Alcoholism is an important medical and social problem, the relevance of which is due to both the high prevalence of this disease and its negative social consequences [1]. Therefore, the development of new effective methods of its treatment is an important and urgent task of modern narcology.
In the last 20 years, a lot of experimental and clinical data have appeared indicating the role of the GABAergic system in the formation of alcohol dependence. Alcohol abuse, by reducing the activity of GABAergic neuromediation in the ventral region of the brain, enhances dopamine neurotransmission, which mediates the implementation of the reinforcing effects of alcohol (“reward system”) and plays an important role in the formation of alcohol dependence [2–4]. It is believed that with the development of alcohol dependence, there is a functional insufficiency of the inhibitory GABAergic system of the brain with simultaneous hyperactivity of monoaminergic systems (primarily dopaminergic). Considering the close functional relationship of all neurochemical processes in the brain, normalization of the state of the dopamine system can be achieved both through direct influence on various links and regulators of dopamine neurotransmission, and through other neurotransmitters and neuromodulators, including the GABA system [5-7].
According to its chemical structure, baclofen is a derivative of chlorophenylbutyric acid (parachlorophenyl-GABA) and can be considered as a derivative of gamma-aminobutyric acid, as well as its stereospecific agonist. The main mechanism of action of baclofen is associated with the activation of presynaptic GABA-B receptors [8, 9].
An experiment on animals established the effect of reducing dopamine secretion, as well as reducing addictive behavior in response to the use of GABA-B receptor agonists (baclofen), while there was no effect of these drugs on feeding and water behavior, as well as on locomotor activity [10-14 ].
The first clinical study of the therapeutic effect of baclofen in persons suffering from alcohol dependence in combination with affective disorders was conducted in 1993 (cited from [15]). The study included 90 patients with secondary affective disorders (anxiety, depression), who were divided into four groups. Group 1 received baclofen, group 2 received diazepam, group 3 received amitriptyline, and group 4 received placebo. The effectiveness of therapy for affective disorders was assessed using clinical methods, psychological tests and electrophysiological (ultra-slow omega potential) techniques. The results of the study demonstrated the effectiveness of baclofen in correcting depression and anxiety in patients with alcohol dependence, comparable to the effectiveness of diazepam and amitriptyline. The advantage of baclofen was that it caused relatively few side effects.
A study of the safety of taking baclofen in combination with alcohol consumption was conducted by S. Evans and A. Bisaga [16] on 18 previously untreated volunteers who drank alcohol in high doses (an average of 28 standard drinks per week), but however, they did not meet the criteria for alcohol dependence. A test series of 6 two-day experiments in a hospital setting was performed in a double-blind, placebo-controlled, double-masked design. Baclofen (0, 40, and 80 mg) or an identical-looking placebo was administered 2.5 hours before alcohol consumption. The individual dose of alcohol for each subject was calculated based on weight (0.75 g/kg) and was divided into 4 doses with an interval of 20 minutes. In this study, there were no serious side effects of combining baclofen with alcohol and, in addition, there was no increase in either stimulant or sedative effects when baclofen was given in combination with alcohol, which allowed the researchers to conclude that the use of baclofen in combination with alcohol was safe.
The results of studies of the effectiveness of baclofen for the treatment of alcohol dependence, carried out in a double-blind, placebo-controlled study design, were contradictory. The first randomized, double-blind, placebo-controlled study of the efficacy and safety of baclofen for stabilizing remission in patients with alcoholic cirrhosis was conducted by G. Addolorato et al. [17]. The choice of baclofen for the treatment of patients suffering from alcohol dependence, combined with impaired liver function, was due to the pharmacokinetic characteristics of the drug, which is not metabolized in the liver (up to 80% of the oral dose is excreted by the kidneys), which makes baclofen the drug of choice for this group of patients. The study screened 148 patients with alcohol dependence and alcoholic cirrhosis, of which 84 patients who met the inclusion criteria were randomized. The patients were distributed in a 1:1 ratio into two groups: the 1st group received baclofen (5 mg 3 times a day for the first 3 days, the remaining days up to 12 weeks - 10 mg 3 times a day), and the 2nd group received took an identical-looking placebo for 12 weeks. Kaplan-Meier survival analysis showed a significantly higher retention of patients in remission in the baclofen group. Cox regression analysis also revealed a significantly lower risk of relapse and relapse among patients taking baclofen. In group 1, a lower severity of craving for alcohol was also revealed on the obsessive-compulsive scale.
