Gabapentin: How It Exploded into the Mainstream

Gabapentin How it exploded into the mainstream

It seems as if this anticonvulsant medicine has recently exploded as a recreational drug. Is this a good trend or a bad trend? If this drug can be easily abused and harm people who abuse it then it is not a good drug to be in such widespread use. There has to be a reason why this drug has became so popular is usage in mainstream society. What is the mass appeal for this drug? Traditionally, this drug has been used to treat neuropathic pain and epilepsy. Strangely, this drug is not grouped with other standard substances of abuse. The drug has a high abuse potential. It also appears this drug is too easy to attain. There is a trend occurring here as gabapentin is becoming abused  because such drugs like Oxycontin and Xanax become increasingly restricted. Phenibut is another drug that does not seem like it would have recreational potential, yet is abused.

 

Gabapentin in Perspective

NIH reports the following facts: “Unfortunately, our clinical experience suggests that gabapentin is now prevalent as a drug of abuse. The drug’s effects vary with the user, dosage, past experience, psychiatric history, and expectations. Individuals describe varying experiences with gabapentin abuse, including: euphoria, improved sociability, a marijuana-like ‘high’, relaxation, and sense of calm, although not all reports are positive (for example, ‘zombie-like’ effects). In primary care, an increasing number and urgency of prescription requests cannot necessarily be explained by the increased number of cases of neuropathic pain. In the substance misuse service, the numbers admitting to using gabapentin (local street name: ‘gabbies’, approx £1 per 300 mg) are also growing. Prescribing data from the Tayside region of Scotland show a rise in the number of patients receiving gabapentin, and an exponential rise in the total number of prescriptions issued, particularly since it was licenced for postherpetic neuralgia in 2002.”

Gabapentin was originally intended to treat epilepsy and chronic neuropathic pain but now it has became a prevalent drug for abuse. Despite the claim that it has a low potential for abuse it has became widely abused. Contrary to what is believed by some professionals the drug is widely abused and it may seem to be very addictive. This is not a good trend that the drug was originally intended to treat serious medical conditions but has became so popular in the streets it goes by the street name “gabbies”. Some revealing numbers show up with closer scrutiny it is reported that “gabbies” are abused by 1% of the general population. But the abuse rises to 40-65% among individuals with prescriptions and 15-22% among individuals who abuse opioids. But gabapentin can elicit euphoria, altered mental states, and disassociation in some users. Recreational gabapentin users have also reported that this anticonvulsant helps alleviate benzodiazepine and/or opiate withdrawal.

 

Life Example

Psychopharmacologists enjoy using the term “Mechanisms of Action

In 2007, it was discovered a 67-year-old woman was abusing gabapentin when she increased the dosage to 7.2 grams a day. She was diagnosed with morbid-depression and she was an alcholic. She obtained the extra gabapentin by lying to pharmacists and purchasing the drug illegally over the internet. She exhibited the traditional withdrawal effects:

These sound like some pretty painful effects especially the one where the eyeballs protrude. With thes kind of effects is this drug really safe to use in recreational settings?  The addictive liability of the drug is ultimately high. Even though studies conducted on healthy individuals showed that they had no increased desire for the drug and there was no dose escalation in open-label trials. (An open-label trial or open trial is a type of clinical trial in which both the researchers and participants know which treatment is being administered.) The authors acknowledged that the studies were limited in some aspects especially in the choosing of non-drug users for their studies.

 

Drug Users Personal Experiences

The following is a list of typical characteristics that users of gabapentin experience. This seems to be a summary of experiences that users of gabapentin have during the gabapentin high:

  • Euphoria (Golden Bliss of the World)
  • Enhanced sociability
  • A state of relaxation, but also “zombie-like” effects
  • A sedative/opiate-like buzz with no discernible comedown
  • Psychedelic / MDMA-like effects

One user comments on their experience using gabapentin:

“One Erowid user emphasizes increased sociability he experienced on gabapentin

“I’m amazed about the social enhancements most of all. I’ve found myself singing joyfully (in front of people!!!) and could envision this drug as treatment for stage fright. Unlike GHB, the sedation effect isn’t as profound, but the social effects are even greater. Anyhow, recreational value definitely exists. Especially in that the drug’s duration can be so extensive. Pop it in the morning on an empty stomach and one could expect to be altered through much of the day. Although it is not a perfect intoxication, there is a zombie feel to it, you feel free to express yourself. The zombie feel is a crapshoot. You may or may not get it.”

