Stimulants How Amphetamine's Half-Life Invariably Leads to Use of Depressants in Regular Users

[SpunkySkunk347]

One aspect of amphetamine that is not nearly as well-known as it should be is its obscenely long half-life:
- 9-11 hours for the Dextro isomer
- 11-14 hours for the Levo isomer
- 9-12 hours for racemic methamphetamine
Now, those are huge.. Large doses of amphetamine (100mg+) will still be in the system producing effects for days after the last dose was taken.

These half lives make the prospect of true sleep implausible. When a person who has taken amphetamine earlier in the day attempts to sleep that night, any sleep they do achieve will lead to a paradoxical phenomenon: the CNS begins to replenish itself during sleep, causing the amphetamine to kick back in again.

And that brings us to another aspect of amphetamine which also is not nearly as well-known as it should be: the "wearing off" of amphetamine's effects is not necessarily due to the drug leaving the system, but rather it is caused by physical exhaustion; exhaustion of both the body and the CNS. After hours of effects, the brain and body simply begin to run out of the resources needed to continue producing desirable effects.

Now, for a daily user of amphetamine, prescribed or otherwise, this leads to one of two scenarios:

A) as a last resort means of protecting itself, the brain will put itself into a constant state of hibernation with a flattened response to external stimuli - which, by some strange mechanism, denies amphetamine from causing its effects (this mechanism is strange; I've read before that the brain will actually shut down or bypass its own dopaminergic pathways simply to protect itself from amphetamine). This commonly happens to routine users (for example, people prescribed to amphetamine on a daily basis).

B) Insomnia and physical/mental distress becomes inescapable. A user might start binge use of amphetamine at this point, to "power through" to the next night, or the user will seek out a depressant to counter-act the effects of amphetamine. Either way, the user will usually end up opting depressants.

Now, the use of depressants in this manner puts the user into an entirely new "balancing act" of drug use, one that is silly to think you can maintain.
First of all, there aren't really any consequence-free CNS depressants out there that will sufficiently counter-act amphetamine or remedy its comedown. Let's review a few we might speculate as candidates:

- Over-the-counter antihistamines : these fail to be a decent candidate due to a long half-life as well as their anticholinergic effects, which worsen the negative side-effects of amphetamine such as memory loss and mis-sensory (amphetamine in high doses will also produce anticholinergic effects on its own)

- Dopamine antagonists / antipsychotics: these are also anticholinergic, so they fail for that reason, but they can also interact with amphetamine in unpredictable ways, such as by pre-loading presynaptic dopamine vesicles, which can cause amphetamine to become uncomfortably more potent (and not in any sort of recreational way, to any would-be drug potentiatorers) the next time it is taken.

- hypnotic GABAergics such as Zolpidem: these drugs have very little sedative effects compared to their benzodiazepine cousins, and will end up putting the amphetamine user in a fast-paced hallucination-filled dream world, which can be dangerous to a person for obvious reasons.


Anyways, what the amphetamine user is left with for a practical (and by practical, I don't mean healthy) choice is the Big 3:

- Alcohol : the GABAergic effects will slightly counter-act the effects of amphetamine in a direct way; the other CNS depressant effects in alcohol's vast pharmacological profile (NMDA antagonism, for example) will end up increasing amphetamine's euphoria, which can end up perpetuating binges rather than halting them in most cases.

- Benzodiazepines : these are probably the safest option for counter-acting amphetamine. The GABAergic effects will directly counter-act the stimulation from amphetamine, but this comes at a price - a high potential for addiction, as well as long half-life which will leave the user's memory impaired after awakening from the post-amphetamine use crash, which is usually a time when the user will be needing all of his focus to deal with the messes he/she made during the previous session of amphetamine use.

- Opiates : although this option will be the best for remedying the physical pain caused by prolonged amphetamine use, it is by far the most costly and detrimental to one's ultimate health and well-being. It will end up twisting the user into a whole new beast of addiction. I will testify that coming down from amphetamine while simultaneously experiencing opiate withdrawals is one of the worst imaginable feelings and I would not wish it on my worst enemy.

So basically, my point in conclusion:
In my opinion you can't really win with amphetamine; an amphetamine user is going to end up doing his own kind of tight-rope balancing act no matter how he goes about it.

For daily users, taking a few day long break is absolutely essential if one even hopes to keep up the facade of "healthy use".
Otherwise, using amphetamine sparingly during a time when it is actually needed and can be used effectively is, in my opinion, the only way the drug's benefit will clearly outweigh its negative effects.

If there's any sort of a secret to avoiding/mitigating the negative effects of the drug wearing off, it's to be making physically healthy choices while the amphetamine is still in effect, rather than being unable to reverse the damage later on. Sitting in one spot for 10 hours without stretching or doing something strenuous for long periods of time without staying hydrated are the simple mistakes that end up causing a person to reach that state of "hell on earth" from their body/mind/brain having serious damage inflicted upon it.

Thanks for reading.

 

[Amphetafiendd]

REALLY enjoyed this read. Thank you for posting it!! I find myself reaching for alcohol at the tail-end of an amphetamine binge. I find it most effective to alleviate symptoms of obvious exhaustion (or at least mask them). A large amount of alcohol isn't needed either, a 6 pack of beer is generally sufficient to put me into a relaxed state to rest but also lifting my mood for the eminent comedown ahead of me. (NOTE: This isn't a large amount in relation to my drinking habits) What I have posted may not directly relate to your post but just a little thing I have noticed throughout my many bad choices.

Thanks again for this post! Very interesting!

