For gabapentin, it is still somewhat controversial whether a substantial overdose of gabapentin used alone is enough to induce life-threatening respiratory or cardiac insufficiency. There have been post-mortem cases describing self-poisoning with gabapentin alone 103, 104. Pregabalin overdosing may have fatal consequences, especially if combined with opioids and sedatives 54, 56, 62.
Further studies to identify risk factors for gabapentinmisuse and to characterize gabapentin’s can i drink alcohol while taking levaquin abuse liability are recommended. The present review attempted to summarize rigorously conducted andwell-presented findings on gabapentin misuse/abuse. As such, the quality of casereports could not be evaluated; therefore, this presentation focused onepidemiological and toxicological studies using case studies as secondary data. Itwould be detrimental to have excluded case reports, as they provide rich contextfrom which the population data may arise. Therefore, unless clearly noted in themanuscript text that the article was a case report, the reader could assume that thestudy was sample-based.
Gabapentinoids are structurally similar to gamma-aminobutyric acid (GABA); however, they do not act on GABA receptors or have effects on GABA synthesis or metabolism. They are selective ligands for the alpha-2-delta subunit of voltage-gated calcium channels (VGCC) and have been demonstrated to restrain stimulus-dependent synaptic transmitter release, mainly the excitatory transmitters glutamate and norepinephrine 3, 4. Gabapentinoids lead to a moderate dose-dependent increase of the extracellular GABA level in the brain 3, 5, causing weak GABA-mimetic features such as relaxation and euphoria. These effects are experienced especially in the beginning of drug therapy and after use of supratherapeutic doses. Case studies have corroborated the epidemiological findings and havealso identified buprenorphine/naloxone and quetiapine as combinations ofabuse with gabapentin (31, 32, 51).
- Patients with various diagnoses such as fibromyalgia, painful neuropathies, post-herpetic neuralgia, and generalized anxiety disorder, but also healthy volunteers were included in these studies.
- In our study, we used only the “prescription drug” category for the extraction of our data.
- In relation to sales, Ojanperä et al. 56 found that the Finnish number of deaths per million defined daily doses per year for pregabalin had an increasing trend from 2005 to 2013.
- In Sweden, 5.2% of 191,971 individuals with at least two consecutive prescriptions for gabapentinoids were treated for suicidal behavior or died from suicide 25.
Many users buy the drug illegally on the black market, often from unregulated websites.
Pregabalin: What is it and why can it be dangerous?
Pregabalin is a prescription medication approved for the management of neuropathic pain related to diabetic peripheral neuropathy and postherpetic neuralgia, partial-onset what is mesculin seizures as an adjunctive therapy in adults, and fibromyalgia (Brockbrader et al. 2010). As an alkylated analogue of ɣ-aminobutyric acid (GABA), pregabalin’s mechanism of action is the inhibition of calcium influx and the release of excitatory neurotransmitters (Brockbrader et al. 2010; Schjerning et al. 2016). In the U.S., pregabalin was placed into Schedule V of the Controlled Substances Act, indicating a low potential for abuse relative to other scheduled drugs (Drug Enforcement Administration 2005).
Gabapentinoids (pregabalin and gabapentin) are a class of drugs that have been widely used-prescribed for neuropathic pain, epilepsy, anxiety, and other psychiatric disorders, while pregabalin showed promise as a treatment for alcohol dependence (1, 2). Gabapentin and pregabalin have a similar structure and are derivatives of the inhibitory neurotransmitter GABA. Their proposed mechanism of action is the inhibition of calcium currents via high-voltage-activated channels containing the a2d-1 subunit (3). Since their first approval, both gabapentinoids are widely prescribed medications in the United States (4, 5). Prescribers in the USA, in contrast to European prescribers, might consider gabapentinoids a safer non-opioid pain medication in the context of the opioid overdose epidemic in the USA 92, 96. However, other differences in regulations, healthcare systems, ease of access, and perceptions by users might also add to these differences.
Study sample
Different reasons why abuse of gabapentinoids is higher among opioid abusers have been proposed. It has been suggested that they might relieve opioid withdrawal syndromes or treat uncontrolled pain 39, 49. Another suggested explanation is that with reduced prescribing of opioids and benzodiazepines, patients are substituting other licit or illicit drugs because of the greater availability 66, 70.
Search Interest Over Time
Three toxicology studies liberty cap lookalikes elucidated the most commonly foundsubstances with gabapentin. Peterson (2009) conducted a study in the US, also utilizingtoxicological data, which examined the presence of gabapentin in drivingimpairment cases. Smith and colleagues (2012) stated thatpostmortem toxicology reports in Scotland revealed 75% of thoseidentifying gabapentin also included morphine and/or methadone, which theauthors said may be indicative of recent opioid dependence (43). The toxicology studies, while helpful forproviding a picture of what classes of medicines were commonly found incombination with gabapentin, did not address unprescribed mixing of licit orillicit drugs. Studies indicate gabapentin is misused/abused over a wide range ofdoses, from within therapeutic range (900–3600 mg/day) tosupratherapeutic doses.
Other studies confirm high rates of gabapentinoid abuse in opioid addicts 20, 21, 42, 64, 66–68. One study 40 reported that more than 60% of opioid addicts misused gabapentinoids. A survey among opioid abusers found that on average gabapentin was used recreationally in 25 of the last 30 days 64.