Benzos Diazepam failing to substitute for zopiclone

[Troppo]

Now that I've quit alcohol and scopolamine, it is time for me to tackle my sedative use. I began using low doses of carisoprodol to cope with the anxiety alcohol use was causing me, although I didn't realise at the time that the anxiety was being stirred up by the alcohol. I have generalized anxiety disorder and so thought the increased anxiety was just due to this. I found a way of finding the equivalent diazepam dose to carisoprodol (an equivalence factor for carisoprodol's active metabolite meprobamate) and it turned out that one 350 mg carisoprodol tablet is equivalent to around 8-10 mg of diazepam. I was using an average of a half to three quarters of a tablet, hence = 4-6 mg diazepam. Carisoprodol was starting to give me serious headaches, so I swapped it for an equivalent amount of zopiclone (7.5 mg of that equals 5 mg of diazepam, so I started with around 7.5 mg). I have since reduced to 4.2 mg, = 2.8 mg diazepam. I asked my psychiatrist if I could take diazepam to get off the zopiclone, and he first prescribed 3 mg of it, which we both thought was enough, but it only allowed me to halve my zopiclone use for the first two days, then on the third day I had to use a much larger amount due to withdrawals. I went back to the doctor and he prescribed 10 mg of diazepam, reducing by 1 mg each week, but even this dose has not fully substituted for the zopiclone. I just cannot understand it, especially as I am not using any other GABAergic sedatives. I have gone back to zopiclone and am dividing it into several mini-doses during the day by dissolving the tablets in water and then measuring out portions. This is not easy but I don't know what else to do, as quitting suddenly produces awful withdrawals. Does anyone have any idea why 10 mg of diazepam failed to take the place of 4.2 mg of zopiclone??

 

[paranoid android]

Now that I've quit alcohol and scopolamine, it is time for me to tackle my sedative use. I began using low doses of carisoprodol to cope with the anxiety alcohol use was causing me, although I didn't realise at the time that the anxiety was being stirred up by the alcohol. I have generalized anxiety disorder and so thought the increased anxiety was just due to this. I found a way of finding the equivalent diazepam dose to carisoprodol (an equivalence factor for carisoprodol's active metabolite meprobamate) and it turned out that one 350 mg carisoprodol tablet is equivalent to around 8-10 mg of diazepam. I was using an average of a half to three quarters of a tablet, hence = 4-6 mg diazepam. Carisoprodol was starting to give me serious headaches, so I swapped it for an equivalent amount of zopiclone (7.5 mg of that equals 5 mg of diazepam, so I started with around 7.5 mg). I have since reduced to 4.2 mg, = 2.8 mg diazepam. I asked my psychiatrist if I could take diazepam to get off the zopiclone, and he first prescribed 3 mg of it, which we both thought was enough, but it only allowed me to halve my zopiclone use for the first two days, then on the third day I had to use a much larger amount due to withdrawals. I went back to the doctor and he prescribed 10 mg of diazepam, reducing by 1 mg each week, but even this dose has not fully substituted for the zopiclone. I just cannot understand it, especially as I am not using any other GABAergic sedatives. I have gone back to zopiclone and am dividing it into several mini-doses during the day by dissolving the tablets in water and then measuring out portions. This is not easy but I don't know what else to do, as quitting suddenly produces awful withdrawals. Does anyone have any idea why 10 mg of diazepam failed to take the place of 4.2 mg of zopiclone??

Zopiclone is a z drug so i guess Valium may not fully substitute for it. I take zopiclone for sleep but not daily. But by conversion charts 10mg of valium should sub for 7.5mg zopiclone i think no problem i think.

 

[Ozymandeus]

I'm sure both drugs hit wildly different arrays of GABA subunits, but why that might necessarily cause any difficulties I can't explain. I've always wondered why a direct GABA agonist like muscimol produces an effect very similar to high doses of zolpidem.

15 mg of muscimol produces an effect not to dissimilar from 15-20mg of zolpidem, yet they have two distinct ways of hitting the GABA receptor.

 

[paranoid android]

I'm sure both drugs hit wildly different arrays of GABA subunits, but why that might necessarily cause any difficulties I can't explain. I've always wondered why a direct GABA agonist like muscimol produces an effect very similar to high doses of zolpidem.

15 mg of muscimol produces an effect not to dissimilar from 15-20mg of zolpidem, yet they have two distinct ways of hitting the GABA receptor.

