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Homotaurine for benzo/z-drug recovery

homotaurine benzo withdrawal z-drug benzo

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#1 Daniel Cooper

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Posted 18 February 2018 - 03:56 PM


I'm 31 months post quitting long term prescribed z-drug (eszopiclone) use and still having issues.

 

As hard as it seems to believe, I think my gaba receptors are still downregulated, decoupled, etc. etc.  A dose of picamilon will back out the worst symptoms (anxiety, fast heart rate, etc) temporarily but that is clearly not a long term solution and it's something I try rarely (a handful of times in the last 31 months).

 

I've tried the standard things to speed recovery - exercise, meditation, bacopa, ashwagandha, etc. to no effect.

 

I was wondering about homotaurine.  I hear some people promote it for benzo recovery, but that surprises me somewhat in that it antagonizes GABAB and I believe that benzos and z-drugs work on GABAA.

 

Anyone with any knowledge?  How about a source for homotaurine?

 

 

 

 



#2 tunt01

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Posted 18 February 2018 - 04:09 PM

If you go look in one of the Alzheimer's threads started by Turnbuckle, there is a discussion about EPPS or HEPPS, which seems to be chemically very similar to homotaurine.  This study shows GABA release inhibition in Alzheimer's mouse model (Figure 5).  They don't really have a control with EPPS, but presumably it has some effect level.  

 

Kim, H., Kim, H., Jo, S., Lee, C., Choi, S., Kim, D., & Kim, Y. (2015). EPPS rescues hippocampus-dependent cognitive deficits in APP/PS1 mice by disaggregation of amyloid-β oligomers and plaques. Nature Communications6(1). doi:10.1038/ncomms9997

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#3 Daniel Cooper

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Posted 18 February 2018 - 04:16 PM

Yeah, I'm in that thread.

 

I don't think taurine or EPPS is going to do much for benzo/z recovery.  We're not trying to dissolve amyloid plaques here, we're trying to repair damaged GABA receptors.

 

Taurine is touted to help and I've tried it and not had any smashing success.  Homotaurine seems to be unique in that it antagonizes GABA B receptors while also being anxiolytic which is a hell of a combination.  It's obvious to me that if you were a GHB user this would be great since GHB works on GABA B receptors.  However, I see people touting homotaurine for benzo recovery and it's not as obvious that this would be effective since benzos and z-drugs work on GABA A receptors.  Maybe there is some sort of cross action that I don't understand.

 

 

 



#4 airplanepeanuts

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Posted 18 February 2018 - 09:50 PM

I wanted to check out homotaurine but I haven't found a single positive review/ experience online, so I didn't.


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#5 Daniel Cooper

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Posted 19 February 2018 - 01:45 AM

Good to know.  The more I research this compound the less promising it looks for my application.

 

 

 



#6 BioHacker=Life

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Posted 20 March 2018 - 03:35 AM

flumazenil would be your best bet. It has over 4 studies in benzo PAWS.



#7 Daniel Cooper

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Posted 20 March 2018 - 03:38 AM

The problem with flumazenil is that it has an incredibly short half life - about 15 minutes. 

 

You really need to soak your GABA receptors in this stuff nearly continuously for a protracted period of time.  Minimally weeks but more likely months.  As a practical matter you'd probably have to do a port and some wearable pump or an implantable pump.  There's a clinic in Australia doing the latter but a fairly expensive proposition.  

 

 

 



#8 BioHacker=Life

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Posted 20 March 2018 - 03:54 AM

The problem with flumazenil is that it has an incredibly short half life - about 15 minutes. 

 

You really need to soak your GABA receptors in this stuff nearly continuously for a protracted period of time.  Minimally weeks but more likely months.  As a practical matter you'd probably have to do a port and some wearable pump or an implantable pump.  There's a clinic in Australia doing the latter but a fairly expensive proposition.  

 

That's not really an issue for the studies you just have to dose it accordingly. 15 mins apart 5 doses total is what some reaearch used and was effective for PAWS. Why weeks or months? Based on? You don't have to iv it either you can use it topically or sublingual. I'll do dosing mine tomorrow.

 

 

Eur J Pharmacol. 1986 Dec 2;132(1):31-8. Periodic benzodiazepine antagonist administration prevents benzodiazepine withdrawal symptoms in.

" Every third day administration of the benzodiazepine antagonist, Ro15-1788, during a similar period of continuous diazepam exposure, significantly decreases withdrawal behaviors."

" It is postulated that physical dependence reverts to a drug naive state after each exposure to the benzodiazepine antagonist. This treatment may represent a possible therapeutic approach for preventing the (time dependent) development of physical dependence and the accompanying severe withdrawal symptoms."

 

 

 

 

 

 

https://www.ncbi.nlm...pubmed/22291380

 

 

J Psychopharmacol. 1992 Jan;6(3):357-63. doi: 10.1177/026988119200600303.

A pilot study of the effects of flumazenil on symptoms persisting after benzodiazepinewithdrawal.

 

The potential of the benzodiazepine antagonist flumazenil (Ro 15-1788) to lessen persisting benzodiazepine withdrawalsymptoms was demonstrated in 11 patients who had been drug free for between 1 month and 5 years. Doses ranging from 0.2 to 2.0 mg divided into three intravenous injections over a few hours relieved long-standing symptoms to varying extents. These included clouded thinking, tiredness, muscular symptoms such as neck tension, cramps and shaking and the characteristic perceptual symptoms of benzodiazepine withdrawal, namely, pins and needles, burning skin, pain and subjective sensations of bodily distortion. Mood disorder, when present, also improved but the reduction in anxiety and depression may have reflected relief of physical symptoms. The onset of maximum response was sometimes delayed by as much as a day but was usually prompt. Side effects were reported to be either absent or typically described as lightheadedness or dizziness, lasted only a few minutes and were usually well tolerated. The benefits last between a few hours and several days despite flumazenil's otherwise short duration of action. However, symptoms did return to varying degrees in most cases, suggesting the need for repeated doses.

