• N&PD Moderators: Skorpio | thegreenhand

Long acting benzodiazepines (not 'half life'), suitable for tapering

On paper, it'd work good, but practically, dosing it is tough without a milligram scale.
 
Hmm, it does have the advantage of being relatively easily available considering legal status, not too weirdly designed or novel either, and potency/dosing challenges could easily be solved by volumetric measurement with ethanol/vodka/pg? by those willing (or 'musting' in case of tapers..).
It is also one of the least recreational ones I've ever tried, but before choosing phenazepam someone tapering should be convinced in their intentions, or denial of the IMO boring effects and highdose abuse relapse could easily cause amnestic blackouts with this one - the other side of its track record.

I am hard pressed to think of potential candidates with longer action.. but I guess options for someone depend on whether they find scheduled meds easier to acquire or research chemicals [online], and also if volumetric measurement is more of an abuse or accident liability than pills for some reason.
 
Two things, first:

Am I correct to assume that diazepam is a first order kinetics drug ?
 
If I were to take it I'd have to do more research, but is 1 mg of phenazepam approximately equal to 0.5 mg clonazepam ? (source: https://psychonautwiki.org/wiki/Benzodiazepine)

Maybe this is a useful reference: http://www.who.int/medicines/access/controlled-substances/5.8_Phenazepam_PreRev.pdf
Does it accumulate in fat cells like diazepam, or is it more like clonazepam ?
The half life is indeed a bit long for a drug that is mostly unknown in Western medical practice. And I can't read Russian ...

How often would I need to dose ? I take clonazepam once a day ...
What's up with that weird bioavailability ... source: https://en.wikipedia.org/wiki/Phenazepam

To be honest, I'm not that eager when I read that stuff ... But I'll have to think about this.

Dosing is most likely not an issue. A solution or suspension should be easy to make.
 
Two things, first:

Am I correct to assume that diazepam is a first order kinetics drug ?

If what you said earlier about how it is eliminated, then no, it's definitely not. In reality no drug's elimination can be perfectly described by first-order kinetics, because biological systems are just way too complex to be described by such a simple concept, but in general there is sufficient overlap so it can be used.

As for your second question, it's hard to tell how a drug is eliminated strictly by looking at its structure for sure. If this behavior (like diazepam's) is a function of lipophilicity, then perhaps comparing log P values can be an indicator. I can't tell for sure, though; maybe somebody else can. But truth be told, in the end you'll have to just try and see if it works, that's the best way to figure it out.

If you have some questions that are perhaps answered in that paper, I understand Russian.
 
Diclazepam and active metabolites have longest T1/2 - can be detected for 24 days after single dose. Of course, the ADME cycle means that a BID reduction works (diazepam is often TID). Expect it to take a long time. 24->2mg/day took 16 months. At that level (same as 20mg diazepam/day), fess up to doctor because those RC guys don't sell low-dose formats. You need whites at the end.
 
What is the lowest dose of diclazepam that is commonly sold ? And it´s a lot like diazepam, with a similar type of accumulation or so it seems.

I can´t say that I feel any enthousiam for either diclazepam or phenazepam.

Too bad that clonazepam is such a harsh drug, with all sorts of mixed and bizarre properties. I think you can say that I´ve experienced some symptoms of both the cholinergic and anticholinergic toxidrome, not in full/blown of course.
 
[not all of this post is chemistry thinking out loud.. ;) ]

Can you give a bit more information about those 'bizarre properties' you experience? How long has your habit been, and at what dosage?

Also why don't diclazepam or phenazepam sound okay?

I am just interested, my intention wasn't to recommend something in the first place, but rather to suggest possibilities as answer to your question: what are long half-life benzo suitable for tapering.

Also I wasn't really right about phenazepam being a record holder, although it does give me an effect for 3 days (I have never really taken more than a 'standard' 1 mg dose, I have also never used it for tapering - just to zombie out for 3 days when I had e.g. a bad candyflip hangover). I tend to get it confused that phenazepam would be relatively unsubstituted, on account of the 'phen' in the name. Those unsubstituted stripped structures are probably not potent.

I think that phenazepam, diazepam and diclazepam are all relatively similar in that they are chloro and/or bromo substituted benzos on the 7 and '2 position. And yeah the N-methyl isn't always there, but that isn't really that interesting here. In terms of being unresearched, these would be the RC benzo's that I would personally worry about least. Cause the chemical differences are subtle, and completely different toxicology unexpected. That doesn't mean that effects are pretty much the same, there are certainly differences.

Diclazepam does have an even longer half-life, though I understand from people who have taken it that the effects aren't quite so balanced as with say diazepam which is a great all-rounder. I hear that for anxiety or sleep very different doses of diclazepam are needed for sufficient effect. That doesn't sound ideal to me. 1 mg seems to be the relatively lower dose sold.

