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  • BDD Moderators: Keif’ Richards

Different property ratios of different benzos

Psychonauticunt

Bluelighter
Joined
Jun 1, 2010
Messages
1,412
I failed to find any kind of information on this. All benzos essentially possess the same properties; sedative, anxiolytic, hypnotic, amnesic, anticonvulsant, and muscle relaxant. Is there any information available on the relative potencies of different properties in different benzos? For example, temazepam is mostly a hypnotic, sedative and muscle relaxant (to my knowledge), but at what ratios in comparison to those are the anxiolytic and other properties, does anybody know, at least for any benzos?

I typically like to think that most benzos are more or less suited to providing all of the above effects and will use, for example, alprazolam for sleep if necessary although it isn't necessarily very sedative, but at what kinds of levels do different benzos act on their "non-primary" GABA effects?
 
I know that valium contains muscle relaxing properties that other benzos do not
 
I know that valium contains muscle relaxing properties that other benzos do not

All benzodiazepines contain muscle relaxing properties. Classical Benzodiazepines are all non-selective which means that they ALL have anxiolytic, hypnotic, anti-seizure, muscle relaxant and amnesiac properties but just to different levels. For instance Diazepam does have powerful muscle relaxant effects, more so than most but every benzo still possesses that effect.

To the OP: I'm sure you know the first of this...

All benzodiazepine agonists exert five primary effects and they are:

1. Hypnotic
(Prescribed for: short-term management of insomnia)

2. Anxiolytic
(Prescribed for: treatment of anxiety disorders and phobias; prevention of panic attacks)

3. Anti-convulsant/anti-seizure
(Prescribed for: seizure control; management of status epileptics; prevention of panic attacks)

4. Antispasmodic (Muscle relaxant)
(Prescribed for: treatment of muscle spasms, for example, Tetanus or spastic disorders and Restless legs syndrome.

5. Amnesic
Used as sedatives for patients receiving mechanical ventilation, or those in extreme distress or severe pain. Midazolam is the most common and effective for sleep-induced procedures.

Different benzodiazepines exhibit these primary effects to varying degrees. For example, diazepam (Valium) is a relatively powerful hypnotic, whereas the more modern benzodiazepines such as alprazolam (Xanax), lorazepam (Ativan), and clonazepam (Klonopin) are less powerful hypnotics, but are very powerful anxiolytics. Do not assume that because one benzodiazepine makes you sleepier than another that this benzodiazepine is more potent than those that don’t produce sleepiness to the same degree.

There are six GABA-a subunits, GABA(a 1), GABA(a 2), GABA(a 3), GABA(a 4), GABA(a 5) and GABA(a 6). Of those six receptors, benzodiazepines have no affinity for (a 4) and (a 6). Most effective anti-anxiety benzodiazepines have affinity to both alpha1 and alpha2 subunits while the more effective hypnotics have higher affinity to just the alpha1 subunit

GABA-A receptor subtype containing:

Alpha1: sedation, amnesiac, alcohol interaction

Alpha2: anxiolysis, muscle relaxation

Alpha3: anxiolysis, muscle relaxation, sedation

Alpha5: amnesiac, anti-seizure

The alpha1-containing has been proposed to be responsible for the sedative action; the alpha2 and/or the alpha3 subtypes have been suggested to mediate the anxiolytic activity and the myorelaxation effects, and the alpha5 subtype has been associated with cognition processes and possible anti-seizure capability when combined with the alpha1 subtype.


All benzodiazepines are anxiolytics. How their effects vary in degree are due to their compound structures. The following:

7-nitro compounds (Clonazepam, Nitrazepam, Flunitrazepam) are potent anti-seizure and muscle relaxants.

3-hydroxy compounds (Lorazepam, Temazepam, Oxazepam) are often more sedating, often hypnotics and have more prominent muscle relaxant effects.

Imidazo compounds (Midazolam, Loprazolam) are powerful amnesics, very sedating and short acting. Also analgesic. They are also water soluble.

Triazolo compounds (Alprazolam, Triazolam, Estazolam) are often sedating, mostly hypnotic and very short acting, have short half-lives. They are very potent on a mg basis.

