Cyproheptadine - Liquid Serotonin Antagonist For Lab/R&D

[managing]

They use spironolactone for pcos

[Effect of the antiserotoninergic preparation cyproheptadine on the levels of luteinizing and follicle-stimulating hormones and testosterone in patie... - PubMed - NCBI

Looks like cypro would work if someone didn’t want to take Spiro

A significant decrease in the level of testosterone (p less than 0.0001) in 1 and 2 h and a tendency to a decrease in the LH level and a LH/FSH ratio in 2 h after cyproheptadine administration were revealed. The effect of the drug on the FSH level was insignificant. A conclusion was made of the involvement of the serotoninergic mechanisms in the regulation of androgenic secretion in patients with polycystic ovaries.

Ray told me that before Bromocryptine, Cyproheptadine was used to treat both Cushing's and PCOS.

And I think it was pretty clear he prefers the latter to the former. I presume he would also prefer it to spironolactone.

 

[managing]

So cyproheptadine, affect someone with PCOS positively, lowering testo and estrogen
What about a health male, is androgens affected positively, increased?

I don't think it anti-androgenic (TTBMK). Its effective against PCOS because (as discussed elsewhere) its an estrogen antagonist.

 

[LUH 3417]

Ray told me that before Bromocryptine, Cyproheptadine was used to treat both Cushing's and PCOS.

And I think it was pretty clear he prefers the latter to the former. I presume he would also prefer it to spironolactone.

Strangely when I was taking a huge dose of Cypro I got the worst period of my life with clots and excessive bleeding which never happened to me before. I was also using high dose progesterone at the time. I wonder if it was an expulsion of estrogen? It didn’t return and was only for one cycle but it was worrisome.

 

[managing]

Strangely when I was taking a huge dose of Cypro I got the worst period of my life with clots and excessive bleeding which never happened to me before. I was also using high dose progesterone at the time. I wonder if it was an expulsion of estrogen? It didn’t return and was only for one cycle but it was worrisome.

Hard to say. But I do note that he favors 1mg/d or so.

 

[LUH 3417]

Hard to say. But I do note that he favors 1mg/d or so.

That’s true. I also emailed him about it and he replied:
“I know someone who took 28 mg/day for several weeks (she was having menstrual hemorrhages and fainting), and stopped when she felt well, and has stayed well without it. My impression, from my own use, is that it corrects something over a period of several days, reducing the amount needed to produce the same effect.”

 

[managing]

That’s true. I also emailed him about it and he replied:
“I know someone who took 28 mg/day for several weeks (she was having menstrual hemorrhages and fainting), and stopped when she felt well, and has stayed well without it. My impression, from my own use, is that it corrects something over a period of several days, reducing the amount needed to produce the same effect.”

Excellent. Thanks for expanding the discussion.

 

[managing]

Thought I would just throw another awesome effect of cyproheptadine into the mix: inhibits proliferation of some cancers in the liver:

Cyproheptadine, an antihistaminic drug, inhibits proliferation of hepatocellular carcinoma cells by blocking cell cycle progression through the activation of P38 MAP kinase

 

[Fletcher]

My rat has been using a cypro dose of .5mg (1 drop) for the past couple of weeks, and has consistently slept through the night for the first time in a long while. He'd tried cypro before (up to 4mg) and it always made him drowsy the next day, so discontinued. With .5mg he feels fine. I'm wondering what is the most likely reason for this improved sleep (reduced serotonin, estrogen?) on such a small dose?

 

[golder]

My rat has been using a cypro dose of .5mg (1 drop) for the past couple of weeks, and has consistently slept through the night for the first time in a long while. He'd tried cypro before (up to 4mg) and it always made him drowsy the next day, so discontinued. With .5mg he feels fine. I'm wondering what is the most likely reason for this improved sleep (reduced serotonin, estrogen?) on such a small dose?

Very interested to hear peoples thoughts.
Topical or oral?
Timing of dose?
Timing of sleep, then time you wake up?

 

[Fletcher]

Oral, no set time but usually before 7pm, sleep 10pm - 6am.

 

[ddjd]

is cyproheptadine a GABA agonist?

 

[ddjd]

does cyproheptadine inhibit 11b-HSD1 expression? (enzyme that converts cortisone to cortisol)

 

[accelerator]

For most people, Ray recommends 1mg cypro daily, no more. For people with serious conditions he has mentioned doing 2mg - 3mg daily. So, at 6 drops you are above even the "serious" doses he mentioned. Cypro can really lower stress hormones and histamine, which can leave a person feeling like zombie the next day (if taken at night) as it has relatively long half-life.

