OTC Anti-histamines With Anti-serotonin Action

haidut

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Given that some people cannot get access to or do not tolerate well drugs like cyproheptadine or mirtazapine, this study offers some possible OTC alternatives for blocking serotonin. As you can see, Benadryl is also in the list but its anti-serotonin activity is much weaker compared to other first-generation antihistamines.

https://www.ncbi.nlm.nih.gov/pubmed/6120505

"...Antihistaminic drugs of various chemical structure (chlorcyclizine, chloropyramine, chlorpheniramine, clemastine, diphenhydramine, mepyramine, promethazine, thenalidine) were tested on their action on the central serotonin system in mice. The test used was the antagonism to behavioral syndrome produced by D, L-5-hydroxytryptophan (5-HTP). Clemastine, promethazine and thenalidine inhibited 5-HTP-induced syndrome in doses of much lower than those inhibiting locomotor activity. Similar but weaker effect was produced by chlorcyclizine and diphenhydramine. It could be suggested that these compounds exert central antiserotonergic action. Chloropyramine and, more strongly, chlorpheniramine potentiated the action of 5-HTP; this may be due to the inhibition of serotonin uptake. Only mepyramine in these tests did not show any action on the central serotonin system."

Of these drugs, clemastine (which is OTC in USA) looks particularly interesting. It is known to be an anti-depressant due to its FIASMA action (but probably also due to its 5-HT blocking) and also it looks like it may reverse the damage caused by multiple sclerosis.
https://en.wikipedia.org/wiki/Clemastine
"...Clemastine does also act as FIASMA (functional inhibitor of acid sphingomyelinase)."
https://en.wikipedia.org/wiki/FIASMA

https://clinicaltrials.gov/ct2/show/NCT02040298
 

Agent207

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Is there any safe drug/supp to be antiserotonin while not affecting dopamine at all? I see almost all of them need another thing to compensate dopamine downregulation.
 

haidut

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Agent207 said:
post 110387 Is there any safe drug/supp to be antiserotonin while not affecting dopamine at all? I see almost all of them need another thing to compensate dopamine downregulation.

The safest that I know of would be theanine, BCAA + tyrosine, caffeine, and higher doses niacinamide. P5P is dopaminergic, so that would make it anti-serotonin as well. I think the combination of theanine, BCAA and tyrosine has some serious potential as anti-serotonin tool organism-wide and as such helpful in issues like weight management, immune system support, libido, and mood.
 
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Agent207

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Thanks haidut, I had already thought on p5p, but I saw its dopaminergic effect more via prolactin inhibiton, and its antiserotonergic effect by tryptophan conversion blockade to serotonin. But this information seems conflicting with other pointing to p5p helping in the conversion to serotonin instead niacin.

"The second step to serotonin production requires vitamin B6, but here we should make a distinction. Not any common chemical-form of vitamin B6 can do the job. Serotonin-producing enzymes can only use the natural, enzymatic form of vitamin B6, pyridoxal 5-phosphate (P5P)."

http://lidtke.com/the-lidtke-letter-why-dont-your-supplements-work/
 

haidut

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Agent207 said:
post 110400 Thanks haidut, I had already thought on p5p, but I saw its dopaminergic effect more via prolactin inhibiton, and its antiserotonergic effect by tryptophan conversion blockade to serotonin. But this information seems conflicting with other pointing to p5p helping in the conversion to serotonin instead niacin.

"The second step to serotonin production requires vitamin B6, but here we should make a distinction. Not any common chemical-form of vitamin B6 can do the job. Serotonin-producing enzymes can only use the natural, enzymatic form of vitamin B6, pyridoxal 5-phosphate (P5P)."

http://lidtke.com/the-lidtke-letter-why-dont-your-supplements-work/

P5P also enhances MAO-A so its overall effect is on reducing serotonin. Riboflavin does the same, as MAO-A is a riboflavin-dependent enzyme.
 
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Makrosky

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haidut said:
Agent207 said:
post 110387 Is there any safe drug/supp to be antiserotonin while not affecting dopamine at all? I see almost all of them need another thing to compensate dopamine downregulation.

The safest that I know of would be theanine, BCAA + tyrosine, caffeine, and higher doses niacinamide. P5P is dopaminergic, so that would make it anti-serotonin as well. I think the combination of theanine, BCAA and tyrosine has some serious potential as anti-serotonin tool organism-wide and as such helpful in issues like weight management, immune system support, libido, and mood.

Taking P5P every time you take tyrosine would help converting that tyrosine straight into dopamine, right?? Looks like it's synergistic
 
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haidut

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Makrosky said:
post 110412
haidut said:
Agent207 said:
post 110387 Is there any safe drug/supp to be antiserotonin while not affecting dopamine at all? I see almost all of them need another thing to compensate dopamine downregulation.

