Melatonin was placebo at best, and doesn't induce sleep it's the chem that maintains ur eating habit n sleep patterns including ur circadian rhythm. But I have bad anxiety, bad insomnia, my Xanax script got stole at da casinos by my ex gf n just got lunesta today. I run 3 miles everyday I wake up n gym 5 days a wk. 2 off days. I smoke ciggs n tan carcinogenic all the way. Can we stay on topic?
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GABA receptors and Sedative/Hypnotics ("Sleep Meds")
- Thread starter Dope_User
- Start date
Melatonin was placebo at best, and doesn't induce sleep it's the chem that maintains ur eating habit n sleep patterns including ur circadian rhythm. But I have bad anxiety, bad insomnia, my Xanax script got stole at da casinos by my ex gf n just got lunesta today. I run 3 miles everyday I wake up n gym 5 days a wk. 2 off days. I smoke ciggs n tan carcinogenic all the way. Can we stay on topic?
How different is Eszopiclone(lunesta) from zopiclone?
I ask this because I kno lunesta is just the isomer of it. But looking at each drugs related wiki article the zopiclone article goes way in depth how zoplicone is active at the gaba A receptors n the 1345 sites I guess? I'm under the influence so memories a lil hazed lol.
From wiki on zopiclone (Under pharmAcology section)
The therapeutic pharmacological properties of zopiclone include hypnotic, anxiolytic, anticonvulsant and myorelaxant properties.[62] Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on α1, α2, α3 and α5 GABAA containing receptors as full agonists causing an enhancement of the actions of GABA to produce the therapeutic and adverse effects of zopiclone.
To save you the trouble and hopefully to answer my ?'s here is wiki on lunesta::
Eszopiclone acts on benzodiazepine binding site situated on GABA-A neurons as an agonist.[6] Eszopiclone is rapidly absorbed after oral administration, with serum levels peaking between 1 and 1.3 hours.[7] The elimination half-life of eszopiclone is approximately 6 hours and it is extensively metabolized by oxidation and demethylation. Approximately 52% to 59% of a dose is weakly bound to plasma protein. Cytochrome P450 (CYP) isozymes CYP3A4 and CYP2E1 are involved in the biotransformation of eszopiclone; thus, drugs that induce or inhibit these CYP isozymes may affect the metabolism of eszopiclone. Less than 10% of the orally administered dose is excreted in the urine as racemic zopiclone.[8] In terms of benzodiazepine receptor binding and relevant potency, 3mg of eszopiclone is equivalent to 10mg of diazepam.[ <---------under pharmacology section.
This leads me to believe there has to be alot more to my lunesta then the usual that craps beat ya kno? Any discussion on this? Thanks guys. I'll provide the sourcelinks at bottom. Tho it is wiki. The worst source. Which is y I came here lol.
Lunestawiki ---------> http://en.m.wikipedia.org/wiki?search=Lunesta
Zopiclone ------------> http://en.m.wikipedia.org/wiki?search=Zopiclone
Ps I meant stereoisomer not isomer of zopiclone
I ask this because I kno lunesta is just the isomer of it. But looking at each drugs related wiki article the zopiclone article goes way in depth how zoplicone is active at the gaba A receptors n the 1345 sites I guess? I'm under the influence so memories a lil hazed lol.
From wiki on zopiclone (Under pharmAcology section)
The therapeutic pharmacological properties of zopiclone include hypnotic, anxiolytic, anticonvulsant and myorelaxant properties.[62] Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on α1, α2, α3 and α5 GABAA containing receptors as full agonists causing an enhancement of the actions of GABA to produce the therapeutic and adverse effects of zopiclone.
To save you the trouble and hopefully to answer my ?'s here is wiki on lunesta::
Eszopiclone acts on benzodiazepine binding site situated on GABA-A neurons as an agonist.[6] Eszopiclone is rapidly absorbed after oral administration, with serum levels peaking between 1 and 1.3 hours.[7] The elimination half-life of eszopiclone is approximately 6 hours and it is extensively metabolized by oxidation and demethylation. Approximately 52% to 59% of a dose is weakly bound to plasma protein. Cytochrome P450 (CYP) isozymes CYP3A4 and CYP2E1 are involved in the biotransformation of eszopiclone; thus, drugs that induce or inhibit these CYP isozymes may affect the metabolism of eszopiclone. Less than 10% of the orally administered dose is excreted in the urine as racemic zopiclone.[8] In terms of benzodiazepine receptor binding and relevant potency, 3mg of eszopiclone is equivalent to 10mg of diazepam.[ <---------under pharmacology section.
This leads me to believe there has to be alot more to my lunesta then the usual that craps beat ya kno? Any discussion on this? Thanks guys. I'll provide the sourcelinks at bottom. Tho it is wiki. The worst source. Which is y I came here lol.
Lunestawiki ---------> http://en.m.wikipedia.org/wiki?search=Lunesta
Zopiclone ------------> http://en.m.wikipedia.org/wiki?search=Zopiclone
Ps I meant stereoisomer not isomer of zopiclone
If you are still wondering how Lunesta is different form Zopiclone, or just other info on Lunesta, I can offer my 2cents:
I have taken many sleep aids, otc, herbal, and RX including ambien, lunesta, mirtazipine, trazadone, xanax, clonazepam, and temazepam.