What do you make of the fact that even low doses can cause low dopamine/zombie/slow feeling in a lot of people, and yet other people you've mentioned, yourself and others with CFS used very high doses to get higher energy and even an anti-depressant effect?

And how long would one need to use it to tell which direction it's taking things?

 

[Grapelander]

Short and Long Term Effects of Cyproheptadine on Spasticity and Spastic Paretic Gait (1986)
(see attachment)
…results suggest that CYPRO is an effective anti-spastic medication which is able to improve locomotor function.

 

[Grapelander]

Cyproheptadine treatment of sexual dysfunction induced by serotonin reuptake inhibitors (1995)
…some patients with sexual dysfunction associated with SRI treatment, mainly decreased libido and anorgasmia, may benefit from cyproheptadine.

 

[Max23]

Do you think there is a chance of addiction with it? Been using 6 drops before sleep. It causes a really good and refreshing sleep. I am worried about an addiction and not being able to fall asleep once discontinued.

 

[Grapelander]

Do you think there is a chance of addiction with it? Been using 6 drops before sleep. It causes a really good and refreshing sleep. I am worried about an addiction and not being able to fall asleep once discontinued.

Really great question - so I looked and there is a tolerance; it will go away after cycling off anti-histamines 3 to 14 days.
The development of tolerance to antihistamines:
1. The majority of a series of patients showed evidence of the development of tolerance to antihistaminic drugs as shown by the failure or diminished effectiveness of the drugs to reduce the wheal and flare response to histamine and ragweed extract.

2. The time necessary to develop tolerance was between 7 and 20 days of maintenance on therapeutic doses of the antihistamine.

3. Tolerance developed to one antihistamine extended to others, even though the chemical relationship was not close.

4. Return of pharmacologic response to an antihistamine after discontinuance of the drug takes from 3 to 14 days.

5. We believe that, clinically, the development of tolerance is only relative. Even though our data would imply complete clinical tolerance in the greater part of our cases, most patients continue to derive symptomatic relief on prolonged antihistaminic therapy. The evidence presented does suggest, however, that patients on prolonged antihistamine therapy may develop clinical tolerance. When this is suspected the dose should be increased or the drug discontinued for a short perior (3 to 14 days) before resuming therapy.

 

[Max23]

Really great question - so I looked and there is a tolerance; it will go away after cycling off anti-histamines 3 to 14 days.
The development of tolerance to antihistamines:
1. The majority of a series of patients showed evidence of the development of tolerance to antihistaminic drugs as shown by the failure or diminished effectiveness of the drugs to reduce the wheal and flare response to histamine and ragweed extract.

2. The time necessary to develop tolerance was between 7 and 20 days of maintenance on therapeutic doses of the antihistamine.

3. Tolerance developed to one antihistamine extended to others, even though the chemical relationship was not close.

4. Return of pharmacologic response to an antihistamine after discontinuance of the drug takes from 3 to 14 days.

5. We believe that, clinically, the development of tolerance is only relative. Even though our data would imply complete clinical tolerance in the greater part of our cases, most patients continue to derive symptomatic relief on prolonged antihistaminic therapy. The evidence presented does suggest, however, that patients on prolonged antihistamine therapy may develop clinical tolerance. When this is suspected the dose should be increased or the drug discontinued for a short perior (3 to 14 days) before resuming therapy.

Mentally the mice are hooked. I am generally afraid of substances that cause sleep. I understand that there is some risk, but that it is not too big from your post. Can always do some xanax for the mice for a few days if necessary. Anyone who is a test mouse and has personal experience with it sleep, addiction wise?

 

[aguineapig]

You could very easily titrate off of it if necessary. I never noticed rebound insomnia when stopping 1mg per day.

 

[Grapelander]

Mentally the mice are hooked. I am generally afraid of substances that cause sleep. I understand that there is some risk, but that it is not too big from your post. Can always do some xanax for the mice for a few days if necessary. Anyone who is a test mouse and has personal experience with it sleep, addiction wise?

You could try Phenibut for a few days; I never used it for more than 3 days in a row as I did not want to get addicted to it. It is less crazy than Xanax/Valium which seems to wipe out my short-term memory.