Limpet_Chicken
Bluelighter
I've been wondering about chlormethiazole a bit lately. What is the risk that as suggested for the Br/I substituted analogs that chlormethiazole itself might act as an alkylating agent? that 2-chloroethyl group is ugly and makes me a little uneasy about taking it too regularly as I have a longterm script for it, for insomnia along with loprazolam. Benzos are not particularly effective for me and whilst they can help stop me waking up continuously throughout the night they won't put me to sleep unless bloody stupid great doses are used, and the Z-drugs are in my experience completely and totally useless for sleep, although zopiclone is alright to change the flavour of an opiate nod a bit but that is about it.
Only viable alternatives for me are either chlormethiazole, or barbiturates, and the latter are on a named patient only basis here in the UK, other than AFAIK, phenobarb/primidone used for treating epilepsy when given in an outpatient setting, don't want to be on them either due to their AMPAr channel blocking properties.
Chlormethiazole seems to be quite similar in action at the GABAa receptor in terms of subunit selectivity to pentobarbital although the binding sites are not identical. Interestingly, a paper I read recently seems to suggest it binds at an anaesthetic binding site, as it reduces the effect of propofol.
Anyone know if as with the barbiturates, when used regularly tolerance rises without a corresponding rise in the LD:50 ? not really a concern for me personally, as despite having a rx for the stuff for nightly use, for as long as I want it I don't actually take it with anything like that frequency.
Leaving recreational use aside, its by far the most effective sleep aid acting on GABAergic systems in my experience with it, only alpha2 adrenoreceptor agonists (par)enterally have proven more effective in inducing and maintaining sleep. The freebase is funky stuff though, really odd smell to it, not the malignant, vile stench of the sulfur metabolite that hit me that time I went on a bender with it years ago, not pleasant though, tolerable, but certainly not delightful. And it melts plastic. The pharmacy keeps giving me my script in plastic pill bottles which is annoying, as if the capsules are stored for any considerable time some seems to diffuse through and start melting the bottle, I've had a bottles neck turn to goo once after some leaked out of a damaged cap, so I always transfer the entire lot into the one glass bottle I had from another pharmacy (which can now, irritatingly, apparently no longer source chlormethiazole)
Apparently the therapeutic index of chlormethiazole is particularly narrow. More likely than most sedatives for a significant OD to prove fatal. Does this include the barbs? An overdose on heminevrin is what killed keith moon from the band The Who. Its wikipedia, so the accuracy of the statement might be questionable, but of the 32 capsules taken, wikipedia states that just 6 opened in his stomach and proved sufficient to top him. Who knows what else was floating around in his bloodstream....quite possibly there might have been blood in his alcohol stream, as I've taken that many before, and I really don't weigh much at all (built up the dose, due to being aware of the aforementioned narrow TI) and it didn't feel at all threatening. Likewise, I'm on 90mg of oxy per day, and 1-2x192mg capsules doesn't seem to vastly increase respiratory depression.
Only viable alternatives for me are either chlormethiazole, or barbiturates, and the latter are on a named patient only basis here in the UK, other than AFAIK, phenobarb/primidone used for treating epilepsy when given in an outpatient setting, don't want to be on them either due to their AMPAr channel blocking properties.
Chlormethiazole seems to be quite similar in action at the GABAa receptor in terms of subunit selectivity to pentobarbital although the binding sites are not identical. Interestingly, a paper I read recently seems to suggest it binds at an anaesthetic binding site, as it reduces the effect of propofol.
Anyone know if as with the barbiturates, when used regularly tolerance rises without a corresponding rise in the LD:50 ? not really a concern for me personally, as despite having a rx for the stuff for nightly use, for as long as I want it I don't actually take it with anything like that frequency.
Leaving recreational use aside, its by far the most effective sleep aid acting on GABAergic systems in my experience with it, only alpha2 adrenoreceptor agonists (par)enterally have proven more effective in inducing and maintaining sleep. The freebase is funky stuff though, really odd smell to it, not the malignant, vile stench of the sulfur metabolite that hit me that time I went on a bender with it years ago, not pleasant though, tolerable, but certainly not delightful. And it melts plastic. The pharmacy keeps giving me my script in plastic pill bottles which is annoying, as if the capsules are stored for any considerable time some seems to diffuse through and start melting the bottle, I've had a bottles neck turn to goo once after some leaked out of a damaged cap, so I always transfer the entire lot into the one glass bottle I had from another pharmacy (which can now, irritatingly, apparently no longer source chlormethiazole)
Apparently the therapeutic index of chlormethiazole is particularly narrow. More likely than most sedatives for a significant OD to prove fatal. Does this include the barbs? An overdose on heminevrin is what killed keith moon from the band The Who. Its wikipedia, so the accuracy of the statement might be questionable, but of the 32 capsules taken, wikipedia states that just 6 opened in his stomach and proved sufficient to top him. Who knows what else was floating around in his bloodstream....quite possibly there might have been blood in his alcohol stream, as I've taken that many before, and I really don't weigh much at all (built up the dose, due to being aware of the aforementioned narrow TI) and it didn't feel at all threatening. Likewise, I'm on 90mg of oxy per day, and 1-2x192mg capsules doesn't seem to vastly increase respiratory depression.