 

Other Comments about Being High on Gabapentin

typical characteristics that users of gabapentin experience

  • “A mild high with no edge” / “A nice and mellow buzz”
  • “Euphoric high, sleepy low”
  • The most I have done has been 4,800 mg of the 600 mg pills whilst the lowest amount that I can take to get any effect seems to be around 900 mg or more … To classify this pharm is a near impossible task. It is everything and anything in one pill. The only downside to gabapentin so far as I can tell, is the onset. These little guys take upwards of an hour to really start to kick in, but luckily, they last for 4–8 h it seems … I feel as if I’m on a super amphetamine rush and can tackle anything, yet feel so content it’s like I’m on a fully sedated opiate buzz. I’m chatty and witty, deep and insightful …
  • I knew that I need at least 10 300’s to get the right effect. Most everyone else I know that takes gabapentin take only 7 or 8 … so about an hour taking after them I feel a disassociation much like DXM, but only in my head and hands. My worries started to fade away. I am a very quiet, shy person normally, but when I am on gabapentin after about 1.5 h I get very friendly, very talkative, very active, very uninhibited … You really need to walk around on gabapentin dancing would be incredible …’ ‘… The feeling was comparable to cannabis with more of a heavy feeling in the body …

 

Negative Experiences

  • Seizures following overdose
  • Impaired immune function and ensuing infection from gabapentin use

 

Common Drugs Misused with Gabapentin

Other Comments about Being High on Gabapentin

These drugs seem to be commonly abused with gabapentin cannabis, alcohol, SSRIs, LSD, and GHB. LSD is a potent psychedelic that distorts the senses and bends the mind. You actually see hallucinations and your perception of reality is definitely altered. The point is that if this kind of drug is used with gabapentin then how strong of a high will gabapentin give an individual? The combination of these two drugs how much damage can they do to the mind and the body. SSRI’s are drugs that are used to counteract depression. It seems like people with depression are abusing this drug on an elevated scale.

 

Some Possible Reasons for this Drug’s Proliferation

  • The ability to get benzodiazepines and opioids is increasingly limited, so substance users are turning to alternatives like gabapentin and abusing it.
  • Gabapentin is a cheap, generic drug that is widely available because it is used to treat epilepsy and neuropathic pain. In other words it numbs the brain
  • Drugs that affect the GABA receptor in the brain tend to relieve anxiety and can elicit euphoria because the neuro pain is eliminated
  • Most physicians won’t think twice about writing a gabapentin prescription for pain or anxiety maybe these prescriptions are to readily available which would help to support the abuse of the drug
  • The drug has a similar high as Cannabis induces
  • The drug may enhance the effects of LSD

 

Mechanisms Of Action

Gabapentin in Perspective

Psychopharmacologists enjoy using the term “Mechanisms of Action” in other words what will trigger a drug to have a certain effect on the brain or body. Furthermore, the truth of the matter is that a lot of times the mechanisms of action are not understood. And the perceived mechanism that is thought to trigger the action of the drug really has nothing to do with the action of the drug. Keeping these things in mind gabapentin is a GABA derivative, like the Russian nootropic phenibut. Gaba is the major neurotransmitter in the brain which means GABA blocks neuronal activity, reducing anxiety, and decreasing seizures and having other effects that cut down on neuronal activities.     

 

Strong Potential for Misuse

Gabapentinoids ( like pregabalin and gabapentin) are in widespread use in neurology, psychiatry and primary health care but there are increasing reports of these drugs being abused. In fact, there is an increase in prescription abuse and fatalities and the ever increasing threat of these drugs being widely sold on the blackmarket  being reported from various countries. The drug is starting to cause deaths.

There was article written that investigated the the potential for this drug to be misused. And from information gathered for this article the trend is definitely being set for this drug to be widely misused on an international basis. It is believed that there is a definite cause for concern relating to the mainstream popularity of this drug. Potent binding of pregabalin/gabapentin at a calcium channel results in a reduction of excitatory molecules. Which basically means the drugs shut down neuronal activities in the brain leaving the person in a numbed euphoric state.  

Upon further research gabapentinoids may possess GABA-mimetic properties  which could possibly have direct/indirect effects on the on the dopaminergic ‘reward’ system this could send confusing messages to the brain as to whether the drug is beneficial or harmful. Overall, pregabalin is of a higher potency,  has quicker absorption rates and greater bioavailability levels than gabapentin. But gabapentin is still a dangerous drug. At therapeutic levels it is still claimed that gabapentin has a low potential for being addictive. Despite this continued claim this seems highly unlikely with the current widespread abuse of this drug. People who abuse this drug perceive it as a viable substitute for other illicit drugs and yes this is a major reason to be concerned. There is no two ways about this concern because it is a valid one.