The safest that I know of would be theanine, BCAA + tyrosine, caffeine, and higher doses niacinamide. P5P is dopaminergic, so that would make it anti-serotonin as well. I think the combination of theanine, BCAA and tyrosine has some serious potential as anti-serotonin tool organism-wide and as such helpful in issues like weight management, immune system support, libido, and mood.

Taking P5P every time you take tyrosine would help converting that tyrosine straight into dopamine, right?? Looks like it's synergistic

Sure, that's the theory at least:):
 
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milk_lover

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haidut said:
Sure, that's the theory at least:):
Isn't there a study that says tyrosine increases prolactin? Online, on many websites, they say tyrosine needs vitamin B6 and vitamin C as cofactors for dopamine pathway. Maybe if not enough vitamin B6 is consumed with tyrosine, tyrosine depletes B6 stores and it is this depletion that leads to increased prolactin? There are some issues with tyrosine supplementation apparently besides prolactin, namely its conversion to catecholamines which is not good in Peat world. So if someone decides to supplement BCAA's, let's say no more than 5 g, along with 2.5 g of tyrosine (assuming this is done away from meal) to be close to the numbers you have in your previous BCAA's posts, what else would you recommend to add to the mix to counterattack the prolactin, adrenaline, and catecholamines issues and what are their appropriate doses? I seem to retain water when I do the BCAA's/tyrosine combo. But if I take BCAA's with a protein meal, I do fine although my mood gets little bit worse, but not depressive or any of that. As an experiment, I ate protein rich meal and then took 4g of BCAA's with 100mg B6 (not P5P) and no tyrosine and I felt so much better, good digestion as expected from lowered serotonin and good mood! I want to do BCAA alone not necessirly with meals but tyrosine seems to give me problems. Maybe the best solution would be BCAA/tyrosine dissolved in OJ for vitamin C and some B6?
 

haidut

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milk_lover said:
post 118662
haidut said:
Sure, that's the theory at least:):
Isn't there a study that says tyrosine increases prolactin? Online, on many websites, they say tyrosine needs vitamin B6 and vitamin C as cofactors for dopamine pathway. Maybe if not enough vitamin B6 is consumed with tyrosine, tyrosine depletes B6 stores and it is this depletion that leads to increased prolactin? There are some issues with tyrosine supplementation apparently besides prolactin, namely its conversion to catecholamines which is not good in Peat world. So if someone decides to supplement BCAA's, let's say no more than 5 g, along with 2.5 g of tyrosine (assuming this is done away from meal) to be close to the numbers you have in your previous BCAA's posts, what else would you recommend to add to the mix to counterattack the prolactin, adrenaline, and catecholamines issues and what are their appropriate doses? I seem to retain water when I do the BCAA's/tyrosine combo. But if I take BCAA's with a protein meal, I do fine although my mood gets little bit worse, but not depressive or any of that. As an experiment, I ate protein rich meal and then took 4g of BCAA's with 100mg B6 (not P5P) and no tyrosine and I felt so much better, good digestion as expected from lowered serotonin and good mood! I want to do BCAA alone not necessirly with meals but tyrosine seems to give me problems. Maybe the best solution would be BCAA/tyrosine dissolved in OJ for vitamin C and some B6?

In the BCAA combo I'd stick to no more than 1.5g of tyrosine and make sure I get enough sunlight as its conversion into dopamine depends on light. As far as B6, I think taking 5mg daily is not a bad idea as most people are P5P deficient. B6, just like zinc, is heavily depleted by stress and PUFA.
 
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milk_lover

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haidut said:
post 118768
milk_lover said:
post 118662
haidut said:
Sure, that's the theory at least:):
Isn't there a study that says tyrosine increases prolactin? Online, on many websites, they say tyrosine needs vitamin B6 and vitamin C as cofactors for dopamine pathway. Maybe if not enough vitamin B6 is consumed with tyrosine, tyrosine depletes B6 stores and it is this depletion that leads to increased prolactin? There are some issues with tyrosine supplementation apparently besides prolactin, namely its conversion to catecholamines which is not good in Peat world. So if someone decides to supplement BCAA's, let's say no more than 5 g, along with 2.5 g of tyrosine (assuming this is done away from meal) to be close to the numbers you have in your previous BCAA's posts, what else would you recommend to add to the mix to counterattack the prolactin, adrenaline, and catecholamines issues and what are their appropriate doses? I seem to retain water when I do the BCAA's/tyrosine combo. But if I take BCAA's with a protein meal, I do fine although my mood gets little bit worse, but not depressive or any of that. As an experiment, I ate protein rich meal and then took 4g of BCAA's with 100mg B6 (not P5P) and no tyrosine and I felt so much better, good digestion as expected from lowered serotonin and good mood! I want to do BCAA alone not necessirly with meals but tyrosine seems to give me problems. Maybe the best solution would be BCAA/tyrosine dissolved in OJ for vitamin C and some B6?

