Why does Cyproheptadine make me super drowsy the next day?

[AdoTintor]

If there is any beneficial effect from Cyproheptadine I wouldn't know because the next day I feel completely zonked out - what is the mechanism for this?

I speculate that if Cyproheptadine blocks the 5HT2 receptor then less serotonin will be mopped up by binding to this receptor. Therefore, more serotonin will be forced down the other pathways which include conversion to melatonin causing excessive drowsiness the next day?

I read elsewhere on the forum that the drowsyness from cypro is caused by histamine. What would be the mechanism for that? - at least the above hypothesis leads directly to increased melatonin.

In general is this what happens when one takes an antagonist against substance X - it just forces X to express itself in one of the other pathways/receptors?

 

[Peatness]

Cyproheptadine down-regulates dopamine D3 receptors and acetylcholine receptors fairly broadly which both contribute to sluggish thinking and flat moods.

What is Acetylcholine? Functions and Effects In The Brain - EvidenceLive

Acetylcholine plays an essential role for many functions in the body and mind. Without proper levels, you could not regulate...

evidencelive.org

 

[dukesbobby777]

If there is any beneficial effect from Cyproheptadine I wouldn't know because the next day I feel completely zonked out - what is the mechanism for this?

I speculate that if Cyproheptadine blocks the 5HT2 receptor then less serotonin will be mopped up by binding to this receptor. Therefore, more serotonin will be forced down the other pathways which include conversion to melatonin causing excessive drowsiness the next day?

I read elsewhere on the forum that the drowsyness from cypro is caused by histamine. What would be the mechanism for that? - at least the above hypothesis leads directly to increased melatonin.

In general is this what happens when one takes an antagonist against substance X - it just forces X to express itself in one of the other pathways/receptors?

Mirtazapine is also a powerful anti-histamine (in the right dose), which can cause the next day to be a complete write off, IME.

The more you take cyproheptadine, the more immune you become to the anti-histamine effects. To the point where they completely dissappear. That aside, it's mild dopamine antagonism causes the flat mood effects, IMO. It's anti-cholinergic effects are actually anti-depressant (acetylcholine antagonizes dopamine).

 

[InChristAlone]

The zombie feeling goes away the longer you use it. The first few days might as well be for resting. But if you don't have obvious need to use it then don't.

 

[Peater]

Is it possible for cypro to cause a 'rebound' effect? I like to use it for sleep, but realised I should probably stop for a while. Really itchy last night. The last thing I can remember being able to verify as causing this was Essentiale Forte (polyene phosphatidylcholine) so I thought the choline link was interesting.

 

[AdoTintor]

I've been trying to read up on the mechanism by which the older style anti-histamines can make one drowsy. I've gone through all mentions of histamine in the mega_master_ray_newsletter and found nothing on drowsiness.

So far gather that they can get into the brain and bind to the H1 receptor and somehow this magically causes drowsiness - but no mechanism is given. Does anyone have a reference for this?

 

[Highserotonin90]

Bump