2-Keto compounds (Diazepam, Flurazepam, Chlordiazepoxide) exert all the five primary effects to a noticeable but various degree and have very long half lives.
 
^^ Great answer! Ha, I've got NO follow up after that one. *what that guy said*
 
Very good question OP.. and very good answer k'd out...

in my experience, valium ha the strongest muscle relaxing properties, and i have read that clonazepam is the most effective anti-convulsant...

but it would be cool to have a chart listting exactly which benzo has the strongest of each of the respective properties you mentioned...
 
It's also a question of dose. Anxiolytic benzos are hypnotics when the dose is raised for instance.
 
Great post K'd out. But do you (or anyone) know which of the properties are the basis for the dose equivalent chart I've seen posted here?
 
long list of good stuff

Thorough and good answer, lots of familiar stuff but plenty of new stuff as well: thanks. And yeah, obviously there are different levels of potency - at least personally, equivalence-wise (ie. 0.5mg alprazolam v. 20mg temazepam) the alprazolam is more potent, although decidedly less sedating. Also, as someone else already partially mentioned, since they all exert the same properties in different quantities, all benzos will eventually be amnesic and sedative at high enough doses.

As said, it also varies from person to person and I imagine it's very difficult to determine, but I would love to find out from somewhere, someday, in great detail the exact ratios of the effects. %)

As in: Eg. Alprazolam:
Hypnotic 10 /Anxiolytic 40/Anticonvulsant 10 /Antispasmodic 15/Amnesic 25

Or something like that. But I guess that's never gonna happen. Good answer though, thanks.
 
That would be nice to have a chart like that but I guess it would have to be something made of assumptions or personal experience by us or someone else. By the way Psychonauticunt, thats a nice ratio for Alprazolam in my opinion.

Here is an interesting chart most people have seen before:

Structural Potency of benzodiazepines

There is already a lot of information about equivalent doses of benzodiazepines on a milligram basis. While this is undoubtedly important for clinical practice, it doesn't give the whole story as to why certain benzodiazepines are much more potent than others.

To do this, the therapeutically equivalent doses in milligrams need to be converted to a molar basis and multiplied by their respective bioavailabilities. This tells us exactly how many molecules of a specific benzodiazepine (that reach the circulation) are needed to achieve a standard anxiolytic level. This arbitrary standard in most publications is the level produced by 10 mg of oral diazepam (Valium).

This thought experiment should reveal the common characteristics of the benzodiazepines that bond strongly to the GABA receptor, and thus require the lowest doses on a micromolar basis.

The potency of benzodiazepines in order from most to least (judging from the molecules on a molar basis):

1. Triazolam (Halcion; hypnotic) 1.31 umol
2. Alprazolam (Xanax; anxiolytic) 1.38 umol
3. Clonazepam (Klonopin; anxiolytic, anticonvulsant) 1.43 umol
4. Flunitrazepam (Rohypnol; hypnotic) 1.60 umol
5. Lorazepam (Ativan; anxioltic, anticonvulsant) 2.65 umol
6. Loprazolam (Dormonoct; hypnotic) 2.90 umol
7. Lormetazepam (Noctamid; hypnotic) 3.58 umol
8. Eszopiclone (Lunesta; non-benzodiazepine hypnotic) 4.24 umol
9. Estazolam (ProSom; hypnotic) 4.73 umol
10. Bromazepam (Lexotan; anxiolytic) 14.61 umol
11. Quazepam (Doral; hypnotic) 17.06 umol
12. Zalepion (Sonata; non-benzodiazepine hypnotic) 19.65 umol
13. Zopiclone (Imovane; non-benzodiazepine hypnotic) 21.22 umol
14. Nitrazepam (Mogadon; hypnotic) 30.48 umol
15. Diazepam (Valium; anxiolytic, anticonvulsant, hypnotic) 32.67 umol
16. Medazepam (Nobrium; anxiolytic) 33.23 umol
17. Nordazepam (Nordaz; anxiolytic) 33.25 umol
18. Clorazepate (Tranxene; anxiolytic) 41.27 umol
19. Prazepam (Centrax; anxiolytic) 41.56 umol
20. Flurazepam (Dulmane; hypnotic) 47.08 umol
21. Halazepam (Paxipam; anxiolytic) 51.03 umol
22. Ketazolam (Anxon; anxiolytic) 53.69 umol
23. Clobazam (Frisium; anxiolytic, anticonvulsant) 59.9 umol
24. Zolpidem (Ambien; non-benzodiazepine hypnotic) 59.9 umol
25. Temazepam (Restoril; hypnotic) 63.9 umol
26. Oxazepam (Serax; anxiolytic) 67 umol
27. Chlordiazepoxide (Librium; anxiolytic, anticonvulsant) 75 umol

