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Amitriptyline and percentages of SERT blockade

Posted by Skeletor on April 10, 2020, at 12:12:07

Can you reach clinically significant SERT blockade [~ 80%] with Amitriptyline?

According to P. K. Gillman and others the tricyclic antidepressant Amitriptyline is a weaker SRI than SSRIs / SSNRIs and Clomipramine / Imipramine. It seems that with Amitriptyline it is difficult to reach Serotonin Toxicity; that's why you can safely combine Amitriptyline with MAOIs.

My question: What is the maximal SERT blockade possible with Amitriptyline standalone? Is there a dosage-SERT-occupation-curve? It surely depends on the individual genetic makeup (slow, intermediate, rapid metabolizer) and other genetic factors, but there surely are median values available? I would be interested to learn if one can reach 80% SERT blockade with Amitriptyline alone (at higher dosages).




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