 

[Heroic]

In my case, I found that a few small sips of beer are a must when I feel the first alerts of amphetamine "wearing off" at the end of a binge. Nothing excessive though, I just take tiny sips when I feel I need them, and its really all I need to get into a "smooth down" instead of going on and on.

 

[ddressdd_fr_space]

This is all of what I've been trying to find out with no answers. I take 60mg of Vyvanse every morning (either 6 or 8am, depends). I've been prescribed on and off for a few years, and I've always had very abnormal reactions. I have experienced all of the scenarios in the original post.
Sometimes, a single early morning as-prescribed dose of lis-damph(correct chemical abbreviation for vyvanse?) will last up to 48 hours, with desired effecs wearing off after around 6 hours. With tolerance, this tends to decrease as well as the severity of the comedown effects.
Sometimes I will take a vyvanse and immediately go to sleep, thinking it will kick in and wake me up. What happens is that I can sleep for 12 hours if no one wakes me up, but about an hour after waking up, it kicks in.
To aid with the comedown and insomnia, over the years I've been prescribed to ambien, intuniv(fuck that), and currently, clonidine and hydroxyzine. I hate my current doctor in a way, because being under 21, I'm stuck with this child-adolescent psychiatrist and his policy is that he will not prescribe benzos or hypnotic benzos to any of his patients. But benzos would be the only route that would even make sense.
Ambien would never put me to sleep, just give me a very strange high that gives me an extremely bizarre Tim and Eric Awesome Show type of personality, and cause perceptual effects that I would describe as being like mxe with the visual distortions of psilocybin.
Hydroxyzine does not help. What happens is that I end up getting wasted drunk in my bed after taking the hydroxyzine, and the only way the drug affects me is by giving me a headache and making it impossible to get out of bed next morning.
However, I have had some help with clonidine. For relieving effects I have to take more than directed by my doc, and although my heart rate/blood pressure go away, I'm still very perceptive to my own heartbeat, I can feel it very pronounced and it's distracting/concerning, because my conscious should block it out. I'm glad I'm on it though, it does help and it should be noted as a useful aid for the comedown. It just needs to be made absolutely clear that although alpha-2 agonists are safe in combination with stimulants, NEVER take beta-blockers while under the effects of amphetamines.

I've been out of clonidine for a while and it doesn't help much anyways, so for my comedowns I usually try to find some benzos and take a few mg's of xanax, temazepam, or klonopin. I have to be careful with this, because a month ago, I became psychologically addicted to benzos and almost physically dependent for this reason. Hence my tolerance. Now I've been able to maintain responsibility with benzos. When I can't take benzos, I just tough it out until I'm in bed for the night, and I drink a lot. I used to use opiates for the comedown, but that was the main justification/cause for me becoming addicted to them, and now I'm pretty much a junkie for life on a year-long break due to Vivitrol. Be very careful and don't underestimate the risks with the idea of using opiates for amphetamine comedowns if you're a daily prescribed user.

 

[SpunkySkunk347]

I used to use opiates for the comedown, but that was the main justification/cause for me becoming addicted to them, and now I'm pretty much a junkie for life .[/U][/B]

I can relate completely.. When you've been up for 2-3 days on speed and in your head opiates are the only thing that will cure the pain, opiates end up becoming the bigger of the two addictions because you tell yourself you need opiates in order to begin to start feeling better. For me, that mentality lead me to end up juggling two drug addictions instead of one.

And man, one of the worst feelings I've ever felt in my life is coming down hard from speed and having physical withdrawals from opiates at the same time - you literally start wondering whether you are in Hell or not

 

[drancer]

Sitting in one spot for 10 hours without stretching or doing something strenuous for long periods of time without staying hydrated are the simple mistakes that end up causing a person to reach that state of "hell on earth" from their body/mind/brain having serious damage inflicted upon it.

Oh my god that has me written all over it. I can't help being compulsive, even though physically I truly want to be elsewhere than in front of my computer jacking off for 10 hours I can't pull myself away, even when I have run out of water. If I could have a bedpan in front of me to do a piss instead of tearing myself away from that seat to the toilet I would do it I bet! If I could channel this energy into doing something productive instead what a blessing that would be!

 

[CFC]

Acidify the urine from the outset to dramatically reduce the half-life (eg Ascorbic Acid - Vit C). A pH of 6 will do fine, easy to achieve.

Also, the usual half-life quoted (which varies depending on urine pH, though high-pH urine will usually just result in less amph excretion - with a mostly inert build-up in body tissues eg adipose) is not really the half-life as experienced by the CNS or specific organs - for the brain it's about 2 hours.

For depression, Alpha1,2 and Beta1,2 blocker combination (eg Alfuzosin + Clonidine - A1 + A2, plus propranolol - B1 + B2) to inhibit NE. This will specifically flush the CNS of toxic build up (which happens during slow wave sleep when the brain shinks) and at least switch off the worst stimlating effects. Make sure you leave a gap from your last dose of amph though - maybe 6 hrs or so (blocking NE while blood levels of amph/meth are high can potentiate DA neurotoxicity).

Also, GBH/BL (GABAb) inhibition (keeping the dose low to offset glutamate rebound) would be more effective choice than benzos GABAa - GABAb produces superior quality sleep. GABAa supresses SWS, leaving groggy and probably too much toxic crud still in brain (plaques, oxidants etc).

Another relatively low-risk option would be a calcium-channel blocker (esp something like Verapamil). Will reduce vasoconstriction, attenutate tachycardia, and is quite relaxing/drowsy via CNS effects. Avoid extended and delayed release versions though.