Benzos Strongest muscle relaxant: Clonazepam vs Diazepam

[Wilson Wilson]

Yes. That was part of it. Were you also refering to the fact that Valium/diazepam hits "all those the receptors" also meaning that it, on paper, would be the better muscle relaxant?

Yes basically, but that's poor wording on my part. It'd probably be more accurate to say it's the wide range of metabolites and benzodiazepine effects caused by those metabolites that make it non-selective, and as a result it will have stronger affinity for sub-receptors that more potent but selective benzos either have less affinity for or don't touch at all. The end result of all that is the strong muscle relaxation among many other things. It's why Valium has pretty much all the benzo properties. Whereas clonazepam, say, is an effective potent benzo for treating seizures and anxiety but not nearly as effective as a hypnotic and for most people at least not as good as a muscle relaxant.

The more potent benzos are very good at targeting specific receptor sites to aim for certain therapeutic indications. Diazepam on the other hand just goes in there and does it all.

And indeed if you are used to using a more selective, although more potent, benzo then diazepam can still provide a strong effect on the receptors that benzo doesn't hit.

As far as muscle relaxation goes, I'm pretty sure temazepam is actually a metabolite of diazepam. Although how significant the levels are I can't be certain, but it'd absolutely explain the muscle relaxant properties it offers.

 

[Speed King]

Yes basically, but that's poor wording on my part. It'd probably be more accurate to say it's the wide range of metabolites and benzodiazepine effects caused by those metabolites that make it non-selective, and as a result it will have stronger affinity for sub-receptors that more potent but selective benzos either have less affinity for or don't touch at all. The end result of all that is the strong muscle relaxation among many other things. It's why Valium has pretty much all the benzo properties. Whereas clonazepam, say, is an effective potent benzo for treating seizures and anxiety but not nearly as effective as a hypnotic and for most people at least not as good as a muscle relaxant.

The more potent benzos are very good at targeting specific receptor sites to aim for certain therapeutic indications. Diazepam on the other hand just goes in there and does it all.

And indeed if you are used to using a more selective, although more potent, benzo then diazepam can still provide a strong effect on the receptors that benzo doesn't hit.

As far as muscle relaxation goes, I'm pretty sure temazepam is actually a metabolite of diazepam. Although how significant the levels are I can't be certain, but it'd absolutely explain the muscle relaxant properties it offers.

Wilson Wilson, you posted just great. If you look at the last few posts that we quoted in, you basically explained the reason Valium/diazepam is technically the superior muscle relaxant, assuming it was an average person taking taking the medication, preferably with a low to zero benzodiazepine tolerance.

Of course, your milage may vary.


Temazepam is a metabolite of Diazepam, btw.

 

[Lorne???]

^ Yes Speed King, (and mostly I?m reference to
the other poster) temazepam, is, completely and 100% irrelevant. MAYBE, if your taking large(or simply massive doses) in a daily (or almost daily) basis, then, high enough levels *might* build up enough. However, Temazepam, although obviously a powerful hypnotic and effective benzo (for some purposes, it?s impractical as an anticonvulsant or neurological disorders) fact is, it takes, 20-30 mg(range 15-40mg, depending on indication and individual response,(and with Valium, a single or occasional dose vs chronic dosing, even PRN) to = 5-10ng dzp. To at double or triple the potency, tenazepam simply isn?t an ?active? metabolite, under any normal circumstances; not enough is simply not produced rapidly enough - for it to have a therapeutic effect - it?s intermedia acting, however it and Oxazepam(*), which is even more mild, (at best the same as tenazepam) so at least 20mg, probably more like 30 40mg (although with a decent duration,) to yield ~10mg Valium, or SDU, So Again,a minor minor metabolite (pretty much, maybe again very ?rge doses?()

Checl the plasma Levels - just not enough, nearly, especially considering some (many) take(or are prescribed) a common dose of 10mg at a time, PRN or 3-4x (40-80 mg is pretty much MAX) So metabolites significantly less potent by weight just aren?t relevant