J. Garbutt et al. [18] a randomized, double-blind, placebo-controlled study of the effectiveness and safety of baclofen in alcoholism was also conducted in the United States. The study included 80 patients randomized into two groups: group 1, taking baclofen, and group 2, placebo. The duration of therapy was 12 weeks, the daily dose of baclofen was 30 mg. Pharmacotherapy was supplemented with low-intensity drug counseling. Effectiveness measures included the number of days of heavy drinking, anxiety levels, and cravings for alcohol. 76% of all subjects completed the study. In general, the researchers noted that the drug was well tolerated, and no serious side effects were noted. Baclofen, unlike placebo, significantly reduced anxiety. At the same time, there was no statistically significant difference in the main and control groups in the number of days of heavy drinking and the frequency of relapses into alcoholism.
Two recent prospective cohort studies [19, 20] have established the effectiveness of high doses of baclofen (up to 330 mg/day) in reducing alcohol consumption. In the first study [19], 80 out of 100 alcohol-dependent patients reduced their alcohol consumption from an initial high level to moderate or low after 3 months of taking high doses of baclofen. After 2 years of observation, 60% of patients remained in the moderate and low alcohol consumption group. Similar results were found in a second study [20], which showed that after taking high-dose baclofen for a year, 80% of 132 heavy drinkers reduced their drinking to low levels. Both studies were open-label and were not accompanied by placebo control, which requires caution in the results obtained.
Thus, given the ambiguity of the data obtained, as well as the good tolerability of baclofen and the absence of serious side effects when used in patients with alcoholism, a real double-blind, randomized, placebo-controlled study (with double masking) was undertaken, the purpose of which was to study the effectiveness of baclofen (baclosan ) with alcoholism.
[edit] History
Structural formula of baclofen.
It makes the article look smarter. The molecule of a new drug for epilepsy with a sabzhe formula was developed by a Swiss chemist back in 1962. The hippies of that time were not interested in the substance, since they had much more powerful things at their disposal, and even for epileptics, the drug baclofen, then known as Lioresal, helped poorly, although it did a good job of stopping the convulsions accompanying epilepsy, relaxing the muscles through its effect on the nervous system. Having seen the profit, the Swiss company released the medicine to the market, fortunately there are a lot of patients with spasms, the same cerebral palsy patients are forced to sit on muscle relaxants for life. After some time, many non-trivial uses were found for the miracle pill.
Signs of Baclofen Use
Due to its potent component, the drug is actively used by drug addicts, mostly of a young age. The fact is that in case of an overdose, Baclofen has a strong, intoxicating effect.
To get high, drug addicts take from 6 to 14 tablets at a time and wash it down with low-alcohol drinks. After 30–40, drug intoxication sets in, which is accompanied by the following symptoms:
- Nausea and vomiting.
- Severe dry mouth.
- The appearance of visual and auditory hallucinations.
- Severe hand trembling.
- Drowsiness.
- A state of complete apathy.
- Dilated pupils.
- Slurred speech.
- Dizziness.
- Impaired coordination of movements.
Amphetamine addicts also often use Baclofen. The drug can easily be diluted with a synthetic analogue of cocaine, thus turning one dose into two. Addicts who take this “mix” experience a strong feeling of euphoria, a surge of energy and auditory hallucinations.
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[edit] Orthodox application
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This rubbish, it turns out, also heals the back. Almost a cyberpunk implant.
