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  • BDD Moderators: Keif’ Richards | negrogesic

Reaction to prochlorperazine (akathisia) - also discussion on gastroparesis

Grapefruit juice is well-known to interact with different drugs, especially stronger opiates like oxy.
Grapefruit juice is a potent inhibitor of the cytochrome P450 CYP3A4 enzyme.

Anything that inhibits the P450s can prolong or increase the effects of a drug.
And oxycodone is known to cause digestive problems like nausea and constipation with continued use!

But gastroparesis onset directly linked to grapefruit....twice.
Hmm.

That is rather severe, so I would assume that any inhibition of P450 enzymes could cause major metabolic changes in your system.
Hydrocodone is a substrate for both CYP3A4 and CYP2D6 enzymes, meaning they react to form a different compound (morphine).
But you are inhibiting the CYP3A4 with grapefruit, causing its effect to slow down.
Oxycodone is mainly metabolized by CYP2D6, so I don't know if there is any overlap.

Enzyme interactions are damned complex and understanding them won't really explain gastroparesis.
Maybe a little nausea and cramping, which is fairly common in some people.
But not hours of food sitting along with a lack of drug activity, then a sudden onset.

I should mention that a much milder version of those events has occurred to me with hydrocodone.
I find myself feeling almost nothing from it, until suddenly my gut starts moving.
It is the serotonin activity involved in digestion that exposes some of the brain pathways to the drug.
On nights when I am completely empty, there might not be ANY effect no matter how long I wait.
If I am too full, the effect is delayed until gastric movement occurs.
I literally have to time it just right to achieve the desired effect, and movement in my intestines is the key.

Its kinda like first and second-pass metabolism with alcohol.
A portion of it is absorbed in the mouth and stomach, but when the stomach empties into the small intestines, there is a sudden increase in blood alcohol content.
This is a big cause of alcohol poisoning, because people are not aware just how much they have had if their stomachs are full.

I have come to believe that there is much more than first and second pass.
I think that each section of the intestines represents its own metabolic potential, exposing more of the brain to the contents of the bloodstream.
Serotonin, which drives digestion, also influences blood distribution throughout the brain!

I imagine that this is a seamless event for most people, undetectable and uninteresting. The gut is firmly bound to the brain.
Only on night of heavy drinking could someone relate to the idea that the further down the gut it travels, the more regions of the brain will feel the effects.
Even all the way down to the large intestines!
In fact, the lower it goes the more euphoric the experience.

The seamless nature of the brain-gut circuitry has been interrupted in both of us.
Whatever the contents of our bloodstreams, be it alcohol or opiates, it does not effect our brains the same way.
Even smoking weed seems to rely on the movement down below!
Some days it feels normal, some days it does NOT.

I do not really believe that each segment of intestines further absorbs the drug...
Many drugs are easily absorbed in the first section of small intestine and stomach.
And the similar effect with smoking pretty much rules that out.
It is the smooth uniform contraction of the GI that allows the brain even, uninterrupted access to ANY drug or drug metabolite in the bloodstream.
I hope this is making sense to you.

Think of your gut like an accordian that is being constantly tugged on.
Sometimes it is not a gentle tug, but a pull or push.
The rhythm of this instrument is critical to the right notes being played in the mind.

It turns out that digestion, along with a number of emotions, are the result of a carefully tuned symphony of events.
And I never would have understood this so well before.

That is the best explanation I can offer you buddy.
Your accordian, your symphony, is out of sync.

In general, I recommend against regular drug use even opiates.
If I understand your other posts correctly, you often fail to feel any euphoric effects in the first place.
And you are tinkering with your metabolic enzymes...

If you didn't take oxycodone, you wouldn't have some of these problems.
But my guess would be that you DO feel some reward from taking it, or you just wouldn't be interested.
Combating gastroparesis with medication like D2 antagonists sounds like a very temporary solution to me - treating the symptom not the cause.
Medicine is capable doing more harm than good, especially when it come to anti-psychotics.

The cause is your damaged serotonin transmission.
And there is no drug to correct this, yet.

