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action of risperdal (risperidone)

M

mike1127

Bluelighter
Joined
Jul 26, 2013
Messages
24
I'm new here and not sure what kinds of topics are covered, for instance I wonder if prescription drugs are covered, and my question in particular is about the action of risperdal. So I'll post here in homeless and the mods can move or close it.

Risperdal helps with my bipolar mixed state (a kind of mania) and it also helps me sleep. I sleep more poorly on days when I use a lot of Ultram (painkiller) and the risperdal really helps. I am trying to understand the chemistry behind how risperdal acts, in the hopes that I can find a more natural substitute or safer drug.

Here's how the action of risperdal is described on wikipedia:

Risperdal is classed as an anti-psychotic medication that has also proven useful in bipolar, and has tranquilizing effects.

"It is a dopamine antagonist possessing antiserotonergic, antiadrenergic and antihistaminergic properties."

So far what I have figured out is that an *antagonist* in general is a medication that blocks a substance from coupling with the equivalent receptor, and therefore blocks some of its action.

It blocks several types of receptors: dopamine, serotonin, epinephrine (also called adreneline I believe) and histamine. The only one of these I can relate to its function in me is the anti-epinephrine action, because what I have read is that epinephrine is associated with the fight-or-flight response, so it could be calming. Regarding dopamine, I haven't found any description on the web its effects that relates to mania. Regarding histamine, I know that antihistamine drugs cause drowsiness so I can see why the risperdal would be sedating for that reason.

But I would like to know more specifically why it might calm mania (racing thoughts). Also it calms irritability in me.
 
mike1127 said:
I'm new here and not sure what kinds of topics are covered, for instance I wonder if prescription drugs are covered, and my question in particular is about the action of risperdal. So I'll post here in homeless and the mods can move or close it.
Click to expand...

Discussion of any drug is allowed here. Hell! Discussion of practically anything is allowed here! So, no, you're not out of line by asking this question. In fact you're very "in line" ;P

I was planning on answering your question in its entirety, but I happened to view this thread as I'm on way out of the house. I'll leave my full answer later. Anyways, Welcome to Bluelight :)
 
i think the calming effect some people get from anti psychotics is caused by lowing levels of dopamine because high levels of dopamine cause simulation also antihistamines calm a lot of people down due to the sedation
 
From what I understand, anti-psychotics don't quite "lower levels of dopamine"--they block dopamine receptors. That seems like a significant difference. I've read that dopamine is metabolized by several routes and can end up as norepinephrine, which implies that if the drug is blocking the action of dopamine it could end up doing something else by metabolizing or breaking down or changing form. I wonder if my system actually has high levels of dopamine in it, and I wonder if they have gone up since I've been taking risperdal due to some kind of effect where the body tries to make more of something when its action is blocked. Just one theory.

I'm also curious about the many roles of dopamine--it's sometimes said to be related to highly pleasureful activities, and also psychosis--is there any explanation of how it can be involved in both of those plus bipolar mania?

I've also been told that it's mainly tranquilizing/calming in bipolar people and doesn't do a whole lot in that department for others.

Mike
 
Not to hijack, but can blocking dopamine account for the plethora of side effects associated with Risperdal and similar drugs? Not the movement related sides, but the weight gain/diabetes/boys growing breasts ones. These seem like toxic hormonal effects that go beyond simple neurotransmitter activity, but IDK.

(I had severe side effects from this drug as a teen, so just wondering what about it is so toxic).
 
Lady Codone said:
Not to hijack, but can blocking dopamine account for the plethora of side effects associated with Risperdal and similar drugs?
Click to expand...

No problem, I'm interested in everything about risperdal, as long as my main focus on its anti-mania activity gets discussed.

Mike
 
At a guess i would say that risperdals ability to 'calm' is through its adrenergic antagonism action.
Norepinephrine is partly responsible for that nervous, agitated sort of feeling along with histamine. So any drug that reduces these chemicals in the brain will produce a calm, sedated feeling.
Another way this could be acheived would be through the GABA receptors, although drugs which work at these receptors have actions a little more complex then simple agonism/antagonism.
Anti-psychotics in general hit alot of receptors and so its hard to pin their actions down to just one set of receptors. Its likely more a case of all its actions contributing to the overall effect.
 
If I were to ask why it has a calming effect mainly on bipolar spectrum people, is that one of these mysteries about the brain that really no one can answer? My understanding is that not a whole lot is really understood about psychoactive drugs.
 
The pharmacology of most meds are fairly well understood. I think its more a case of the illness not being understood completely.
Maybe its similar to the way that people with bad anxiety get more intense effects and a better high from benzos then a person without anxiety?....i think its all just speculation really, but either way its an interesting question to consider, if i can find out anything backed by solid evidence then ill post it here.
 