A doctor can prescribe baklosan for frequent muscle spasms or spastic paralysis, especially if the patient has suffered a traumatic brain injury without mental complications, suffers from cerebral palsy, senile sclerosis, meningitis and other lesions of the interauricular ganglion , because an unnecessary spasm in the right place is like death for such people, they can be prescribed to soften tonic convulsions in epilepsy, while resulting in an increase in attacks, but this purpose is often served by proven and more powerful benzodiazepines, barbiturates (used only by resuscitators), intravenous forms of valproate or levetiracetam, if necessary - with peripheral muscle relaxants. Used as a corrector for extrapyramidal disorders (tremors, tics) during treatment with certain antipsychotics. A course of baclofen is also prescribed to chronic alcoholics as replacement therapy, but the treatment has not yet expanded beyond the scope of the experiment, and few provincial narcologists are aware of it. Athletes occasionally drink buckle in small (up to 50 mg) doses after rigorous training to relax and relieve pain from lactic acid accumulated in the body. Nerds take the maximum daily dose (70-100 mg) in order to study more successfully before the exam, because baclofen is just the psychotropic that allows you to think outside the box, feel like a kind of Kerouac and dash off your thesis project in one night. Soon, cunning drug addicts found out about the wonderful medicine at the instigation of forum psychonauts-experiments, who satisfied their much more fun needs.
First aid for baclofen overdose
Since the main users of baclofen are young people, loved ones should monitor the condition of drug addicts and identify any changes. The best solution to the problem is to contact professional narcologists, but you must also be able to provide first aid with dosage in order to save a person’s life. To do this, you must immediately call an ambulance, rinse the stomach, and if breathing stops and the heart stops, perform artificial respiration and chest compressions. Resuscitation measures must be continued until the ambulance arrives.
[edit] Impact application
Nofap guru approves of pharmacy staff.
325 mg. I'm proud of Yichan! No dissertation is written on this topic, but a knowledgeable person on the Internet can talk more than one megabyte about baclofen. Buckle is eaten recreationally in the following three cases:
- As an independent substance for the purpose of strong or weak sticking.
- As an accompanying substance for priming, when it is necessary to enhance the effect of the main substance - booze, grass, tussin, etc.
- Like yad, in order to relax forever; the shit out of it is, to put it mildly, so-so.
Almost all baclosan users are polydrug addicts; strictly baclofen addicts are rare online and in real life. The tank is sold in two variations of tablets - 10 and 25 mg (in some places even 75 mg!), and in order not to overdo it, you need to be extremely careful. In addition, it is absorbed through the gastrointestinal tract for quite a long time, about 3-4 hours, so those who like to catch up can be in for a very unpleasant surprise.
[edit] As an independent substance
What what?
Oops, no fucking way! “Everything is poison, and everything is medicine, the only difference is the dose,” said Paracelsus, and this statement is perfectly suited to describe baclofen. Before you, my dear stubborn friend, decide to ruin your liver and MNU, be a beaver, study the hardware thoroughly before you run to the nearest pharmacy.
There are three types of trips in which baclofen can be a conductor, so first you should firmly decide what you want to get from it: a weak high, a strong high, or psychonautics. The action of baclofen is reminiscent of butyrate, and this is not surprising, since sodium oxybate is the same GABA receptor agonist as the subject.
Bad advice from a pickup guru
For a weakly erect adult who weighs 70-80 kg, 50 mg per eye is enough, no more. The sensations in this case are reminiscent of mild alcoholic intoxication with a bias towards euphoria - there is a wild desire to wander around the city, pick up girls who have suddenly become attractive (booze also has the effect of turning crocodiles into princesses, so you need to be vigilant), talk about anything with comrades, even about the “Three Sevens” who were devoured the day before - you won’t give a fuck about their negativity towards you. Wankers like a particularly long fap coupled with empathy for the desired object, and because of the bakla they do not cum for a long time, and this will also please alpha guys with premature ejaculation.
Those who like it heavier should opt for 100-125 mg. Idle weakness will now be replaced by staring at the floor with a paranoid thought in the dying neurons of the suprapharyngeal nerve ganglion. The euphoria will intensify and turn into empathy, like from a shitty fake of ecstasy: this feeling will spread you out on the sofa and dissolve you in the vastness of gray reality with full awareness of your “I”, and when the high ends, this will probably be followed by vomiting and passing out for several hours, but you can get away with only terrible fatigue with aches throughout the whole body (a muscle relaxant) and dizziness like a hangover.
