Health - GHB and sleep, important information for rec users.

[MrG]

First a brief explanation for those unfamiliar with Xyrem:

Xyrem is, primarily, prescribed for Narcoleptics who suffer from daytime cataplexy. Cataplexy manifests itself as muscular weakness which may range from a barely perceptible slackening of the facial muscles to the dropping of the jaw or head, weakness at the knees, or a total collapse.

The patient is prescribed a, twice nightly dose (titrated to begin with in order to reduce the chances of nausea) of 4.5g of Xyrem taken at bedtime and another 4.5g taken upon awakening 4<> hours later.

Xyrem has, by all accounts, shown a remarkable efficacy at reducing or even eliminating these cataplexy attacks and, in some cases, allowing a number of patients to reduce their daytime stimulant medication.

What does this mean for the recreational GHB user?

Well, Xyrem is Sodium Oxybate is NaGHB, the sodium salt of GHB ( Gamma-hydroxybutyrate ).

Leaving aside the obviously ludicrous situation in the USA of GHB being on schedule I, meaning that it is considered a highly dangerous and addictive drug with no medical uses, but GHB marketed as Xyrem and prescribed for specific conditions is on schedule III, which includes many drugs considered safe when used properly, we should look at what Xyrem (GHB) actually does for these patients.

It is not a topical medicine, nor a cure, neither is it some sort of exotic drug designed to target the deficiencies within the Narcoleptic's brain. It does not correct their defective brain chemistry.

It simply aids their sleep.

Really? Is it that simple? - Pretty much.

The sleep of narcoleptics is abnormal and characterized by: a short sleep latency; frequent sleep onset REM periods (i.e., REM sleep begins within 30 minutes of going to sleep); REM period interrupted by arousals; higher than normal amount of time spent in stage 1 but less than normal amount spent in slow wave sleep; and frequent arousals from sleep. This results in the patient suffering regularly from very poor quality sleep which can lead to many cataplexy attacks during the day despite the use of prescribed stimulants.

Their brain is simply exhausted and is unable to recover or repair during the night as the patient cannot maintain quality slow wave sleep.

GHB counteracts these abnormalities by increasing slow wave sleep, lessening stage 1 sleep, and reducing arousals from rapid eye movement (REM) sleep.

Simply put, they spend less time in "shallow" sleep and more time in the reparative slow-wave sleep stages ("Deep" sleep).

One similarity in an otherwise healthy person is the parent of a new-born baby. They will likely experience a similar state of regularly interrupted sleep which reduces their ability to reach and maintain the slow-wave stages which can lead to extreme states of mental exhaustion during the day. Although at least they will, eventually, recover as soon as junior can sleep through the night regularly!

In fact, as a quick asides, there are many, many, physiological problems that are the direct result of a poor night's sleep. Even though a person may be unaware of the poor quality sleep they are frequently experiencing, stress, worry, environmental factors (excessive noise, light etc.) and drug abuse can easily result in a night's sleep consisting of bouncing between stage one and REM sleep without properly reaching the reparative stages.

After a length of time, there can be serious implications for the person who is frequently unable to reach and maintain quality slow-wave sleep.

All well and good but rec GHB users are usually more interested in the intoxicating effects of smaller doses of GHB, that's not the same thing as these pharmaceutical sleep doses, is it?

Therein lies the rub. NaGHB is often used by people in a recreational setting either on it's own as a substitute for the similar effects to alcohol (but must never be taken with alcohol!) or in combination with stimulant drugs such as MDMA or Cocaine. Research has proven to actually support the recreational users belief that NaGHB can counteract some of the negative effects of these stimulant drugs (high blood pressure, anxiety etc.), even proving to cancel the craving associated with cocaine use.

But back on topic, what's the issue with recreational use of GHB?

It's all in the dose. A rec user will, typically, take a dose of <>1.5g of GHB repeatedly during the course of an evening in order to experience the desired effects without falling asleep. When they are finished, they will often choose to fall asleep in their beds and wake up the next day, sans hangover.

So where is the problem?

First you need to understand the stimulating and sedating effects of GHB

Stimulating?

Yes, as any regular GHB user will tell you, small <>1g doses of GHB actually serve to act as a mild stimulant, increasing metabolism (profuse sweating under physical activity), sociability and talkativeness without the intoxicating effects. Unfortunately, this can often lead to those who suffer from anxiety and other social disorders to chronically abuse GHB by taking it every couple of hours in order to avoid these mental stresses. If maintained over an extended period, this can lead to the, much publicised and hyped, GHB addiction. But that's another issue.

