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Opinions - Severe chronic insomnia...rotation of antihistamine and GABA sleep drugs

Discussion in 'Downers and sleeping pills' started by Troppo, Feb 7, 2011.

  1. Troppo

    Troppo Titanium Member

    Reputation Points:
    Feb 17, 2010
    from Australia
    One of my friends suffers from chronic insomnia and has not found lasting relief from any treatments offered to him by doctors, since tolerance sets in if he tries taking a sleeping drug regularly (and he has found CBT and natural remedies ineffective).

    Then he had this idea...how about using a drug that sedates via antihistamine effects for several days, then stopping it and using another drug that sedates via effects on GABA receptors for several days. After that, go back to the antihistamine and do the same thing over again. His reasoning is that tolerance should not build up to either drug type, and cross-tolerance should not occur between them. Obviously dependence on having a drug of some sort to sleep each night will happen....but he considers this a fair price to pay in exchange for not having endless sleepless nights, daytime fatigue and irritability, and problems at work and in social situations due to extreme tiredness.

    My friend has found success using this method so far, although he has only been doing it a short while. He prefers short-acting drugs, so that next-day sedation is minimised, or at least wears off fairly quickly after getting up. Possible medications include:

    1) Antihistamine type--diphenhydramine, doxylamine, quetiapine (not sustained-release), some antidepressants (eg. sedating tricyclics, mirtazapine), although some of the antidepressants may be too long-acting.

    2) GABA-acting type--short acting benzodiazepines (eg. alprazolam, temazepam, oxazepam, triazolam), z-drugs (zolpidem, zaleplon, zopiclone, eszopicone).

    Other substances that aid sleep could be used to help, or to allow a break from these drugs...examples are melatonin, ramelteon, and L-tryptophan...although my friend has not yet tried these since starting his rotation idea. Some sedating short-acting anticonvulsants may also be effective as sleep aids but they may NOT be rotatable with the GABA-acting drugs due to being too similar in effects (ie. cross tolerance may occur)...examples may include pregabalin, gabapentin, and tiagabine (EDIT:rare possible risk of induced seizures with tiagabine)....they could be taken in place of the benzo or z-drug but my friend has also not tried this so far.

    Unfortunately this idea may not work very well if a person is already regularly taking other drugs that affect H1 histamine receptors such as sedating antidepressants or antipsychotics, or drugs that affect GABA receptors such as benzodiazepines taken regularly for anxiety (or alcohol). Naturally these important medications should not be stopped just to try this idea. Also it is extremely dangerous to abruptly stop benzodiazepines if a person is already dependent on them. Furthermore, alcohol, opiates, and other sedating substances should never be mixed with each other, due to the risk of severe or even lethal respiratory depression.

    My friend and I are both aware that this is a harm-reduction site, and so this post is not intended as a recommendation to anyone to start taking drugs or engage in self-treatment. It is intended for informational purposes only. Anyone suffering a medical problem should consult a doctor, and the dangers of potentially addictive medications like benzos must be fully understood. Any criticism of this idea is greatly welcomed, since my friend would be interested in knowing if he is heading into dangerous waters doing this!
    Last edited: Feb 7, 2011
  2. PsychoActivist

    PsychoActivist Palladium Member

    Reputation Points:
    Oct 28, 2008
    36 y/o from U.S.A.
    I like your idea and if one is able to do it correctly, it should work to keep their tolerance down especially with the GABA agonists.

    However, unfortunately, it seems that it would require quite a bit of patience and discipline.

    I have a bony pony named Peter. He suffers from severe chronic insomnia as well. I would like to note that he is Bi-polar. He also suffers from a LACK of patience and discipline. Especially when his insomnia is at it's worst. It becomes very irritating to him when he hasn't slept in 2 or 3 nights. His body and mind will reach a state of exhaustion and he will be able to feel it taking it's toll, but he will still have trouble falling asleep. When he reaches this point, he is willing to do just about anything to make it stop and slip away into dreamland. Several times, silly as it may sound, he has even contemplated trying to knock himself out.

    Point being, if he reaches this point and has access to a benzo script, he is going to take them, regardless of whether he has been taking them everyday or hasn't touched them in a month. If I REALLY want to get honest, he doesn't even have to reach that point. As I said he lacks discipline and if he has Benzo's or another GABAergic, he will end up rationalizing and justifying till he conjures up a reason to take them.

    Peter used to be prescribed Alprazolam (2 mg's three times daily) and 60 mg's Temazepam before bed (two 30 mg capsules). Of course, he certainly did not start out with doses this high, so tolerance most definitely WAS becoming an issue. This, for a while was the most effective treatment he ever had for his insomnia (and anxiety as a side note.) Unfortunately, he began to get way out of hand with his scripts until he would be lucky if he could make both bottles last a week.

    I understand that many people do not have this problem with benzo's or at least not to that extent. As I mentioned earlier, if your idea is done correctly it seems like it would be quite efficient.

    Though Peter the pony no longer takes benzo's he still uses a wide range of herbal supplements, OTC drugs, and other prescription drugs to try and combat his insomnia, most of which you have already mentioned. While he takes some of these in combination, he DOES alternate them. Not so much to avoid tolerance, as most of the stuff he takes now (which I will list in minute) doesn't seem to cause much of an increase in tolerance, but more-so to keep trying different combination's until he can establish which one works the best for him.

