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Picamilon - fast acting (mild) anxiolytic

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edgar07

Greenlighter
Joined
May 3, 2011
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25
Hi,

Just wanted to share some of my experiences with picamilon in relation to anxiety. I'm more anxious than the average person but I'm not so bad that I require prescription meds for it (really don't want to take benzos if I don't have to). When I first tried it I tried dosages ranging from 50mg to 150mg orally, and found it to have an effect, although pretty much non-existant. Would make me a little more relaxed but would not get rid of all anxiety.

Then the other night, after I'd gone for weeks without experiencing any serious anxiety, my brother went to hospital after having suicidal ideations (wasn't that it was necessarily serious but it was at night and the only place he could go for help). This pretty much flicked a switch in my brain as soon as I found out, and the anxiety came back with a vengeance - the last time I'd had to deal with this it left me having a full on panic attack.

So, I was looking for something to calm me down. So i desperately packed a capsule of picamilon and prayed it might have some effect. Then I thought, fuck it, i'll insufflate it, it's gonna get to my brain quicker that way. Boy was I right.

Within 5-10 minutes of insufflating about 150-200mg of picamilon (I couldn't be bothered weighing out the amount, going on my estimation) the anxiety was completely gone, accompanied with a feeling of my body being very, very relaxed. I still obviously wasn't too pleased about the situation my brother was in, but I could cope with it soooo much better. It's seems to be a very effective way to quickly raise GABA levels, and has none of the side effects of GABAergics like alcohol, phenibut, benzos, etc. Just a very pleasant, completely relaxed, but still stimulated feeling.

So I find picamilon to be a very effective anxiolytic when insufflated but pretty piss weak orally. Has anyone else had much experience with picamilon at combatting anxiety?
 
You don't know the dose that was in the capsule you emptied out?

Perhaps oral bioavailability is low but intranasally it is substantially higher, enough to produce a more noticeable effect. This isn't uncommon among drugs.

Also, is this drug available within Australia? You don't have your location listed, and I can't find the product listed on the Standard for the Uniform Scheduling of Medicines and Poisons.

This is a very interesting drug; and the first I've heard of a decent method of getting GABA across the Blood-Brain-Barrier. This does sound like a good alternative to the other GABA-ergic drugs out there, most of which work by modulating GABA receptors at allosteric sites (i.e. not directly on the receptor but on a different location on the protein).
 
I didn't empty it out from capsules, I have the drug in pure powder form. I usually do the capping myself - I don't really like paying for a bunch of magnesium stearate and other fillers :) I'm guessing the dosage was 150-200mg going from my experience of partially filling capsules and then weighing the capsules on a scale (taking capsule weight into account of course). I've since that post weighed out 200mg and snorted it, pretty much the same effect as before, except I wasn't anxious to start off with.

Yes I'm in Australia, have gotten picamilon through customs many times, even with letters saying customs checked out the package. It's not listed on any drug schedules anywhere in Australia.

I agree with you that this is a fascinating molecule. It may also be effective in treating migraine headaches due to niacin being an effective vasodilator - unfortunately I've never had any around when I've had a migraine, so I haven't been able to test that.
 
^ You can get niacin from pharmacies and vitamin stores, it is probably more commonly known as nicotinic acid. The vasodilation it causes though leads to flushing and itching of the skin. Secondly, vasodilation is basically the opposite of what pharmacologists are trying to achieve with migraine control. The current thinking is that cerebral vasodilation leads to increased pressure and then the migraine; many of the migraine drugs on the market now such as sumatriptan act as serotonin agonists, causing vasoconstriction within the brain and aborting the migraine.

ETA: Sorry I didn't read your original post correctly, thought you were getting the picamilon in capsule form. :)
 
I'm going based off of http://www.ncbi.nlm.nih.gov/pubmed/15673472 to suggest that niacin released from breakdown of picamilon may be able to treat migraines. It hasn't been subjected to any decent sized clinical trials though.

You are correct that a lot of anti-migraine agents are vasoconstrictors (ergoline, caffeine, etc.) There are even some interesting ones that are in fact 5-HT 2A agonists but they can't cross BBB, sadly.
 
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^ Which interesting things can't cross the BBB yet agonize 5HT2A?

Most psychedelics antagonize this receptor, and it may be that agonism at 5HT2A causes vasoconstriction (hence why psychedelics help with migraines). There are many antagonists in clinical use, including an OTC antihistamine I like called cyproheptadine (Periactin). Conversely, Periactin is also used to treat migraine in children and adolescents (but not adults). Antagonism of this receptor is associated with increased appetite, and so they use cyproheptadine to stimulate appetite in children who won't feed properly. This same antagonism effect was the cause of a side effect of a migraine treatment my mother was on; again, increased appetite and weight gain.
 
Mr Blonde said:
^ Which interesting things can't cross the BBB yet agonize 5HT2A?
Click to expand...

