This is going to be my one of my most delightful articles yet, and over a period of weeks will be wholly complete.
Often one question people will ask - what are the 'other' mechanisms of anti-depressants...the 'hidden' effects which may correlate to drug efficacy and / or neurological side-effects.
Let's start off with an example, one that isn't shown in pharmacy booklets. MAPROTILINE sold as Deprilept, Ludiomil, Psymion; is an anti-depressant medication cited as being a norepinephrine reuptake inhibitor (NET Inhibitor) (1) , OK so it enhances norADRENALINE levels creating sensory and motor effects and stimulation. Second to this, it also antagonizes serotonin 7A receptors (2) - or simply the 7th serotonin receptor...which can result in a decrease in cAMP and an increase in dopaminergic neurotransmission(3)(4).
The part not cited, even on the wiki, is maprotiline's ability to inhibit K+ (POTASSIUM) inward rectifying currents (5) (6). Inhibiting these currents would provide additional stimulation parallel to or mimicking histamine activity(7). AND IT'S NOT JUST MAPROTILINE FOLKS, it's also imipramine, desipramine, amitriptyline, nortriptyline, clomipramine,, and citalopram that inhibit potassium channels(8). < CLICK IMAGE TO GET BETTER VIEW >
Often one question people will ask - what are the 'other' mechanisms of anti-depressants...the 'hidden' effects which may correlate to drug efficacy and / or neurological side-effects.
Let's start off with an example, one that isn't shown in pharmacy booklets. MAPROTILINE sold as Deprilept, Ludiomil, Psymion; is an anti-depressant medication cited as being a norepinephrine reuptake inhibitor (NET Inhibitor) (1) , OK so it enhances norADRENALINE levels creating sensory and motor effects and stimulation. Second to this, it also antagonizes serotonin 7A receptors (2) - or simply the 7th serotonin receptor...which can result in a decrease in cAMP and an increase in dopaminergic neurotransmission(3)(4).
The part not cited, even on the wiki, is maprotiline's ability to inhibit K+ (POTASSIUM) inward rectifying currents (5) (6). Inhibiting these currents would provide additional stimulation parallel to or mimicking histamine activity(7). AND IT'S NOT JUST MAPROTILINE FOLKS, it's also imipramine, desipramine, amitriptyline, nortriptyline, clomipramine,, and citalopram that inhibit potassium channels(8). < CLICK IMAGE TO GET BETTER VIEW >
Another not well-known mechanism of some anti-depressants - is the unspecified action on histamine H2 receptors...some anti-depressants have such a weak potency for the receptor that it may not matter - however, some like mianserin(9)(10), amitryptiline(11) and trimipramine/imipramine(12) have relative effects and can to a moderate extent, inhibit histamine H2-related responses(13).
If, in process, cAMP is reduced effectively by H2 inhibition - this may be a mechanism in which some* anti-depressants can exacerbate psychosis(14)(15)(16).
However, not all anti-depressants will have these side-effects, it is mainly amitryptiline, noritryptiline, imipramine and trimipramine, mianserin is less likely to cause these specific side-effects, and mirtazapine is on average, much safer than all of the above and has seemingly zero affinity for H2R's, as opposed to it's cousin drug mianserin.
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