Nordazepam is a different story ; although not as significant as people seem to think, it takes ~15mg Nordazepam to equal~ 15mg dzp (SDU varies from 10-20mg, so 10-20 ng corresponds to 5-10mg of Valium, again Chronic (or frequent) is exposure effects this; it (Nordazepam) is also a partial agonist (nonetheless effect, for many purposes) and despite a T1/2 of over 100hrs roughly on average, it doesn?t last any longer than Closing Clonazepam, and is actually given 3-4x daily, although Chronic administration, for whatever reason seems like bid or ?tis should suffice, athough again, a partial agonist less potent as dzp itself, and again, produced in lesser amounts, isn?t at all the primary force beihind Valium administration, although it is the only important (relevent) or Active Metabolite, although if you take Nordazepam/Tranxene (Common Name for Clorazepate) it ?feels very much different, being more intermediate acting, although both(at least at low(er) tolerances seem to be fairly relaxing

However, Chronic administration of higher doses, Clonazepam would certainly be my bet - Thanks for Speed King, taking them at what seems to be fairly equivalent doses makes you/ your experience noteworthy (sorry for the belated response,?its been a tough, couple days; rough year, though tough couple days

 

[Lorne???]

Stress again, to Wilson W That Dzp doesn’t hit all thesubunits because it’s “metabolites” are, for all practical purposes, inactive.

Dzp itself has selectivity for A2, though not A3, if not mistaken

Acute administration, or at “Normal doses PRN, Dzp all the way

Truly, your mileage shall vary (Seriously, read about Tranxene (almost 100% converted in the stomach to Nordazepam and subsequently absorbed) and compare potentcies and plasma levels (solubility for that matter and protien binding) of the other metabolites; They may as well not be mentioned

 

[Wilson Wilson]

Again I don't mean for my words to be taken so literally. I am certainly no chemist or pharmacologist. All I mean to say is that diazepam does have a variety of metabolites which are active, and as a result diazepam is a less selective drug than most other benzodiazepines.

That's why I rescinded my bad wording where I talked about it "hitting all the receptors." That's obviously an oversimplification. But alas you get the idea.

 

[Doclad]

Personally, I find Diazepam much more myorelaxing than Clonazepam. Diazepam I notice it in the body at 20 minutes after putting it under my tongue, on the contrary, Clonazepam knocks me out in 1 hour but I do not feel the same "bodily pleasure" that Diazepam gives me.


DocLad

 

[Lorne???]

Except NONE of them are active except the partial agonist,nordazepam

Please don't take this as disrespect, my words are literal - Dzp is double-triple the potency of its metabolites, and they are only produced in minor amounts except nordazepam, and valium itself(Dzp) is 1.5x as potent

They are in effective completely inactive, except nordazepam, with chronic dosing or large doses - How it effects you, of course, varies

 

[Blind Melon]

To the OP: I just can't figure that out. I'm inclined to say Clonazepam but maybe that's just because it's effects are more pronounced at lower doses? I dunno... guess I'd say Clonazepam, with Diazepam causing the greatest euphoria when taken at higher doses.

I purposely left out Bromazepam, Flubromazepam and Diclazepam to simplify the question and because the OP didn't include them, but they are way up there with muscle relaxation to me, maybe Diclazepam for the win.

 

[Lorne???]

Quoting my friend so he is notified he has been quoted!


I have been taking 40 mg of Valium a day for ?. I saw my doctor and asked if I could give some receptors sub units a break and switch benzodiazepines.The doctor tried giving me 0.5mg Klonopin, but I managed to get 3mg of Klonopin perscribed.

Naturally I took some to compare the subjective effects and differences between the two medications.

I feel if one were not tolerant to either drug, Valium/diazepam would still be a better muscle relaxer.

Klonopin/clonazepam relaxes muscles also, until tolerance builds up. Don't get me wrong, it was a nice heavy duty benzodiazepine which I havn't had in quite a while. However, I remember switching to Valium, because the Klonopin wasn't working all that well. At that point, Valium kicked Klonopins ass in my head, due to tolerance. I gave it a long rest and the Klonopin feels stronger currently.