Well, I can help you out a bit. You're on the right track as far as the antagonist effect w/regard to adrenergic receptors--and this heading off a fight/flight response..so congrats on your research and reasoning in that regard. You're also dead on in that its antihistamine effects are calming--it acts on histine sites, and is referred to as an H1 inhibitor...similar to benadryl, which we all know makes one drowsy. Now to confront the dopamine phenomenon: accepted theory is that it's excess action of dopamine that produces psychosis. This is, in fact, the basic fundamental principle of all medications termed "antipsychotics". Excess dopamine action is responsible for racing thoughts (for example, amphetamines produce exactly the opposite effect, they increase dopamine levels--the result being the racing thoughts associated with stimulant abuse). This dopamine release is also part of the fight/flight response system...but is more responsible for the inclination to fight, than to flee....so it's effect in dampening the effects of dopamine in you prefrontal lobes is, in itself pacifying--and reduces the irritability which is, when you think about it, a response of fight, rather than flight.
I"m not sure how you missed info on the internet about the role that excess dopamine plays in mania, but it's the main factor responsible for mania...excess dopamine in the prefrontal lobes. It sounds as though you've just started it recently...and you might find that the seroton dampening effects result in depression, obsessive compulsive preoccupation and anxiety, if you're on it longer term. It's for this reason that many docs add an SSRI after a patient has been stabilized for a while on an antipsychotic like risperdal. Keep that in mind if you start to feel unexpectedly dejected, blue, and discouraged. That's a sign an SSRI is called for, to offset the antiserotonin effects of the risperdal. Sounds like it's a relief, and has made a positive difference for you, though, so congrats. If noone else mentions it, though, if you're on it long long term it can result in Tardive dyskinesia (although not as bad as the older versions)--which means you have uncontrolllable head, neck facial and even tongue movements.
It's for this reason that after a patient is stabilized, most docs try to move toward a mood stabilizer and away from the antipsychotics. Even if you find you're more comfortable with something in that class, though, seroquel is a better choice long term, because it doesn't have the Tardive dyskinesia risks.
And by the way, you're on a non-psych drug focussed board. I hope that doesn't mean that, at this early stage in your stabilization, you're out there choking down random street drugs. Big no-no right now. Not that Im your dad or anything, but I"ve got a background in mental health and pharmacology, and I've seen too many people who are just getting back on their feet and getting their humanity back go too far too soon, get careless thinking they're immortal, and just launch themselves into the void, never to return--be placed forever beyond reach. Be grateful you've found a step up, and don't forget to be grateful, and where you came from. True dat.
 
^
very true!
The feeling that your "all better" when a psych med begins to become stable in your system, is a dangerous illusion that accounts for alot of relapses and emergency mental healthcare (like sectioning).
Not wanting to worry you OP, just thought promicarus's point beared repeating.
Although it seems im not nearly as eloquent.lol
 
There aren't really any natural alternatives to potent anti psychotics like risperdal. However, if you wish to be stabilized at a lower dosage there are some things that you can try to do. One of these is using less tramadol(Ultram) as tramadol is both an opioid, as well as seratonigenic compound. As such, it raises the levels of serotonin in your brain, which combined with your mania(mania also increases levels of serotonin), can make it difficult to feel normal without anti psychotics.
 
Thanks for the detailed reply, promicarus, and the warning is a good point. Actually I've been on Risperdal for a long time, and started on it for extreme irritability. It was only much later that another psychiatrist figured out I have a form of bipolar mixed state, and then we added Lamictal (anti-seizure, mood stabilizer) and Luvox (SSRI). But I also have chronic body pain and fatigue and recently went on disability.


The reason I'm suddenly here at Bluelight is that I'm getting interested in treating myself better rather than taking more drugs. I first found Bluelight through doing google searches on various neurotransmitters and it seemed like Bluelight was the perfect combination of friendliness and expertise. I mean, if I want to talk pharmacological actions, I don't know how to go about looking up experts on the web, and can't imagine they would want to talk to me--but then I discovered they were all here at Bluelight, ready to help people.

BlueStar13, your point about using less Ultram is exactly the kind of thing I'm looking for. I already discovered that I need more Risperdal to counteract Ultram, but I am having a hard time getting off the Ultram. I think I have some physical and psychological dependence. I take your warning about reckless behavior seriously... a year ago I experimented with some of the stronger prescription pain meds that I got from a friend and stupidly took without asking a doctor or even looking up the interactions on the internet. I didn't have any problems but I learned later that I could very easily have died from combining Risperdal and one of those.

