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N&PD Moderators: Skorpio | someguyontheinternet
Sedatives of the Future
- Thread starter nuke
- Start date
MagickalKat777
Bluelight Crew
I am becoming increasingly curious about Etifoxine. It seems like it might be a promising drug but there is pretty much nil out there on it.
mgrady3
Bluelighter
I find anti-histamine sedation to be more direct - DPH will sedate me quickly in large enough dosages but it isn't prone to good sleep. I wake up feeling dehydrated and lacking memory.
GABA sedation is more subtle and pleasant due to anxiety relief thats co-entangled with the sedation- though i've never tried barbs, halcion, or rohypnol - im sure they can be just as in your face as histamine-sedation.
I find that with Histamine sedation, if I don't allow my self to sleep right away as they kick in they quickly loose their efficacy. So i'd say there;s pros and cons of both - you can build tolerance to both kinds of medication. Idk if there's an easy answer to say which one is a 'better' sedative.
GABA sedation is more subtle and pleasant due to anxiety relief thats co-entangled with the sedation- though i've never tried barbs, halcion, or rohypnol - im sure they can be just as in your face as histamine-sedation.
I find that with Histamine sedation, if I don't allow my self to sleep right away as they kick in they quickly loose their efficacy. So i'd say there;s pros and cons of both - you can build tolerance to both kinds of medication. Idk if there's an easy answer to say which one is a 'better' sedative.
kaiba
Bluelighter
- Joined
- Sep 24, 2010
- Messages
- 191
Which one's better for long term use?
I'm prescribed ambien/zolpidem. And I alternate it with an anti-histamine.
mgrady3
Bluelighter
None that I know of.
I believe of the Z-drugs, Lunesta [ (S)-Zopiclone ] , may be the only one considered 'safe' for long term use in treating insomnia. That said its still cross tolerant with other GABA-ergic drugs and still has issues with addiction, tolerance, rebound insomnia, etc...
I haven't experienced them but I assume the same thin applies to anti-histamine mediated sedatives - you become tolerant to them and need to increase your dosage. This can be bad for the simple anti-histamines like DPH because when you start venturing into larger dosages you are treading on dissociative territory and that can be extremely unpleasant for many people. I don't have any experience but would assume there are other problems with less typical anti-histamines. Take mirtazipine for example. Its an anti-depressant with a plethora of binding actions (various 5-HT, adrenergic, and namely H1 antagonism!) So yes it sedates you via H1-antagonism, but over time (i didn't give it a long enough chance when i took it) I'd imagine you grow tolerant to the H1-antagonism just like you do to DPH. With Mirtazipine you can't simply just keep increasing your dosage, however, because of all those other receptors its binding at. When the dosage goes over say at most 60mg (my doc told me 30-45), the anti-depressant effects start to really take over and it loses its sedative effects. So it may work long term in that its anti-depressant effects are beginning to help ya out but I doubt that the anti-histamine properties are going to help out in the long run.
Rotating between taking GABA-ergics, Histamine-ergics, and taking nothing at all is maybe the only long term solution. Your tolerance to GABA and H1 will go up over time, so keeping the rate at which that happens low is key. You certainly don't want to be stuck taking pills the rest fo your life to sleep - there isn't really a medication out there thats tailored to being used nightly for extended periods of time,3+ months, at least that I know of.
Plain benzos work the best for me, a mixture of clonazepam and temazepam - but I'm aware that its not a sustainable regiment. In the long run you have to take some time to make lifestyle adjustments to help deal with the underlying causes of you insomnia.
Many people get by perfectly fine just taking benzos 'as needed' to help with sleep. And if that's something you are capable of doing then there's nothing inherently wrong/dangeorus about it as long as you are aware that the drugs shouldn't be abused. When you slip into taking them recreationally your tolerance gets fucked and you find it harder to sleep.
I believe of the Z-drugs, Lunesta [ (S)-Zopiclone ] , may be the only one considered 'safe' for long term use in treating insomnia. That said its still cross tolerant with other GABA-ergic drugs and still has issues with addiction, tolerance, rebound insomnia, etc...
