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  • BDD Moderators: Keif’ Richards | negrogesic

Clobazam (Frisium)

P

pally pete

Bluelighter
Joined
Feb 21, 2010
Messages
2,428
I have acquired a number of 10mg Clobazam tablets and was wondering if anybody has any experience with them?

I realise that they are marketed for severe Anxiety and also for Epilepsy (I guess due to there anti convulsant properties?) I can not seem to find too much information about them compared to other Benzodiazepines, on wiki they are listed as "Atypical benzodiazepine receptor ligands" whatever that means? Also there is no mention of them being a sedative/hypnotic, muscle relaxant or amnestic unlike most other Benzodiazepines, which makes me slightly wary. The equivilant dose is 20mg Clobazam = 10mg Diazepam.

Any advice would be greatly appreciated, thanks.
 
pally pete said:
I have acquired a number of 10mg Clobazam tablets and was wondering if anybody has any experience with them?

I realise that they are marketed for severe Anxiety and also for Epilepsy (I guess due to there anti convulsant properties?) I can not seem to find too much information about them compared to other Benzodiazepines, on wiki they are listed as "Atypical benzodiazepine receptor ligands" whatever that means? Also there is no mention of them being a sedative/hypnotic, muscle relaxant or amnestic unlike most other Benzodiazepines, which makes me slightly wary. The equivilant dose is 20mg Clobazam = 10mg Diazepam.

Any advice would be greatly appreciated, thanks.
Click to expand...

Well I can help, even if late. Here in Canada you'll only get them from a neurologist, like Clonazepam in some countries, (clonazepam is really good for nerve pain too) as it is only indicated for epilepsy.They indeed have some anxiolytic power, let me show you this german diagram :
iLhfYxf.gif


It's still better than clonazepam...which truely is weak as an anxiolytic...until you take a good dose everyday and a certain plasma concentration is achieved in your blood.
It is not very anxiolytic but taking 30mg did me good this one time a friend gave me some for a meth comedown. Knowledge is power! Even if delivered late ;)
 
It's a 1.4 benzo, iirc that means it has affinity for only 1 of the 2 common receptors that benzos have affinity for usually, thus being "weaker" or having a less pronounced effect.

/e: let me look that up.

Oops, I was wrong about the number, but it means pretty much that.

Clobazam is a 1,5-benzodiazepine, meaning that its diazepine ring has nitrogen atoms at the 1 and 5 positions (instead of the usual 1 and 4). Like other 1,5-benzodiazepines (e.g., arfendazam, lofendazam, CP-1414S), it has less affinity for the ω1-allosteric binding site on the GABAA receptor compared to the 1,4-benzodiazepines. It has selective affinity for the ω2 site, where it has agonistic activity.[10]
Click to expand...
 
They were pretty aweomse. I only had them once, but I liked them more than klonopin.
 
I have never even heard of a bunch of those benzos. There truly are shit-ton of different ones.
 
I'm prescribed a lot of clobazam. I felt sleepy for a couple of weeks but once it had settled down, I found that it dealt with my myoclonic jerks FAR better than clonazepam. It's a 1,5-benzodiazepine so it binds at a different point at the GABA receptor. This means it won't stop abstinence-syndrome in people dependent on 1,4 benzodiazepines (I E-mailed Professor Ashton about that - even specialists were not aware). The docs swapped me over 2 weeks. I would say it has little-to-no abuse potential.

My friend overlayed clobazam with etifoxine in ChemBio3D (such cool software - with I had the £1000s to buy it!) after performing an MM2 energy-minimization and both benzene-rings overlap absolutely perfectly ad did the lone-pair of the 2-N.

'2-Cl clobazam is patented (US 3711509) as is '2-Cl etifoxine US 3725404 (thank you nameless friend at uni!) and guess what - the 2'Cls overlay as well. Pity they never seemed to try the 2'F or anything but -Cl at the 6/7 position.

I think the overwhelming research into benzos killed off further research into this interesting compound.

I promise - all of the technical stuff isn't me, it's a good friend who is in the middle of studying. He noted the precursor for etifoxine is the same one as for nordiazepam so please, don't think I'm pretending to know any chemistry.

