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Amisulpride — A Multipurpose Drug for ME/CFS

Hip

Senior Member
Messages
17,858
I successfully tried Amisulpride 10 mg but I put on weight and stopped. Has anyone tried doses like 5mg?

Do you know where you put this weight on (was mainly on the abdomen, ie central obesity; or was it all over the body)? I've put on a lot of weight over the last 10 years, mainly as abdominal obesity, and I wonder if this is linked to my very low-dose amisulpride regimen I have been taking all this time.
 

sb4

Senior Member
Messages
1,659
Location
United Kingdom
Do you know where you put this weight on (was mainly on the abdomen, ie central obesity; or was it all over the body)? I've put on a lot of weight over the last 10 years, mainly as abdominal obesity, and I wonder if this is linked to my very low-dose amisulpride regimen I have been taking all this time.
I haven't tried my Amisulpride I got over a year ago due to worrying about the prolactin effect.

Recently I have been re-trialing bromocriptine based on Lyle Mcdonalds book on how it helps with weight loss. Bromocriptine is mainly used for its anti prolactin effect, this occurs I think due to its pro dopamine effects which according to Lyle are the reasons it helps with weightless. If this is true then the same mechanism is perhaps responsible for Amisulpride weight gain?

Anyway the anti prolactin effect seems to be legit as my libido has improved significantly upon using it.

I decided to try it again to help me lose weight and so far it seems to be working though I am only 2.5weeks into using it. I have reduced my caloric intake to around 1500kcal which would usually result in hunger, decreased libido, and lower energy however this has not been an issue, presumably thanks to the bromocriptine.
 

Hip

Senior Member
Messages
17,858
Bromocriptine is mainly used for its anti prolactin effect, this occurs I think due to its pro dopamine effects

By some quick Googling, I read that dopamine D2 or D3 receptor agonists will inhibit prolactin release, which in turn may reduce weight. And bromocriptine is a potent D2 agonist, so this should help with reducing prolactin.

And I found this study which says:
administration of bromocriptine is a safe method for treating antipsychotic-drug-induced hyperprolactinemia


And this paper mentions cabergoline may also be effective (cabergoline is a potent D2 agonist, and weak D1 agonist):
Cabergoline has proven to be more effective and safe when used to treat hyperprolactinemia, but whether cabergoline is also safer than bromocriptine in antipsychotic induced hyperprolactinemia remains unproven.



However, amisulpride, when take in very low doses, is also activates the dopamine D2 and D3 receptors. This is because at low doses, amisulpride blocks the dopamine autoreceptors, and that then causes more dopamine to be released in the synapse, which will activate the regular D2 and D3 receptors.

So on paper you might expect amisulpride to also lower prolactin, rather than increase it. But this study I just found says that is not the case: even low dose amisulpride causes elevations in prolactin (even though the paper says "low dosages of amisulpride are expected not to increase prolactin").


This paper explains why low dose amisulpride increases prolactin, even though it is not expected to.
To quote the paper:
Relative amisulpride levels in the pituitary, a region outside the blood–brain barrier, are much higher than levels of lipophilic antipsychotic compounds. Dopamine D2 receptor occupancy is, therefore, higher at the level of the pituitary than in the striatum.

Since amisulpride activates the dopamine system at low doses, but inhibits it at higher doses, this higher level of amisulpride found in the pituitary would tend to block the dopamine system there, leading to prolactin release.



Maybe I should try adding a D2 and D3 agonist drug like bromocriptine to my daily regimen, and see I lose weight.

It says here:
Cabergoline is taken only once or twice weekly because of a longer elimination half-life, whereas bromocriptine is dosed multiple times a day



Bromocriptine and cabergoline are not the only dopamine agonist drugs; you also have:

Memantine — dopamine D2 agonist (as well as an NMDA blocker).
Ropinirole — acts as a D2, D3 and D4 dopamine receptor agonist with highest affinity for D2.
Pramipexole — agonist for the D2, D3 and D4 dopamine receptors, but strongest agonism is on D3.

