Ritanserin Restores Energetic Function (metabolism) During The Night

Discussion in 'Scientific Studies' started by haidut, Jun 29, 2016.

  1. haidut

    haidut Member

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    I wanted to post this study as a separate thread as it caught my eye with its obvious relevance to Peat's views on sleep and metabolism. The restorative slow wave sleep (SWS) is highly dependent on metabolism and disturbances in oxidative metabolism immediately manifest in SWS. As such, SWS disturbances in SWS have been observed in pretty much all chronic conditions (especially psychiatric ones) and the aging process in general. It seems that ritanserin is able to reverse the disturbances in SWS by improving metabolism during the night.

    Does ritanserin, a potent serotonin-S2 antagonist, restore energetic functions during the night?
    http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1290899/pdf/jrsocmed00173-0013.pdf

    "...As to sleep related to illness, and more particularly psychiatric illness, Hawkins et al.10 suggested that sleep may protect against depression and that if the individual sleep mechanisms work less well, the subject may be more susceptible to depression on the one hand, and attacks may be more severe on the other hand. In this context, it is stated that depression tends to be more frequent and more severe with aging."

    "...A first exploratory polygraphic sleep study in 4 volunteers has been undertaken by De Clerck in the Netherlands (in preparation). The results were very surprising: SWS increased, Stages 1 and 2 decreased. Moreover, subjects reported an improvement in sleep quality and sleep depth. In a randomized placebo-controlled crossover sleep study in 9 subjects in Great Britain, 10 mg ritanserin given either in the morning or in the evening was compared with 5 mg nitrazepam32. The polygraphs were scored blind. As expected, nitrazepam reduced REM and SWS. Ritanserin again significantly increased SWS after both morning (+ 97%) and evening administration (+ 70%), the morning dose being significantly more potent than the evening dose (Figure 1). The significance of this doubling of SWS was observed on an individual basis. Ritanserin did not affect wakefulness or Stage 1 parameters or sleep onset latency. Seven healthy male volunteers took 10 mg ritanserin each morming for 14 days and its effects on sleep were measured on the 1st, 7th, 13th and 14th night. Baseline data were collected on the two nights immediately prior to the start of ritanserin administration. Data on the sleep stages are given in Table 1. The effects on sleep of a subehronic administration of ritanserin were found to be similar to those observed in the previous study after single doses. These findings have been confirmed in a subsequent double-blind placebo-controlled crossover study conducted by Clarenbach in Germany (personal communication). Ritanserin 10 mg administered over a 10-day period to 7 healthy male volunteers increased SWS to an important extent, whilst the latencies to Stage 2, Stages 3 & 4 and REM did not differ significantly from placebo."

    "...If the assumption that SWS is important because of its restorative function is true, beneficial effects from ritanserin treatment should be expected in patients with the following symptoms: sleep disturbances, chronic tiredness, feelings of inadequacy, decreased effectiveness, decreased attention, social withdrawal, loss of interest, irritability, inability to respond to praise or reward, decreased activity, and pessimism. There are at least two clinical situations in psychiatry in which these symptoms are present to a greater or lesser extent: in patients with 'dysthymic disorder', with their typical complaints of apathy, lack of drive, anxiety and depressive mood; and in chronic schizophrenic patients with anergy and predominantly negative symptoms."

    "...Neurophysiological studies on human sleep have provided evidence of the drastic increases of SWS induced by the S2 antagonist ritanserin 32 33. In addition, subjects reported an improvement in sleep quality and sleep depth. It is attractive to speculate that the increase of SWS might explain the increased level of energy observed in patients with a variety of psychiatric disturbances in whom symptoms of dysthymia are present. Ritanserin may help to restore energetic functions during the night, resulting in an improvement of a number of symptoms related to anergy and in normalization of affective states."

    Btw, it looks like famotidine may also be useful as an OTC sleep aid that improves bioenergetics during the night.
    "...Radulovacki et al. found that adenosine elevated SWS and reduced waking time in rats. Nicholson et al."9 stated that H,-antagonism may reduce wakefulness, H2-antagonism may increase slow-wave activity and that these effects imply a complementary role of the H, and H2 systems in the control of the sleep process. Inoue & Borbely20 reviewed the role of endogenous sleep substances, including a number of polypeptides."
     