But I HIGHLY recommend exercise when you have a full stomach.
Healthy diet with lots of fiber and fluids should be a daily part of your life!
But if you stray from this healthy diet for even a day, I firmly believe that getting your BLOOD PUMPING will combat the lack of digestive ability.
It will push your symphony back into sync.

Anytime I have a bad feeling in my gut, especially when it effects my mood...I do pushups on the spot.
Especially if I really don't want to.

It is when I am the least comfortable that it makes the most difference.
I do quite a few - up to 300 in a night!
But it takes a lot to get me winded now.
The whole point is to do something that makes your heart pump faster.
This will increase enzyme activity, metabolism throughout the body, and encourage gastric emptying.

And it increases plasticity in the serotonin nerves in your brain!
Exercise is about the ONLY treatment that exists for MDMA related serotonin toxicity.
I wish I had more advice for you, but I don't.

Maybe a mild amphetamine like selegeline would help you.
Maybe low-dose ketamine.
I have considered both.

I will stick to my daily exercise regimen for now.
I really can't imagine what level of function I would be at without it.
You should be exercising every single day.

Good luck.
 
First Bad Comedown, Thanks so much for all your help. I am glad you posted as you seem to know a lot.

You found my comment about not feeling anything euphoric from oxycodone and you made an observant judgement saying "you DO feel some reward from taking it, or you just wouldn't be interested"...

It is true I get no euphoric feeling at all, if anything I get the opposite by often feeling dysphoria from Oxycodone but I will be honest, the only reason I keep going back to it is because Oxycodone helps me get my mind off the physical and emotional pain, even having an adverse reaction to it sometimes makes me forget the pain and as crazy as it sounds I have come to look forward to the adverse reactions, i know i must be one sick puppy ey? the other reason i take Oxycodone is because it makes sex last longer both through its depressant effect and its adverse reactions by distrupting my vitals, which is why I keep coming back to it, otherwise there is absoloutely no other benefit for me from Oxycodone or any other pain killer.

I will definetly take up your advice on excercising, you are too right about that, in the past I have seen its benefits and it has even stabilised a lot of my symptoms, thanks for such an excellent advice.

I did a bit of research on the topic of Grapefruit Juice and Gastric emptying and right away my search results found several articles stating that the potentiation effects of Grapefruitjuice are not only due to inhibition and effect on enzyme activity but also due to its effect of slowing of gastric emptying.

This study shows that grapefruit juice interferes with the metabolism of NIF by inhibiting NIF metabolism and slowing down the rate of gastric emptying. This study also confirms that the metabolic inhibition is not a first pass effect, but is a secondary oxidative step.
http://www.ncbi.nlm.nih.gov/pubmed/15811168

the delay in nifedipine absorption by GJC or OJC results from delayed gastric emptying.
http://www.ncbi.nlm.nih.gov/pubmed/9570001

Grapefruit juice or grapefruit: significantly increases plasma levels of buspirone. The possible mechanism of this interaction caused by grapefruit juice is delayed gastric emptying and inhibition of cytochrome P450 3A4.
http://www.sideeffectsofmedication.com/buspar-side-effects/

As a result of delayed gastric emptying, grapefruit and pineapple juices may moderate sharp increases in postprandial plasma TAG concentrations accompanying peak digestion and absorption.
http://www.ncbi.nlm.nih.gov/pubmed/16319784
 
Opiates are agonists at dopamine receptors.
And you are living with hindered dopamine transmission because of the serotonin damage.
Although the typical feelings of pleasure may be absent, the uncomfortable feelings may be a result of dopamine release which temporarily makes you feel just a little better.
You are pushing back against the onslaught of serotonin!

Exercise is the best way to do this, of course.
Aside from BDNF induced serotonin growth...
It both releases dopamine and restores adrenal function.
Healthy adrenals mean lower serotonin...

I'm glad to hear your response.
Push yourself for a solid 20minutes a day, 5 days in a row.
Then come back and tell me how you feel on day 6 and 7.
I really want to know.

Great studies you found on Grapefruit.
I never knew...

I am normally cautious about recommending drugs to people....but I will make an exception for you.
Since you like opiates, there is an astonishing option available that provides a very unique and LONG lasting opiate high.
Poppy pods.