Phenazepam shares with clonazepam's effects IMO that they are heavy on the anxiolysis and also on the potential for amnesia / vague blurry feelings and fucked up memory. While hearing that is not appealing at all, what *might* be smart is to taper with a benzo that has a relatively similar effects profile as that of the one you have been taking, and failing that, then just covering all fronts with an allrounder like diazepam. If you choose a very different benzo I think you risk a type of partial withdrawal or unsteadiness when switching.. What you need is no bumps in the road but a steady cross-over followed by steady decline.

There is also meclonazepam, which is structurally very close to clonazepam but I cannot really comment on whether that would be a wise move. I do have the stuff, I got a gram for dirt cheap.

Expect long acting benzo's like diclazepam, diazepam and phenazepam to bind a lot to your fat tissue yes - since there are less polar groups such as nitro or oxo. I've been through benzo taper and withdrawal and it took an agonizingly long time, but it's the only wise option nevertheless. That first stage was one of the harder but also important and strengthening things I did, the later chronic stage was just a bitch..

Fortunately I have it under control ever since, though there are periods with etizolam that i better cut out.

If you insist on not going the professional way, you might wanna see if someone can monitor or even administer the taper benzo you will choose?
 
And yeah the N-methyl isn't always there, but that isn't really that interesting here.

I was actually thinking about clonazepam and diazepam the other day in regard to what Kdem said about diazepam being stored in fat cells extensively while clonazepam not so much. If you compare the structures, then clonazepam only has an additional nitro group on the aromatics and doesn't have a methyl group on the amide nitrogen. That would probably go a long way in explaining why, because for one amide N-H is capable of producing a nice hydrogen bond, decreasing lipophilicity, plus that nitro group. Dunno, just something I noticed.
 
Solipsis,

'Can you give a bit more information about those 'bizarre properties' you experience? How long has your habit been, and at what dosage?'

I wouldn't call it a habit, but I have taken it for over five years on a daily frequency by now. Prescribed by former GP.
2 mg a day, single dose. I can't split the dose because of the 'issues'. Of which one example would be that splitting a dose would make the daytime dose more sedating, the evening dose more stimulating thus making it much harder to fall asleep, even when increasing the dose. Or shifting a dose to the daytime would make me feel 'messed up'. But it has been a very long time since I tried shifting doses. And this is just one reason why splitting doses is not an option, at best it would create problems as well as solve them.

'issues' In short: mixed properties. For example, stimulating and sedating. Either at the same time, or not.
For whatever reason, since some time ago it has caused hypercortisolism (not formally diagnosed), muscle wasting (pretty much goes with tapering). Temporary (?) hypothyroidism may also have played a role, as well as other hormones. (to be succinct: I am very displeased with the very minimal 'healthcare' I have received)
Back to the 'mixed' issues I guess: when I took clonazepam in the evening it seemed to affect my circadian rhythm. If I felt sleepy, that went away after taking the dose. I became a late sleeper. I sense that up to this day it still affects my circadian rhythm.

Years ago, it could cause 'mood' issues, from either flattening, to mood swings either way.
'mixed' or not: this drug is more sedating in the summer than in the winter. Wheather/season. (location: northern Europe) which causes its own set of issues.
Let's get the cholinergic and anticholinergic toxidrome as a comparison: https://en.wikipedia.org/wiki/Toxidrome#Anticholinergic
What I have experienced at times:
Cholinergic: confusion, emesis (as experiencing an urge to vomit, not actually vomiting), miosis, muscle fasciculations, increased production of saliva, seizures (?? something that felt like a 'partial absence seizure', no full loss of consciousness), increased urination/general loss of water weight, temporary hypothermia.
Anticholinergic: somewhat blurred vision, decreased bowel movement, mild delirium-type state at times ???, really poor memory, temporary urinary retention.
Cardiac arrythmia during a previous attempt to taper.
I'm not saying it's the full toxidrome, just that it seems to have mixed cholinergic/anticholinergic properties. And I know the powerful effects that antimuscarinic drugs can have on me ...
It is well known that clonazepam has important 'secondary' effects on serotonin and acetylcholine.
 
Solipsis,

diclazepam: 'What is the lowest dose of diclazepam that is commonly sold ? And it´s a lot like diazepam, with a similar type of accumulation or so it seems.' The accumulation, very long half life. Available doses ? But the 'duration of action' is about 12 hours ? If so, that's better than diazepam.
Phenazepam, powerful drug, very long half life, a lot is unknown. I would prefer not to work with a 'research chemical'.
RCs have the difficulty that getting help other 'medical' issues may be difficult ...

Honestly, I'm not that good with benzos in general. It seemed just a harmless muscle relaxant at the time ... It took a long time for real dependence to develop.
Infrequent use of hypnotic benzos, that went well.