    For the past few years he has been working with:


    -Melatonin (currently he uses a Melatonin pill which also contains Theanine)
    -Passion Flower - Fresh bulk material - not capsules
    -Chamomile - Fresh flowers. (Fresh Chamomile and Passion Flower together make an EXCELLENT tea btw)
    -Kava Kava - Fresh (Occasionally)
    -Phenibut - Pure bulk powder (Occasionally)
    -Sceletium Tortuosum (Kanna) - Fresh plants (Occasionally)



    RX (Occasionally)

    -Quetiapine (Seroquel)
    -Olanzapine (Zyprexa)
    -Amitriptyline (Elavil)
    -Mirtazapine (Remeron)

    I will not get into too much detail about which combination's work better than others for Pony Pete. Most likely, anyone who attempted various combo's with these drugs would come up with a different answer. I will say though, The way he usually does it is, the first 4 herbs I have listed up there are taken pretty much every night regardless, and most of the time, in combination with ONE of the OTC antihistamines.

    Seldomly, he will add to or take by itself, one drug from the prescription category. He really does not like to take the Seroquel at all. He finds that it is a nasty drug with nasty side effects. The Zyprexa is quite similar, except the side effects are a little more tolerable to him.

    Peter used to have a prescription to Mirtazapine and he found it to be one of the only effective and even almost pleasant prescription drugs for combatting his insomnia. It's low abuse potential was very ideal for his situation and while he would describe it as rather pleasant, it didn't get him high or make him want to take more. Unfortunately He is broke and without a job or insurance right now ( I mean he is just a pony) so getting it again would be tough.

    This leaves the Amitriptyline in the bony pony's little RX category. If he must resort to any of the prescription drugs, this is usually what he goes for. It actually does help him sleep at times and while there are still some negative side effects, he finds them much more tolerable than the Seroquel and Zyprexa.

    I do believe you are correct there. I remember reading somewhere that there has been evidence of cross-tolerance between these drugs and Benzodiazepines.

    My pony said Gabapentin had absolutely no effect on him whatsoever. This would make sense with the cross tolerance, because he was put on Gabapentin about 2 months after he stopped taking his daily Alprazolam and Temazepam. He has never tried Pregablin or Tiagabine. He would like to though. He has heard that Pregablin is so much better than Gabapentin that there is just no comparison.

    As far as the antihistamines are concerned, I don't know if anyone else experiences this but as far as use as a sleep aid the dose can be very "hit or miss" for my horse (he's not a pony anymore. He has grown up since I started this post ;))What I mean by this is, particularly with Diphenhydramine, if he takes just a LITTLE to much, he can't fall asleep at all. He will feel the effects of the DPH but will lay in bed tossing and turning, unable to get comfortable.

    Oh and for the record, he didn't experience much of an increase in tolerance with Diphenhydramine. Only a light incline at first and then it seemed to plateau out. For one year of nightly use, he started out taking 25-50 mg's each night. After about a month or two he was taking 75 mg's and OCCASIONLY 100 mg's. But for the rest of that year and ever since, he has NEVER needed more than 100 mg's. Just thought that was kind of interesting.

    One final and very important thing I would like to touch on is exercise! This is crucial to the horse! He was at a point about 3 months after his bad bout with the benzo scripts, where he felt like he was just gonna give up all hope on any of the herbal supplements or OTC shit. They really did not work that well for him and still don't... alone. It used to piss him off so bad when his father or someone use to say to him "you just need some exercise, and you will be able to sleep easier". They were right though to an extent. While he still does not sleep like most people do, wearing himself out through physical activities makes a huge impact. Then he throws a little bit of supplements into the mix, and it makes a big difference. Certainly not perfect or sleeping normal, but a vast improvement.

    Okay... fuck.. I'm done! lol

    Keep us updated!

    Last edited: Feb 7, 2011
  3. Troppo

    Troppo Titanium Member

    Reputation Points:
    Feb 17, 2010
    from Australia
    Hey PA, thanks for the interesting read! My friend is interested in all ideas for treating insomnia. He agrees that the rotation idea could be difficult for anyone who has trouble regulating benzodiazepine use, and he is taking a lot of care to try and keep this under control. He has a history of alcoholism, so he has to be ultra careful with drugs such as benzos. He is hoping to find methods that don't even involve GABAergic drugs if possible.

    This guy remains interested in herbal treatments, and only gave up on them for a while because many sources don't seem to contain much active ingredient. This was the case with pills and capsules anyway. The ones you mentioned remain of interest but he would have to use fresh material as you suggested.

    Interesting comments about the prescription drugs...my friend had a similar experience to your horse's diphenhydramine experience, but it was with promethazine, a similar antihistamine (maybe longer acting). He managed to take it for 2 months, going up from 25 mg to 75-100 mg as required, when he wasn't drinking in the past.

    And yes exercise does help. He tries to get as much as he can these days. He says he'll also report back here later if/when he does any further "experiments" with medications for insomnia.