Benzodiazepines and Acetylcholinesterase inhibition

[Jamshyd]

I was quickly looking up a benzo on wikipedia when I notice that several pages quote studies that show that benzos inhibit cholinesterase enzymes, particulary Temazepam, Nitrazepam, and Flunitrazepam.

What does everyone think (or know) are the ramifications of such actions?

 

[SynAmnesia]

OOhhh... Nifty. I may have to go back to using Temazepam for sleep.

Ach-ase inhibition can be kind of cool--in small amounts. I definitely read a paper where they gave a memory test, and then gave an anticholerigenic. After the anticholerigenic, people responded more poorly to the memory test. Then they gave them an Acetylcholeresterase inhibitor, and their memories went back to normal.

Having a bit of excess Ach floating around might help with memory. The effects are probably not profound enough to cause too many problems from excess ach around. People seem to do ok on Aricept--if they have alzheimers. Furthermore, nicotine is an Ach nicotinic receptor agonist, and that doesn't seem to cause to many problems.

However, I don't know how having increased memory from an Ach-ase inhibitor would balance with the long half life of temazepam, which causes memory problems in itself.

This is just speculation. I don't actually have much data to back this up. (except for the anticholerigenic, Ach-ase inhibitor experiment. I will find the paper when I get the chance.)

 

[Limpet_Chicken]

I can recall reading bits and pieces about intoxications with low-dose organophosphate nerve agents, and up to a certain low level, seemingly, soldiers tested were more accurate per shot fired in the tests, reaction time was up, and other performance related tasks were performed better.

It would make sense really, increasing ACh uptake is the main method of action of some nootropics, not exactly the same thing, but having more ACh acting, is more or less what happens in both cases.

Did the study say how potent the cholinesterase inhibition was? compared with things like say, physostigmine,rivastigmine, neostigmine, etc?

Perhaps at least it would help counteract some of the tendency to amnesia in either medical or low level recreational use? I don't see how it could hurt.

 

[vecktor]

all the experiments with reversal of scopolamine-hyoscine amnesia show that if you make peoples memory bad with scopolamine then it can be reverse to an extent using esterase inhibitors, or piracetam or 5ht6 agonists etc, there is little to suggest that in normal as in not poisoned subjects acetylchoinesterase inhibitors have any merit at all.
scopolamine makes you forgetful
things that partially reverse scopolamine make you more normal again. there are a shortage of models for amnesia especially in animals hence the use of amnesia inducing agents.

avoid taking scopolamine in the first place would be the best plan. :


V

 

[Limpet_Chicken]

Yeah, its nasty stuff on the whole, although with morphine, its nice.

Diphenhydramine seems to cause me a hell of a load of cognitive problems in even low doses, scopolamine doesn't, but I can't form a coherent thought after 50mg or so of diphenhydramine.

Not sure how they compare in anticholinergic potency though.

 

[shamus]

there is little to suggest that in normal as in not poisoned subjects acetylchoinesterase inhibitors have any merit at all.

Two AChesterase inhibitors, Huperzine-A & galatanine (sp?), generally get very good reports as nootropics.

 

[acetylcholine]

According to this abstract:

http://www.ncbi.nlm.nih.gov/pubmed/6133407

Clonazepam, Flunitrazepam, and Diazepam decrease release of acetylcholine in the cat brain.

Bummer.

This information was found through the Clonazepam wikipedia.

Jamshyd, do you have links to the source of the "inhibition of cholinesterase" information? I can't find any such info.

Also, the wiki on Diazepam has more disappointing information about decreased acetylcholine release in mice. Are you sure you didn't misread?

 

[ebola?]

all the experiments with reversal of scopolamine-hyoscine amnesia show that if you make peoples memory bad with scopolamine then it can be reverse to an extent using esterase inhibitors, or piracetam or 5ht6 agonists etc, there is little to suggest that in normal as in not poisoned subjects acetylchoinesterase inhibitors have any merit at all.
scopolamine makes you forgetful
things that partially reverse scopolamine make you more normal again. there are a shortage of models for amnesia especially in animals hence the use of amnesia inducing agents.

avoid taking scopolamine in the first place would be the best plan. :

Assuming all of the above empirical information is correct, would benzodiazapines themselves constitute a "poison" that hinders formation formation of long-term memories? Or is it that in this case, cholinergic memory-enhancement depends on cholinergic memory insults? If so, what's up with 5ht6 agonism proving useful (does it affect the cholinergic system downstream or something?)?

ebola

 

[morphiquet]

it seems that nearly all chemicals do possess ach-inhibitory effects, at least in the micromolar range (that means you have to ingest hundreds of mgs to grams of such compounds, very unlikely in the case of benzos)

btw, 5-ht6-agonists actually worsen memory skills, from what i've read.
ANTagonists are the sought drugs in this case.
they'd imo deserve an own thread, btw again.

 

[Hammilton]

Wasn't scopolamine the stuff the brazilians gave to their kidnapees to turn them into pliant subjects to make bank withdrawals?

It must leave motor function relatively uneffected then, correct?

 

[acetylcholine]

Wasn't scopolamine the stuff the brazilians gave to their kidnapees to turn them into pliant subjects to make bank withdrawals?

Yes.

It must leave motor function relatively uneffected then, correct?

At least a little. A criminal can still take advantage of someone even if they are hobbling around.

I was prescribed scopolamine after a concussion to relieve dizziness, nausea, and vertigo. It worked quite well, and I didn't notice any problematic side effects at the minuscule recommended dosage.