I haven't experienced them but I assume the same thin applies to anti-histamine mediated sedatives - you become tolerant to them and need to increase your dosage. This can be bad for the simple anti-histamines like DPH because when you start venturing into larger dosages you are treading on dissociative territory and that can be extremely unpleasant for many people. I don't have any experience but would assume there are other problems with less typical anti-histamines. Take mirtazipine for example. Its an anti-depressant with a plethora of binding actions (various 5-HT, adrenergic, and namely H1 antagonism!) So yes it sedates you via H1-antagonism, but over time (i didn't give it a long enough chance when i took it) I'd imagine you grow tolerant to the H1-antagonism just like you do to DPH. With Mirtazipine you can't simply just keep increasing your dosage, however, because of all those other receptors its binding at. When the dosage goes over say at most 60mg (my doc told me 30-45), the anti-depressant effects start to really take over and it loses its sedative effects. So it may work long term in that its anti-depressant effects are beginning to help ya out but I doubt that the anti-histamine properties are going to help out in the long run.
Rotating between taking GABA-ergics, Histamine-ergics, and taking nothing at all is maybe the only long term solution. Your tolerance to GABA and H1 will go up over time, so keeping the rate at which that happens low is key. You certainly don't want to be stuck taking pills the rest fo your life to sleep - there isn't really a medication out there thats tailored to being used nightly for extended periods of time,3+ months, at least that I know of.
Plain benzos work the best for me, a mixture of clonazepam and temazepam - but I'm aware that its not a sustainable regiment. In the long run you have to take some time to make lifestyle adjustments to help deal with the underlying causes of you insomnia.
Many people get by perfectly fine just taking benzos 'as needed' to help with sleep. And if that's something you are capable of doing then there's nothing inherently wrong/dangeorus about it as long as you are aware that the drugs shouldn't be abused. When you slip into taking them recreationally your tolerance gets fucked and you find it harder to sleep.
mgrady3
Bluelighter
It looks to me like as researchers get better at making drugs that are receptor subtype selective there could be some improvement in gaba-ergic sedatives. But as stated before, in the long run there's still a lot of long term issues with gaba-ergic drugs.
I've yet to see anything promising moving into clinical trials but there has been a lot of chatter about sedation via antagonism of the Orexin receptor.
"Orexin Receptors: Pharmacology and Therapeutic Opportunities"
http://www.annualreviews.org/doi/abs/10.1146/annurev-pharmtox-010510-100528?journalCode=pharmtox
I've yet to see anything promising moving into clinical trials but there has been a lot of chatter about sedation via antagonism of the Orexin receptor.
"Orexin Receptors: Pharmacology and Therapeutic Opportunities"
http://www.annualreviews.org/doi/abs/10.1146/annurev-pharmtox-010510-100528?journalCode=pharmtox
SwirlyBird
Greenlighter
- Joined
- Jul 24, 2011
- Messages
- 32
Pregabalin is shit, seroquel is shit. Actually I can see how one get addicted to seroquel to waste life away: fluctuate between 200mg one day and 75mg the next to avoid tolerance, gives you a dirty antipsychotic rush, beautiful sleep with dry mouth for 14 hours. Eventually you loose track of what is reality, what are dreams; seroquel serotonin messes with emotions def.
Yellobello
Greenlighter
- Joined
- Jun 18, 2009
- Messages
- 2
Qetiapine is soo nasty!
I remember taking the prolong form as a sleep aid and, I can tell you I was totally useless the following day for even the simplest tasks.
Antipsychotic brain nailer at its best. Maybe the problem was the prolong formulation that carried blood levels to the next day.
What I wanted to contribute to this thread is Erythrina vera or Mulungu.
Since Kratom is the Herbal OTC opioid , this would equal the herbal OTC Benzodiazepine.
25-30g of bark brewed as a tea produce very noticeable effects which totally remind me on benzos. Even the afterglow feels like a benzo hangover. Does anyone have some deeper insight on its active compounds?
Since it is totally available and definitely active it should be mentioned here.
I remember taking the prolong form as a sleep aid and, I can tell you I was totally useless the following day for even the simplest tasks.
Antipsychotic brain nailer at its best. Maybe the problem was the prolong formulation that carried blood levels to the next day.
What I wanted to contribute to this thread is Erythrina vera or Mulungu.
Since Kratom is the Herbal OTC opioid , this would equal the herbal OTC Benzodiazepine.
25-30g of bark brewed as a tea produce very noticeable effects which totally remind me on benzos. Even the afterglow feels like a benzo hangover. Does anyone have some deeper insight on its active compounds?
Since it is totally available and definitely active it should be mentioned here.