So how come GHB can be both stimulating and sedating?

There is evidence that activation of the GHB receptor in some brain areas results in the release of glutamate - the principle excitatory neurotransmitter. GHB's effect on dopamine release is biphasic, low concentrations stimulate dopamine release via the GHB receptor. Higher concentrations inhibit dopamine release via GABA(B) receptors.

This explains the paradoxical mix of sedative and stimulatory properties of GHB, as well as the so-called "rebound" effect, experienced by individuals using GHB as a sleeping agent, where they awake suddenly after several hours of GHB-induced deep sleep. That is to say, that over time, the concentration of GHB in the system decreases below the threshold for significant GABAB receptor activation and activates predominantly the GHB receptor, leading to wakefulness.

Why then is Xyrem not given in a single large dose so the patient can sleep eight hours in one go?

Because doses above 4.5g can result in a severely depressed CNS (Central Nervous System) which could lead to unwanted complications or seizures.

4.5g of GHB will induce sleep for about 4 hours, hence the twice-nightly dose. In all the patient will receive a total of 8 hours of quality slow wave sleep cycles.

And the recreational users choice of multiple small doses?

Well, whilst they may enjoy the intoxicating effects during the evening, when they choose to actually go to sleep the continuing level of GHB in the brain is likely to assist them in drifting off but, once that level has fallen sufficiently, the stimulating effect still kicks in even though they are asleep and will result in a period of poor quality sleep which, once the ingested GHB has been eliminated from their body (usually within a couple of hours at rec doses), will then allow them to resume their normal sleep pattern. Only they will, by then, have probably lost half of their proper full night's sleep.

What is the likely effect of this?

Anybody who uses GHB as an intoxicant should be aware of the fact that, whilst they may find it does help them achieve sleep easily, they will not actually be getting a full night of quality sleep. If this is maintained regularly they are likely to suffer from symptoms associated with sleep deprivation.

What would be the best way to counteract this?

If someone chooses to use GHB recreationally, they should ensure that their last dose is taken at least two hours, maybe even three depending on the size of the dose, before they intend to go to sleep. This should ensure that it is eliminated from the body in time for the stimulant effect to have passed in order for the user to get their usual night's sleep.

What if they are interested in experiencing a full night of GHB induced sleep?

Then they should not be using it during the same evening. There is a wealth of research to support the safety and efficacy of GHB at the twice-nightly dose of 4.5g, but not following an evening of GHB induced intoxication.

Again, this cannot be stressed highly enough, nobody should attempt to use GHB after consuming alcohol as this can result in a severely supressed CNS which could lead to death.

Otherwise, in a healthy person, a night of GHB induced sleep (2 x 4.5g) can, allegedly, offer a remarkably refreshing experience, especially given that many of today's ill's can be attributed to the poor quality of sleep often suffered by those in the modern world.

What about GBL instead of GHB?

Again, there is a wealth of research to support the safety and efficacy of GHB at the twice-nightly dose of 4.5g, but not a scrap concerning attempting the same with GBL. Nobody should assume the same is applicable for GBL as for GHB, because it isn't, don't be a human guinea-pig.

Reputation Comments on this post:

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[soundfactory]

someone heavily addicted to ghb would be ubable to find a dose high enough to keep them asleep for more than 2 hours. even with 1000mg of seroquel in addition to the g swim couldn't stay asleep.

[MrG]

Someone heavily addicted to GHB is not classed as "healthy".

There is a wealth of research to support the safety and efficacy of GHB at the twice-nightly dose of 4.5g, but not following an evening of GHB induced intoxication.

This should pretty much negate the 24/7 GHB addict too.

[Milk man]

Would it be possible to make an extended release version, so that it would maintain the levels of GHB in one's system? Or is there too many variables in determining the correct rate of adding GHB to one's system. I understand this would be a VERY large pill(or very many) and the company would be liable if the extended release was mal manufactured and it all released at one time.

[MrG]

My, current, understanding is that the mechanism of action is the reason why an XR version is unlikely to be released.

Whilst the jury is still out on stating exactly what the full physiological picture is, with regards to GHB, the smart money is on the fact that it is known to bind with both GABA-B and GHB receptors with the sedation being caused by the GABA-B binding at an appropriate dose (usually greater than 1g) and the sudden wakefulness, or mild stimulation, occurring as the dose wears off leaving only the GHB receptor being activated for a period.