I was mistaken, for some reason I thought they were used to treat migraines, but it's for glaucoma (reducing intra-ocular pressure - increased pressure is a symptom of migraines so that's probably why I connected the two). They are still interesting though:

AL-34662
180px-AL-34662_structure.png


AL-37350A
140px-AL-37350A_structure.png


It's easy to see what they are based off of, and with some alkyl groups coming from the primary amine they would be made more lipid soluble whilst likely still reatining activity at the receptor (going off of DMT, DET, DPT, DBT, DALT, etc.) although there isn't much research about the alpha-methylated varieties of those mentioned psychedelics. From what I have been able to find (basically anecdotal reports here on BL) they appear to be active.
 
^ Those are interesting structures indeed... and I would like to see the results of adding alkyl chains to that amine. ;)
 
Sorry to go off on a tangent, but what you said Mr Blonde
this is a very interesting drug; and the first I've heard of a decent method of getting GABA across the Blood-Brain-Barrier. This does sound like a good alternative to the other GABA-ergic drugs out there, most of which work by modulating GABA receptors at allosteric sites (i.e. not directly on the receptor but on a different location on the protein).
Click to expand...
has interested me; so is baclofen, a derivative of GABA, something that modulates GABA receptors at allosteric sites (I don't know what this means :S), or is it not a GABA-ergic drug...?
 
^ No worries, happy to talk about pharmacology. :)

Allosteric sites are locations on the receptor other then the main binding site. Take for example, the GABAa receptor. GABA binds to a location on this receptor and then creates it's effect, which in this case is to allow chloride (Cl-) into the neuron causing hyperpolarization. This prevents the neuron from firing it's action potential, which is what happens when it is depolarized. So, the GABAa receptor is what is known as a ligand-gated ion channel; when the ligand (GABA) binds, it opens a pore that allows the ion (Cl-) to flow through the cell membrane.

A benzodiazepine will bind to the GABAa receptor, but at a different location to GABA. The GABAa receptor can be divided into subunits; benzodiazepines bind at a site between the alpha and gamma subunits. When this happens, the GABAa receptor morphs into a configuration where it has a much greater affinity for the GABA neurotransmitter, which leads to the Cl- ion channel opening more frequently and the neuronal action potential being inhibited. This is similar to how barbiturates work; they also bind to a site on the GABAa receptor separate from where GABA binds, and in the case of the barbiturates the duration the Cl- channel is open is longer. Keep in mind that not all GABAa receptors have a site for benzodiazepines or barbiturates to bind to, but the majority do.

As for baclofen; it is a direct GABAb receptor agonist. The GABAb receptor operates differently to GABAa receptors. Remember how I said GABAa receptors are ion channels that directly allow Cl- into the cell? Well GABAb receptors do not do that. When GABA, or baclofen, binds to these receptors, it instead causes a signal to be passed to a separate ion channel that allows potassium (K+) into the cell. Increased amounts of K+ enter the cell and this again leads to inhibition of the neuronal action potential; so no neurotransmitter release.

You might be wondering why baclofen isn't as recreational as benzodiazepines if it seemingly has the same overall effect. This I am not sure on, but it could be that GABAb receptors are associated with processes in the brain that are related to neuromuscular responses. Hence why baclofen is great for treating muscle spasms, but not so good for anxiety, whereas GABAa receptors are more important for regulating excitatory processes in the CNS as well as the rest of the body.

Here is an interesting figure that illustrates what I have discussed, from an article about the possible role of GABAb receptors in the action of GHB.

Sorry if that was too in-depth for you, but I do have a real passion for pharmacology. :)
 
I read through this when you posted it but I forgot to say thankyou for that! I'm unfamiliar with some of the terms but that's a good description, very interesting.

I've always heard that baclofen is meant to have little or no abuse potential, but both times I've been prescribed it now I've felt mild opiate like effects from it, though I get no recreational effect from benzos.
 
Very interesting guys, first time I've heard of it! And a very cute name for a drug right?! ;) :p
 
Sorry to bring up an old thread but found it in searc, anyone had any experience with this? is it any good compared to benzos? dosage?
 
Very interesting drug indeed after doing a lil' research!
 
Picamilon is able to cross the blood–brain barrier[5] and then is hydrolyzed into GABA and niacin. The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response.[6] The second released component, niacin acts as a strong vasodilator,[7] which might be useful for the treatment of migraine headaches.[8][9] *Google

Will definatly explore this drug more as I've never heard of it till now and I suffer acute anxiety/Depression and cluster head aches (worse than migranes) and am also an alcoholic which is listed as approved uses in Russia. I'm on 2 benzos and codeine and this sounds like it has potential!
 
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Azron said:
I suffer acute anxiety/Depression and cluster head aches (worse than migranes) and am also an alcoholic which is listed as approved uses in Russia. I'm on 2 benzos and codeine and this sounds like it has potential!
Click to expand...

I know how bad cluster headaches can be, I dont want to really derail this thread but I thought itd be good to mention, have u considered using psilocybe mushrooms for the headaches? It can ease and in some cases eliminate the symptoms.
 
Could anyone here speculate on what the possible implications for taking this drug while physically-dependent to benzo's? could it perhaps be a non-benzo alternate to taper with? a quick google search only found limited information- is it physically addictive itself?
 
acidicweed_69 said:
Could anyone here speculate on what the possible implications for taking this drug while physically-dependent to benzo's? could it perhaps be a non-benzo alternate to taper with? a quick google search only found limited information- is it physically addictive itself?
Click to expand...

This
 
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