The reason I have hope for getting off some of these meds is that I recently discovered Dr. Amy Yasko's work with characterizing biochemical dysfunctions through genetic testing. Dysfunction in something called the "methylation cycle" can be a common link in all my symptoms. I can get genetic testing that shows mutations (SNPs) that affect enzymes in this cycle, and there are ways to use supplements to speed up things or slow down things as needed. An important supplement is vitamin B12 (as any of four forms), and I already discovered that B12 powerfully affects my mood and energy levels in a very good way. That's just the beginning; there are many more things that can be learned from testing, and combinations of supplements to try. So I'm pretty optimistic.

Mike
 
One of the things most people miss with ultram (tramadol) is that a main mechanism of action is to increase noradrenaline/epinephrine...an increase of which is to lessen pain. Think about it...when you're 'keyed up' on adrenaline, you fell less pain...after a fight, for example, you rarely feel the soreness and other pain that your thereby incurred...until quite a bit later, when your heightened adrenaline as leveled off.

This is one of the main principles of the mechanism of action of tramadol. Tramadol also has a lesser, incidental, peripheral "down-stream" effect of heightening levels of serotonin..but as much as I hate to contradict another poster--such as bluestar, above--these serotoninergic effects are neglible, really.

So overall point...it's the effect of the increase in noradrenaline/epinephrine for which the ultram is responsible which is more likely to make you feel ill at ease, and more prone to "fight/flight" reactions...much more so than any effects that ultram has on serotonin levels.

so we arrive at the same conclusion, but for different reasons. Ultram isn't optimal for anyone with either a)trauma issues b) psychosis, or 3) bipolar issues.
The stress of the "fight/flight" impulse provoked by the noradrenaline based approach at pain relief implicit in Ultram just doesn't mix with those who have anxiety issues or who have an otherwise prolonged sense of inadequacy associated with any variety of mental illnesses.

you say " I sleep more poorly on days when I use a lot of Ultram (painkiller) and the risperdal really helps. I am trying to understand the chemistry behind how risperdal acts, in the hopes that I can find a more natural substitute or safer drug." The reason is clear. The Ultram is raising your noradrenaline levels, and activating your adrenergic, 'fight/flight" receptor arrays.

It sounds like you have significant pain issues, as well. Considering your profile, there would be much better agents to adress your pain issues than Ultram. I would even go so far as to say that, were you to cease taking Ultram, it's likely your bipolar symptoms would be less pronounced and more easily managed. It's a simple matter of stress. Stress provokes bipolar symptoms--and the mechanism of action fo Ultram mimics physiological stress.

If you have a history of opiod abuse, then obviously that's out. But there are many supplements that you should consider. Kratom, a "borderline" acceptable herbal remedy for pain would be one. It's legal, but effects are similar, and addiction is not unknown. I'm not sure what the ultram's for, meaning exactly what form your pain takes...different pain requires different approaches. But it's common for those who are depressed and/or who suffer from other psychiatric disorders to have pronounced pain where others would find it negligible. One of the best approaches to pain, in the long-term, especially for those w/psych compaints, is Omega-3 fatty acids--specifically eicosopentazoic acid consituent of same. The alternate component, DHA, is of relatively neglibible effect. In addition, supplementation with Conjugated Linoleic Acid--or CLA (the best most standardardized brand name of which is "tonalin") accomplishes pain reduction by a similar, wholistic route.
The basis of exaggerated pain in those with psych complaints is, to be blunt-- a sense of defeat. Studies have shown that an overall sense of defeat, or inadequacy, sensitizes subjects not only to the emotional states of others, but to somatic--physical-- sensory perceptions.
This comes down to a reduction of stress...meaning the more stress you experience, the more "defeated" you sense that you are. There is a complicated basis for this theory originating in epigentics, and the role in the epigenome in tightening or loosening to reveal methyl groups which translate into greater sensitivity. The theory is that, the more defeat you experience, the lower you are likely to be on the social pecking order, and therefore the more sensitive you need to be to the needs and expectations of those above you on that ladder. In other words, it's evolved, as a means of insuring the cohesion of groups, necessary to survival in a dangerous environment, also necessary to which is a hierarchical organization implicit in which are those at the bottom of such an order who must needs be sensitive to the needs of others of a higher rank in order to maintain some acceptable position, even if it be at the bottom of the totem pole.
But i digress. The point is that you need to effect a physiological response of success in order to counteract this phenomenon, and the first basic step in this driection is the relief of the stress which by definition implies an inadequacy of personal coping skills necessary to gain acceptance in your social group as a succes.
Needless to say, anyone suffering from psychiatric symptoms faces this difficulty as part and parcel of their condition
But there are tricks...means by which these levels of gluccocorticoids--the stress hormones--can be reduced, resulting in a greater overall sense of well-being which is in itself a self-fulfilling prophecy: you present to the world as less stressed, and the world treats you as more successful--the world treats you as more successful, you feel more successful, and stress is reduced, etc. etc. And upward spiral, if you will.
So you need to focus on a) reducing levels of gluccocorticoids (one of which is the norepinephrine increased by your Ultram, so that should be your first concern--dropping that)...and the blocking of the receptors which respond to these gluccoorticoids and produce a stress reaction.
To this end clonidine is still one of the most effective agents. It blocks alpha 2 adrenergic receptors, and thereby prevents the physical effects of stress. Doctors are more likely to try to prescribe you propranolol, an beta adrenergic blocker, and more popular for use in anxiety--but clonidine has better all around effects, even reducing pain, in and of itself.
Unless you have severly low blood pressure, insist on the clonidine. A little known fact, even among docs, is that propranolol regularly depresees mood to the point of clinical depression when given in any significant dose.