I think the Valium is weaker by weight, but produces more muscle relaxant qualities. This is all purely subjective. YMMV !!!

Back quote!

I think it's cool a doctor switched on the spot... If I mention subunit selectivity or try to tell them 1mg Clonazepam = 2-3mg Lorazepam, and that Lorazepam doesn't peak immediately because of solubility, and especially if I mention Clonazepam working for me (and some abstinence symptoms) because of modest a-serotonergic properties unique to it(among common benzodiazepines; I suspect clonazolam to have a very similar effect) , well the reactions are not very nice, if I get a reaction(sometimes an unpleasant stare, occasionally (rarely even) an acknowledgment that is positive, little else)

Benzodiazepine rotation is a good way to maintain effectiveness, though I'm starting to lean more toward Valium for muscle relaxation, although w/ a tolerant person, Clonazepam is simply the only choice I can imagine

Why they do not prescribe tetrazepam, or other benzodiazepines that would work specifically for the aforementioned purpose, kinda beyond me

Clonazepam is selective to A3(among others); need to find a good source on subunit selectivity

Edit:s A3 causes muscle relaxation, among other effects; dip may actually be selective for it, need a source though (anti-anxiety or anti-convulsive (both ???? )

 

[AlphaMethylPhenyl]

Benzodiazepine rotation is a good way to maintain effectiveness,

Timeless fallacy

Clonazepam is selective to A3(among others); need to find a good source on subunit selectivity

I can't make sense out of this. It's false...Klonopin is used for insomnia (a1), panic attacks (mostly a2), and basically any benzo indication.

 

[Speed King]

I simply take a break from a particular benzo for a bit. It does something that I can't pinpoint.

 

[Transcendence]

I'm off benzos now but was prescribed Clonazepam 2mg for ~3 years and then diazepam 30mg for another 3 years to treat generalized anxiety disorder. Diazepam seems to work better as a muscle relaxant.

Clonazepam has better muscle relaxant qualities than alprazolam or lorazepam as far as I can tell.

 

[Lorne???]

Timeless fallacy



I can't make sense out of this. It's false...Klonopin is used for insomnia (a1), panic attacks (mostly a2), and basically any benzo indication.

... I said selective, for A3, not exclusive; it is obviously selective to A2 as well, and has an absurd binding affinity

What I can?t make sense of, clonazepam is would be a terrible hypnotic, it?s long acting, with a gradual onset and delayed peak, and it?s rarely if ever used as a sedative/hypnotic(in countries am aware of)

The Z drugs are highly selective for A1, hence them being effective, (yet atypical Benzodiazepine type ) sedative/hypnotics, yet the negligible bzd effects otherwise at standard doses, and completely impractical as anti-convulsants

A3, apperaantly has anti-panic, muscle relaxation and anti-convulsant

And opioid rotation doesn?t make sense on paper, yet apparently works ....

OF COURSE, rotating to say, methadone, or even oxycodone, with its Kappa receptor possibly contributing, or just a higher binding affinity

Should have worded it differently, just liked what speedKing said and the idea

 

[Lorne???]

D^ I stick with one, (well one type) but read his post... Opioid rotation is questionable on paper, yet works seemingly

Clonazepam binding affinity is ABSURD; I mean comparable by weight, to buprenorphine - and, no, Clonazepam takes 2-3 hours to peak, and has long duration because of solubility (among others !) so no, insomnia is a horrible use, it's specifically known for being less hypnotic than other common benzodiazepines, including Valium, probably every Tribenzo, those and temazepam are good sedative/hypnotics, well, unless you wanna take rohypnol( a nitrobenzo, though the only, uh, hypnotic, if you wanna call it that

Dont take me as rude, just trying to correcting something (as you ) although poor wording, was really focusing on the idea of of what speedking said, and also, wishing could discuss things like that with medical professionals, freely