Last little thing - does anyone know anything about chlormezanone? It's such an odd structure. Tocris says 'Anxiolytic and skeletal muscle relaxant that acts at the benzodiazepine site of GABAA receptors and Drugbank states 'Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.' It sounds like the (+) isomer is the more active and it's often grouped with carisoprodal & Chlorzoxazone.

Until the late 1980s, it was prescribed in the UK as an anxiolytic but the rare-but-fatal side-effect saw it's use end. It's still widely used in china.

It has that oh-so-common amide moiety and if you overlay the chlorophenyl groups, the amide of each match up well... so it almost looks like the top 1/2 of diazepam?

Sorry... uninformed wander.

Save time - ignore ;-)
 
bennyZA said:
Yea, like wtf is dikaliumchlorazepat
Click to expand...

The drug released after eating Tranxene (clorazepate), we have it in Canada, so you probably also have it in the US. Clorazepate is a prodrug. But yeah germans don't have some benzos we have here in .ca and they have additional ones. Most european countries have many other benzos. The netherlands especially has some I am absolutely obsessed with trying ;) Lormetazepam and loprazolam comes to mind.

and no I won't ignore it! that was a pretty interesting post clubcard.
 
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Thanks TRO - I AM trying to learn so please feel free to slam any rubbish I post; never attribute to malice that which can be explained by stupidity ;-)

I'm just getting into reading patents. It's so great having millions of hours of work summed up and available (mostly) for free. The problem with the etifoxine stuff is a lot is ZA (South African) patents and I cannot find where to get them free. I tried etifoxine over some 1,4-benzodiazipines and the (halo)benzenes don't come close so etifoxine is like 1,5 but not 1,4. I also found that adding the triazolo-ring (like in Xanax) has been added to the 1,5-scaffold US Patent 4133809 and the (halobenzene) overlays PERFECTLY. I added a '2-F and perfect.

I've sure enjoyed borrowing his laptop for an afternoon!

For the proper chemists, I overlayed:

IUPAC 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-benzo[1,2,4]triazolo[4,3-d][1,4]diazepin-5(6H)-one
SMILES ClC1=CC(N(C(C2)=O)C3=CC=CC=C3F)=C(C=C1)N4C2=NN=C4C

with

IUPAC (S)-6-chloro-N-ethyl-4-(2-fluorophenyl)-4-methyl-4H-benzo[d][1,3]oxazin-2-amine
SMILES ClC1=CC=C2N=C(O[C@](C2=C1)(C)C3=CC=CC=C3F)NCC

nfprfm.jpg


2ugmmpz.jpg
 
Interesting that the N of the ethylamine in (f)etifoxine overlays (almost) one of the nitrogens of the triazolo.

Obviously, no synthetic details but I was interested that the same kind of benzophenone will serve as the starting point of both of these. As I said, the etifoxine patent mentions the 2-Cl but no details of activity. A BIG ***IF*** the potency increases like the benzophenones, fetifoxine (hey - I had to use some name) might be x20 etifoxine which is usually 50mg (2 isomers, only 1 active) then 2.5mg would be about right.

I was given the Klosa paper (Synthese von 2,3=substituierten Chinazolon-(4)-derivaten mit Hilfe von Phosphoroxychlorid) on methaqualone analogues and WOW did they ever make a lot. The o-Me can be swapped for all manner of things in the ortho,meta and para positions.

Nitromethaqualone (2-methyl-3-(2-methoxy-4-nitrophenyl)-4(3H)-quinazolinone) failed the Ames test (US 3162634) but the (2-nitro-4-methyl) was stronger (x5 rather than x4 parent). I am guessing the -OCH3 was to give a good point to metabolise the drug reducing duration which is why it was chosen? The 2-nitro-4-methoxy is just as potent but maybe that metabolised TOO fast? Whatever the case, I think the ever increasing number of benzos (much safer in OD and 'non-addictive) meant that people gave up rather than ran out of ideas. If the 2-acetamidobenzoic acid is swapped for 2-(2-fluoroacetamido)benzoic acid, all of the products are roughly x2 the potency. Replacing the o-Me with an o-TFM has a similar impact. I think the cost of trialling another version after the nitromethaqualone disaster (they didn't do Ames, so only much later in the development was the toxicity noted) along with the benzo takeover ended the life of this class.

I am GUTTED. Many years ago (late 1970s), I was offered a 'Mandy' (UK version called Mandrax) and I said no because at that point, I had only ever had hash and, frankly, I was afraid of the stuff... what a fool!