WIthout knowing why you;re takng the ultram to begin with, its hard to be more specific. But for someone with bipolar, its bad news all around. There are any number of other approaches to controlling pain, and I think youll find that when you cut the Ultram, your symptoms will be much more manageable All the best
 
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Well risperidoine is a strong antagonist at the D2 receptor and also the 5-ht2a receptor. This is what is thought to give risperidone it's anti-manic properties and why it also helps control schizophrenia. It is also a antagonist at the H1 and a1 and a2 adrenergic receptors. The later accounts for the orthostatic hypotension that risperidone and many other anti-psychotics can cause. I find Quetiapine to be bad for causing that actually. Due to it's very potent 5-ht2a antagonism risperidone is the anti-psychotic often used to treat bad trips that are bad enough to need a anti-psychotic.

I have been on it in doses of up to 4mg's a day for bipolar disorder. I usually only took 2mg's a day (this seems to be the dose in which the zombie effect kicks in for most people) but when i was really manic i would sometimes take 4mg's a day. For some reason when i'm manic i can take higher doses without feeling the zombie effect. Risperidone is the worst anti-psychotic i have taken for causing this. I have also taken seroquel, zyprexa, methotrimeprazine, Stemetil/Compazine (usually with either Demerol or morphine for severe pain) and Thorazine/Largactil. These drugs caused more drowsiness then risperidone i found but didn't cause nearly as much of a zombie effect. While risperidone didnt cause much actual drowsiness it did make me feel far more zombish. This is probably because risperidone seems to be the haldol of the atypicals when it comes to D2 antagonism.

I find that olanzapine especially the Zyprexa Zydis form which are the orally disintegrating wafers work way better and way faster at controlling my mania then risperdal does but my insurance only covers seroquel and risperdal. So these days i take seroquel along with lamotrigine as my mood stabilizer and i also take wellbutrin. I find that seroquel helps with the depression part as well as the mania so i take that instead. I find that risperidone doesn't help depression and is more unpredictable in helping acute manic episodes then olanzapine is. It has on a few occasions not really helped mixed state mania very much and made the depression worse. I have taken olanzapine and also good ol Largactil/Thorazine for acute mania and i found them to be more reliable then risperdal in controlling mixed states. Mixed episodes are the worst for me by far.
 
Promicarus,
Well I can say more about my situation.

My pain is something like fibromyalgia. I don't like the term "fibromyalgia" because it is kind of a catch-all diagnosis and seems to represent many possible underlying conditions.

But basically everything hurts. I feel pain from pretty much everywhere in my body. It seems like my pain system is ramped up... hypersensitive.

I also was trying to keep it simple so I didn't mention that I was on Luvox before, and now I'm on Cymbalta. I lost a bunch of weight when switching, but it seems like the Cymbalta potentiated addictive behavior. I started drinking caffeine all the time (mainly green tea) after starting it, and also my tendency to be risky with opioids started at that time. I upped the dose of Ultram, and between that and the caffeine I needed more risperdal. Clearly this is not good for me. I don't want to go back to Luvox because I don't want to gain the 60 pounds back. But maybe I could reduce the Cymbalta dose. I normally take 30 mg.

I normally take about 3 mg risperdal.

I also take 4000 mg/day of Neurontin and that helps with body pain, sleep, and restless legs syndrome.

Oh Cymbalta helped with the body pain, too.

Recently when I started taking vitamin B12 as adenosylcobolimom (spelling? sorry) sublingually I got a huge boost in energy and mood. I think I might be able to get off the Cymbalta entirely. I'll talk it over with my doctor. If my underlying problem is a methylation cycle dysfunction, that could explain the fibromyalgia, bipolar (due to neurological inflammation) and other things, and that can be addressed with supplements like B12 and folate.

Mike
 
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