4DQSAR
Bluelighter
- Joined
- Feb 3, 2025
- Messages
- 5,498
@Syntherize - Good point well made. around here we have a hospital ward where alcoholics who pass out in public are sent to. In essence all the hospital does is to feed them Librium until their hand's stop shaking, give them something akin to Stoss therapy (huge doses of IV vitamins), feed them up and after 24 hours of observation, push them out of the door.
It's always sad to watch someone you care for drink themselves to death. Upsetting when it's someone young enough to be your own child. MGTG did just that and Tom was just a kid. We got him a TV, bought him food, took him to the cinema and other places where alcohol wasn't available & ensured he always had someone to phone 24/7 - but all we know is that on one Friday evening he bought 1.5L of cheap whiskey, drank the lot in a few hours and his body wasn't discovered until the following week. I believe it took a couple of white-lies to get the Police to perform a welfare check. His GF was in bits. Both were lovely people. I mean two of the nicest people it's ever been my privilage to know.
For many years there was a [P] benzodiazepine only used in Spain (bentazepam/Tiadiona™), similarly in Russia phenazapam (феназепама™) and in India eitzolam (Etilaam™) and from what I can gather, in each case the idea was that a pharmacist could suggest them for the treatment of alcoholism. I don't think for a moment that an inebirated person would ever be served. It seemed more like a concerned family member or friend could buy them on the basis that they wouldn't provide the patient more the stated dose. Certainly a friend who visited Spain related how they had to have the medicaton explained to them, provide ID and so on - I assume this was intended to prevent smurfing. A bit like how Valoid™ (cyclizine) was sold in the UK.
Now, I've never tasted phenazepam but I suspect onset is quite slow and it isn't much fun. The other two I have tasted and really cannot imagine anyone thinking them 'fun'. Again, can's speak for phenazepam but the other two both have a plateau dose i.e. taking more may increase duration but will not subjectively be 'stronger'.
In a better world clobazam would become a [P] medication. It's an odd one. Uniquely it's a 1,5-benzodiazepine; all the others are 1,4-benzodiazepines. So by defintion clobazam cannot bind to the α1 or α5 subunits. The former subunit being the target of the Z-drugs, both subunits being targetted by alcohol i.e. clobazam is no 'fun' at all if alcohol-like intoxication is the goal. But far more importantly, alcohol doesn't 'amplify' it's effects AND clobazam demonstrates a plateau at 40mg/day which is 20mg [BID] i.e. even if someone ate a whole box, it may sedate for many days but will not render them unconscious.
The LD50 of clobazam has been measured as 100mg/kg in canine models and 6,000mg/kg in rodent models. However you look at it, it's the safest benzodiazepine in use. In a study of patients with refractive epilepsy, so called 'supertheraputic' doses of clobazam were prescribed and from every metric, the patients prescribed 160mg/day were no more sedated/disoriented or liable to physical side-effects than the patent prescribed 40mg/day. The cohort size was 241 patients i.e. 80 were given a placebo, 80 were given the official maximum dose of 40mg/day and 81 given 160mg/day.
It's even the case that neither clobazam nor any 1,5-benzodiazepine would be attractive targets for someone developing novel RCs. It seems no amount of complex modification produces a compound much more potent than clobazam itself. I belive CP-1414S is no more potent than clobazam - it's simply more sedating, but more akin to how first-generation antihistamines sedate i.e. in no way pleasent.
It's always sad to watch someone you care for drink themselves to death. Upsetting when it's someone young enough to be your own child. MGTG did just that and Tom was just a kid. We got him a TV, bought him food, took him to the cinema and other places where alcohol wasn't available & ensured he always had someone to phone 24/7 - but all we know is that on one Friday evening he bought 1.5L of cheap whiskey, drank the lot in a few hours and his body wasn't discovered until the following week. I believe it took a couple of white-lies to get the Police to perform a welfare check. His GF was in bits. Both were lovely people. I mean two of the nicest people it's ever been my privilage to know.
For many years there was a [P] benzodiazepine only used in Spain (bentazepam/Tiadiona™), similarly in Russia phenazapam (феназепама™) and in India eitzolam (Etilaam™) and from what I can gather, in each case the idea was that a pharmacist could suggest them for the treatment of alcoholism. I don't think for a moment that an inebirated person would ever be served. It seemed more like a concerned family member or friend could buy them on the basis that they wouldn't provide the patient more the stated dose. Certainly a friend who visited Spain related how they had to have the medicaton explained to them, provide ID and so on - I assume this was intended to prevent smurfing. A bit like how Valoid™ (cyclizine) was sold in the UK.
Now, I've never tasted phenazepam but I suspect onset is quite slow and it isn't much fun. The other two I have tasted and really cannot imagine anyone thinking them 'fun'. Again, can's speak for phenazepam but the other two both have a plateau dose i.e. taking more may increase duration but will not subjectively be 'stronger'.
In a better world clobazam would become a [P] medication. It's an odd one. Uniquely it's a 1,5-benzodiazepine; all the others are 1,4-benzodiazepines. So by defintion clobazam cannot bind to the α1 or α5 subunits. The former subunit being the target of the Z-drugs, both subunits being targetted by alcohol i.e. clobazam is no 'fun' at all if alcohol-like intoxication is the goal. But far more importantly, alcohol doesn't 'amplify' it's effects AND clobazam demonstrates a plateau at 40mg/day which is 20mg [BID] i.e. even if someone ate a whole box, it may sedate for many days but will not render them unconscious.
The LD50 of clobazam has been measured as 100mg/kg in canine models and 6,000mg/kg in rodent models. However you look at it, it's the safest benzodiazepine in use. In a study of patients with refractive epilepsy, so called 'supertheraputic' doses of clobazam were prescribed and from every metric, the patients prescribed 160mg/day were no more sedated/disoriented or liable to physical side-effects than the patent prescribed 40mg/day. The cohort size was 241 patients i.e. 80 were given a placebo, 80 were given the official maximum dose of 40mg/day and 81 given 160mg/day.
It's even the case that neither clobazam nor any 1,5-benzodiazepine would be attractive targets for someone developing novel RCs. It seems no amount of complex modification produces a compound much more potent than clobazam itself. I belive CP-1414S is no more potent than clobazam - it's simply more sedating, but more akin to how first-generation antihistamines sedate i.e. in no way pleasent.
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