adder
Bluelighter
- Joined
- Mar 28, 2006
- Messages
- 2,851
Temazepam being one of the most "recreational" (whatever that means in the benzodiazepine derivatives class) - now that's an interesting opinion. I can be in minority here but I'm not in minority in my society. Google trade name "Signopam", they're 10mg temazepam tablets here. My grandma was prescribed this for ANXIETY after trauma, my mum was prescribed this for ANXIETY after trauma. And this wasn't once. Temazepam is also used in hypothyroidism so my grandma was prescribed it later because of it(I suffer from it myself, that's another story, look at increase in hypothyroidism, hyperthyroidism, and thyroid cancer in countries closest to then Ukrainian SSR where a catastrophe in Chernobyl Power Plant). The story is just that I was 14 and 20mg of temazepam just made me relaxed and that's all.
Firstly, let's a have a look at receptor binding of some of bezodiazepine derivatives:
alprazolam - 1.38 umol
clonazepam - 1.43 umol
flunitrazepam - 1.60 mol
lorazepam - 2.65 umol
estazolam - 4.73 umol, the next is bromazepam - 14.61 umol
diazepam - 32.67 umol
temazepam - 63.90 umol very sorry I can't find the source but IIRC the same values were presented here on the forums before.
That's about it (X umol - amount of substance needed to take the same effect). Temazepam may be marked as "hypnotic", it's hardly hypnotic for me but I'm not good as a guinea pig because of big tolerance overall, even zolpidem (non-benzodiazepine) has a higher binding affinity for bzp-receptors. Google it. Scholar-google it. Whatever. I went wikipedia, I didn't just look at sources, I clicked on links. This proves nothing. It's about toxicity. Well, Not long after my first experience with temazepam, I was taken to the hospital after taking a pack of it IIRC but wasn't my choice, I was just mad because I couldn't find something and there goes my dad. I was fucking fine, it was quite a long time since I took tabs so it all must have absorbed by the time I got to hospital. Well but that was when I was really benzo-naive person. Now I could eat an equivalent to 60mg of clonazepam I would be fine (or not if 2,4g of temazepam would be really toxic) just I like feel nothing after 40mg of estazolam and there were days estazolam was one of my favorites. It doesn't work anymore. Back to the topic:
Temazepam metabolism. There's no way 3-OH group is deattached as it is attached there in many cases of benzodiazepines that don't have it there. The only active metabolite may be oxazepam then (various sources don't even mention there is N-demethylation but if it happens in case of diazepam then I guess it happens here too). Now tell me a metabolite that is even weaker than the starter gives temazepam that superiority. Other metabolites are just conjugated compounds at 3 position, at 4' position (after 4'-hydroxylation).
If temazepam is so special, then lormetazepam should be "overspecial" because it's got 2'-chloro group and as we know any halogen at position 2' boosts activity and should make a simple 5-phenyl-1,4-benzodiazepin-2-one derivative more hypnotic. I saw no big differences between lorazepam and lormetazepam (the difference is a methyl group on nitrogen 1), lormetazepam was sadly weaker but still great, colors were bright (just like after lorazepam) but everything was darker. Why isn't lormetazepam "overspecial"? Now I've got something more worth than wikipedia's article:
Translated from http://www.mp.pl/leki/desc.php?id=755. Yes, you've got to have an access.
It's just a part about effects.
Short-acting, not cumulating in body bezodiazepine derivative with little affinity to the receptors. It shows hypnotic, anxiolytic and sedative effects, and also moderate anticonvulsant action, and weak muscle relaxing effects. [about benzodiazepines' mechanism of action - (...) a complex with GABA{A} receptors, benzodiazepine receptors and chlorine channels. By allosteric interaction with with GABA{A} receptors Benzodiazepine receptors cause opening of chlorine channels and increase infiltration of chloride anions into neurons. Benzodiazepine derivatives, acting through GABA-ergic system, increase depressant action of GABA in CNS, especially on limbic system, hypothalamus, and thamalus - just for the sake of clarity...]