I reallly wanna try amanitas. They used to grow here years ago but people always regarded them as poisonous. Now i think the fall is to warm for them to grow

 

[Ozymandeus]

I reallly wanna try amanitas. They used to grow here years ago but people always regarded them as poisonous. Now i think the fall is to warm for them to grow

Do isolated or extracts. Refer to the other active thread about amanita I just posted in

 

[agoraphobe]

Now that I've quit alcohol and scopolamine, it is time for me to tackle my sedative use. I began using low doses of carisoprodol to cope with the anxiety alcohol use was causing me, although I didn't realise at the time that the anxiety was being stirred up by the alcohol. I have generalized anxiety disorder and so thought the increased anxiety was just due to this. I found a way of finding the equivalent diazepam dose to carisoprodol (an equivalence factor for carisoprodol's active metabolite meprobamate) and it turned out that one 350 mg carisoprodol tablet is equivalent to around 8-10 mg of diazepam. I was using an average of a half to three quarters of a tablet, hence = 4-6 mg diazepam. Carisoprodol was starting to give me serious headaches, so I swapped it for an equivalent amount of zopiclone (7.5 mg of that equals 5 mg of diazepam, so I started with around 7.5 mg). I have since reduced to 4.2 mg, = 2.8 mg diazepam. I asked my psychiatrist if I could take diazepam to get off the zopiclone, and he first prescribed 3 mg of it, which we both thought was enough, but it only allowed me to halve my zopiclone use for the first two days, then on the third day I had to use a much larger amount due to withdrawals. I went back to the doctor and he prescribed 10 mg of diazepam, reducing by 1 mg each week, but even this dose has not fully substituted for the zopiclone. I just cannot understand it, especially as I am not using any other GABAergic sedatives. I have gone back to zopiclone and am dividing it into several mini-doses during the day by dissolving the tablets in water and then measuring out portions. This is not easy but I don't know what else to do, as quitting suddenly produces awful withdrawals. Does anyone have any idea why 10 mg of diazepam failed to take the place of 4.2 mg of zopiclone??

My opinion is this. You've made great progress by ridding yourself of the alcohol and scopolamine.

Don't feel pressured to remove something that could be helping you, faster than you need too. There is no shame holding where you are for a bit to stabilize and then tackle the valium.

 

[4DQSAR]

In sufficient doses diazepam will fully substitute for zopiclone.

The HUGE difference is zopiclonse has a very short half-life so 7.5mg is actually a large dose.

The other important difference is that zopiclone is a1 selective so if nothing else a nitrobenzodiazepine would substitute far better (as they also have a lot of a1 affinity).

But 3mg is a joke. 5mg of nitrazepam at night, maybe, but almost no benzodiazepine is a1 selective so in fact unless you restrict use to a week or two - you end up with a WORSE dependence.

Sounds like your clinician is a fuckwit.

 

[shreddedlettuce]

Sounds like your clinician is a fuckwit.

I think we are missing the main question that hasn't been answered and if @Troppo can answer this one question we can assist more accurately.

Does your prescribing doctor know you are taking zopiclone during the day?

let's take it from there, I have experience with Meprobamate and Zopiclone (basically what I use for purpose for what my needs/requirements are). Zopiclone nightly and when needed Meprobamate for purpose.

Please let us know the answer to the Zopiclone during the day being known by the prescriber.

Stay safe and I am confident we can help with our experiences and safety. But most importantly, what actually works and with little effort compared to what you are saying in your desperate attempt to move forward.

PS wanted to add that you have done the hard work already, and there is a way to use those exact meds to get to the end goal effectively and as stress free as possible.

 

[jose ribas da silva]

Zopiclone is a z drug, valium a benzo, there is no substitution here

 

[Ki3ly]

That's what I need. A ' v.'

 

[Troppo]

Zopiclone is a z drug, valium a benzo, there is no substitution here

That's a good point. Even my specialist pointed this out to me. Benzo equivalent charts say that 7.5 mg zopiclone is equivalent to 5 mg diazepam but I now no longer believe that.

 

[Troppo]

Zopiclone is a z drug so i guess Valium may not fully substitute for it. I take zopiclone for sleep but not daily. But by conversion charts 10mg of valium should sub for 7.5mg zopiclone i think no problem i think.

Thanks, that's in line with what others have said.

 

[Troppo]

I'm sure both drugs hit wildly different arrays of GABA subunits, but why that might necessarily cause any difficulties I can't explain. I've always wondered why a direct GABA agonist like muscimol produces an effect very similar to high doses of zolpidem.

15 mg of muscimol produces an effect not to dissimilar from 15-20mg of zolpidem, yet they have two distinct ways of hitting the GABA receptor.

Yes I now realise this difference. I don't know why benzo equivalence charts compare zopiclone with diazepam.

 

[Troppo]

In sufficient doses diazepam will fully substitute for zopiclone.

The HUGE difference is zopiclonse has a very short half-life so 7.5mg is actually a large dose.