Please note that the potency of a benzodiazepine has no correlation with euphoria. For example, among drug abusers, Temazepam is and has always been known as a euphoric benzodiazepine and in fact has been banned in many countries due to its recreational abuse, yet its one of the least potent benzodiazepines.
 
Perhaps a little off topic, but I'm prescribed Xanax monthly, and until very recently I had no clue, but tobacco use can lower the effectiveness of benzos up to 50% ie smoking a cig near b4, after dosing can cause 1mg of Xanax or Ativan to act as 0.5mg. Not sure why this is although IME seems to be true.
 
K'd-OUT-in-AZ laid it out pretty nicely.

benzos are grouped in several different groupings (ie. 7-nitro, 3-hydroxy, 2-keto, etc).

The 3-hydroxy (temazepam, lorazepam, lormetazepam, oxazepam) and the 7-nitro (nitrazepam, clonazepam, flunitrazepam) are mainly hypnotic and anti-convulsant. like K'd-OUT-in-AZ already mentioned, both of these groups have prominent sedative and muscle relaxant properties aswell.
 
I failed to find any kind of information on this. All benzos essentially possess the same properties; sedative, anxiolytic, hypnotic, amnesic, anticonvulsant, and muscle relaxant. Is there any information available on the relative potencies of different properties in different benzos? For example, temazepam is mostly a hypnotic, sedative and muscle relaxant (to my knowledge), but at what ratios in comparison to those are the anxiolytic and other properties, does anybody know, at least for any benzos?

I typically like to think that most benzos are more or less suited to providing all of the above effects and will use, for example, alprazolam for sleep if necessary although it isn't necessarily very sedative, but at what kinds of levels do different benzos act on their "non-primary" GABA effects?

All benzodiazepines contain muscle relaxing properties. Classical Benzodiazepines are all non-selective which means that they ALL have anxiolytic, hypnotic, anti-seizure, muscle relaxant and amnesiac properties but just to different levels. For instance Diazepam does have powerful muscle relaxant effects, more so than most but every benzo still possesses that effect.

To the OP: I'm sure you know the first of this...

All benzodiazepine agonists exert five primary effects and they are:

1. Hypnotic
(Prescribed for: short-term management of insomnia)

2. Anxiolytic
(Prescribed for: treatment of anxiety disorders and phobias; prevention of panic attacks)

3. Anti-convulsant/anti-seizure
(Prescribed for: seizure control; management of status epileptics; prevention of panic attacks)

4. Antispasmodic (Muscle relaxant)
(Prescribed for: treatment of muscle spasms, for example, Tetanus or spastic disorders and Restless legs syndrome.

5. Amnesic
Used as sedatives for patients receiving mechanical ventilation, or those in extreme distress or severe pain. Midazolam is the most common and effective for sleep-induced procedures.

Different benzodiazepines exhibit these primary effects to varying degrees. For example, diazepam (Valium) is a relatively powerful hypnotic, whereas the more modern benzodiazepines such as alprazolam (Xanax), lorazepam (Ativan), and clonazepam (Klonopin) are less powerful hypnotics, but are very powerful anxiolytics. Do not assume that because one benzodiazepine makes you sleepier than another that this benzodiazepine is more potent than those that don’t produce sleepiness to the same degree.

