August 8th, 2016: Understanding and Remembrance Day for Severe Myalgic Encephalomyelitis
Jody Smith joins with other ME voices in honor of Understanding and Remembrance Day for Severe Myalgic Encephalomyelitis.
Discuss the article on the Forums.

rotating gaba receptor agonists to prevent tolerance

Discussion in 'Sleep' started by drew, May 16, 2015.

  1. drew

    drew

    Messages:
    47
    Likes:
    4
    Will using various gaba receptor agonists once a week prevent tolerance build up for all medications that upregulate the gaba receptors? In other words, will using phenibut increase my tolerance to Xyrem and Baclofen becuase they are all gaba receptor agonists?

    I was considering using each of the following gaba receptor agonists once a week to prevent tolerance and limit long term side effects: Phenibut, Xyrem, and Baclofen (10mg). I was also considering using Ambien CR on the other days Lunesta.

    Are there any safety concerns using one gaba receptor agonist one day and another one the next day?

    I don't have CF I'm just a really poor sleeper: 0.5% SWS, 11.6% REM
    EEG arousal CAP count = 19; CAP index = 3.8
     
  2. adreno

    adreno PR activist

    Messages:
    4,704
    Likes:
    9,766
    If you use compounds with the same mechanism of action, there will be overlap in tolerance induction.
     
    Thinktank and leokitten like this.
  3. minkeygirl

    minkeygirl But I Look So Good.

    Messages:
    4,678
    Likes:
    4,639
    Left Coast
    @drew I take several benzos and Z drugs. Halcion, Ambien, oxazepam, gerodorm and phenibut. I never take the same thing more than 2 days in a row.

    I use them to initiate sleep but also use otc antihistamines, trazodone, kava, zanaflex, seroquel, doxepin, Passion flower and suntheanine to sustain sleep. I do not take any of those more than 2 nights in a row except trazodone.

    Phenibut says on the bottle not to take it more than 3 days in a row so be careful with that.

    On the advice of @heapsreal i also take Dextromethorphan (ingredient in tussin DM) which is supposed to help with tolerance.

    I've been doing this almost a year and have not had any problems with tolerance.

    I have tried to sleep with no benzos to give myself a break but I cannot sleep at all without a benzo to initiate it.
     
    Last edited: May 16, 2015
    meeKO, catly and Countrygirl like this.
  4. leokitten

    leokitten Senior Member

    Messages:
    579
    Likes:
    1,874
    Maryland
    Stay away from z-drugs, ie Ambien, Lunesta. They work just like benzos and have all the same long term disastrous effects.

    http://en.m.wikipedia.org/wiki/Effects_of_long-term_benzodiazepine_use

    Xyrem and Baclofen work on GABA differently (on GABA-B instead of GABA-A which benzos and z-drugs agonize) and have slightly less addictive potential and somewhat fewer long term negative effects but they are still going to cause you problems, all GABA agonists are only meant to be taken short term.

    Before going for hardcore pharma and also since you don't have ME/CFS I would recommend working on other aspects of your health and lifestyle first.

    Do you exercise regularly? If not you should and try to do fairly vigorous exercise it really helps with sleep. Are you overweight or have a bad diet with a lot of sugar and bad foods? Do you drink/take a lot of stimulants? If so these should all be examined and improved. Do you have bad sleep hygiene? Have you gone to the doctor and examine other causes of poor sleep, such as endocrine abnormalities? There are so many things that can be improved.

    Also there are so many other sleep meds that are not GABA agonists that you could try? Especially there are certain classes that increase SWS which we all want and many indirectly increase GABA without all the nasty long term effects of GABA agonists. These classes are:
    • 5-HT2A antagonists (e.g. trazodone, remeron)
    • GAT-1 reuptake inhibitors (e.g. tiagabine)
    • α2δ ligands (e.g. gabapentin, pregabalin)
    • MT1 agonists (e.g. rozerem)
    • alpha-2 agonists (e.g. clonidine, guanfacine)
     
  5. minkeygirl

    minkeygirl But I Look So Good.

