7 replies to this topic

[connorphenix]

Okay, hopefully somebody can explain this but when it comes time to sleep (which is hard most nights) I take a small dose beta blocker with a small dose benzo with a few beers, just to get to sleep. I realize that I had to keep increasing the amounts of each so I backed off and went sleepless a couple days. One day example is today. I got 2 hours of sleep, and one of the best herbs for me is Skullcap. I'm out. I noticed 5-HTP makes me sleepy and is serotonin exhibiting, but SAM-e makes me feel well but offers nothing in regard to sleep.

So are there any daytime things to take to 'desensitize' my night time problems? GABA-A-B-orC antagonists, that might make everything 'right' at night?

I realize the Beta B+benzo+alcohol IS dangerous, but it really doesn't sedate me well, to be honest.

[KimberCT]

Beta blockers always give me insomnia. Alcohol, followed by benzos, are probably the worst things to use for sleep. Skullcap is a weak benzo.

When I was coming off alprazolam and had horrible insomnia, I used doxylamine to knock myself out. Cyproheptadine works very well too and doesn't leave you groggy the next morning.

[medievil]

I wonder wheter ultra low doses of flumazenil combined with a benzo would inhibit tolerance, just like this works with naltrexone and an opiate.

[outsider]

Can someone explain to me why benzodiazepines are still in use today since they all produce tolerance hence more problems when you stop taking them ? (see rebound stress)

[medievil]

Can someone explain to me why benzodiazepines are still in use today since they all produce tolerance hence more problems when you stop taking them ? (see rebound stress)

Because there arent many good options, some people really need them. (They also work in the long run in many cases even when being dependend on them).

But yeah they shouldnt be taken to just manage a bit of stress.

Edited by medievil, 14 May 2010 - 10:09 AM.

[Guacamolium]

Skullcap is more of a weak Barbie, from what I remember from its constituents. Has a hangover effect but is better overall than most herbals I've tried for sleep. Actually, now that I think about it, skullcap is the best herbal sleep aid I can think of.

Two tips: Eat your last meal earlier in the day, even if it's 45 minutes earlier. Your blood sugars should be down more by that time. Also, replace your beta blocker (with your doctors advice) with garlic. It takes a while to kick in though, so plan ahead!

About actually desensistizing GABA receptors, maybe just through serotonergic alliance, keep trying serotoninergics I guess, but you definitely don't want to go the glutamatergic route to solve your problem.

The glutamatergic system is fraught with peril and one simply cannot travel its paths without certain danger!!


(you'd think I was a D&D freak or LOTR, but no, I'm not)

[Lestat Rett]

Just in case anybody else continues to miss this.

Blocking the effect of GABA is exactly the OPPOSITE of what is wanted here.

GABAa antagonists are mostly highly anxiogenic, most are convulsants, at least, inverse agonists are, notable examples are picrotoxin, pentetrazol, and bicucculine on the part of inverse agonists, these cause anxiety at very low doses, and seizures at more than tiny doses.

There are SOME antagonists at GABAa that apparently display nootropic properties (due to enhancing ACh release) while being devoid of convulsant activity, these are usually weakish partial inverse agonists at the alpha5 subunit containing, benzodiazepine-sensitive GABAa subtypes while having agonist or partial agonist activity at alpha-3 or alpha-1 subunit expressing receptors.


Sedative wise, only one I have ever found to be without unnacceptable side effects are alpha-2 adrenoreceptor agonists like clonidine, although its long acting and can leave a hangover, I use tizanidine nightly (rectally) and it puts me out for the count within a few minutes without fail, nonaddictive, and seems to form relatively little tolerance even over fairly extended periods.

[Guacamolium]

Oh, and a histamatergic powerhouse - ketotifen fumarate. Just google it and read up on it. It's cheap like other anti-histamines, but I think is the strongest out there that is commonly available. Might knock you out too much, but better than increasing your gabaergics causing more downregulation and that popular rubber-band snap of glutamatergic response after the GABA receptors start to unwind halfway through the night.

This may give your gabaergic system the up-regulation it needs.