Temazepam after p.o. administration is absorbed from GI tract well and quickly. About 8% of the dose goes through first-pass metabolism. Binds to proteins in 96-98%. T1/2 is on average 8,8h (3,5-18,4h). Metabolized mainly in the liver by conjugation with glucuronic acid, doesn't have active metabolites. In 80-90% excreted via kidneys, mainly as metabolites. Medicine doesn't cumulate in organism.
Yes, it's registered in Poland also as a hypnotic benzodiazepine to treat insomnia but also in hypothyroidism and a few other illnesses. But considering how weak it is, I see it prescribed by first-contact doctors for anxiety along Relanium 2mg or 5mg (diazepam).
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So what would be my explanation? Temazepam is very nice and mellow at the beginning, just like I said. If people have no access to other benzodiazepines, they abuse temazepam to a terrible extent. You don't have to remind me of guys injecting some extractions from tablets or gel-caps into their muscles.
After I finish some work now, I will give it a shot for benzodiazepines despite the fact I was to quit (yeah, I know, this is very general), chemistry, way of action etc. Standard procedure. Getting a 1,4-benzodiazepine ring isn't hard (if it were, some of users wouldn't show up with nimetazepam in bulk...) but STOP, here where it ends.
Look at gidazepam structure (must be on English wikipedia already). Do you really think it's active? It must be a compound similar to nordazepam but with bromine on position 7 instead of chlorine (electronegativity difference isn't big and trust me, I've seen guys taking 40mg of gidazepam, feeling nothing and bang, they got fucked up really and they're not little boys). I don't know if working on benzodiazepine derivatives is worth it, maybe a waste of time as there have been thousands of them synthesized already (but so morphine derivatives, too and it was worth it).
- - - - - - -
Concerning driving stuff... Look at me. What can I say? I have to drive to get to various places. I feel nothing after such a low dose of clonazepam and methadone but if I were stopped by some police jerks, the fact I had those substances in my system would play a huge role in the court.
- - - - - - -
EDIT:
I've just remembered I've got nordazepam and its 2'-chloro derivative, delorazepam in bulk. But it's been, say, 2 months since they were synthesized.
Anyone knows how long they can be kept without any degradation? Of course they're stored like things are stored in labs. And N-demethylated version of the widest used benzodiazepine derivative - diazepam - is a good starter for anything (despite easiness of 1,4-benzodiazepine synthesis like I said, I don't really feel like going from the beginning when I have something ready).
Firstly, let's a have a look at receptor binding of some of bezodiazepine derivatives:
alprazolam - 1.38 umol
clonazepam - 1.43 umol
flunitrazepam - 1.60 mol
lorazepam - 2.65 umol
estazolam - 4.73 umol, the next is bromazepam - 14.61 umol
diazepam - 32.67 umol
temazepam - 63.90 umol very sorry I can't find the source but IIRC the same values were presented here on the forums before.
That's about it (X umol - amount of substance needed to take the same effect). Temazepam may be marked as "hypnotic", it's hardly hypnotic for me but I'm not good as a guinea pig because of big tolerance overall, even zolpidem (non-benzodiazepine) has a higher binding affinity for bzp-receptors. Google it. Scholar-google it. Whatever. I went wikipedia, I didn't just look at sources, I clicked on links. This proves nothing. It's about toxicity. Well, Not long after my first experience with temazepam, I was taken to the hospital after taking a pack of it IIRC but wasn't my choice, I was just mad because I couldn't find something and there goes my dad. I was fucking fine, it was quite a long time since I took tabs so it all must have absorbed by the time I got to hospital. Well but that was when I was really benzo-naive person. Now I could eat an equivalent to 60mg of clonazepam I would be fine (or not if 2,4g of temazepam would be really toxic) just I like feel nothing after 40mg of estazolam and there were days estazolam was one of my favorites. It doesn't work anymore. Back to the topic:
Temazepam metabolism. There's no way 3-OH group is deattached as it is attached there in many cases of benzodiazepines that don't have it there. The only active metabolite may be oxazepam then (various sources don't even mention there is N-demethylation but if it happens in case of diazepam then I guess it happens here too). Now tell me a metabolite that is even weaker than the starter gives temazepam that superiority. Other metabolites are just conjugated compounds at 3 position, at 4' position (after 4'-hydroxylation).