My, personal, theory is that the problematic effects created by 24/7 dosing may be due to the continual GHB receptor activity from the repeated GHB administration whereby, after the GABA-B activity has subsided as the dose wears off and the stimulatory effects begin to show, the addict then feels the need to redose in order to feel calm again. This ultimately results in the no-win situation whereby the addict cannot help but to keep redosing meaning the GHB receptor is permanently affected by the repeated dosing of GHB.

An XR release version of GHB is likely to result in the GHB receptor being stimulated for a greater length of time than is currently proven as safe (2x4 hours).

Given that GHB has a very short half-life in-vivo it has been quite puzzling as to how people become addicted to it, this theory would make for a reasonable explanation.

[JoeM]

Found this, http://www.erowid.org/archive/rhodiu...istry/ghb.html, which I'm sure most people have seen before. Among the list of alternatives to GHB is Methyl 4-Acetoxy Butanoate (MAB) with a 6-12 hour duration. ie might allow for a good night's sleep with one dose. Not much is said about it except 'somatic effects are very nice' Maybe that a reference to pro-sexual effects.

Another one there is trans-4-Hydroxy-Crotonic Acid (T-HCA) which is said to be a 16% more potent GABA receptor agonist, but again little is said about it's effects. Where would SWIM find out more about these synthetics?

[MrG]

Exactly, where does one find out about a substance that has had little or no independent research conducted?

Be advised that statements made in patent applications are not necessarily verified and, just because a product is granted a patent, it does not actually mean that it works.

The lack of available information on these two compounds is a concern and I would advise anybody who, as a result of their government's heavy-handed GHB prohibition, is looking for a novel alternative, to tread extremely carefully in this regard.

[JoeM]

Agreed yet it is very frustrating trying to get information on this and similar substances, frustration pushes rash people to do stupid things. I'm sure someone knows but they aren't letting on. Selfish buggers.

And now something useful. SWIM was reading today on this forum of another SMIMMER who claims 1,4-B is good for avoiding the passout and rebound effects that he/she got with gbl/ghb. They said, whereas with gbl they were often either in danger of falling asleep or vigorously bouncing back, with 1,4-B they were pretty much always balanced in the middle until effects wore off. Something to think about.

[freekdl]

Originally Posted by MrG

Stimulating?

Yes, as any regular GHB user will tell you, small <>1g doses of GHB actually serve to act as a mild stimulant, increasing metabolism (profuse sweating under physical activity), sociability and talkativeness without the intoxicating effects. Unfortunately, this can often lead to those who suffer from anxiety and other social disorders to chronically abuse GHB by taking it every couple of hours in order to avoid these mental stresses. If maintained over an extended period, this can lead to the, much publicised and hyped, GHB addiction. But that's another issue.

Interesting part.. After a good night of going out on G, swim always has the symptoms described above.

Swim must admit that he is a person that suffers from anxiety from time to time, guess that's the price he has to pay for his amfetamine & cocaine abuse in the past..
For example he can't smoke weed before work or when he has an appointment with people he hasn't met before. If he does, he can't make eyecontact for more than 10 milliseconds, he has cold, sweaty hands and making a conversation is like going trough hell.

After a night of G, it's even but worse! He feels depressed for 2 days, it feels like his hands are shaking altough they aren't, that weird sense of fear & panic all the time.

To be honest it's an issue that's been bothering swim for quite a while.
He didn't have all that s*** in the past & it would be a dream to live without it again..

freekdl added 0 Minutes and 51 Seconds later...

Swim must add that he is not a chronic user.. Not at all!

Maybe once in a month..

[Synesthesiac]

Originally Posted by MrG

GHB's effect on dopamine release is biphasic, low concentrations stimulate dopamine release via the GHB receptor. Higher concentrations inhibit dopamine release via GABA(B) receptors.

Thats weird. And interesting. I've read elsewhere that using GHB can actually give you the opposite of a hangover the next day, you'll feel quite energised and alert... Ah here it is:

http://biopsychiatry.com/

Most remarkably, the moderate user may awake refreshed after a deep restful sleep: GHB appears temporarily to inhibit dopamine-release while increasing storage, leading to the brightened mood and sharpened mental focus of a subsequent "dopamine-rebound".

Sounds good, if only more drugs were like this

[Denny007]

swim an ex junkie,i lived in SE asia,sorry if this kind a bit stupid to ask,but what is GHB?what form(pill,tabs,powder,or liquid)?how do swim take it(oral,soke it,snort,IV'ing)?
this will helps a lot,guys,thanx