Benzos Clorazepate - How efficient is it for those who used it for things like GAD

[THE_REAL_OBLIVION]

I'm curious about clorazepate (Tranxene). Just as I get interested in it though, my insurance does not pay for it as of october 14th. I'm on valium 10mg TID and bromazepam 6mg BID for GAD although I'm starting to dislike bromazepam, it's giving me headaches, which apparently is more common with that one than all other benzos, apparently the bromine in it does become loose after first-pass metabolism and accumulation is possible. It's the benzo prescribed the most in France and I read some medical papers from France speaking about how "Lexotan"...it's called Lectopam here, the brand name; can cause accumulation of bromine and that's kind of scary. I've been getting "typical" headaches a bunch lately and I never really get those, proof, I have a big bottle that originally had 120 Fiorinal with 30mg codeine here scripted to me along with a couple free packs of Relpax (some triptan) and since that stuff isn't efficient for nerve pain, only really good for bad tension headaches...right?

If I want to replace the bromazepam by something, I don't mind paying the pretty low price of a script of 60 15mg clorazepate pills, I don't need something like xanax or other very short lasting pills, I don't have panic attacks, I have GAD big time only. I'm looking at the generics of tranxene 15mg pills...brand name tranxene is entirely non-available, they got rid of many brand name benzos lately in the actual supply, one would have to have a pharmacy order it and such and maybe some additional fees, so whatever. With my tolerance I imagine the 3 and 7.5mg ones are useless, so would 30mg clorazepate a day replace 12mg bromazepam a day just fine? I'm having difficulty finding onset time and half-life....I lost a good pdf I found in 2008 or so that was a table for canadian nurses about every benzo available here and all of their characteristics, even saying on them that Nicotine and Caffeine lowered plasma levels with a downward arrow and things on alprazolam such as "Anti-depressaant effects?". Somebody with actual experience using clorazepate would be useful or anecdotal (believable) data would be welcome to reply.

Stay well.

 

[Lorne???]

Tranxene is simply nordazepam, the semi- active metabolite of Valium


Some people find it quite effective; I did not. It is an intermediate acting benzo with a weird duration, and fairly long t1/2 / 100 hrs


It's supposedly a partial agonist, basically, its a lot like a longer lasting Valium; it still doesn't really hold as long as clonazopam


Study valium and its metabolite
(Brand name benzos would be interesting) I THINK GAD may be an indication, net makes it hard to check / Luck and post Q's

 

[Hodor]

apparently the bromine in it does become loose after first-pass metabolism and accumulation is possible.

Actually producing enough bromide ions via the de-bromination of bromazepam to elicit any sort of pharmacological effect would be *extremely* unlikely. For one thing, there isn't a lot of bromine in bromazepam. Sure, that bromine atom makes up roughly 25% of its molecular mass, but at 12 mg of bromazepam that would be just 3 mg of bromine per day even if *all* of it got debrominated. Which it doesn't. In fact, due to the high stability of aryl bromides, very little to no bromide is liberated due to the metabolism of bromazepam (the major metabolites are 3-hydroxybromazepam and 2-(2-amino-5-bromobenzoyl)pyridine, both of which still have the bromine attached).

And even 3 mg of bromine wouldn't even do anything. The average adult US citizen takes in twice that much from their diet alone each day. People used to get drug-induced bromism way back when people ate several grams of bromoureides (or even straight-up potassium bromide) per day, but not so much today.

Tranxene is simply nordazepam, the semi- active metabolite of Valium

Tranxene is technically clorazepate (3-carboxy-nordazepam), a pro-drug for nordazepam, but yes, they seem to have very similar pharmacology.

 

[THE_REAL_OBLIVION]

Tranxene is simply nordazepam, the semi- active metabolite of Valium


Some people find it quite effective; I did not. It is an intermediate acting benzo with a weird duration, and fairly long t1/2 / 100 hrs


It's supposedly a partial agonist, basically, its a lot like a longer lasting Valium; it still doesn't really hold as long as clonazopam


Study valium and its metabolite
(Brand name benzos would be interesting) I THINK GAD may be an indication, net makes it hard to check / Luck and post Q's

I'm speaking of Clorazepate. Which is Tranxene in Canada...we don't have Nordazepam by itself here. I wouldn't want a weaker diazepam metabolite to complement it when I already take 30mg of diazepam a day. It's often called Clorazepate Dipotassium if I recall well.

 

[THE_REAL_OBLIVION]

Tranxene is technically clorazepate (3-carboxy-nordazepam), a pro-drug for nordazepam, but yes, they seem to have very similar pharmacology.