The most questionable off-label use of baclofen is hallucinogenic. Jah, Buddha and Tenant forbid you eat more than 125 mg, and even catch up, but otherwise you won’t be able to see the cartoons.
N.B. |
Honestly, for beautiful visual people it is much safer to swallow DOBA, and for a deeper immersion into your psyche, it is better to opt for tryptamines like LSD and psilocybin mushrooms. |
During the cuts, slides depicting strange worlds will appear before your eyes, which in fact will turn out to be only the fruits of an electrified imagination; after drinking 200 mg, it is better to roll over onto your stomach, otherwise there is a negligible chance of choking on your bilious vomit.
It may happen that someone discovers the city shaman lying unconscious and calls an ambulance, and then the announced list is followed by resuscitation, toxicology and durka, the last point in the case of a particularly powerful psychosis with an inadequate person. The retreat will last for at least three days, during which you are unlikely to want to sleep, on the wallpaper and carpets you can see everything you can think of, and from the unlocked closet, meanwhile, the coat looks out with the unblinking gaze of a cold-blooded killer. If you managed to end up in the yellow house with a buck overdose, and the government shrinks did not find any mental deviations more serious than drug addiction in you, the unlucky glyukolov will be kept in the madhouse for a couple of weeks, but if they find something more serious, then the price for the experience of a dangerous game will be at least a couple of months spent wasted time, a dubious certificate with a diagnosis on discharge and a lifelong registration in a psychiatric hospital at the place of residence. A dod who has eaten more than 500 mg without timely medical assistance can easily throw off his hooves: baclofen has no antidote, and at lethal doses it disables not only the lungs, but also the brain. Because of its deadly effect, the subject is loved by beginners who demonstrate suicide (spoiler:
and also mowers from the army - if it doesn’t lead to suicide, then it will turn out to be due to schizophrenic status, after such a dose you can’t get away from psychosis
)
. To cleanse the gene pool of cargo, there are much more orthodox things like amitriptyline in the pharmacy.
[edit] As a related substance
Baclofen + blue = killer combination
Baclofen interacts well with almost all surfactants from alcohol to heroin, enhancing their effect and occasionally smoothing out side effects.
- Booze. Ethyl alcohol is a related GABA ergic, but unlike sabzh, it binds to GABAA receptors, while the subject of the article is a GABAA agonist. 50 mg of bakla, pumped into the mouth before drinking a bottle of beer or a bottle of wine, relieves the unpleasant emotions of an alcoholic depressant and in some cases eliminates nausea, giving, among other things, periodic headaches with dizziness. It is important not to overdo it with both booze and baklosan, because in the event of an overdose, a substandard state will not take long to occur.
- Grass. Planokurami of the post-Rastman trend also love baclofen, as it allows you to slightly enhance the psychedelic effect of Mary Jane when she is uncool or the drug addict is already hooked on her. But if you have plenty of herbs, don’t worry about poisonous barbiture and be happy. Just in case, there is no need to mix it with spices - after the relatively harmless JWH, they now contain everything from dope to fentanyl.
- DXM. There is nothing special to say about this - the substances have too different effects on the brain, because dextromethorphan is an antagonist of NMDA receptors, but some still note a faster arrival at high plateaus and a longer stay there. Again, those users who are already pretty addicted to tussins, who are discovering the wonderful world of dissociatives, are getting in the way of the syrup, it’s better not to pollute the receptors with such shit. The ease of obtaining also speaks in favor of the unusual combination - “Baklosan” and “Glik” are often on adjacent shelves, so the pioneer does not have to wander around the shops for a long time.
- Psilocybin mushrooms. All nootropics distort the effects of psychedelics, and Buckle is no exception in this regard, so be careful or, on the contrary, act decisively if you want to say goodbye to the roof for a long time and see the sky in diamonds.
- AIDS. Fast fuckers eat baclofen on amphetamine aftereffects, and also often use both drugs together - buckle smoothes out the unpleasant side effects of the joint venture, prolongs euphoria and partially relieves amphetamine impotence.