In the BCAA combo I'd stick to no more than 1.5g of tyrosine and make sure I get enough sunlight as its conversion into dopamine depends on light. As far as B6, I think taking 5mg daily is not a bad idea as most people are P5P deficient. B6, just like zinc, is heavily depleted by stress and PUFA.
An hour ago, I took 4g BCAA's with 1.5g tyrosine and 8mg B6 (mixed with BCAA's powder) while shining red/infrared light on my eyes, and I can honestly say I feel so much better. Very good mood! Thanks haidut. I will continue experimenting with this combo to get the best results. I will try real sun next. Maybe the red light is not as effective.
 
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hi haidut and anyone. Any experience with clemastine effectiveness with sleeping and shakiness/tremors
 

< Rain

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Given that some people cannot get access to or do not tolerate well drugs like cyproheptadine or mirtazapine, this study offers some possible OTC alternatives for blocking serotonin. As you can see, Benadryl is also in the list but its anti-serotonin activity is much weaker compared to other first-generation antihistamines.

The effect of the antihistaminic drugs on the central action of 5-hydroxytryptophan in mice. - PubMed - NCBI

"...Antihistaminic drugs of various chemical structure (chlorcyclizine, chloropyramine, chlorpheniramine, clemastine, diphenhydramine, mepyramine, promethazine, thenalidine) were tested on their action on the central serotonin system in mice. The test used was the antagonism to behavioral syndrome produced by D, L-5-hydroxytryptophan (5-HTP). Clemastine, promethazine and thenalidine inhibited 5-HTP-induced syndrome in doses of much lower than those inhibiting locomotor activity. Similar but weaker effect was produced by chlorcyclizine and diphenhydramine. It could be suggested that these compounds exert central antiserotonergic action. Chloropyramine and, more strongly, chlorpheniramine potentiated the action of 5-HTP; this may be due to the inhibition of serotonin uptake. Only mepyramine in these tests did not show any action on the central serotonin system."

Of these drugs, clemastine (which is OTC in USA) looks particularly interesting. It is known to be an anti-depressant due to its FIASMA action (but probably also due to its 5-HT blocking) and also it looks like it may reverse the damage caused by multiple sclerosis.
Clemastine - Wikipedia
"...Clemastine does also act as FIASMA (functional inhibitor of acid sphingomyelinase)."
FIASMA - Wikipedia

Assessment of Clemastine Fumarate as a Remyelinating Agent in Multiple Sclerosis - Full Text View - ClinicalTrials.gov

I tried the Clemastine to check out the anti-serotonin aspect. First time in my life I ever took an anti-histamine. Even though it is OTC – it was a little hard to find, like they were pushing the other products. After looking at the PubMed for Clemastine, they probably wish they could take the chemical back and re-market as Rx.


Being researched for: Neuroinflammation in ALS, T3 transport disorders, enhancing myelination in the Prefrontal Cortex; reversing social isolation.

Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.

P2X7 receptors have emerged as potential drug targets for the treatment of medical conditions such as e.g. rheumatoid arthritis and neuropathic pain.


I have been taking one tablet in the evenings. My sleep is very deep and undisturbed. It does seem like there are a lot of dreams; especially at the end of the sleep cycle. They are very mellow however and do not push too deep into my waking memory. I also see an abundance of bright colors when I wake up – same thing when I used fresh coleus.


I do feel clear headed the next day; and also less adrenalin in my morning.

Also has a much longer affect then Theanine.


So I would say “Clemastine is a Winner”. Thank You for the recommendation.
 

A.R

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An hour ago, I took 4g BCAA's with 1.5g tyrosine and 8mg B6 (mixed with BCAA's powder) while shining red/infrared light on my eyes, and I can honestly say I feel so much better. Very good mood! Thanks haidut. I will continue experimenting with this combo to get the best results. I will try real sun next. Maybe the red light is not as effective.
How long did you keep this protocol up for and did you experience loss of water weight from it?
 

milk_lover

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How long did you keep this protocol up for and did you experience loss of water weight from it?
I did it only twice because I found out that the tyrosine has silica in it. The first time was with red light and it went well. The second time was with the real sun and I got sunburn lol.
 

ddjd

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Is there any way benadryl could increase estrogen. I got very high estrogen symptoms after taking benadryl a few times
 

murdoc

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clemastine works really well for sleep issues. sometimes even a quarter of a pill. (one has about 1 mg)
i liked it more than benadryl. not so foggy in the morning.

i had the same experience with pharmacies. they do not sell it any longer, because it is to old... I have ordered mine from online pharmacies. they sell it dirt cheap.
 
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