The other important difference is that zopiclone is a1 selective so if nothing else a nitrobenzodiazepine would substitute far better (as they also have a lot of a1 affinity).

But 3mg is a joke. 5mg of nitrazepam at night, maybe, but almost no benzodiazepine is a1 selective so in fact unless you restrict use to a week or two - you end up with a WORSE dependence.

Sounds like your clinician is a fuckwit.

Worse dependence is what happened to me. I'm now slowly weaning off zopiclone and have recently replaced it with the original carisoprodol, which I am finding much easier to taper off than zopiclone.

 

[Troppo]

I think we are missing the main question that hasn't been answered and if @Troppo can answer this one question we can assist more accurately.

Does your prescribing doctor know you are taking zopiclone during the day?

let's take it from there, I have experience with Meprobamate and Zopiclone (basically what I use for purpose for what my needs/requirements are). Zopiclone nightly and when needed Meprobamate for purpose.

Please let us know the answer to the Zopiclone during the day being known by the prescriber.

Stay safe and I am confident we can help with our experiences and safety. But most importantly, what actually works and with little effort compared to what you are saying in your desperate attempt to move forward.

PS wanted to add that you have done the hard work already, and there is a way to use those exact meds to get to the end goal effectively and as stress free as possible.

Yes my prescriber knows I have been taking smaller doses of zopiclone during the day, as a substitute for the original carisoprodol, which I nearly always used during the day. I started reducing the zopiclone with some help from the diazepam but was unable to just suddenly quit zopiclone and start diazepam. The withdrawals were way too intense, even with 10 mg diazepam. Now that I have reduced a lot, I have found that returning to the original carisoprodol is allowing me to further reduce much more easily that using zopiclone, which I have now quit. I am now down to about 40 mg carisoprodol, as opposed to a single 250 or 350 mg tablet.

 

[4DQSAR]

Sci-Hub. The mechanism of action of zopiclone / European Psychiatry, 1995

It's the usual thing, researchers had noted that it was the a1 sub-unit that produced the hypnotic activity of benzodiazepines and that nitrobenzodiazepines were more a1 biased. So they used radio-labelled flunitrazepam (Rohypnol™) to test the theory.

Now benzodiazepines are β2γ2 selective i.e. things like flunitrazepam can only act on the a1β2γ2 units.

So the developers were tasked with finding a class of ligand that could act on the a1 subunits of ALL of the a1 units.

Hence if you ignore the various 2D diagrams and begin from overlaying the amide moiety found in all benzodiazepines and all Z-drugs (carbamate esters being bioisosteres of amides) in a proper 3D modelling tool which first calculates the minimum-energy conformation of both, you see how they overlay.

L1 - aromatic anchor
H1 - hydrogen-bond acceptor
H2 - amide/carbamate ester (weak acceptor)
L2 - pendant aromatic

As I noted, the key thing is that they are actually quite potent, but that brief-duration of action means no hangover (but can result in rebound anxiety) and since a1 ligands are known to produce anteriorgrade and retrograde amnesia, cause loss of executive function and disregulation of dopamine, at once they represent in theory a better and less abusable hypnotic.

The odd thing is I have had clients who LOVED Z-drugs. Absolutely adored them. Like many hypnotics, abuse involves trying to stay awake and end up in an ASC where the user feels 'insulated' but that loss of executive function is why so many famous people have defended episodes of 'air rage' on the basis of 'automation' i.e. they didn't know what they were doing.

The above is why I suggested that a nitrobenzodiazepine such as clonazepam prescribed on a short (1-2 week) basis MAY be of benefit as specifically nitrobenzodiazepines will provide relief from AWS better than other benzodiazepines BUT be aware that while people have survived eating GRAMS of diazepam - nitrobenzodiazepines are far less forgiving. So I would suggest asking someone else to hold them as they can produce similar side-effects and the typical issue is someone taking their medication, forgetting they already took it and redosing.

As to the most appropriate dose, I'm not qualified to say but low-dose diazepam, the benzodiazepine famous for having the longest duration of action of all seems badly considered to me. That's why I guessed at simple nitrazepam. Yes, taken late at night it can produce a hangover but while personally I suspect clonazepam might be better, I have ZERO experience in this form of treatment so it IS purely my best guess.

 

[shreddedlettuce]

Yes my prescriber knows I have been taking smaller doses of zopiclone during the day, as a substitute for the original carisoprodol, which I nearly always used during the day. I started reducing the zopiclone with some help from the diazepam but was unable to just suddenly quit zopiclone and start diazepam. The withdrawals were way too intense, even with 10 mg diazepam. Now that I have reduced a lot, I have found that returning to the original carisoprodol is allowing me to further reduce much more easily that using zopiclone, which I have now quit. I am now down to about 40 mg carisoprodol, as opposed to a single 250 or 350 mg tablet.

