentinoids (e.g. pregabalin and gabapentin) are widely used in neurology, psychiatry and primary healthcare but are increasingly being reported as possessing a potential for misuse. In fact, increasing levels of both prescriptions and related fatalities, together with an anecdotally growing black market, have been reported from a range of countries. This article reviews the current evidence base of this potential, in an attempt to answer the question of whether there is cause for concern about these drugs. Potent binding of pregabalin/gabapentin at the calcium channel results in a reduction in the release of excitatory molecules. Furthermore, gabapentinoids are thought to possess GABA-mimetic properties whilst possibly presenting with direct/indirect effects on the dopaminergic 'reward' system. Overall, pregabalin is characterized by higher potency, quicker absorption rates and greater bioavailability levels than gabapentin. Although at therapeutic dosages gabapentinoids may present with low addictive liability levels, misusers' perceptions for these molecules to constitute a valid substitute for most common illicit drugs may be a reason of concern. Gabapentinoid experimenters are profiled here as individuals with a history of recreational polydrug misuse, who self-administer with dosages clearly in excess (e.g. up to 3-20 times) of those that are clinically advisable. Physicians considering prescribing gabapentinoids for neurological/psychiatric disorders should carefully evaluate a possible previous history of drug abuse, whilst being able to promptly identify signs of pregabalin/gabapentin misuse and provide possible assistance in tapering off the medication. Key pointsGabapentinoids are thought to possess GABAmimetic properties, whilst possibly presenting with direct/indirect effects on the dopaminergic 'reward' system.Gabapentinoid experimenters are profiled here as individuals with a history of recreational polydrug misuse, who self-administer with dosages clearly in excess (e.g. up to 3-20 times) of those that are clinically advisable.Physicians considering prescribing gabapentinoids for neurological/psychiatric disorders should carefully evaluate for a possible previous history of drug abuse, whilst being able to promptly identify signs of pregabalin/gabapentin misuse and provide possible assistance in tapering off the medication.

show abstract

Section: Methods/literature Search Strategymentioning

confidence: 99%

Section: Pregabalin Vs Gabapentinmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Misuse and Abuse of Pregabalin and Gabapentin: Cause for Concern?

2014

Self Cite

View full text Add to dashboard Cite

show abstract

“…The European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) recently highlighted early reports from pharmacovigilance data from four countries, including the UK, regarding the potential for misuse of these medications and indications from toxicological analyses of the involvement of these medications in deaths of users [4]. There is also concern regarding their access from online pharmacies and misuse of legitimately prescribed medication [5]. Furthermore, dependent users of recreational drugs may seek access to these medications in an attempt to prevent or treat withdrawal symptoms [3,6,7].…”

mentioning

confidence: 99%

Misuse of the γ‐aminobutyric acid analogues baclofen, gabapentin and pregabalin in the UK

Kapil

Green

Lait

et al. 2014

Brit J Clinical Pharma

View full text Add to dashboard Cite

“…52 Benzidaminin rekreasyonel kullanımı bazı ül-kelerde giderek yaygınlaşmaktadır. 55 Opaleye ve ark., benzidaminin gençler arasında rekreasyonel kullanımını saptamak için gençlere yönelik kesitsel bir anket çalışması yapmışlardır. İkibin sekiz yüz yedi katılımcının olduğu bu çalışmada; 78'inin çok uzun bir süre boyunca, 30'unun da son bir ayda rekreasyonel amaçla benzidamin kullandığı saptanmış-tır.…”

Section: Benzi̇dami̇nunclassified