    Messages:
    4,678
    Likes:
    4,639
    Left Coast
    Yes ambien is a Z drug and it is probably worse than benzos in side effects with long term consistent use. However if you alternate them and are responsible then you should be ok. There aren't that many short acting benzos so Z drugs are an alternative that some of us have to use.

    As for the other meds Leokitten mentioned, here are my thoughts.

    • Gabapentin and pregabalin have some serious side effects including major weight gain and not necessarily any better than a benzo.
    •Trazodone is not necessarily a sleep initiator
    •Rozarem works like melatonin. If melatonin doesn't work this won't and it takes weeks for this to take effect.
    •clonidine is a blood pressure medication and needs to be used cautiously if you have cardiac issues.
    •gabatril very expensive and basically the same as gabapentin

    @drew If you are careful and alternate then you minimize your risk. It is ultimately up to you. It appears you understand the downsides. People who don't have epic insomnia just don't understand the need for benzos. I fought taking them for months because it took me a long time to get off klonopin. But finally, after not sleeping, I had to take them. I will not sleep without them.
     
    olegsel, josephine2 and catly like this.
  6. drew

    drew

    Messages:
    47
    Likes:
    4
    I used to exercise 5-6 days a week very rigorously but recently discovered that I have low cortisol and hypothyroidism which I'm addressing before resuming my workouts. I've been doing tai chi when I have the energy.

    I'm on a low lectin, epi-paleo diet, don't drink alcohol, drink lots of water, bone marrow broth in the morning, no stimulants, take supplemets that increase ATP in the morning like PQQ, MitoQ, NAD+, creatine, etc, try to get some sun every day, try to eat lots of DHA (ie live oysters, cold-smoke salmon, lamb chops).

    sleep hygiene: dark, cool room, white noise machine, magnetical sleep pads, fasting after 6pm, TD magnesium, pre bed meal consists of magnesium calm, 5g ghee, 5g trehalose. 5g glycine, honey, l-theanine, uridine, one egg

    anxiety reducers: low stress job, acupuncture 3 times per week, tai chi several times a week, meditation

    I've been a poor sleeper since I was a kid.

    trazodone can lead to pripism so I won;t touch that
    remeron I was considering once or twice a week but it leads to weight gain
    gabapentin and pregabalin decreases spermcount, cause ED, and is antiandrogenic
    rozerem is melatonin and it does not keep me asleep

    I'll have to research alpha-2 agonists as I don;t know anything about them. However, I have low blood pressure as it is so I don;t think this med would be appropriate. Thanks

    So I guess I'm left with rotating Phenibut, xyrem, remeron, and baclofen
     
    Last edited: May 17, 2015
    searcher likes this.
  7. leokitten

    leokitten Senior Member

    Messages:
    579
    Likes:
    1,874
    Maryland
    None of those side effects happen in most people, everything you mention are very rare side effects. Trust me I know because I take or have taken the meds you think will cause you ED, priapism, low spermcount, etc. None of those things ever happened to me.

    Do you want me to list for you the long list of side effects and long term effects of xyrem (which is really just GHB), Baclofen, and phenibut? They are way worse than trazodone and gabapentin.

    For example in addition to the well known dangers and side effects of GHB, it is possible that at even low doses it is neurotoxic:

    Neurotoxic effects induced by gammahydroxybutyric acid (GHB) in male rats.

    Rozerem is not melatonin, it's an MT1 agonist with a much longer half life than melatonin and thus more potent. I mentioned this class of drugs because they are good to use in combination with other meds.

    And you don't mention your aversion to GAT-1 reuptake inhibitors? Tiagabine is an excellent sleep med.
     
  8. drew

    drew

    Messages:
    47
    Likes:
    4
    @leokitten

    Are Gaba reuptake inhibitors more safe than GABA agonists?
     
  9. leokitten

    leokitten Senior Member

    Messages:
    579
    Likes:
    1,874
    Maryland
    Yes
     

See more popular forum discussions.

Share This Page