There are six GABA-a subunits, GABA(a 1), GABA(a 2), GABA(a 3), GABA(a 4), GABA(a 5) and GABA(a 6). Of those six receptors, benzodiazepines have no affinity for (a 4) and (a 6). Most effective anti-anxiety benzodiazepines have affinity to both alpha1 and alpha2 subunits while the more effective hypnotics have higher affinity to just the alpha1 subunit

GABA-A receptor subtype containing:

Alpha1: sedation, amnesiac, alcohol interaction

Alpha2: anxiolysis, muscle relaxation

Alpha3: anxiolysis, muscle relaxation, sedation

Alpha5: amnesiac, anti-seizure

The alpha1-containing has been proposed to be responsible for the sedative action; the alpha2 and/or the alpha3 subtypes have been suggested to mediate the anxiolytic activity and the myorelaxation effects, and the alpha5 subtype has been associated with cognition processes and possible anti-seizure capability when combined with the alpha1 subtype.


All benzodiazepines are anxiolytics. How their effects vary in degree are due to their compound structures. The following:

7-nitro compounds (Clonazepam, Nitrazepam, Flunitrazepam) are potent anti-seizure and muscle relaxants.

3-hydroxy compounds (Lorazepam, Temazepam, Oxazepam) are often more sedating, often hypnotics and have more prominent muscle relaxant effects.

Imidazo compounds (Midazolam, Loprazolam) are powerful amnesics, very sedating and short acting. Also analgesic. They are also water soluble.

Triazolo compounds (Alprazolam, Triazolam, Estazolam) are often sedating, mostly hypnotic and very short acting, have short half-lives. They are very potent on a mg basis.

2-Keto compounds (Diazepam, Flurazepam, Chlordiazepoxide) exert all the five primary effects to a noticeable but various degree and have very long half lives.

excellent thread and excellent post. %)

all answers any benzo user would surely be interested to know.

thankyou very much.

i have always tried to learn as much as possible about the substances i have ever used.

you can never learn to much.

knowledge is power.
 
Perhaps a little off topic, but I'm prescribed Xanax monthly, and until very recently I had no clue, but tobacco use can lower the effectiveness of benzos up to 50% ie smoking a cig near b4, after dosing can cause 1mg of Xanax or Ativan to act as 0.5mg. Not sure why this is although IME seems to be true.

I always crave a cig after taking some pills. Do you happen to have a link? I would like to read more about this.

I guess you're right! Nice to know that...

12. Drug Interactions with benzodiazepines
a. enhanced CNS sedation with other sedatives
b. smoking and tobacco use reduces the effectiveness of benzodiazepines
c. enzyme inhibitors such as cimetidine (Tagamet) can elevate levels of benzodiazepines in the blood
d. may reduce the effectiveness of larodopa, used for Parkinsonism
http://www.animatingapothecary.com/dh5.htm
 
Last edited:
I always crave a cig after taking some pills. Do you happen to have a link? I would like to read more about this.

I guess you're right! Nice to know that...

12. Drug Interactions with benzodiazepines
a. enhanced CNS sedation with other sedatives
b. smoking and tobacco use reduces the effectiveness of benzodiazepines
c. enzyme inhibitors such as cimetidine (Tagamet) can elevate levels of benzodiazepines in the blood
d. may reduce the effectiveness of larodopa, used for Parkinsonism
http://www.animatingapothecary.com/dh5.htm

smokings for losers anyway. :p =D
 
People are divided on this; some say the tobacco nullifies the benzo effect (and on my diazepam package it said nicotine reduces the effect) and others say it slightly amplifies it. I think it probably slightly reduces the effectiveness, but on the other hand the pleasant effects of the cigarette, particularly by people who normally enjoy smoking anyway, are greatly pronounced due to the well-being brought on by the benzo, so the overall experience is positive for them. Not that the benzo potentiates the cigarette or anything, just that they enjoy it that much more 'cause they're high.
 
I switched from xanax to valium for the muscle relaxation qualities... it multi tasks for my anxiety and chronic pain.

I find valium to be great for both. I also take klonopin.

K'd out covered it all!
 
It seems to effectively dull the effects of the benzo by half. N I don't get the relaxation of my inhibitions which creates a sort of euphoria which I used to enjoy. It sucks because of course taking a Xanax makes me want a cig that much more lol. Guess you can't have your cake and eat it too? Lol. Your welcome and sorry for not posting sources I'm on my iPhone!!
 
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