Misc Antihistamines efficacy and recreational use

[morphinolamine]

Like the title says, i've been looking into 1st generation antihistamines.

i'm diagnosed with adhd, chronic treatment resistant depression, social anxiety disorder, and cptsd. I've been in a perpetual cycle of trying to have a decent day/night cycle, which is likely a symptom of any combination of my diagnoses.

Antihistamines are great for hives and allergies, but i mostly love them for their sedation and anxiolysis, recreationally or therapeutically.

They might not be as effective as Benzodiazepines, Z-drugs or Barbiturates, but; a: you can usually take some of them for years, b: the withdrawals are a piece of cake and aren't fatal, c: they usually don't interact with anything else you're recreationally taking.

I struggle a lot with sleep, usually sleep deprived, only being able to sleep the night after an all nighter or when taking some kind of sleep aid. When i succeed with sleep, it's 2-3 hours uninterrupted at most. But i'm often not even able to at all so i stay up, and even then, the night after an all nighter i'm only able to get 4 hrs of shuteye.

I have tried quite a few meds for this, OTC and RX.

So far I'd rank them as follows;
1. Trazodone
2. Promethazine
3. Doxylamine or Cyproheptadine
4. Diphenhydramine
5. Mirtazapine
6. Quetiapine
7. Dimenhydrinate (DPH+Theophylline)
8. Melatonin
9. Valerian
10. CBD/CBN

*Last 3 dont have any antihistamine activity but ive tried them for sleep and/or anxiety.

Trazodone was the only one where i could take it for months daily without it losing efficacy, compared to dph which lose efficacy after 3-4 weeks.

Mirtazapine is the same, but already stopped being effective in less than a week at prescribed dose (15mg).
I wanted to try higher doses, but my psych moved to a diff facility. Then i got one of those anti-medication psychiatrists temporarily. He didn't want to change any of my doses, try new meds, but he was hella eager to help me stop with anything I wanted to.
Terrible experience lmao.

Quetiapine is horrid, it made me psychologically drained, as if my life force was sucked out. It made me feel sluggish, out of it, and even more depressed lol. I still had all anxiety and depression in the world, but at the same time I didn't care, about anything bad, nor anything good.

Not to forget to mention, all of these except Melatonin, Dimenhydrinate and CBD/CBN cause crazy weed like munchies which seem to be insatiable, which suck big time of you have issues with food.

Anyhow, here are a some i'm interested in, and was hoping people with experience could comment on, ill be naming some novel, not necessarily antihistamines options too btw.

1. Cyproheptadine
Haven't been able to find much, other than that some report it being quite sedating and good for insomnia as an inverse H1 agonist. Also being used as an antidote for serotonin syndrome, and can cause hallucinations? In high doses.* i ordered some that's arriving today. × addendum; tried and pleasantly surprised, only used for sleep so far, so I'm interested to see how it will affect the other things I struggle with.
OTC

2. Hydroxyzine
Ive been wanting to try this one for a very looooog time, for both anxiety and insomnia, but never got the opportunity, I'd rather have it prescribed than to buy it illegally, so ill ask my next psychiatrist about it. My last didn't know about it or didn't want to prescribe it, but did give me a 2 year rx for Trazodone. RX only

3. Triprolidine
Seems to be a pretty old and niche medicine, I can't find much anecdotal reports other than being very sedative, more so than Diphenhydramine or Doxylamine. OTC

4. Tripelennamine
Rather obscure, i see it in a couple of EU countries, used in compounded allergy and cold medicine, barely any reports other than simply being called sedative.
OTC

5. Ophenadrine
Sounds very interesting, a "dirty drug" just like Cyproheptadine, skeletal muscle relaxant. NMDA antagonist, NDRI, HERG+NA channel blocker, muscarinic anticholinergic, h1 antagonist. Some trip reports online, not as delirious as DPH or Doxylamine, but a high doses will still cause it. Hard to find and Unfortunately RX only.

6. Meclizine, Cyclizine, Clemastine
Not sure about these, i hear some rave about cyclizine and the combo dipipanone (man I wish I could get dipapnone or dextromoramide)

7. Pheniramime and halogenated derivates, especially Chlorpheniramine
Some more very potent antihistamines, 2mg occupies 54% of H1 receptors, vs for example DPH at 30mg occupying 56.4%.
The people over at the /DPH sub say it's more euphoric and sedative than DPH. Albeit euphoria isn't my goal, it's a nice side effect, I have some physical euphoria with Promethazine as well for example.