I have listed lots of other dopamine drugs in this post.



Supplements That Reduce Prolactin

This study found that high dose vitamin B6 (300 mg twice daily) given to patients taking antipsychotic drugs results in 68% reduction in serum prolactin levels (from 96 to 30 ng/ml).

This study gave vitamin B6 (100 mg three times daily) to women with hyperprolactinemia, and found their prolactin decreased 49% from prolactin from 51 to 26 ng/ml.

The same study found that cabergoline 1mg per week reduce prolactin by 61% (from 56 to 22 ng/ml).

This study on hemodialysis patients found that vitamin E at 300 mg once daily reduced prolactin by 71% (from 51 to 15 ng/ml).

This study on hemodialysis patients found that zinc at 50 mg once daily reduced prolactin by 62% (from 29 to 11 ng/ml).
 
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nsdn

Senior Member
Messages
183
¿Sabes dónde pusiste este peso (principalmente en el abdomen, es decir, obesidad central, o en todo el cuerpo)? He aumentado mucho de peso en los últimos 10 años, principalmente debido a la obesidad abdominal, y me pregunto si esto está relacionado con mi régimen de dosis muy bajas de amisulprida que he estado tomando todo este tiempo.

Abdomen, yes. Thank you for the various inputs.

In 8 days I will see if I can get a prescription for Amisulpride again and I can start Moclobemide which is on its way to my local pharmacy.
 

nsdn

Senior Member
Messages
183
How was it successful? Was symptoms did it help with and by how much? Thanks.

I started it along with the Abilify and the only thing I noticed when I took it off was a slow weight loss and my mood got worse, I wake up with no desire to get up.
 

Hip

Senior Member
Messages
17,858
In 8 days I will see if I can get a prescription for Amisulpride again and I can start Moclobemide which is on its way to my local pharmacy.

I take moclobemide 75 mg daily for antidepressant purposes. It is unfortunate that moclobemide also increased prolactin.
 

Hip

Senior Member
Messages
17,858

nsdn

Senior Member
Messages
183
I think vitamin E is going to be the cheapest prolactin inhibitor. On Amazon UK they sell 400 IU x 360 capsules for £15. You can start adding other anti-prolactin supplements like B6, zinc, American ginseng, etc, but the cost mounts up

A friend told me that the natural vitamin E is absorbed much more and the cheap one can be absorbed even less due to my poor methylation. I ordered 100 capsules of Solgar 400 IU for 18.38 euros.
 
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nsdn

Senior Member
Messages
183
A friend told me that the natural vitamin E is absorbed much more and the cheap one can be absorbed even less due to my poor methylation. I ordered 100 capsules of Solgar 400 IU for 18.38 euros.

"Equivalent levels of vitamin E in the blood are obtained with 100 mg of natural vitamin E and 300 mg of synthetic vitamin E. (Kiyose et al., 1997). The degree of excretion of the synthetic source is 3 times faster than that of natural vitamin E. (Traber et al., 1998)"
 
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Hip

Senior Member
Messages
17,858
"Equivalent levels of vitamin E in the blood are obtained with 100 mg of natural vitamin E and 300 mg of synthetic vitamin E. (Kiyose et al., 1997). The degree of excretion of the synthetic source is 3 times faster than that of natural vitamin E. (Traber et al., 1998)"

Very interesting, shows how natural vitamin E is so much better. I always buy natural vitamin E.
 

nsdn

Senior Member
Messages
183
I don't quite know where to put this, but since my dosage of Amisulpride is going to be exceptionally low I am putting it here. If I should open an exclusive thread for my treatment let me know.

As unbelievable as it sounds due to living in Africa (Canary Islands) I have not been able to get all the Manerix I wanted so my drug treatment remains like this in the morning:

Solian (amisulpride) 5 mg
Manerix (moclobemide) 75 mg
Abilify (aripiprazole) 0.5 mg
Natural vitamin E for prolactin lowering
Mestinon (pyrodostigmine bromide) 60 mg

Overnight LDN (naltrexone) 3.5 mg.

