Cyproheptadine

links: Drugs reference: 9-4-2021

Cyproheptadine #

• 5-HT2 antagonist, specifically. 5-HT1A antagonist. Ki off 8 at D3.

• H1 antagonist - significant increase in NREM. 5-HT2C antagonism is also antihistamine.

• mAChR antagonist. M1-5 Ki is 12, 7, 12, 8, 11.8

  • Which is a bitch. Pretty constipating and reduces urination.

• D2 antagonist, and inhibits D1 and D3 at certain doses.

• Inhibits prolactin in low concentrations, increases it in higher doses

• Lowers Blood Pressure

• Antagonizes Aldosterone (so it’s magnesium-sparing) and has calcium blocking action.

• Improves glucose tolerance in diabetics

• ERα antagonist.

• On idealabs: https://raypeatforum.com/community/threads/cyproheptadine-liquid-serotonin-antagonist-for-lab-r-d.14217/

  • As a serotonin antagonist, the list of virtues is exhaustive. Many more threads are linked, themselves with hella references.

• Messses with prolactin; anhedonic and depression-inducing. Also gives you a serious serotonin rebound. RPF

• Lokzo’s epic rebound:

  • RPF It makes me feel so fearless and numb on the drug, as in, I can’t feel any emotions, and my appetite goes through the roof. My energy in the gym is shit on cypro, I feel weak and miserable. No motivation, no life, no vigor, just blah - existence. During this grim days, after using cypro over 25 times in the past 7 months - I know that the rebound is ALWAYS worth it. This rebound comes EVERY SINGLE TIME…. 4 days AFTER a single 1mg dose. That is, if I take it on a sunday night at 5pm, I will feel like shit for 3 days and then on day, I get this REBOUND, where my PSSD disappears and this last for a few days on. HOW?!?!?!?
    • Redsun thinks it’s histamine rebound. Cypro is a really potent antihistamine.
  • https://raypeatforum.com/community/threads/can-someone-please-explain-cyproheptadine.28885/post-445169
    • He attributes it to rebound in Aldosterone of all things! Since he replicated it with licorice root. Pumps in the gym and holding water/salt properly again.

• https://raypeatforum.com/community/threads/cyproheptadine-lsd-based-drugs-can-regenerate-damaged-liver.3398/

  • Having elevated Liver enzymes doesn’t mean it’s being affected negatively. Since serotonin can be a culprit in liver damage, anti-serotonin drugs can stimulate the liver to regenerate.
  • Cypro, along with Lisuride, and maybe Ritanserin, they are the safest anti-serotonin drugs out there.
  • Has a ‘well-known’ withdrawal after taking large amounts and discontinuing suddenly.
  • After cessation, serotonin and glucocorticoid receptor density/sensitivity can increase, lowering baseline synthesis of those chemicals.

• Effect of cyproheptadine on episodic ACTH and cortisol secretion 16mg!

• Chihiro’s thoughts on the matter:

  • On that vein, my preference for fats went away as my endotoxin issues resolved. Similarly, drugs which block serotonin’s actions, such as cyproheptadine, produce a craving for something light, watery, and sweet — noodle soups, fruit juice, even rice! Now I gag at the sight and texture of fats in my mouth.
  • https://www.quora.com/profile/Chihiro-161/Cyproheptadine-Protection-against-a-mentally-ill-culture
  • It controls every single pituitary secretion in a positive direction.
    • Metergoline and cyproheptadine suppress prolactin release by a non-5-hydroxytryptaminergic, non-dopaminergic mechanism
    • The effect of cyproheptadine on plasma growth hormone (GH) and on somatostatin response to GH-releasing hormone in man
    • Effect of the antiserotoninergic preparation cyproheptadine on the levels of luteinizing and follicle-stimulating hormones and testosterone in patients with polycystic ovaries
      • A significant decrease in the level of testosterone 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.
        • Granted these are females, so…?
  • It wasn’t too far from a time I’d started on Cyproheptadine (a well-known anti-serotonin drug used to treat Serotonin Syndrome) and started feeling the way I used to music. It felt like I was listening through fresh ears, as a kid, all over again.My sensitivity to the stimuli greatly increased. It felt like I was feeling it on a whole nother level.. just as I had sometime back in 6th grade.I started considering courses of action that I normally wouldn’t have considered. Myways of solving problems adopted a far more radical philosophy.I also became more playful, my bodily movements looser, less restricted. Everytime I did a routine task, I saw an endless number of potentials in it.I also became a great deal empathetic since being able to understand the endless potential.. there is a certain truth to everything, a possibility to every passing human no matter what current form he may present in.

• Brain cholesterol and phospholipid levels in cyproheptadine treated albino rats

  • Increases brain cholesterol synthesis

• https://raypeatforum.com/community/threads/did-cyproheptadine-made-me-diabetic.27669/post-434098

  • the hyperglycemic/insulin-inhibiting effect of cypro seems to be limited to rats and hamsters. It producers different effects in humans or rabbits

Trip killer #

• https://old.reddit.com/r/Biohackers/comments/tes03r/an_unkown_way_to_end_a_bad_psychedelic_trip/ I think it is indeed a trip killer. People in the comments are also talking about Niacin megadoses like 200 mg will kill a trip. And also cure schizophrenia.
• https://old.reddit.com/r/Psychonaut/comments/u873pf/is_it_ok_to_trip_after_taking_cyproheptadine/
  • Not only will it kill trips, it might prevent you from tripping if you take it long enough, say for 2 weeks? He claims both agonists and antagonists downregulate/desensitize.
    • As expected, ChatGPT is totally useless for this type of question.
  • Yep: Acute and chronic effects of serotonin (5HT) antagonists on serotonin binding sites
    • Cyproheptadine, BC-105 and methysergide, but not metergoline, decreased the density of 5HT2 sites in frontal cortex 48 h after a single dose
  • Haidut: Unlike cyproheptadine, I have not seen studies with metergoline showing it upregulates the serotonin receptors it antagonizes.

Dose #

• Half life: 9 hours. Topical might technically last a little longer.
• Try 0.5-1mg/day, usually a few days a week. As a prescription antihistamine though, it’s sold as 4 mg tablets, which might be a megadose.
• After a day or two, the knockout/sedation subsides. Or maybe a week or 2.
• Cyproheptadine: a potent in vivo serotonin antagonist
  • Reported to block 85% of 5-HT2 receptors in the human brain at a dose of 4 mg three times per day (12 mg/day total) and to block 95% of 5-HT2 receptors in the human brain at a dose of 6 mg three times per day (18 mg/day total) There’s something of a tolerance, which should go away after cycling off for a few days.
    • Is this insane? Idek; I recall Landshark saying that level doesn’t even affect him. Real Peatbros that take it on the regular can steadily increase the dose after they get used to the grogginess. Haidut has rower friends that take 4-8 mg daily.
• https://raypeatforum.com/community/threads/cyproheptadine-liquid-serotonin-antagonist-for-lab-r-d.14217/post-488474
  • Tolerance to the anti-histamine effect should go away after cycling off for ~3-14 days. Free modafinil in the meantime.