Opioid rotations may work, when switching to/or from specific opioids, with unique properties, which may have been better suited in the first place, or even if otherwise similar and at a roughly equipotent dose, the new medication may have a (sometimes much) higher binding affinity, or higher intrinsic activity, at Mu mostly, thought some think the kappa effects of oxycodone play a part in its effects, while methadone, well methadone just seems to rock as an analgesic and overall therapeutic opioid, though aside from being more potent at steady state, and the ability to (better) maintain effectiveness compared to other opioids, it's used for specific pain

I stick with chloro-nitro, some tri(nitro), benzos, though, for the most part. Wonder if the serotonin effects of Clonazepam have any other possible applications? That would be practical I mean? Some muscle relaxers have serotonergic properties, pretty sure it's the opposite though. Anyway, no, alprazolam or dzp would be more along the lines, if somehow a chart could be made, and it may be the only one that the Z drugs have any (significant) affinity for, though of course they are selective as hypnotics to A1-2; A3 has similar effects, muscle relaxation and possibly anti anxiety (possibly anti panic?) and presumably anticonvulsant effects

 

[Wilson Wilson]

Except NONE of them are active except the partial agonist,nordazepam

Please don't take this as disrespect, my words are literal - Dzp is double-triple the potency of its metabolites, and they are only produced in minor amounts except nordazepam, and valium itself(Dzp) is 1.5x as potent

They are in effective completely inactive, except nordazepam, with chronic dosing or large doses - How it effects you, of course, varies

But this isn't accurate either. It's not that the other metabolites are inactive, it's that they are not major metabolites, and therefore are not created in large quantities by diazepam in normal therapeutic doses.

If I take in the range of 50-100mg diazepam which is a pretty normal dose for recreational purposes, I'm going to feel the metabolites.

And like you say, it also varies depending on the individual. How one person metabolises diazepam is different from how another person does.

 

[Doclad]

50-100mg a normal dose for recreational use? Oops, 10mg of Diazepan knock me out lol. In favor of the reduction of damages I will say that you do not try that dose without tolerance if you do not want to have an accident.


DocLad

 

[AlphaMethylPhenyl]

... I said selective, for A3, not exclusive; it is obviously selective to A2 as well, and has an absurd binding affinity

What I can?t make sense of, clonazepam is would be a terrible hypnotic, it?s long acting, with a gradual onset and delayed peak, and it?s rarely if ever used as a sedative/hypnotic(in countries am aware of)

The Z drugs are highly selective for A1, hence them being effective, (yet atypical Benzodiazepine type ) sedative/hypnotics, yet the negligible bzd effects otherwise at standard doses, and completely impractical as anti-convulsants

A3, apperaantly has anti-panic, muscle relaxation and anti-convulsant

And opioid rotation doesn?t make sense on paper, yet apparently works ....

OF COURSE, rotating to say, methadone, or even oxycodone, with its Kappa receptor possibly contributing, or just a higher binding affinity

Should have worded it differently, just liked what speedKing said and the idea

Okay so "selective" was a bit vague. Yes it is used for insomnia. Asked several doctors this question. A3 modulation is mostly anxiolytic, otherwise weekly active as a muscle relaxant and anti-epileptic, weakly reinforcing....

Having a "schedule" of rotating drugs of overlapping actions does not work. If you say it does, well that won't change the viewpoint of myself and other learned psychopharm experts on this site....

Klonopin is very useful for about any benzo indication. It's something like Xanax, which is meant to be a daytime anxiolytic, that doesn't readily make people sleepy at decent doses.

Did some research. Seems Klonopin is most effective for disorders in sleep. But it's an all-around medication, so for instance if someone has a lot fo anxiety when the lights are turned out, Klonopin can help that and also provide sedation. Similar deal with strained muscles.

Among BZDs, clonazepam (optional), midazolam (optional) and estazolam (optional) can be used. The other BZDs are not recommended.


anxiolytic benzodiazepines that are not approved for insomnia (alprazolam, clonazepam, lorazepam, diazepam) are prescribed off-label for this purpose


Clonazepam (Klonopin) is highly effective in the treatment of REM sleep behavior disorder (RBD), relieving symptoms in nearly 90% of patients with little evidence of tolerance or abuse.