8. Alimemazine
A rather obscure one, related to tricyclics Cyproheptadine and Promethazine. As far as I know, this is OTC in France, but has pretty raving reviews, it doesnt seem to be very fun or euphoric, but is extremely wonky, wobbly, drowsy, veey long lasting and dreamy. Some people dislike it for that, and others love it. People say it's like drinking too much at high doses (and you look the part too). If i had this in acute opioid withdrawal along w clondine it would've been a godsend.

9. Ketotifen
Another tricyclic antihistamine, related to Pizotifen, used a lot in MCAs, CFS, POTS, Asthma, not much info about how sedative it is other than generic wiki page info.

Honourable mentions, not necessarily antihistamines;

1. Clonidine, Prazosin or Guanfacine
been wanting to try this for years, mainly because it could help my anxiety, Dexamphetamine side effects, insomnia, and PAWS, but no doc has been willing to prescribe it, unless I stop with the ADHD meds (I asked to take it for ADHD specifically in the past)

2. Orexin antagonists
A relatively new, exciting novel class of drugs used for Insomnia, like Seltorexant, Daridorexant, Lemborexant, Suvorexant.
The moment these came out of trials i got pretty excited, but still needed to wait before they could be prescribed. Seltorexant is in phase 3 for depression, and Suvorexant is in phase 4 as an adjunct for Major Depression Disorder. They're all high on my list of things i want to try.

3. Here are a couple extra i'm interested; Doxepin, Niaprazine, Muscimol, Tasimelteon, Zuranolone, Sunobinop, Aticaprant, Navacaprant, Samidorphan

 

[emkee_reinvented]

Maybe you know this one and disqualified it bu worth to mention Opipramol.
Bought OTC during vacation the one selling advised it over Doxylamine att
Didn t know about anti-Histamine and sleep back then.

But then it was very effective and without day after effect s.
Took Promethazine twice and that and bizarre 'deliriant dreams'.

https://en.wikipedia.org/wiki/Opipramol
[no longer prescribed here, check for adverse effect s first, ~30 year s ago]

 

[Allylbenzene]

...i've been looking into 1st generation antihistamines. I'm diagnosed with adhd, chonic depression, social anxiety disorder, and cptsd.

Antihistamines are great for hives and allergies, but for me, sedation and axiolysis are their best use case.

If you're interested, you might find these options much more suitable for your situation. Most of these address the fundamental root issues behind your symptoms. Another advantage is they are all OTC.

Agmatine works similarly to Clonidine and Guanfacine (alpha-2A agonists), except agmatine offers a better therapeutic profile and is OTC. Agmatine, Clonidine and Guanfacine are effective because they block adrenaline's negative effects and increase endogenous GABA. Agmatine daily doses range from 300mg to 3g.

Cyproheptadine is a very good choice since it reduces several things involved in your symptoms. It also blocks one of the dopamine receptors so people prefer to use low doses to minimise this effect.

Theanine is potent anti-anxiety & anti-stress substance with antihistamine effects. Theanine also works via GABA. Theanine is suitable for repeated daily doses of 100mg to 1g depending on how strong an effect you're looking for.

Niacinamide and Taurine have powerful anti-anxiety effects. They have several properties (including GABA) and will help to resolve some of the root issues behind your symptoms. A daily dose of Niacinamide (50mg with carbs) and Taurine (100-300mg with carbs) is appropriate.

Creatine and Aspirin are often overlooked but they have potent anti-anxiety effects. Aspirin has worthy antihistamine effects. Both will help to resolve some of the root issues behind your symptoms. A daily dose of Creatine (200mg to 1g) and Aspirin (50-100mg) is appropriate.

Thiamine is aka vitamin B1. It shares similarities with all the substances mentioned above and is necessary for proper metabolic function. It is also OTC. Doses range from 100mg to 1g and should ideally be combined with carbs.

 

[The Holy Quadruplty]

Chlorpheniramine has a chemical structure not too far off from DMTs chemical structures, and Chlorpheniramine is also a potent Serotonergic drug. It's barely an anticholinergic, but has those effects too, and very potent antihistamine effects like you said. I take it, and Diphenhydramine everyday (use to be Chlorpheniramine, and Promethazine everyday tho).