 

 

Pharmacol Biochem Behav. 2010 Aug;96(2):148-51. doi: 10.1016/j.pbb.2010.04.023. Epub 2010 May 6.

Reduction of aggression during benzodiazepine withdrawal: effects of flumazenil.

 

Benzodiazepine withdrawal has been associated with hostile and aggressive behavior. The benzodiazepine antagonist flumazenil has reduced, increased or not affected hostility and aggression in animal and human studies. In the present study we analyzed data collected in a placebo-controlled study of the effects of the benzodiazepine antagonist flumazenil in patients previously treated for benzodiazepine dependency, and healthy controls. The aim was to analyze the effects of flumazenil on hostility and aggression. Ten patients and 10 controls received, on two separate occasions, cumulative doses of flumazenil (0.05, 0.1, 0.25, 0.5 and 1mg at 15min intervals) or placebo. Withdrawal symptoms were rated after each injection. Patients had been free from benzodiazepines for 47 (4-266) weeks on the first occasion. A three-way interaction (groupxtreatmentxdose) was found, and was explained by: 1) patients rating aggression and hostility higher than controls at all times during placebo, while 2) during the flumazenil provocation i) the initial significant difference between patients and controls was no longer significant above the 0.5mg dose, and ii) patients rated aggression and hostility significantly lower above the 0.5mg dose compared to base-line. The results suggest that self-rated aggression and hostility in patients treated for benzodiazepine dependency was reduced by the partial benzodiazepine agonist flumazenil.

 

 

Addict Biol. 2002 Oct;7(4):385-95.

Intravenous flumazenil versus oxazepam tapering in the treatment of benzodiazepine withdrawal: a randomized, placebo-controlled study.

 

Flumazenil (FLU), a benzodiazepine (BZD) partial agonist with a weak intrinsic activity, was previously found unable to precipitate withdrawal in tolerant subjects submitted to long-lasting BZD treatment. The potential use of FLU to treat BZD withdrawal symptoms has also been evaluated tentatively in clinical studies. In the present experiment, FLU (treatment A) was compared with oxazepam tapering (treatment B) and placebo (treatment C) in the control of BZD withdrawal symptoms in three groups of BZD dependent patients. Group A patients (20) received FLU 1 mg twice a day for 8 days, and oxazepam 30 mg in two divided doses (15 mg + 15 mg) during the first night, oxazepam 15 mg during the second night and oxazepam 7.5 mg during the third night. FLU was injected i.v. in saline for 4 hours in the morning and 4 hours in the afternoon, in association with placebotablets. Group B patients (20) were treated by tapering of oxazepam dosage (from 120 mg) and with saline solution (as placebo) instead of FLU for 8 days. Group C patients (10) received saline instead of FLU and placebo tablets instead of oxazepam for 8 days. FLU immediately reversed BZD effects on balance task and significantly reduced withdrawal symptoms in comparison with oxazepam and placebo on both self-reported and observer-rated withdrawal scales. The partial agonist also reduced craving scores during the detoxification procedure. In addition, during oxazepam tapering, group B patients experienced paradoxical symptoms that were not apparent in FLU patients. Patients treated with FLU showed a significantly lower relapse rates on days 15, 23 and 30 after the detoxification week. Our data provide further evidence of FLUs ability to counteract BZD effects, control BZD withdrawal and normalize BZD receptor function. The effectiveness of FLU may reflect its capacity to upregulate BZD receptors and to reverse the uncoupling between the recognition sites of BZD and GABA, on the GABA(A) macromolecular complex, that has been reported in tolerant subjects.

 

Psychopharmacology (Berl). 1997 May;131(2):153-60.

Effects of flumazenil in the treatment of benzodiazepine withdrawal--a double-blind pilot study.

 

Flumazenil, a partial benzodiazepine agonist with low intrinsic activity, was tested for potential use in patients experiencing withdrawal symptoms after traditional treatment for benzodiazepine dependency. On two occasions, separated by 1-13 weeks, ten patients treated for benzodiazepine dependency and ten controls received cumulative doses of flumazenil (0.05, 0.10, 0.25, 0.50 and 1.00 mg at 15-min intervals) or placebo, with assessments of withdrawal symptoms and physiological variables after each dose. As expected, there was an overall difference between patients and controls, with patients scoring higher on negative and somatic items and lower on positive psychological items. Flumazenil reduced symptoms thought to be important in withdrawal in patients treated for benzodiazepine dependency. In contrast to the patient group, controls reacted in the opposite direction with increases in negative experience when given flumazenil. Further research may develop flumazenil as a therapeutic option in the treatment of benzodiazepine withdrawal.


Edited by BioHacker=Life, 20 March 2018 - 03:55 AM.


#9 Omega 3 Snake Oil

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Posted 02 October 2018 - 03:00 AM

I'm looking at ordering from this place: http://www.homotauri...omotaurine.html

Did anyone end up trying it? I seem to have GABA receptor problems but not from drug use, from something neurodegenerative. 



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#10 John250

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Posted 02 October 2018 - 04:32 PM

Seems like homotaurine is beneficial for dopamine repair as well.





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