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Amphetamine (stim) during the day, then blocker (Ziprasidone) at night for sleep

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yoyoman

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Jun 11, 2006
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I was on high dose dexedrine for many years (but not in the last few years). One of the big problems I had was that I couldn't sleep good at night, so i'd need to take extra dex during the day.. which led to me being burned out and had to totally stop eventually.

Well lately i've been playing around with some d-methamphetamine, and happened to score a bottle of 30 x 40mg Geodon's (ziprasidone). Wow the stuff is amazing even when I binged on the meth - last night taking 40mg IM pure d-methamp around 11pm, around 1am I took one 40mg geodon, and I slept like a baby all night (it kicked in around 3am, totally killing the meth's effects). Woke up feeling GREAT!

So I got this idea in my head - do certain anti-psychotics like Geodon or Seroquel work good to kick amphetamine's off the receptors? Geodon just happens to have a short half life, and seems that its duration of effect (stopping meth from working) is about exactly 8 hours. This just seems like it could be a near total solution for people taking daily amph scripts, because during those 7-8 hours at night the brain can upregulate those receptors a little (possibly lower tolerance a little til the next day's amph)

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So is it really working like i'm thinking/guessing its working? A google search on the pharmacology says:
Ziprasidone exhibited high in vitro binding affinity for the dopamine D2 and D3, the serotonin 5HT2A, 5HT2C, 5HT1A, 5HT1D, and α1-adrenergic receptors (Ki s of 4.8, 7.2, 0.4, 1.3, 3.4, 2, and 10 nM, respectively), and moderate affinity for the histamine H1 receptor (Ki=47 nM). Ziprasidone functioned as an antagonist at the D2, 5HT2A, and 5HT1D receptors, and as an agonist at the 5HT1A receptor. Ziprasidone inhibited synaptic reuptake of serotonin and norepinephrine.
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Is blocking D2 and D3 (or any of the other ones) enough to stop amphetamines from totally working? What about the DAT transporter and VMAT2?

I feel stimulated today but I did not take any more meth, so it seems the ziprasidone just temporarily stops it from working for about 8 hours.
 
In theory a short-acting dopamine receptor antagonist will cause an upregulation of dopamine receptors, so when it wears off your CNS will be primed for dopaminergic stimulation. Some people describe this phenomenon as tolerance-reversal.
 
Slapdragonx said:
I am in Risperidone withdrawal right now, would that mean that I will need less amphetamine to get high?
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yes, absolutely

But why do you take amphetamine an resperidone at the same time ??? It's totally unthinkable... It's exactly like driving a sportcar while putting the handbrake on...
 
sounds like a crazy way to get parkinsons or mess up your dopamine receptors
 
^it is. In my and others experience with meth and dex, I encounter a distinct and reoccurring phenomenon which may have something to do with this; what actually happens after continued amphetamine use is neuroadaptation and up-regulation of β-adrenergic output. This is most evident during the acute withdrawal syndrome when you can actually feel the effects of the adrenalin overage. At first it feels like you "wake up feeling great" or "stimulated" but with continued use and tolerance the effect becomes more pronounced and feels quite uncomfortable up to the point of actually causing palpitations and panic. This is because the β-adrenergic receptors have a direct effect on the sympathetic nervous system and the fight-or-flight response. Although this syndrome is not very common, if you do reach this point and symptoms don't reside you may need to be put on a beta-blocker such as propranolol for a while.
 
Well it was working great (the geodon at night, meth during the day) for a few days.. then it seems i got a tolerance to the geodon, so even 80mg wasn't enough to put me out after doing some meth :(.
 
Methamphetamine IV or IP is a neurotoxic standard. You might want to ease up on that, if you like things like sleeping, functioning, feeling good in general...
 
^^ I was on 60mg dexedrine for years (prescription) but do not take it anymore. This meth thing is just cause I stumbled across some and i'm almost out of it - I know I can't take stims daily it always screws everything up... But the geodon thing had my hopes up, that one day I could get back on daily dexedrine and have a way to regulate sleep etc (one of the biggest problems being on daily stims, coming down enough to sleep)

Always hoping for some "cure" for the downsides of taking stimulants on a daily basis. It worked for a few days anyway..
 
I have a bunch of Geodon also.Will it help with anxiety like benzo's do?...I dependant on opiates,and have to take suboxone when I run out,and benzo's really help out,either to sleep,or just during the day if I feel anxious(which I do all the time if Im not on anything)I took it once,and it was whan I was out of everything,and I mean everything! So I took one,in hopes of getting sum shut eye,but I kept waking upand feeling anxious,and the next morning I woke up was HORRIBLE!!!..I felt like I was going thru worse withdrawls,my legs were hurting,and I had extreme RLS.my heart was beating so and I felt do bad that I wanted to go to the hospital to see if they would give me a shot of diphenhydramine.
Instead I scrambled around the house,looking for any antihistamines.I ended up taking sum cold pills with I think claritin,doxylamine or diphenhydramnine or somn.in about a couple hours is wen I started feeling better.
But,since I do now have suboxone will it be o.k to take for sleep if I need it?Does anybody think it will add a nod to my suboxone dose?
 