If temazepam is so special, then lormetazepam should be "overspecial" because it's got 2'-chloro group and as we know any halogen at position 2' boosts activity and should make a simple 5-phenyl-1,4-benzodiazepin-2-one derivative more hypnotic. I saw no big differences between lorazepam and lormetazepam (the difference is a methyl group on nitrogen 1), lormetazepam was sadly weaker but still great, colors were bright (just like after lorazepam) but everything was darker. Why isn't lormetazepam "overspecial"? Now I've got something more worth than wikipedia's article:
Translated from http://www.mp.pl/leki/desc.php?id=755. Yes, you've got to have an access.
It's just a part about effects.Short-acting, not cumulating in body bezodiazepine derivative with little affinity to the receptors. It shows hypnotic, anxiolytic and sedative effects, and also moderate anticonvulsant action, and weak muscle relaxing effects. [about benzodiazepines' mechanism of action - (...) a complex with GABA{A} receptors, benzodiazepine receptors and chlorine channels. By allosteric interaction with with GABA{A} receptors Benzodiazepine receptors cause opening of chlorine channels and increase infiltration of chloride anions into neurons. Benzodiazepine derivatives, acting through GABA-ergic system, increase depressant action of GABA in CNS, especially on limbic system, hypothalamus, and thamalus - just for the sake of clarity...]
Temazepam after p.o. administration is absorbed from GI tract well and quickly. About 8% of the dose goes through first-pass metabolism. Binds to proteins in 96-98%. T1/2 is on average 8,8h (3,5-18,4h). Metabolized mainly in the liver by conjugation with glucuronic acid, doesn't have active metabolites. In 80-90% excreted via kidneys, mainly as metabolites. Medicine doesn't cumulate in organism.
Yes, it's registered in Poland also as a hypnotic benzodiazepine to treat insomnia but also in hypothyroidism and a few other illnesses. But considering how weak it is, I see it prescribed by first-contact doctors for anxiety along Relanium 2mg or 5mg (diazepam).
- - - - - - -
So what would be my explanation? Temazepam is very nice and mellow at the beginning, just like I said. If people have no access to other benzodiazepines, they abuse temazepam to a terrible extent. You don't have to remind me of guys injecting some extractions from tablets or gel-caps into their muscles.
After I finish some work now, I will give it a shot for benzodiazepines despite the fact I was to quit (yeah, I know, this is very general), chemistry, way of action etc. Standard procedure. Getting a 1,4-benzodiazepine ring isn't hard (if it were, some of users wouldn't show up with nimetazepam in bulk...) but STOP, here where it ends.
Look at gidazepam structure (must be on English wikipedia already). Do you really think it's active? It must be a compound similar to nordazepam but with bromine on position 7 instead of chlorine (electronegativity difference isn't big and trust me, I've seen guys taking 40mg of gidazepam, feeling nothing and bang, they got fucked up really and they're not little boys). I don't know if working on benzodiazepine derivatives is worth it, maybe a waste of time as there have been thousands of them synthesized already (but so morphine derivatives, too and it was worth it).
- - - - - - -
Concerning driving stuff... Look at me. What can I say? I have to drive to get to various places. I feel nothing after such a low dose of clonazepam and methadone but if I were stopped by some police jerks, the fact I had those substances in my system would play a huge role in the court.
- - - - - - -
EDIT:
I've just remembered I've got nordazepam and its 2'-chloro derivative, delorazepam in bulk. But it's been, say, 2 months since they were synthesized.
Anyone knows how long they can be kept without any degradation? Of course they're stored like things are stored in labs. And N-demethylated version of the widest used benzodiazepine derivative - diazepam - is a good starter for anything (despite easiness of 1,4-benzodiazepine synthesis like I said, I don't really feel like going from the beginning when I have something ready).
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