Clonazepam is suggested for the treatment of RBD


This study provides evidence of important objective effects of clonazepam on NREM sleep in RBD


Clonazepam reduced vigorous verbal and motor behaviors, with two thirds of patients free from sleep-related injuries.

 

[AlphaMethylPhenyl]

D^ I stick with one, (well one type) but read his post... Opioid rotation is questionable on paper, yet works seemingly

Clonazepam binding affinity is ABSURD; I mean comparable by weight, to buprenorphine - and, no, Clonazepam takes 2-3 hours to peak, and has long duration because of solubility (among others !) so no, insomnia is a horrible use, it's specifically known for being less hypnotic than other common benzodiazepines, including Valium, probably every Tribenzo, those and temazepam are good sedative/hypnotics, well, unless you wanna take rohypnol( a nitrobenzo, though the only, uh, hypnotic, if you wanna call it that

Dont take me as rude, just trying to correcting something (as you ) although poor wording, was really focusing on the idea of of what speedking said, and also, wishing could discuss things like that with medical professionals, freely

Opioid rotations may work, when switching to/or from specific opioids, with unique properties, which may have been better suited in the first place, or even if otherwise similar and at a roughly equipotent dose, the new medication may have a (sometimes much) higher binding affinity, or higher intrinsic activity, at Mu mostly, thought some think the kappa effects of oxycodone play a part in its effects, while methadone, well methadone just seems to rock as an analgesic and overall therapeutic opioid, though aside from being more potent at steady state, and the ability to (better) maintain effectiveness compared to other opioids, it's used for specific pain

I stick with chloro-nitro, some tri(nitro), benzos, though, for the most part. Wonder if the serotonin effects of Clonazepam have any other possible applications? That would be practical I mean? Some muscle relaxers have serotonergic properties, pretty sure it's the opposite though. Anyway, no, alprazolam or dzp would be more along the lines, if somehow a chart could be made, and it may be the only one that the Z drugs have any (significant) affinity for, though of course they are selective as hypnotics to A1-2; A3 has similar effects, muscle relaxation and possibly anti anxiety (possibly anti panic?) and presumably anticonvulsant effects

Sublingual Klonopin can work within an hour.

With regard to serotonergic effects, this may offset any otherwise depressive symptoms. Was told that it doesn't produce depression as readily as something like Valium, isn't as recreational too (strangely enough), and is used for mania in bipolar illness.

Apart from sheer stigma, I think that with Valium any medicinal dose is (at least initially) recreational, whereas with Klonopin it almost always isn't, so that risk of abuse and addiction isn't nearly as present.

 

[crazedloom175]

You already know, no duh...

 

[Lorne???]

It's metabolites are innactive:"; sure, take over a 100mg, though this is NOT speculation; check the plasma levels; if you took well over 100mg and are dependent, a single dose uniy of oxazepam/temeazepam, converted after Valium itself has been redistributed, doesn't make it any more effective, for these purposes

And clean clOnazepam is simply a bad choice for a hypnotic among the many benzo; sublingual isn't any faster That Know of,)slower some medications, albeit also longer duration typically) it peaks ~ 2-3hrs on average, yes, I forget a normal persom can feel it faster

Xanax would be better for falling asleep, and it's, as you said, of more limited (medical/accepted) uses; temazepam is a good intermediate. Clonazepam has an elimination similar to
DZP/Balium itself
- 30-40 hours, mean - and a longer duration. At least in US, it is not normally recommended for these reasons, and for known for being less sedating at effective doses, and a unique (though modest) secondary Moa

Btw, this is interesting discourse, always kinda thought Clonazepam and lorazepam had potential as hypnotics, though not first line. Am open, and try to check refere, though I once had literature, half of which seemed to speak to
clomazep, and have done a lot of research, and "common"
sedative/hypnotic, just doesn't ring any bells? Though maybe Britain? And other countries, who knows?(likely you) Anyway, enjoy it