Anybody else got any thoughts about 2-methyl-3-(4-methyl-2-nitrophenyl)quinazolin-4(3H)-one - the x5 lude?

2zp32oj.jpg
 
THE_REAL_OBLIVION said:
The drug released after eating Tranxene (clorazepate), we have it in Canada, so you probably also have it in the US. Clorazepate is a prodrug. But yeah germans don't have some benzos we have here in .ca and they have additional ones. Most european countries have many other benzos. The netherlands especially has some I am absolutely obsessed with trying ;) Lormetazepam and loprazolam comes to mind.

and no I won't ignore it! that was a pretty interesting post clubcard.
Click to expand...
Yeah The Netherlands is great. I've tried Lormetazepam which is nice.

EDIT: There's some heavy shit going down on this thread that is going over my head. =D
 
pally pete said:
YouKnowsIt.

The Netherlands is as close to faultless as can be ;)
Click to expand...

Also some VERY cool people.

Brood (national junkie) - dead but dies with style, ring him to ask his friend which was the most fashionable hotel to defenestrate (Was it Deelder?)
Jules Deelder - Dutch John Cooper Clarke (just replace rock & roll for jazz) - nuff said
Frøland - One of the worlds best comedy/horror series missed by most Dutch people. Ruben van der Meer & Horace Cohen would be FAMOUS if more people bothered to learn Dutch or just read subtitles.
vlaamse frites - Best fries (chips) in the world.
FEBO - a government instrument to test how drunk their citizens are - if a FEBO makes you want to eat... your drunk!
Attitude to weed - it isn't actually legal, but 'allowed'.
Most relaxed police in the world - they see 'looking after people' as their job. BTW, 'looking after' doesn't translate to the US 'take care of'.

Just learn the language and your OK with them...
 
clubcard said:
Interesting that the N of the ethylamine in (f)etifoxine overlays (almost) one of the nitrogens of the triazolo.

Obviously, no synthetic details but I was interested that the same kind of benzophenone will serve as the starting point of both of these. As I said, the etifoxine patent mentions the 2-Cl but no details of activity. A BIG ***IF*** the potency increases like the benzophenones, fetifoxine (hey - I had to use some name) might be x20 etifoxine which is usually 50mg (2 isomers, only 1 active) then 2.5mg would be about right.

I was given the Klosa paper (Synthese von 2,3=substituierten Chinazolon-(4)-derivaten mit Hilfe von Phosphoroxychlorid) on methaqualone analogues and WOW did they ever make a lot. The o-Me can be swapped for all manner of things in the ortho,meta and para positions.

Nitromethaqualone (2-methyl-3-(2-methoxy-4-nitrophenyl)-4(3H)-quinazolinone) failed the Ames test (US 3162634) but the (2-nitro-4-methyl) was stronger (x5 rather than x4 parent). I am guessing the -OCH3 was to give a good point to metabolise the drug reducing duration which is why it was chosen? The 2-nitro-4-methoxy is just as potent but maybe that metabolised TOO fast? Whatever the case, I think the ever increasing number of benzos (much safer in OD and 'non-addictive) meant that people gave up rather than ran out of ideas. If the 2-acetamidobenzoic acid is swapped for 2-(2-fluoroacetamido)benzoic acid, all of the products are roughly x2 the potency. Replacing the o-Me with an o-TFM has a similar impact. I think the cost of trialling another version after the nitromethaqualone disaster (they didn't do Ames, so only much later in the development was the toxicity noted) along with the benzo takeover ended the life of this class.

I am GUTTED. Many years ago (late 1970s), I was offered a 'Mandy' (UK version called Mandrax) and I said no because at that point, I had only ever had hash and, frankly, I was afraid of the stuff... what a fool!

Anybody else got any thoughts about 2-methyl-3-(4-methyl-2-nitrophenyl)quinazolin-4(3H)-one - the x5 lude?

2zp32oj.jpg
Click to expand...

I don't know about these ludes analogs clubcard, except etaqualone, oh how I love it, and I understand the appeal of the Ludes now and their legendary status. They're like benzos and barbs together with much less danger of choking to death compared to barbs (except the weak ones). It is available out there is all I can say.

eeeee
clubcard said:
Also some VERY cool people.

