Author: Alex Thompson

Gabapentinoid Benefit and Risk Stratification: Mechanisms Over Myth PMC

is gabapentin addictive for sleep

For example, a study by Winkelman, Orfeu, Buxton, et al. (2008) discovered that average brain concentrations of GABA were approximately 30% lower in persons with primary insomnia compared to persons without insomnia. Other research has linked deficits in GABAergic signaling to HPA axis hyperactivity and CNS hyperarousal. PubMed was searched for randomized, double-blinded, placebo-controlled trials that reported sleep changes during gabapentin treatment up to November 2015.

is gabapentin addictive for sleep

Moreover, recipients of the 600 mg dose exhibited enhanced slow-wave sleep (SWS), less rapid-eye movement (REM) sleep, and fewer arousals. Although the polysomnographic assessments clearly indicated improved sleep following gabapentin administration, no differences were discovered on subjective scales of drowsiness and functioning. Nonetheless, researchers concluded that single-dose gabapentin appears to enhance many aspects of sleep [after alcohol consumption]. Another possibility is that multiple mechanisms contribute in varying amounts to the generation of a hypnotic effect.

How should I take gabapentin?

It would eventually be discovered that each of the women experienced recurrent nighttime awakenings as a result of premenopausal-related hormone fluctuations. In menopause, frequent nighttime awakenings are thought to occur due to fluctuations in serum hormones such as decreased estradiol and increased adrenocorticotropic hormone (ACTH). While asleep, the aforestated hormonal fluctuations stimulate the sympathetic nervous system to provoke hot flashes, night sweats, and disconcerting nighttime awakenings.

  1. Individuals experienced double vision, slurred speech, drowsiness, diarrhea and sluggishness.
  2. However, after a 2-week duration, the awakenings reemerged along with the sweats.
  3. A variety of data sources and publications suggest that opioid abusers are more likely to misuse and abuse the gabapentinoids [57].
  4. The branded gabapentin enacarbil product Horizant is approved for restless legs syndrome and PHN.
  5. Reports note that gabapentin is often used by people abusing other medicines, such as opioid painkillers like oxycodone, muscle relaxants, and anxiety medications such as Valium and Xanax to boost the high.

A 25–100 mg dose may help a person fall and stay asleep with fewer side effects than traditional sleep aids. Gabapentin has been reported to be used by patients in substance use disorder treatment programs, as it is not typically screened for during treatment. Even though gabapentin may be used as a treatment option for alcohol and substance abuse, it is important to monitor for all drug-seeking behaviors in patients.

Mechanism: Amelioration of Central Sensitization

Based on the fact that polysomnography data were consistent across trials (RCTs and non-RCTs), it’s likely that the favorable effect of gabapentin on sleep architecture was not attributable to a placebo response nor random chance. It was concluded that gabapentin might enhance sleep quality in menopausal women with hot flashes. Based on the fact that a host of significant improvements were observed in measures of sleep quality, sleep efficiency, and global sleep scores – this study supports the idea that gabapentin can enhance sleep.

is gabapentin addictive for sleep

Multiple investigations have corroborated a lack of dopaminergic signal alterations in the NAc with the administration of gabapentin and pregabalin [48–52], or elevation only in experimental groups subjected to chronic painful stimulus via surgical ligation of a spinal nerve. Both drugs have also been shown to decrease or even block opioid-induced NAc dopaminergism [53]. Serious breathing problems can happen if you take gabapentin with drugs that cause severe sleepiness or decreased awareness. Some examples include narcotic opioids, anti-anxiety medicines, antidepressants, and antihistamines.

The hot flashes and sweats led her doctor to suspect that menopause-related hormone imbalances may have been culpable for her ongoing sleep disturbances. In 2016, results from an open-label pilot study conducted by North, Hong, and Rauck were published in which extended-release gabapentin was administered to individuals with fibromyalgia. The primary aim of the study was to determine whether gabapentin could alleviate pain, but a secondary aim was to determine whether gabapentin could enhance sleep. For the study, researchers assigned 34 fibromyalgia-diagnosed individuals to receive gabapentin ER (extended-release) starter packs for a duration of 12 weeks. To determine whether gabapentin is efficacious for the enhancement of sleep and/or treatment of insomnia, it is necessary to examine results from relevant studies [in which gabapentin was formally assessed as a sleep aid].

