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http://www.cnsspectrums.com/userdocs/articleimages/146/1208CNS_Stahl_fig6big.jpg
The above link more or less shows that certain drugs like antihistamines and tricyclic antidepressants, as the dose increases more receptors are affected or saturated. Both class of meds are very closely related and are often referred to as dirty drugs as they affect many different receptors unlike say ssri antidepressant.
Blocking the effects of histamine is thought to be the main reason these meds are sedating and histamine receptors are saturated quicker with low doses than other receptors which can be stimulating. One eg is of mirtazapine which is very sedating at low doses as it hits mostly histamine but as doses are increased the sedating effects are less as noradrenaline receptors start to get hit.
I came across some of this information when researching the low dose doxepin which has been repackaged as a sleep med called silenor in 3mg and 6mg doses. I wanted to know if 6mg was a big difference in effect compared to 10mg of doxepin which is the same drug but much cheaper. Doxepin as an antidepressant comes in the lowest dose of 10mg caps and also comes in a liquid, its also much cheaper. I think the reasoning for 6mg strength is that they say that is the saturation point for histamine receptors in most people that also has the least hangover effect.
My experience is with doxepin is that i dont think there is much of a difference between 6 and 10mg doxepin. I also find with doxepin that sedation increases with the dose. My experience with amitriptyline is that it isnt anywhere near as sedating as doxepin, probably because in me the lower doses hit noradrenaline and serotonin much more. But it seems others have a different experience which shows everyone reacts differently to these meds.
I have found low doses of mirtazapine 7.5mg quite sedating and increasing the dose to 15mg doesnt really increase the sedation but does seem to increase the length of sedation. I havent tried higher doses but supposedly should be less sedating??
Also appears that 5ht2a antagnosts also increase sedation?
This is the link to the main article, interesting.
http://www.cnsspectrums.com/aspx/articledetail.aspx?articleid=1916
The above link more or less shows that certain drugs like antihistamines and tricyclic antidepressants, as the dose increases more receptors are affected or saturated. Both class of meds are very closely related and are often referred to as dirty drugs as they affect many different receptors unlike say ssri antidepressant.
Blocking the effects of histamine is thought to be the main reason these meds are sedating and histamine receptors are saturated quicker with low doses than other receptors which can be stimulating. One eg is of mirtazapine which is very sedating at low doses as it hits mostly histamine but as doses are increased the sedating effects are less as noradrenaline receptors start to get hit.
I came across some of this information when researching the low dose doxepin which has been repackaged as a sleep med called silenor in 3mg and 6mg doses. I wanted to know if 6mg was a big difference in effect compared to 10mg of doxepin which is the same drug but much cheaper. Doxepin as an antidepressant comes in the lowest dose of 10mg caps and also comes in a liquid, its also much cheaper. I think the reasoning for 6mg strength is that they say that is the saturation point for histamine receptors in most people that also has the least hangover effect.
My experience is with doxepin is that i dont think there is much of a difference between 6 and 10mg doxepin. I also find with doxepin that sedation increases with the dose. My experience with amitriptyline is that it isnt anywhere near as sedating as doxepin, probably because in me the lower doses hit noradrenaline and serotonin much more. But it seems others have a different experience which shows everyone reacts differently to these meds.
I have found low doses of mirtazapine 7.5mg quite sedating and increasing the dose to 15mg doesnt really increase the sedation but does seem to increase the length of sedation. I havent tried higher doses but supposedly should be less sedating??
Also appears that 5ht2a antagnosts also increase sedation?
This is the link to the main article, interesting.
http://www.cnsspectrums.com/aspx/articledetail.aspx?articleid=1916