No, it will make you pass out. This stuff shuts OFF your dopamine, so you will have no energy. No nod, only terribly long passed out sleep.
 
I would be a little wary of Geodon. Of all the antipsychotics, it's the one that I've heard the most serious side effects about, mostly heart-related issues. On top of amphetamines, I'd be particularly careful about heart problems. I know a couple people who had to go off of it as a result. Also, it's contraindicated with a huge number of drugs, some of which are listed past the jump:

NSFW:
Before taking Geodon

Geodon is not for use in psychotic conditions related to dementia. Geodon may cause heart failure, sudden death, or pneumonia in older adults with dementia-related conditions. Do not use this medication if you are allergic to ziprasidone, or if you have:

a personal or family history of "Long QT syndrome";

history of recent heart attack; or

uncontrolled or untreated heart failure.

Geodon should never be taken together with any of the following drugs, or a life-threatening heart rhythm disorder could occur:

arsenic trioxide (Trisenox);

droperidol (Inapsine);

halofantrine (Halfan);

tacrolimus (Prograf);

antibiotics such as clarithromycin (Biaxin), erythromycin (E.E.S., EryPed, Ery-Tab, Erythrocin, Pediazole), levofloxacin (Levaquin), moxifloxacin (Avelox), or pentamidine (NebuPent, Pentam);

anti-malaria medications such as chloroquine (Arelan), or mefloquine (Lariam);

heart rhythm medicine such as amiodarone (Cordarone, Pacerone), dofetilide (Tikosyn), disopyramide (Norpace), ibutilide (Corvert), procainamide (Pronestyl), propafenone (Rythmol), quinidine (Quin-G), or sotalol (Betapace);

medicine to prevent or treat nausea and vomiting, such as dolasetron (Anzemet) or ondansetron (Zofran);

medicines to treat psychiatric disorders, such as chlorpromazine (Thorazine), clozapine (FazaClo, Clozaril), haloperidol (Haldol), pimozide (Orap), or thioridazine (Mellaril);

migraine headache medicine such as sumatriptan (Imitrex, Treximet) or zolmitriptan (Zomig); or

narcotic medication such as methadone (Methadose, Diskets, Dolophine).


Does anyone with more phamacologic knowledge than me have a guess why all these drugs are contraindicated? Why methadone for example?
 
Yes Geodon seems to have heart problems, and it is especially bad for recreational drug users who might have accumulated cardiotoxicity. Why not try something like risperidone? Honestly I found all other antipsychotics to feel just plain nasty. Also, don't be surprised if risperidone doesn't up-regulate your dopamine receptors, this stuff isn't set in stone, do we know which receptors exactly up-regulate with antagonists / inverse agonists?
 
I had olanzapine/Zyprexa administered IM in a hospital due to an IV methamp 'overdose' (I had psychotic symptoms after being up only a single day, hearing voices and extreme paranoia, but level headed enough to admit myself to a hospital, but I think that's due to my own education on the subject). I am/was very experienced with that route and that substance at the time; I believe sensitization to negative side effects with it accrued over time. (I formerly have been able to stay up for 10 days in a row with minimal negative effects, now immediately after the initial dose I can have instant psychotic symptoms)

The day after (and sleeping about 24 hours in the hospital itself) I experienced dysarthria for the next two days, which is supposedly a "overdose" symptom: i.e. I had a speech impediment, I couldn't articulate anything I was about to say without an extended slur/stammer at the beginning of any word. Reading the long term neural toxic after effects of those type of dopamine antagonists, it isn't something I'd recommend; actual shrinkage of the brain, etc.
 
I have found that taking seroquel after taking amphetamine is highly uncomfortable -- quetiapine causes akathisia which is amplified tenfold by amphetamine; quetiapine also causes vascular constriction which will compound with the vascular constriction caused by amphetamine.

Keep in mind that although some anti-psychotics may block some of amphetamine's mental effects via DA antagonism; the amphetamine will still very much be active on your peripheral nervous system (which is where many of amphetamine's negative physical effects are derived from). So most anti-psychotics (the ones that are H1 antagonists at least) will worsen symptoms such as coldness in the extremities, muscle tension, hypertension, and tachycardia.
 
SpunkySkunk347 said:
I have found that taking seroquel after taking amphetamine is highly uncomfortable
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Seems intuitive that such would be the case. In tandem seems a different story though; I do know from experience that observed individuals seem to act rather odd when taking n-methylamp & seroquel at the same time. Falling over like a board flat to the ground with eyes kept closed, resulting in a reclining near fetal position, all while in a calm and perfectly articulate tone with reasonable demeanor proclaiming how they are perfectly alright to drive, as they feel around crawling 'in the darkness' of their closed eyes (which they do not seem to realize are or how to remedy)
 
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