Although this study was relatively small-scale (with just 18 participants) and short-term, its findings support the hypothesis that gabapentin can effectively treat primary insomnia while favorably modulating sleep architecture. That said, a larger randomized controlled trial is needed to rule out placebo responses and strengthen the quality of data. That said, there were no differences in breakthrough pain frequency, pain severity, and pain duration based on the titration regimen. Considering the results, researchers concluded that administration of gabapentin four times per day during an initial titration phase among persons with neuropathic pain yields the most significant reduction in pain-related sleep disturbances and minimizes gabapentin side effects. From a macro-perspective, this study provides further support for the idea that the administration of gabapentin improves sleep.

It can also lead to anaphylactic reactions, CNS depression, worsening depression, and withdrawal effects in some people. Doctors can prescribe estazolam (Prosom) for the short-term treatment of insomnia. Lunesta is a controlled substance with a tendency to lead to misuse and dependency.

Have you used Gabapentin for sleep or insomnia?

It was concluded that gabapentin and clonazepam appear efficacious for the treatment of residual sleep disturbances among persons treated for major depression. Overall, this provides evidence to support the idea that gabapentin is a useful sleep aid. Results indicated that patients experienced significant pain relief within 4 weeks as evidenced by reductions in NPRS scores. What’s more, the MOS survey indicated that participants exhibited increases in average sleep duration per night (~1.2 hours) and significantly enhanced sleep quality.

One study applied the 49-question version of the Addiction Research Center Inventory (ARCI) in the assessment of abuse potential of gabapentin in alcoholics. The ARCI is the most well-studied and validated instrument used to compare abuse liability of a substance to five standard drug groups (Morphine-Benzadrine, Pentobarbitol-Chlorpromazine-Alcohol, LSD, Benzadrine, and Amphetamine). The investigators found no difference between gabapentin and placebo among all the various axes of subjective effect [58]. Given that gabapentinoids are meanwhile widely distributed and easily obtainable via the internet or black markets, one would expect many more of these cases if gabapentinoids possessed meaningful addictive power.

Various medications can help people fall asleep, stay asleep, or both, such as doxepin (Silenor) and Ramelteon (Rozerem). It has also been used “off-label” to treat other conditions like fibromyalgia, anxiety, alcoholism or other types of nerve pain. Gabapentin may also be used as an alternative to opioid medications to help manage pain. “Off-label” use means it may be prescribed by your doctor for a generally accepted use not specifically approved by the FDA or listed in the package labeling.

However, the individuals in these reports experienced symptoms after discontinuing higher-than-recommended doses of gabapentin and for uses for which the drug was not approved. For this reason, they organized a study and recruited 19 healthy adults – 9 of whom served as controls. All participants were assessed at baseline and endpoint with polysomnographic assessments and sleep scale questionnaires. After baseline measures were collected, 10 individuals were assigned to receive gabapentin and were titrated upwards to a maximum dosage of 1800 mg per day. Not only did the gabapentin attenuate the patient’s refractory insomnia, it facilitated additional mood enhancement.

Overall, the results of this study highlight the fact that gabapentin ER can alleviate symptoms of fibromyalgia-related pain plus improve sleep quantity and quality. Slow discontinuation, as directed by healthcare professional, can help to relieve symptoms. Behavioral and supportive medical care, such as treatments for nausea, anxiety or insomnia can help to support the withdrawal. Treatment for any other substance use disorder should be initiated (for example, opioid or alcohol use) if this accompanies gabapentin misuse. In a large review of 26 studies on gabapentin and sleep in patients with other medical conditions, the average dose taken daily was about 1,800 mg. Although positive sleep outcomes were reported, the researchers noted that gabapentin was not tolerated as well as placebo and some patients stopped taking it.

To gauge the efficacy and tolerability of each gabapentin dosing regimen during an initial titration, researchers recorded participants’ daily pain scores, breakthrough pain frequency, pain severity, pain duration, sleep disturbances, and adverse reactions to the drug. Results indicated that recipients of gabapentin four times per day (q.i.d.) in divided doses exhibited the greatest reductions in daily pain scores and pain-related sleep disturbances plus the fewest side effects during an initial titration phase – as compared to recipients of gabapentin three times per day (t.i.d.). This helps explain why individuals devoid of preexisting neurochemical imbalances and/or medical conditions report sleep enhancement from gabapentin. In sum, because inhibition of voltage-gated calcium channels is the chief mechanism of gabapentin’s action, it’s fair to suspect that this is the most relevant mechanism by which the drug enhances sleep. The gabapentinoids exhibit a broad spectrum of analgesic benefit, with a wide range of neurobiologic effects and a correspondingly increasing off-label use profile (Table ​(Table1),1), the discussion of which is beyond the scope of this review.