I tried doing it the 'professional way', which was a disaster. A very long story, suffice it to say that choices were made that i wouldn't have made. Tapering by means of lorazepam ? That went fine till I developed tolerance to/dependence on its hypnotic, amnestic and sedative proerties in the second month ... I haven't regained the relative stability I had.
My GP can prescribe drugs that are not too 'exotic', but I have not been able to get help from really knowledgable professionals. There must be very few of them in this country. Nobody has any experience with clonazepam (except a few victims...), and a standard diazepam taper is four to 6 weeks.
Former GP: 'just stop taking it'. Current GP: he tried to get me off based on his experience with helping people get off antidepressants ! He had a schedule of five to 6 months, but it wasn't doable because I wasn't physically stable (medical issue that has since been resolved). He didn't know/understand the importance of being stable/in good health for tapering this drug.

I could force myself on diazepam, but it's a nasty drug and for me once the 'duration of action' is over, it is mostly over. And I'd be switching between two very different drugs. An option ...

I actually talked to an experienced addiction doc who apparently knew less than I did. He didn't return about ten scheduled calls, very unprofessional behavior. Ultimately, that's what led me to that lorazepam taper ... Partly idea of the GP. I tried two shrinks, both of them were not interested 'back to the GP'.

Clonazepam's molecule is the most powerful benzo in use in this country. It would be nice if I had something with a duration of action of at least 12 hours, and be non-accumulating like lorazepam.

Edit: there is Tranxene, basically desmethyldiazepam. I know of someone who got it in a detox in the USA and it really helped her.
But really, it is very hard to get information about this drug. I would have to ask for a prescription to even try it, and I'm not sure if it is strong enough to 'carry' the withdrawal from clonazepam.
Pro: less accumulation. Duration of action, unknown, 1-3 times a day ?

Note: disadvantage of diazepam and drugs that accumulate in a similar way: after the duration of action the drug hangs around, and does all sorts of things except having a desired effect. The accumulation of diazepam is massive, 5-8 times the daily dose, not even counting the desmethyldiazepam. 'if it doesn't help it won't hurt ?' I don't believe that.
 
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FYI diclazepam was DESIGNED to help people reduce. The shame is, only 1 & 2mg tablets exist. If you can find the pure powder, the Chinese method works. Don't think for a minute that designers didn't foresee this issue and address it. 1mg cut in 2 BID gets you down to 5mg diazepam BID. From there, a doctor will happily help (it's in the range that they are used to dealing with). It took 15 months to go from 24mg/day to 2mg/day BID. As for opiates, people selling U-47700 as powder are evil, put simply. Try getting someone to make an opiate detox drug. The answer to that one, BTW, is the reduced, acetylated version of R-4066.It last's a day and isn't toxic like ORLAAM.

Don't presume designers were purely into profit... or at least the chemists. Given a choice, Thienorphin turned up at the right moment but U-4700 powder = evil, profit-obsessed scum.
 
Maybe diclazepam is worth looking into.

Oficially not intended for human consumption and such, I suppose there is a risk.
 
Maybe diclazepam is worth looking into.

Oficially not intended for human consumption and such, I suppose there is a risk.

It's probably got very very similar properties to the well known diazepam; they are almost identical in structure.
 
Maybe diclazepam is worth looking into.

Oficially not intended for human consumption and such, I suppose there is a risk.

The "not for human consumption" disclaimer is for legal purposes to get around certain laws.
 
Well, I was more thinking along the lines of 'what is the purity like' and 'what if there are any pollutants' ? With short term recreational, low dose use your body can handle more than when taking something for months or so ...
I don't know how it's 'cooked' in a bathtub in 'China' or so. If you get my point.
 
The farmaceutical industry should design a benzodiazepine depot similar to antipsychotic depots:\
 
I'll throw in a question about bromazepam.
It's hard to get information about this drug. From my point of view, anyway.
How long does it last ? 'duration of action', not 'half life'. Suitable properties ? Recreation is not the issue.
 
Bromazepam is a relatively rare benzo in general. I'm guessing that someone along the line for some idiotic reason decided to demonise it as "highly abusable", pretty much ensuring it was boycotted by nearly everyone. Although in the interest of fairness, it does appear structurally to be very closely related to phenazepam, so it is plausible that there's a degree of truth about the claims regarding its abuse potential.

For me, it lasts significantly longer than Xanax, but much less than Valium; an approximate equivalent in terms of duration would be lorazepam (although bromaz lasts a little longer, or at least has more noticeable aftereffects). Xanax + bromaz actually used to be one of my favourite anxiolytic combos - the Xanax would kick in quickly, and by the time it started to wane the bromazepam would be reaching its peak; the combination of the two effectively acted as a medium-lasting anxiolytic but with a very short onset time.
 
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