Poppy is of course the flower that all opiates, including oxycodone, come from.
And heroin.

What is surprising is that poppy pods are available for purchase online legally, as decorative items.
This is an interesting loophole and it results from the fact that poppy grows easily across North America - and there is nothing the government can do to stop it.
Owning a poppy plant or purchasing the dried pods is necessarily legal.
Only when you begin processing the pods into a useable form have you committed a crime.
Of course having posted online about your knowledge of pods recreational value can be used as incriminating evidence...

All of this aside, poppy contains many alkaloids that oxycodone does not.
The best pods are called tazmanian and they contain a much higher level of morphine.
This is the species of poppy that the world's pharmaceutical supply comes from.

I recommend pods to you for a simple reason - they are stronger than people assume and the buzz lasts many hours.
Even heroin addicts are surprise by their potency.
It is not the increased dosage I am recommending for you, it is the increased alkaloid profile.
Perhaps with the right mixture, you would actually enjoy the feeling.

But I must warn you - they are STRONG.
Many posts can be found of people that underestimate the strength.
Some idiots will grind up five whole pods their first time.
Then they claim near-death experiences!

Even a whole pod is a HUGE dose for me.
I find that about a fourth of one pod will last me many blissful hours.
And it is indeed a very deep, blissful body high.

Unlike pills, which normally hit me within an hour, pods take at least two hours to start.
And they do not peak until FOUR hours!
This is a big cause for retarded dosing - people don't feel anything and just take more.

Another warning - pods create cramps in normal people.
And nausea in others.
I find the stomach discomfort to be tolerable, but strong.
And it is also stimulating like a cup of strong coffee at some points.

It is not the most comfortable opiate high, compared to hydrocodone or oxy.
But considering tramadol makes me fucking freak out, I consider mild discomfort from poppy to be well worth the intense euphoric buzz they provide.
Since your system is so different and responds to drugs with lots of anxiety - I highly recommend you start with tiny doses.
If it turns out to be really uncomfortable for you, it will last much longer than you want it to.

But there is a chance it will turn out to be the best opiate buzz you have felt in a long time.
I highly recommend it, but stay AWAY from grapefruit on that stuff.
And whatever you do, do NOT make a habit of taking it.

I have read heroin addicts that claim poppy withdrawal is WORSE than heroin!
The same varied alkaloid content that makes it so satisfying also makes it more addictive and difficult to stop taking.
People have really fucked themselves up by taking the stuff weeks in a row.

I hope you try it and enjoy it - responsibly.
Especially after a week of exercise.
Let me know.
 
We don't usually have long discussion threads in BDD but this one is clearly useful (and interesting!) so I'm not closing it - I am however going to change the title to attempt to reflect the change in direction of the thread, hehe. Hope that is okay :)
 
For such an awesome thread, Altered Perception should tell his story.
Remind people about what happened to you.

Neffie, I appreciate that you have allowed this topic to continue and I am pleased with the title change as it is much more descriptive and accurate.

First Bad Comedown, thank you for your interest and I will do my best to tell the events leading up to my condition as briefly as possible, however I don't want to push my luck by straying too far offtopic as Neffie has been very understanding in allowing this thread to continue.

About 12 years ago my life was all about going out to raves and clubs every weekend, taking ecstacy, amphetamines and dancing excessively into the morning hours. I had been doing this for 5 years without encountering any problems or ill effects. After another night of drug binge at a rave party I went home with a companion and took a combination of mda, mdma and meth and got into some sexual activity. A few hours into it I suddenly began to burn up severely, unlike anything I've ever encountered before. My condition rapidly deterorated and I realised I was in serious trouble when the hyperthermia encompessed my whole body and I began to experience a range of symptoms that had me certain my life was about to end.

I ran for the cold shower and sat under there waiting for the paramedics. My heart felt very irregular and I had balckouts my vision and and loss of events. I recall momentarily being in the ambulance, then suddenly at the hospital where I was placed in an ice bath and apparently given dantrolene to reduce the hyperthermia. When I regained conciousness enough to realise I had just survived what was described by the doctors as a life threatening incidence, I felt relief. But at that time I did not realise cheating death would have come at a price and that I had been left disabled with a damaged Autonomic Nervous System.