- Heroin, other opiates and drugs. Since baklosan is also a mild non-benzodiazepine tranquil, it increases the effect of sedatives, and in the case of opiates, it will also enhance euphoria, which is why it and phenibut are mixed with codeine to enhance the latter. Heroin addicts eat bakla during withdrawal symptoms, but they can also use it on their legs.
Baclofen - development of addiction
This drug is often used by patients to enhance other drugs, so it is often combined with alcohol. The development of addiction is due to the fact that the drug opens up potentially hidden capabilities in a person. Fears, complexes, depression, nervousness - all this disappears.
The addict is filled with energy and wants to do something just as long as the effect of the next dose lasts. Chemical dependence is not typical for this drug; the main threat is the development of psychological attraction.
The mechanism of development of addiction can be represented as follows:
- Drug use.
- The effect of the substance on the body.
- Experience of euphoria.
- The end of the pleasure effect.
- Repeat dose to restore effect.
After developing persistent mental dependence, a person feels bad without taking the next dose.
[edit] Perekumar
If you are seriously addicted to baklosan, you can try to get off yourself if he disdains hanging in toxins and dope during washes, phenazepam injections and matings. Baclofen withdrawal is a very unpleasant thing, which is akin to a hangover, or, well, a squirrel - when you take it with extreme cruelty. You should discontinue the drug step by step, reducing the dose of milligrams by 10 every day until you reach zero, and then long-term rehabilitation with healthy sleep, fresh air and complete abstinence from hard drugs. Those caught in baclofen psychosis should give up drugs altogether and learn to think positively. To avoid dependence on bullshit, you should take it no more than once a month in doses of no more than 100 mg, and you need to swallow all the wheels in the indicated size in one fell swoop, in no case catching up, the consequences of jokes with baclofen are deplorable. A slimmer like you won’t be able to get away with it, so you shouldn’t take comfort in your excellent knowledge of theory and natural accuracy - there are a lot of things like accelerated metabolism and individual intolerance that you haven’t taken into account and haven’t even thought about.
Conclusion
Baclofen is a drug that has recently become increasingly popular among young people. We have to deal with facts of its non-medical use more and more often. Its consumers, who seek specifically narcotic effects, are citizens who do not have the means to purchase more expensive prohibited substances.
The constant desire to regularly feel euphoria and cause hallucinations leads to the need to systematically increase the dose of the drug, which is dangerous due to severe poisoning and death of a person.
Using this product is deadly. Relatives should remember this and seek help at the first signs of addiction in a person close to them. In rehabilitation, they can count on a free consultation, drawing up an individual treatment program, and psychological support for the patient at all stages. For help to be effective, it is important to contact specialists as early as possible, before the drug has completely enslaved the mind.
[edit] Memeticity
Baklodram
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Baclofen for dummies
The same Nofap-kun
Until recently, baclofen remained a little-known substance in narrow circles of therapists and pharmacologists, but with the popularization of the psychonaut vale by forums like Bihai, a wide circle of students and schoolchildren learned about baclofen. The relatively low price of around 200-300 rubles made it affordable, and the set of positive effects made it also desirable. Despite the side effects and without reading the instructions, the indoor Siddy Barretts ate white wheels in bottles, after which they continued annealing in the appropriate institutions with orderlies. One of these pretzels described it in the “Book of a Psychonaut”, and another copied this chapter into the “ABC of Domestic Terrorism”, and the last comrade clearly did not stick to it, otherwise he would not have written it down among the substances safe for the carcass, but, in general, then, it is forbidden for phishists to take drugs on kagbe.
An important role in the popularization of baclofen among the new beatniks was played by the imageboards Ychan, Dobrochan and Dvach, where the official baclofen thread was posted in //, which later migrated to Sosach, and after it to Chukhach. At one time there was a neumphag on Ychan, who advocated nofap and regularly took baclofen. During one of the Anonymous gatherings, the character rolled 15 wheels in a couple of sittings and, with the words “I won’t even fall,” sprawled on the ground, babbling incoherent speeches, after which he safely drove off to the hospital.
Still, videos with baclofen gopniks are found on the pipe less often than with bottled carriers, but the hero of the article still has a long way to go in this regard, since psychotropic de facto and de iure bottle is becoming more and more difficult to stir up every year, and it is becoming more difficult to add buckle to the lists of Onishchenko and They haven't made up their minds yet.