Drug abusers profiled briefly in this article are defined as such when they administer to themselves a much higher dose than is typically prescribed. They also have a prior history of drug abuse. This amount pushing up to 3 to 20 times a day. Physicians need to be aware of the potential for this drug to be abused. They should not be so ready to prescribe this drug at a drop of the hat. Before they prescribe the drug they need to look at the patient’s medical history. If there is a historical trend in the user’s background for drug abuse than the prescription should not be administered. They need to look for obvious signs of pregabalin/gabapentin misuse and make themselves available to help the patient taper off on the medication.

 

Further Evidence for Drug Misuse

In 2011, in Europe there were 30 cases pregabalin of withdrawal, dependence, or abuse symptoms reported to Swedish and French pharmacovigilance centres and the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA). About 20 cases of gabapentin addiction were published in detail. The most frequently reported cases were of withdrawal and more than half the patients were admitted to the hospitals for withdrawal symptoms. Cases of excessive increases in the doses of gabapentin or pregabalin, unauthorised routes of administration, and combination with other substances were also reported which is setting a disturbing trend. If this trend is not harnessed it will only increased in the coming years.

Another cause for concern is that patients have no known history of drug abuse. This abuse must be stopped because the risk for abuse is not worth taking. The perceived benefits of gabapentin are just that perceived and the effects are not really proven.  

In another finding it is still held that gabapentin is not as addictive as pregabalin. This is due to the fact that pregabalin is absorbed much quicker and acts much faster once it enter the brain. There were 343 deaths related to this drug and 43 deaths related to gabapentin. It seems to be a recurring theme on the internet that gabapentin has a low addictive ratio. But if this is true why is there such grave concern the drug will be abused?

As was stated earlier there were 43 deaths reported from gabapentin abuse these cases were reported in Finland.

 

Gabapentin and Bipolar conditions    

This is another possible angle as to why gabapentin is so prevalent in mainstream society today. There was a study done on its effects on 43 bipolar subjects who had DSM-III-R bipolar disorder who were resistant to standard mood stabilizers. Since the mood stabilizers were ineffective for these subjects they were administered gabapentin. Here is an excerpt of the results of this study:

“Eighteen (41.9%) of 43 patients who began treatment were considered responders. Mean total HAM-D score showed a significant reduction during the 8 weeks of treatment. Analysis of the various HAM-D dimensions showed that the anxiety-somatization factor was the one with the greatest change. Seventeen of the 18 responder patients remained in remission for a period ranging from 4 to 12 months without clinically significant side effects or adverse events. One patient had to interrupt GBP treatment and be administered neuroleptics because of the reappearance of manic symptoms. Regarding response predictors, logistical regression analysis showed that the presence of panic disorder and alcohol abuse was associated with positive response. The results of the present study replicate prior studies indicating that GBP is an effective and well tolerated treatment in a large proportion of bipolar patients who are resistant to traditional mood stabilizers. More specifically, this drug appears to have antidepressant and anxiolytic properties. What is new in the present report is the suggestion that the utility of GBP in resistant bipolar disorder resides in its effectiveness against comorbid panic disorder and alcohol abuse.”

Again, this drug was effective in patients who also suffered from alcohol abuse and if left to their own devices there is the possibility they may abuse the drug like the 67-year-old woman did. This woman was a case study described earlier of abusing the drug while abusing alcohol. These other 17 patients may have been help to stop alcohol abuse by taking gabapentin. It could be a trade off of abusing gabapentin instead of alcohol.

 

Concerned Conclusion      

concerns as to the drug gabapentin being abused

In this article concerns as to the drug gabapentin being abused was discussed. Part of the reason for this abuse is the drug is widely available. It has shot into the mainstream for its easy accessibility, numbing of the brain, other illicit drugs becoming more controlled and hard to acquire. Another reason for its mainstream popularity is it gives the user a high similar to smoking cannabis. It helps the person to feel euphoric while experiencing no neurological pain. The drug is also abused in connection with other powerful drugs some of which are illegal. It is available on the internet and the medical profession is too liberal in administering prescriptions of this drug to the public. Remember, this drug has some harmful side effects and there were 43 deaths reported in Finland from this drug being abused.

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