I'm surprised, I was expecting clorazepate to be more related to clonazepam.

Well I notice that Bromazepam tends to give me headaches, the type that advil will eliminate but I'm taking enough meds, I'm not throwing regular NSAID taking into that.

Hmm, I guess clonazepam is my best bet then, although I think I will have to pay for it, my insurance started to suck really bad this year, lots of stuff being removed from the covered list even if you for it and it's the government med insurance because I work by contract at home and my employer is foreign so I can't have their insurance one gets after 8 months working for them, over in Europe. I can't see other good for GAD benzos available in Canada though, the issue is that clonazepam is only paid for when used for neurological reasons as of this year, seizures, HPPD, migraines...if it's signed by a neurologist it's paid for. Although it's pretty cheap if I just get a couple 1mg a day, 60 1mg clonaz is real cheap.

 

[Hodor]

I'm surprised, I was expecting clorazepate to be more related to clonazepam.

Most benzos (including clorazepate) have a chlorine substituent in the 7-position, to the point where they often didn't even bother including the "clo-" prefix in their names because it was pretty much redundant (ex.: diazepam, temazepam, alprazolam, oxazepam, triazolam, prazepam, midazolam, flurazepam...).

"Clonazepam", on the other hand, has the chlorine substituent in the 2'-position, and a nitro group in the 7-position. So yeah, completely different animal.

Clorazepate should be just about functionally identical to nordazepam, maybe somewhat weaker and slower to take effect. Since the rate of conversion depends on your stomach's pH, its effects may be delayed and/or diminished if you're taking antacids.

Edit: Clorazepate being sold as the dipotassium salt, 15mg of clorazepate should be equivalent to 10mg of nordazepam, assuming a near-total metabolic conversion.

 

[Hodor]

a couple free packs of Relpax (some triptan) and since that stuff isn't efficient for nerve pain, only really good for bad tension headaches...right?

Triptans are mostly for migraines and cluster headaches, not sure they even work for tension headaches at all.

Triptans are structurally derived from psychedelic tryptamines which activate various serotonin receptors, thus causing cool hallucinations, as well as a constriction of blood vessels. Triptans have been structurally modified so as to get rid of their hallucinogenic qualities, but retain their vasoconstrictive effects.
They will thus rapidly stop engorged blood vessels from pressing on nerves and causing pain.

If I want to replace the bromazepam by something, I don't mind paying the pretty low price of a script of 60 15mg clorazepate pills, I don't need something like xanax or other very short lasting pills, I don't have panic attacks, I have GAD big time only. I'm looking at the generics of tranxene 15mg pills...brand name tranxene is entirely non-available, they got rid of many brand name benzos lately in the actual supply, one would have to have a pharmacy order it and such and maybe some additional fees, so whatever.

Ah least here in Europe, even name-brand benzos are cheap as hell at this point... not that it even matters whether you get generic or name-brand anyway, though, IME.

and things on alprazolam such as "Anti-depressaant effects?".

Alprazolam's "anti-depressant effects" have been seriously called into question in recent years (same with clonazepam). Chronic anxiety or repeated panic attacks are liable to make anyone depressed, so it is pretty obvious that any sort of effective anxiety relief (which alprazolam and clonazepam undoubtedly provide, at least in the short term) could be construed as having an "anti-depressant" effect on mood.

 

[Lorne???]

It IS dm-dzp; it is almost immediately and fully converted im the stomach to Nordazepam

Would likely recommendation something else

 

[Hodor]

It IS dm-dzp; it is almost immediately and fully converted im the stomach to Nordazepam

I will agree that the ~10 minutes it takes for clorazepate to be converted into nordazepam usually don't really matter all that much, especially since clorazepate isn't really intended to be used as a fast-acting benzo for panic attacks.
Still, you do have to account for the difference in molar mass when considering dosages: You need 15 mg of clorazepate dipotassium to form 10 mg of nordazepam.

Would likely recommendation something else

I concur, it would certainly be far from an ideal replacement for bromazepam.

 

[Lorne???]

Yeah, nordazepam is a bit more potent likely, although it's equivalent dosage is listed 10-20mg , Tranzene (sic) is almost always given SDU of 15, and nordazepam is a partial benzo "agonist ", and is less potent than its parent drug(surely?)