DoctorChemX
Bluelighter
Well in the future we won't be consuming chemicals in order
to change our body chemistry, it will be done with other-ways,
nanorobots that enter our bloodstream and then our brain, but
that may be some time off, until then, i think as some have said,
less-addicting sedatives will be given. Just think of chloral hydrate
that drug is almost 200 years old!!!! Synthesized in 1832, and it still
has the power to knock down an elephant at the right dosage, wow.
to change our body chemistry, it will be done with other-ways,
nanorobots that enter our bloodstream and then our brain, but
that may be some time off, until then, i think as some have said,
less-addicting sedatives will be given. Just think of chloral hydrate
that drug is almost 200 years old!!!! Synthesized in 1832, and it still
has the power to knock down an elephant at the right dosage, wow.
Psychedelic Jay
Bluelighter
There is a lot of highly regulated drugs that just aren't used in humans, that were set aside because of not having a place or just there was already something to use for the same purpose.
They have NMDA antagonist in trials for anxiety. <----That needs to be looked into.
They have NMDA antagonist in trials for anxiety. <----That needs to be looked into.
DoctorChemX
Bluelighter
Haha, that would indeed be one hell of a cough-ball. Muscimol has pretty
potent GABAergic properties, ketamine has strong NDMA antagonistic effects
and there are certainly research compounds stronger than atropine, combine
them all, and the effects might be more than sedating : deathating. Hehe.
mgrady3
Bluelighter
You may be asking too much with that combo..
Nothing comes to mind that fits the bill, and perhaps for good reasons...
As DocX said, there's plenty of chemicals that fit the bill for one of those 3.
I am probably just naive but from what I've experienced generally strong Gaba-ergic drugs are simply that, strongly gaba-ergic, with little or no major activity at the other transmitters.
When you delve into the anti-d's and anti-psycs as people mentioned earlier, seroquel, mirtazipine, etc... you get drugs that hit all sorts of different receptors, 5-HT, H1, M1, etc...
But the drugs that tend to be strongly Gabaergic, atleast imo, don't have this wide plethora of binding sites (unless you consider the gaba system it self to be a rather expansive receptor complex)
Nothing comes to mind that fits the bill, and perhaps for good reasons...
As DocX said, there's plenty of chemicals that fit the bill for one of those 3.
I am probably just naive but from what I've experienced generally strong Gaba-ergic drugs are simply that, strongly gaba-ergic, with little or no major activity at the other transmitters.
When you delve into the anti-d's and anti-psycs as people mentioned earlier, seroquel, mirtazipine, etc... you get drugs that hit all sorts of different receptors, 5-HT, H1, M1, etc...
But the drugs that tend to be strongly Gabaergic, atleast imo, don't have this wide plethora of binding sites (unless you consider the gaba system it self to be a rather expansive receptor complex)
ebola?
Bluelight Crew
No offense, but you just spent 2 paragraphs pretty much just saying, "Drugs that bind to a single type of receptor bind to a single type of receptor." 
ebola
ebola
DoctorChemX
Bluelighter
I Too find the gabaergic agonists to be fascinating, they seem to not
be as researched as other receptors like dopamine, serotonin & acetylcholine
to name just a few. But i may be wrong there, i'm just coming from my experience
that's all. But as i said, i'm definitely fascinated by this class of compounds and
there effects, as i am no expert, i can't say for certain, but it seems as though
there are at least six different sub-units in the gaba center of the brain, and different
compounds effect different subunits. Benzodiazepines obviously are the most famous
gaba agonists, and many have different effects on the subunits, diazepam seems to
effect all of them, whereas temazepam affects mostly the sleep one, however, i am
aware of no benzo that induces hallucinations, so there must be a sub-receptor of the
gaba system which does include hallucinations, since gaba agonists like zolpidem and
muscimol are extremely famous for inducing hallucinations and visual distortions alike.
- DrChemX -
be as researched as other receptors like dopamine, serotonin & acetylcholine
to name just a few. But i may be wrong there, i'm just coming from my experience
that's all. But as i said, i'm definitely fascinated by this class of compounds and
there effects, as i am no expert, i can't say for certain, but it seems as though
there are at least six different sub-units in the gaba center of the brain, and different
compounds effect different subunits. Benzodiazepines obviously are the most famous
gaba agonists, and many have different effects on the subunits, diazepam seems to
effect all of them, whereas temazepam affects mostly the sleep one, however, i am
aware of no benzo that induces hallucinations, so there must be a sub-receptor of the
gaba system which does include hallucinations, since gaba agonists like zolpidem and
muscimol are extremely famous for inducing hallucinations and visual distortions alike.
- DrChemX -