If you can get by by using Meprobamate (the active drug created when taking carisoprodol) and no Zopiclone during the day, and find this is helping, then keep the diazepam for the days as a "backup" and the extra Zopiclone you have stopped using as a backup, for its hypnotic effect (what it actually is = a sleeping tablet) at night if sleeping is an issue. If not leave it.

Keep us up to date on any progress or lack thereof and we can address it then.

If the carisoprodol at that dosage is keeping the alcohol at bay ( so to speak ), and it is working for you, then all is good.

Good luck and hope you stay safe.

 

[Kurt Cobain]

Now that I've quit alcohol and scopolamine, it is time for me to tackle my sedative use. I began using low doses of carisoprodol to cope with the anxiety alcohol use was causing me, although I didn't realise at the time that the anxiety was being stirred up by the alcohol. I have generalized anxiety disorder and so thought the increased anxiety was just due to this. I found a way of finding the equivalent diazepam dose to carisoprodol (an equivalence factor for carisoprodol's active metabolite meprobamate) and it turned out that one 350 mg carisoprodol tablet is equivalent to around 8-10 mg of diazepam. I was using an average of a half to three quarters of a tablet, hence = 4-6 mg diazepam. Carisoprodol was starting to give me serious headaches, so I swapped it for an equivalent amount of zopiclone (7.5 mg of that equals 5 mg of diazepam, so I started with around 7.5 mg). I have since reduced to 4.2 mg, = 2.8 mg diazepam. I asked my psychiatrist if I could take diazepam to get off the zopiclone, and he first prescribed 3 mg of it, which we both thought was enough, but it only allowed me to halve my zopiclone use for the first two days, then on the third day I had to use a much larger amount due to withdrawals. I went back to the doctor and he prescribed 10 mg of diazepam, reducing by 1 mg each week, but even this dose has not fully substituted for the zopiclone. I just cannot understand it, especially as I am not using any other GABAergic sedatives. I have gone back to zopiclone and am dividing it into several mini-doses during the day by dissolving the tablets in water and then measuring out portions. This is not easy but I don't know what else to do, as quitting suddenly produces awful withdrawals. Does anyone have any idea why 10 mg of diazepam failed to take the place of 4.2 mg of zopiclone??

You can try to add kava to the mix?

 

[Kurt Cobain]

Now that I've quit alcohol and scopolamine, it is time for me to tackle my sedative use. I began using low doses of carisoprodol to cope with the anxiety alcohol use was causing me, although I didn't realise at the time that the anxiety was being stirred up by the alcohol. I have generalized anxiety disorder and so thought the increased anxiety was just due to this. I found a way of finding the equivalent diazepam dose to carisoprodol (an equivalence factor for carisoprodol's active metabolite meprobamate) and it turned out that one 350 mg carisoprodol tablet is equivalent to around 8-10 mg of diazepam. I was using an average of a half to three quarters of a tablet, hence = 4-6 mg diazepam. Carisoprodol was starting to give me serious headaches, so I swapped it for an equivalent amount of zopiclone (7.5 mg of that equals 5 mg of diazepam, so I started with around 7.5 mg). I have since reduced to 4.2 mg, = 2.8 mg diazepam. I asked my psychiatrist if I could take diazepam to get off the zopiclone, and he first prescribed 3 mg of it, which we both thought was enough, but it only allowed me to halve my zopiclone use for the first two days, then on the third day I had to use a much larger amount due to withdrawals. I went back to the doctor and he prescribed 10 mg of diazepam, reducing by 1 mg each week, but even this dose has not fully substituted for the zopiclone. I just cannot understand it, especially as I am not using any other GABAergic sedatives. I have gone back to zopiclone and am dividing it into several mini-doses during the day by dissolving the tablets in water and then measuring out portions. This is not easy but I don't know what else to do, as quitting suddenly produces awful withdrawals. Does anyone have any idea why 10 mg of diazepam failed to take the place of 4.2 mg of zopiclone??

You're older, been a addict for a long time so the kindling effect fried out all your gaba receptors i bet if you tried 15 20mg diazapam you'd be fine. Theyre slightly different drugs so they fail to mask entierly and being youve been around the block a long time thus becomes.much more apparent than someo.e jusy starting out. Imo instead of upping the valium and asking for more.troubles later try 5mg diazapam.with a tablespoon of instant micronized kava root its legal and cheap.online

 

[Kurt Cobain]

Worse dependence is what happened to me. I'm now slowly weaning off zopiclone and have recently replaced it with the original carisoprodol, which I am finding much easier to taper off than zopiclone.

Why doesnt your psych just give you baclofen if nothing else in conjunction?