eszopiclone versus zolpidem

[mgrady3]

Can anyone comment on the pharmacological differences bewteen these two drugs (lunesta and ambien respectively)

I was assured by the pharmacist today that eszopiclone acts differently than zolpidem in the brain.

I was under the assumption that both drugs bind to the GABA-A receptor neurons.
The only difference being, in the paper I read, it states Zolpidem binds specifically to GABA-A_(alpha1), which is the sub receptor corresponding to sedation/hypnotic effects.

I didn't see the same statement about Eszoplicone, just that it binds to GABA-A. Yet, I would assume that since Eszopiclone is primarily sedative and a weak anxiolytic, that it can't have much binding for efficiency for the other alpha sub receptors.

Is there something inherently different in the way the two drugs behave in the brain or was the pharmacist just trying to convince me that the Lunesta would work. I had told her I had taken Ambien before and it did not help my insomnia at all.

 

[asecin]

isnt lunesta some weird mutation of the true zopiclone sold only in europe ?
anyway zopiclone is 10 times better than ambien will ever be and yes i believe they all affect GABA one way or another but there are claims that they are not benzo related.

 

[Hammilton]

Of the 'true' zopiclone? Eszopiclone, as you should be able to figure out yourself, is S-zopiclone. It contains only the optical isomer with activity. Arzopiclone (R-zopiclone) is without appreciable affinity for GABA-A receptors.

i believe they all affect GABA one way or another but there are claims that they are not benzo related.

No, there are claims that they're not benzos. They aren't. They have no structural similarity in common with the benzodiazepines. That doesn't preclude activity at 'BZD' receptors.

Imagine five towers of casino chips put together in a ring. A pentagonal structure appears. This can be thought of as a GABA-A receptor. Each tower represents a different subunit. Going around the pentagon, there is an alpha1 subunit next to a beta2 subunit next to a gamma2 subunit next to an alpha1 subunit next to a beta2 subunit (which itself is next to the first alpha1 subunit). The binding sites for various ligands are located at the intersection of the subunits.

The binding site for benzodiazepines is located between alpha subunits and the gamma subunit. GABA-A receptors expressing alpha subunits 1, 2, 3, and 5 are benzodiazepine sensitive (that is, they are GABA-A receptors that are effected by benzos).

Zolpidem and zopiclone are both selective for alpha1-containing GABA-A receptors, and are about as similar as you can get I'm afraid.

 

[Solipsis]

So the idea is that the alpha1-containing receptors control sleep-wake effects (hypnotic) but the receptors containing the other subunits that benzo's affect also extend to additional anxiolysis, euphoria, and what not?
In other words, that is what makes the non-benzodiazepine Z-drugs more selective for hypnotic purposes? Hmm thanks a lot for explaining that a little hammilton, now I am extra interested to check out what type of GABA receptors or subunits thereof are targeted by muscimol and gaboxadol.

This is definitely an interesting read on the subject, also good if you are not a total expert!

 

[mgrady3]

OK,
thanks for the information.
You verified what I thought to be true.
I wanted to tell the pharmacist this when she said they were different but wasn't 100% sure of my knowledge.
Thanks for that article, its very helpful concerning GABA_A

needless to say, the eszopiclone did not help me sleep, at a dosage of 3mg. Just like Zolpidem, it kept me asleep for 2-3 hours at max and the morning was rough.

 

[flacky]

I find that zopiclone is leaps and bounds better than zolpidem. I think the problem is with your dosing. I get zopiclone as a mixture of both isomers in 7.5 mg tabs. This is equivalent to 3.25 mg of lunesta (the strongest available strength is 3 mg, though).

One tab used to have me asleep all night, never frequently. However, after a couple months of using it maybe once every 2 weeks, I began waking up in 3 hours like you describe. I doubled the dosage to two tablets (15 mg zopiclone => 7 mg eszopiclone "lunesta").

I hope that that was helpful.

What dose do you have? You might want to scale it up to 3 mg, and if that doesn't work, maybe to 5, 6, or 7 mg.

 

[mgrady3]

as far as I know, Eszopiclone (S-Zopiclone) is active, where as Arzopiclone (R-Zopiclone) is barely active
so... a Racemic mixture even of 7.5 mg is still equiv to 3.25mg of S-Zopiclone... which is essentially the dose i am taking.

sorry didn't read your post in full
I wasn't sure if t was safe to take more than 3mg of eszopiclone.

I guess I'll try taking more..
I took 20+mg ambien (Zolpidem) with little to no effects..

 

[danceofdays]

my friend takes between 15 and 30mg of zopiclone a night. he gets really fucked up after he takes it, lol. so yeah, it's safe to use more than one pill at a time.

 

[anterrabae]

Fucked up how? Is there any sense of euphoria or possibility of tripping like ambien? I only need these for sleep, I get my kicks other ways...just curious.