Lunesta is the S-enantiomer of zopiclone (racemic blend). It is more potent than the racemic blend. Zopiclone is Rx'd in (I believe) up to 7.5mg dosages. Whereas Lunesta is Rx'd (atleast in USA) in only up to 3mg dosages.
For me, Lunesta was nearly no different than ambien. I found it helped me fall asleep decently but didn't help me stay asleep. Many people report a gross metallic after taste when taking lunesta. Even at doses over 6mg I never experienced that. Perhaps that thats only from zopiclone and not Luensta? Couldn't tell you as i've only ever had Lunesta, not the racemic mix.
From what I remember, Lunesta is designed to target the alpha1 subunit of GABA_A though it will probably bind to the other receptors with a lower affinity. I found very minimal anxiolytic or muscle relaxant effects which supports the idea that it binds primarily to the alpha1 GABA_A subunit.
I've never had a very clear explanation as to how metabolism of different benzos and z-drugs can be so different. Many drugs are listed as being metabolized by CYP3A4, however, only a few of them seem to be affected by things like white grapefruit juice, a CYP3A4 inhibitor. I would expect there is no interaction between Lunesta and GFJ but perhaps that would be one way to extend its effects. I've never tried, I never think to eat a grapefruit at night, but I love them in the morning. I assume because CYP2E1 is also involved that CYP3A4 inhibition may not have any effects at all.
I don't want to go down the road of benzo addiction, but I find clonazepam and temazepam to help me as much if not better than lunesta does.
So, overall my rating of lunesta has to just be so-so. Nothing special, I don't find it better than ambien or better than other commonly Rx'd sleep aids.
However I try to not take straight benzos every night. Sometimes i'll take a lunesta with some benadryl or another anti-histamine, or some nights i'll take trazadone or mirtazipine, or just have a few more beers than normal and not take any meds, that way I'm not solely relying on benzos.
I have taken many sleep aids, otc, herbal, and RX including ambien, lunesta, mirtazipine, trazadone, xanax, clonazepam, and temazepam.
Lunesta is the S-enantiomer of zopiclone (racemic blend). It is more potent than the racemic blend. Zopiclone is Rx'd in (I believe) up to 7.5mg dosages. Whereas Lunesta is Rx'd (atleast in USA) in only up to 3mg dosages.
For me, Lunesta was nearly no different than ambien. I found it helped me fall asleep decently but didn't help me stay asleep. Many people report a gross metallic after taste when taking lunesta. Even at doses over 6mg I never experienced that. Perhaps that thats only from zopiclone and not Luensta? Couldn't tell you as i've only ever had Lunesta, not the racemic mix.
From what I remember, Lunesta is designed to target the alpha1 subunit of GABA_A though it will probably bind to the other receptors with a lower affinity. I found very minimal anxiolytic or muscle relaxant effects which supports the idea that it binds primarily to the alpha1 GABA_A subunit.
I've never had a very clear explanation as to how metabolism of different benzos and z-drugs can be so different. Many drugs are listed as being metabolized by CYP3A4, however, only a few of them seem to be affected by things like white grapefruit juice, a CYP3A4 inhibitor. I would expect there is no interaction between Lunesta and GFJ but perhaps that would be one way to extend its effects. I've never tried, I never think to eat a grapefruit at night, but I love them in the morning. I assume because CYP2E1 is also involved that CYP3A4 inhibition may not have any effects at all.
I don't want to go down the road of benzo addiction, but I find clonazepam and temazepam to help me as much if not better than lunesta does.
So, overall my rating of lunesta has to just be so-so. Nothing special, I don't find it better than ambien or better than other commonly Rx'd sleep aids.
However I try to not take straight benzos every night. Sometimes i'll take a lunesta with some benadryl or another anti-histamine, or some nights i'll take trazadone or mirtazipine, or just have a few more beers than normal and not take any meds, that way I'm not solely relying on benzos.
exhaustedinsomniac
Greenlighter
- Joined
- Jun 2, 2011
- Messages
- 1
looking for very targeted GABA receptor drug
I've had exhausting insomnia for over twenty-five years. I've tried anti-depressants and benzos off and on but am now pretty convinced that the basis of my insomnia is simply that my GABA receptors that just won't allow me to shut my over-active mind down at night. My understanding is that Ambien, Sonata, and Lunesta are the class of drugs that are most targeted to only the GABA system. Can someone help me understand whether this is true, and if so, what are the differences between these three sleep aid drugs? Thank you for this forum of science-based discussion!
I've had exhausting insomnia for over twenty-five years. I've tried anti-depressants and benzos off and on but am now pretty convinced that the basis of my insomnia is simply that my GABA receptors that just won't allow me to shut my over-active mind down at night. My understanding is that Ambien, Sonata, and Lunesta are the class of drugs that are most targeted to only the GABA system. Can someone help me understand whether this is true, and if so, what are the differences between these three sleep aid drugs? Thank you for this forum of science-based discussion!