Although the hyperthermia was over I continued to feel feverish day after day, I was no longer the same person when I left the hospital, I was now stuck with a whole new range of symptoms to accompany the start of my new life as aperson with Dysautonomia. For the first 10 months I could not even leave the my house due to the high fevers. The only mild relief I found was from sitting in front of the air cooling unit all day. I felt like a vampire as any amount of exposure to the sun made my temperature worse, I could no longer have warm showers or sleep under a blanket. Soon it became evident that the overdose and the hyperthermia had damaged my hypothalamus responsible for temperature control. Furthermore I could no longer engage in sexual activity or feel arroused without experiencing hyperthemia and going into uncontrallable spasms and mucsle twitching and emberassingly landing me in hospital with high fevers everytime I got aroused.

As a result of damaging my Autonomic Nervous System all my bodys automatic functions such as heart rate, digestion, temperature control, blood pressure, arousal, sexual activity, breathing, sweating were all now malfunctioning and unstable. Most bothering has been the chemical sensitvity and adverse reactions I now have to a range of substances and it is somewhat ironic that a drug overdose resulted in a drug intolerance making it impossible for me to ever take ecstacy amphetamines or use drugs recreationally ever again. Even taking opiates for chonic pain has been extremely challenging and taken almost a year of desensitisation and countles ER trips with adverse reactions.

It has now been 12 years since my overdose but everyday continues to be a challange living impaired body functions and I continue to experince complications from any substance that acts on my Autonomic Nervous System hence the reasin why I use Bluelight for help whenever I run into problems. I am grateful to this community and for those who have been so willing to offer me support and assistance. Thank you guys.
 
Wow.
Great summary.

I should learn something about brevity from you.
Well done.

I believe that the continued fevers are PART of a prolonged rewiring of your brain.
Every time I get a mild fever, it feels a lot like the onset of flu.
The sick feeling in my head is just persistent and terrible.

But i believe it increases the plasticity of the brain, allowing for changes to be made that would otherwise be impossible.
I must admit that several fevers occurred throughout the year that felt like serotonin syndrome.
They were so scary I would rub ice all over my head, back, neck etc.

Now they are mild and easily tolerated.
And a sign of continued changes in my brain.
That is why I think yours are too.

Any fever over 101 would definitely cause me major concern.
So it is hard to recommend that you change the way you view these events.
But I wanted to express my opinion that it may be causing a very slow improvement...possibly leading to a day when you no longer get fevers.

Thanks for sharing your story again.
I know some people in ED that need to read this.
 
Hi AP
Am writing due to my son being in hospital for excessive vomiting brought on by a THC toxicity. He can't take Maxalon because it gives him extreme akathisia. We know that from episodes in the past. This time they gave him Stemetil which has given him milder but still annoying akathisia. He's been putting up with it for a few hours now as I convinced him to stay calm as it should eventually pass. But it's now 3am and the Stemetil was given to him intravenously at about 6pm. He's asking me now when it will stop as he's very tired from the day's episode (which started 24 hours ago). From what I gather from your posts, it took more than 12 hours for your symptoms of akathisia to diminish after the stemetil. Is that correct?

I've just given him a dose of mirtazapine which he takes daily for anxiety and sleeplessness - which I'm thinking is brought on by his cannabis use. This dosage started after his previous episodes of THC toxicity about 12 months ago. I got him off cannabis late last year but he is smoking again and now another episode of the toxicity. I've just read that mirtazapine is useful for treating akathisia brought on by anti psychotics. Especially for those who are not good with beta-blockers. In any case here I am awake at 4am waiting to see if the mirtazapine has had any affect. Such is the role of a parent who cares about a 17 yo who is unaware of the ramifications of his drug use. Which is fortunately only cannabis.

I'll post here what the result is and how long the akathisia lasted in case anyone needs that information.
 
Dopamine controls motor function so to lower your dopamine to low can cause some pains like RLS and a very uncomfortable body...

Ask the doctor how long te meds with last (half life) and then expect them to subside with in that time frame or after..
 
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