Best regards.
 

Rvanson

Senior Member
Messages
312
Location
USA
Manerix (moclobemide) was great for my ability to lift heavy objects, while I was driving a truck, and for my depression, but it was not good for insomnia, and also not good for making me a bit too wound-up and
aggressive. Perhaps I was using too much, but it's not FDA approved for use in the USA. It's a "reversible"
MAO inhibitor, but still might be good idea to use the Monoamine Inhibitor diet, regardless. My .02 cents.
 

nsdn

Senior Member
Messages
183
Hi.

2 weeks after taking 5-10mg of Solian together with natural vitamin E I have not put on any weight.

Good!
 

godlovesatrier

Senior Member
Messages
2,554
Location
United Kingdom
Just wanted to say RE prolactin, if it's super high vitamin e and b6 are not going to shift it down. I did a lot of tests over teh last 14 months with 4 interim blood tests and I can tell you if it's high as mine was at about 800 (twice the normal) the vitamin e addition and b6 doesn't bring it down at all. If it does bring it down it's not enough to notice.

In my case though oat bran is known to cause high prolactin secretion, so I just stopped taking it.

This sounds like an amazing drug, I never felt too demotivated, beyond age 17, so maybe I somehow managed to grow out of that...who can say. Glad it works for you tho!
 

nsdn

Senior Member
Messages
183
Hi.

2 weeks after taking 5-10mg of Solian together with natural vitamin E I have not put on any weight.

Good!

Some time later I still do not gain weight, I take approximately 10mg.

I want to ask you about a matter that worries me. If Amisulpride temporarily blocks dopamine receptors, wouldn't it be good to separate the Abilify intake from the Amisulpride intake by 12 hours? Or better together?

@Hip
@serg1942
 

Hip

Senior Member
Messages
17,858
I want to ask you about a matter that worries me. If Amisulpride temporarily blocks dopamine receptors, wouldn't it be good to separate the Abilify intake from the Amisulpride intake by 12 hours? Or better together?

That's a complicated question, which would require many hours of research and thinking. The mechanisms of action as dopamine system stabilizers for these two drugs is different (detailed in the first post).
 

nsdn

Senior Member
Messages
183
That product seems to contain all of the anti-prolactin supplements. Not that cheap though.

I think vitamin E is going to be the cheapest prolactin inhibitor. On Amazon UK they sell 400 IU x 360 capsules for £15. You can start adding other anti-prolactin supplements like B6, zinc, American ginseng, etc, but the cost mounts up

Hi!

What do you think of carbegoline? I have more than x10 the high limit on my prolactin test. 86.18 ng/ml.

The package insert for carbegoline says: "To reduce the concentration of prolactin in the body: Treatment is usually started with 0.5 mg per week, but higher doses may be necessary afterwards. Your doctor will advise you on the duration of treatment.".

Price €8.26 per month.

Thanks.
 
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sb4

Senior Member
Messages
1,659
Location
United Kingdom
Hi!

What do you think of carbegoline? I have more than x10 the high limit on my prolactin test. 86.18 ng/ml.

The package insert for carbegoline says: "To reduce the concentration of prolactin in the body: Treatment is usually started with 0.5 mg per week, but higher doses may be necessary afterwards. Your doctor will advise you on the duration of treatment.".

Price €8.26 per month.

Thanks.
I have been using bromocriptine for the last 4 months for weight loss. I don't know my prolactin levels but based on my increase in libido I would say its having a prolactin lowering effect. Either way the drug is pretty safe, has been in use for years, and is relatively cheap.
I understand carbegoline is very similar and is also used for lowering prolactin but I don't know much more than that. I have been getting my bromocriptine from inhousepharmacy.vu and haven't had any problems yet with customs for delivery to the uk.