Brood (national junkie) - dead but dies with style, ring him to ask his friend which was the most fashionable hotel to defenestrate (Was it Deelder?)
Jules Deelder - Dutch John Cooper Clarke (just replace rock & roll for jazz) - nuff said
Frøland - One of the worlds best comedy/horror series missed by most Dutch people. Ruben van der Meer & Horace Cohen would be FAMOUS if more people bothered to learn Dutch or just read subtitles.
vlaamse frites - Best fries (chips) in the world.
FEBO - a government instrument to test how drunk their citizens are - if a FEBO makes you want to eat... your drunk!
Attitude to weed - it isn't actually legal, but 'allowed'.
Most relaxed police in the world - they see 'looking after people' as their job. BTW, 'looking after' doesn't translate to the US 'take care of'.

Just learn the language and your OK with them...
Click to expand...

They can also test their LSD blotter/dots/liquid and "x pills" for a small fee and a small wait in many labs in Amsterdam to verify for impurities/looking if you were screwed with bad stuff. I wish I had access to that a decade ago when DOB blotters (which i had no experience with) were sold as just "buvard (blotter)" (im french canadian or even better Québécois if you didn't know, I'm just much more bilingual than most out there ;) ). It was hell, I took 5 hits, had massive experience with LSD, not with DOB. Something like they have would have spared me 6 years of (intense) benzo use, still need clonazepam for neurological reasons. I know it was DOB due to the fact there was not any other DOx in circulation yet in 2000 and there was a bust that identified "x ridiculous amount of "fake lsd blotter" in the news not that long after.
 
Last edited:
clubcard said:
The Netherlands is gezellig... the WHOLE country!
Click to expand...
It is but dr's opinion on drugs is totally crooked. Old thread but this has to be cleared up.

When in pain, parecetamol not opiod's.

When in panic, epileptic or sleep deprived. No benzodiazepinen are prescribed, not even Clobazam. If so you pay for it your self. about 1.5 euro a tab. about 10 times more expensive as RC's.

Medicin suck's in general as most dr's have no clue about medicinn let alone. But confronted with overlaps between physical mental they are clueless.
 
clubcard said:
Last little thing - does anyone know anything about chlormezanone? It's such an odd structure. Tocris says 'Anxiolytic and skeletal muscle relaxant that acts at the benzodiazepine site of GABAA receptors and Drugbank states 'Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.' It sounds like the (+) isomer is the more active and it's often grouped with carisoprodal & Chlorzoxazone.

Until the late 1980s, it was prescribed in the UK as an anxiolytic but the rare-but-fatal side-effect saw it's use end. It's still widely used in china.

It has that oh-so-common amide moiety and if you overlay the chlorophenyl groups, the amide of each match up well... so it almost looks like the top 1/2 of diazepam?

Sorry... uninformed wander.

Save time - ignore ;-)
Click to expand...
Bringing back the dead or living , i don't know.

But as your post indicates CloMezanon or Chloor. Was till 1998 prescribed in Nl. as a muscle relaxant, so that makes sense grouping it with Carisoprodol.

But like Meprobamaat, Dextromoramide and Clomethiazole. Its since been removed from the dr's drug bible. My edition is fro 98 but online the recent one, the 2021 edition, can be found its called 'FarmacotherapeutischKompas'
 
Wow! I can recall originally posting this thread 8 years ago - the one and only time I ever had Clobazam - which sledgehammered my anxiety at the time.

I have no knowledge when it comes to their health system: unlike emkee_reinvented... But it has jogged my memory of the benzos I used to get sent to me from a crooked Dutch pharmacist at that time.

Lormetazepam
Flunitrazepam
Midazolam
Temazepam eggs
Flurazepam
Estazolam
Bromazepam
Oxazepam

Which were all quite unusual/rare here in the UK. My favourites being Lormetazepam, Flunitrazepam (they were generic 2 mg tabs, not the Roche branded Rohypnol), Flurazepam (super long lasting) and Estazolam (which was great for sleep) He also had your common ones like Alprazolam 1 mg Purple Rugby Balls, 10 mg Diazepam, 2 mg Clonazepam (Rivotril over here in Europe) and Oxy OC 40's that were super cheap... Though I can't mention the prices on here.

Sorry about all the reminiscing, but it was a good time for me to be a benzo head. Even though in truth it's never really good to be a benzo head, as there is always payback waiting further down the road.
 
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