Discussion
The results of this study showed that baclofen was not statistically significantly different from placebo in terms of effectiveness in stabilizing remission in patients with alcoholism, as well as in its effect on craving for alcohol, anxiety and depression, which is obviously due primarily to an insufficient sample size. It should be emphasized that in most evidence-based studies of the effectiveness of pharmacotherapy for alcoholism, the sample size was hundreds of patients [31]. In our study, despite the small sample size, rates of remission retention and alcohol consumption (number of days of heavy drinking and average alcohol consumption in grams of pure ethanol) in the baclofen group were slightly better than in the placebo group, and differences between groups in the data the indicators approached the level of statistical significance, which suggests a tendency towards greater effectiveness of baclofen in alcoholism compared to placebo identified in this study. In addition, baclofen was more likely than placebo to significantly reduce cravings for alcohol, anxiety, and depression. Thus, although this study did not clarify the contradictory results of the use of baclofen in the treatment of alcoholism, described in the introduction to this article, it nevertheless allows us to justify the feasibility of further research in this direction.
Baclofen did not differ significantly from placebo in terms of the number of side effects and the effect on the activity of liver enzymes, which indicates its good tolerability and safety of use in this group of patients. These results compare well with other studies of baclofen in alcoholism, described in detail in the introduction to this article.
To make a substantiated conclusion about the effectiveness of baclofen for the treatment of alcoholism, further studies on large samples of patients are necessary.
The team of authors expresses gratitude to the pharmaceutical industry for supporting the study.
[edit] Competitors
A VIP-hacha's nightmare
There are a great many GABA receptor agonists, starting from the bespont aminalon, which is a little less than pure GABA, and all of them, as a matter of choice, have nootropic and inhibitory activity. There are frankly few narcotics among them - these are phenibut, baclofen itself, and another drug that is ready to compete with the hero of the article in terms of psychoactivity. The creators of Viagra also synthesized their anticonvulsant GABAergic drug with blackjack and whores under the trade name Lyrica, also known as pregabalin. Pregabalin, like baclofen, stopped seizures and relieved neuropathic pain (for example, in diabetic polyneuropathy), and also tried to treat drug addiction and relieve abdomen, but patients who had already used it for its intended purpose saw the pinning potential of the new “panacea.” The initiative was taken up by inventive assholes who consume Lyrica clearly not for the purpose of healing, noting its similarity to baclofen, only with the material effects multiplied by 1.5. The junkies didn’t start buying it en masse: the price is steep, for three mowers you can get normal substances. “Lyric” has particular success among the proud residents of sunny Caucasus. Considering the potential teratogenic effect that occurs when males use pregabalin, we are waiting for the result...
Due to its indistinct action and relatively low popularity among rednecks, most gams are not included in the lists of psychotropic and potent substances; pregabalin, however, has been put on the PCU since October 2015. As mentioned above, the exception is butyrates, and then due to wide public outcry.
Medical use
Depending on the purpose, the drug is used in several ways, namely:
Oral route:
- A state of increased muscle tone.
- For tumors.
- Cerebral palsy.
- Stroke.
- Meningitis.
- With alcohol withdrawal syndrome.
Intrathecal method (injection into the spinal cord):
- Pronounced static.
- Multiple sclerosis.
- Damage to the brain or spinal cord.
The intrathecal method can also be used if the patient is intolerant to certain components when taken orally.
[edit] Links
- Instructions for medical use
- About treating alcoholism with baclofen
- Journey to Sklif by the co-author of “The Book of the Psychonaut”
- How to have a snack after it
- Legal drug baclofen
- Baclofen from a psychiatric point of view
- We had five tablets of 25 baclosan, 2 phenotropil, 5 picamilon, 4 phenibut, 1 capsule of 300 lyrica, 4 sodium caffeine benzoate, a bottle of taufon
- Baclofen and pregabalin on Encyclopedia Pathologica
- Narcogenic potential of Lyrica
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[ + ] Baclofen has everything to do with substances | |||||||||||||||||||
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