 

[THE_REAL_OBLIVION]

Thanks for the good info guys. I forgot to mention that doctors will script clonazepam for anxiety despite many insurances starting to cover it only for seizures and HPPD these days, I have to go with the gov med insurance and the list of covered generics or reasons they will cover it for are changing, although my doc could change the bromazepam for clonazepam "off-label" and there would be no issue and they would pay for it. As for brand name...when I first started a long term script for benzos it was clonazepam, cured me of HPPD caused by a bad, awful surprise DOB blotter (I've spoken about this before, it didn't burn me out, but it made me feel strange for a year afterwards then my continued LSD consumption, every couple months even after that surprise mindfuck...I know it was DOB since the Hell's were having some guy cook it because they no longer were able to procure real L in the quantity they wanted or something like that, media reports and an actual lab seizure and they were gone in my area of Canada, back in late 2000/early 2001).

The clonazepam cured the HPPD and it was 2 Rivotril brand-name 0.5mg a day. They don't have brand name 1mg ones, only 0.5 and 2mg, but I felt a difference when the pharmacy was out and they were giving me 2mg rivos and cutting them in half). Also felt a major difference when given 1mg Xanax brand instead of the pms-alprazolam 1mg. Could be placebo...i can't say I felt a difference with brand name 5mg valium, which does not look cool like american brand name valium nor the roche Rivotril, it's not Klonopins, I guess a carved R would be had to make. They're just yellow pills. Only used them when tapering from 4mg clonazepam a day down to 25mg valium a day when I started to feel like clonazepam's strong effects on the temporal lobes, due to its very strong anti-seizure even mood stabilizing effects at that dose, I would see awful things on the news and feel numb to it, I would watch the Habs taking out the Washington Capitals and Pittsburgh Penguins and have almost no emotion and that was some amazing playoffs, losing 3-1 on a 4 out of 7 twice in a row to teams much stronger than them, at least on paper.

Anecdotes, aside, I remember feeling better when I was on 20mg valium a day and 1.5mg clonazepam with it as opposed to my current 30mg (10mg TID) valium and (6mg bromazepam BID). At first I really liked bromazepam, it's as strong an anxiolytic as alprazolam not by potency (it takes 12mg to equal 2mg xanax) but lasts way longer, about 8 hours. It's too bad it's not allowed in the US, I'm only jealous of your Estazolam, we don't have it here and I wonder how good it would be for sleep, I get 30x30mg temazepam a month which I don't take everyday, I alternate with hydroxyzine 50mg for 4-5 days because tolerance to temazepam increases very quickly, I manage to have great sleep when I take it for 4-5 days in a row then give it a pause, sometimes I won't even need anything for insomnia which is good, I have a much lower tolerance still than when I was on 4mg clonazepam a day hence why I tried something else for a couple years now. I need the combined effect with diazepam so I don't get let-down by the half-lives of other substances. Maybe I could ask for 25mg Libriums, I remember liking these a lot, although, taking a 2-3 of these would put me to sleep real bad of course it would be chlordiazepoxide, brand name Librium being also no longer paid for. I know clonazepam's half-life can in theory be very long lasting, up to 105 hours, but the range is 25-105 or such and I definitely metabolize it really quickly, explaining why I needed 4mg to feel zero background anxiety, but that also meant basically being an automaton... there was no pain thus no joy, I've come to terms with issues that caused me to suffer from GAD, but some of them would demand speaking with a very stubborn person who's getting pretty old and is starting to have memory issues (not that she ever had great memory, thankfully it is the complete opposite for me, didn't get that from the gene mix).

I need some people to admit some bad things, they were good parents, I'm not another beaten and raped person, a little of the former, but that was very minor and not from that person. But imagine your mother because you come back from kindergarten with some "behaviour card" where the teacher says I did such and so pretty often 'cuz well I was a little kid full of energy who didn't take insults from other kids, and your mother due to her own issues (she was an orphan by 18 y/o), packing my clothes in those old brown grocery bags and using psychological violence all the time, and going mad one day, doing what i said and saying she is kicking me out, leaving me in the hallway of our apartment with my winter clothes on and seeing her empty angrily my drawers, putting all the stuff in those grocery bags and locking me out. That came to my mind one day and I was literally...what the hell, yeah she did that. That explains a lot of further stuff...as I got calmer due to being put in a hockey and baseball league playing sports all year long, by the third grade the ADHD was pretty much gone, still have remnants of ADDI but it's mild enough for me not to go back on Dexedrine.

It's funny because they love to pay for all forms of alpraz, lorazepam, oxazepam (lol) and diazepam (which is okay), but they are thinning the choices we have and Lyrica is great for GAD but unlike in Europe it is not approved for that here, which blows. But I manage, not even buying RC benzos since many years.