  2. ecstatichamster

    ecstatichamster Member

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    people take bromocriptine in the morning due to dopamine affect and circadian rhythms. In these studies do they administer ritanserin at night?
     
  3. Koveras

    Koveras Member

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  4. ecstatichamster

    ecstatichamster Member

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    duh, thank you!
     
  5. A.Dosko

    A.Dosko Member

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    @haidut for some reason its not showing it in the idealabs store?
     
  6. Ras

    Ras Member

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  7. GAF

    GAF Member

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    For my upcoming experiment, I am going to dose both the male rat and his partner rat so both get better sleep and neither one becomes a bother to the other, if you know what I mean. Only makes sense because if one of the rats is all pumped up and the other is limp there might not be a happy ending to the relationship.
     
  8. keith

    keith Member

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    @haidut I am curious if you have any thoughts about ritanserin and sleep apnea. I found a couple of studies that seem to contradict each other, if I'm reading them right, which is far from a given:

    The effects of serotonin antagonists in an animal model of sleep-disordered breathing. - PubMed - NCBI
    Chronic upper airway obstruction induces abnormal sleep/wake dynamics in juvenile rats. - PubMed - NCBI

    They are both small, animal model studies, so may not be applicable anyway, but I know your are much better at reading these, and I thought you might have some other thoughts anyway. If so, I would appreciate whatever you can share.
     
  9. OP
    haidut

    haidut Member

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    Most of the cases of sleep apnea I have seen were due to low CO2 (confirmed by multiple blood tests). As soon as these people upped their sugar and vitamin B1 intake their symptoms went away. Some people tried lower dose acetazolamide (250mg) and that solved it too. Some people found breathing in a paper bag also helped but the results were not as consistent as with thiamine and acetazolamide. So, anti-serotonin drugs may help bu I think addressing the low CO2 more directly would be a better approach. And there are the rare cases of mechanical issues like swollen vocal cords and severe phlegm buildup. Both are related to clinical hypothyroidism, so both seem to respond well to T3. If there is some structural damage due to trauma or disease, then I don't know how helpful these methods will be.
     
  10. keith

    keith Member

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    Thanks Haidut. I guess I wasn't clear enough in my question. What I meant to ask was whether it is likely to be contraindicated for someone with sleep apnea; I wasn't looking to use it as a treatment, I just wanted to make sure it wouldn't be a waste of money for someone who has sleep apnea. Your advice on treating sleep apnea is excellent as usual, and I appreciate your thorough response. I wish we had this discussion 15 years ago. I have had great results with thiamine, and although I still use a device (tongue stabilization) for an apparent mechanical issue, the combination has been practically life changing for me.
     
  11. DaveFoster

    DaveFoster Member

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    Very interesting how ritanserin improves SWS to a greater extent when administered in the morning. I guess ensuring a healthy metabolic state during the day does more than prepping for sleep as if it's a separate event.
     
  12. ecstatichamster

    ecstatichamster Member

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    Madame with bromocriptine. Dopamine is lower in the am. Apparently taking these in the morning makes the most difference.
     
  13. Pointless

    Pointless Member

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    I was just wondering if you think baking soda could be as effective as acetazolamide for something like this?
     
  14. OP
    haidut

    haidut Member

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  15. zooma

    zooma Member

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  16. nullredvector

    nullredvector Member

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    should we be concerned that the ritanserin molecule contains fluorine atoms?
     
  17. scarlettsmum

    scarlettsmum Member

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    Wish we could get a response on this...
     
  18. scarlettsmum

    scarlettsmum Member

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    Found this. Should be ok then?
     

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  19. OP
    haidut

    haidut Member

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    There is probably no need for that supplement. Oral thiamine when taken over 7 day period achieves the same concentrations as IV thiamine. So, the supplement would not be adding much and many people dislike the DMSO anyways.
     
  20. OP
    haidut

    haidut Member

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