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Potency of clomipramine? - very high! » Brainbeard

Posted by ed_uk2010 on July 3, 2010, at 15:49:45

In reply to Re: what is 50mg anafranil = to as SSRI ?, posted by Brainbeard on June 29, 2010, at 6:10:28

Thanks for the link to the PET study. Fascinating results RE clomipramine.

Here is my impression of comparable doses of SRIs as far as serotonin transporter (SERT) occupancy is concerned........

Sertraline 50mg
Fluoxetine 20mg
Paroxetine 20mg
Citalopram 20-40mg
Escitalopram 10mg
Fluvoxamine 100mg
Venlafaxine XL 75mg
Duloxetine 60mg
Clomipramine, could be as little as 10-20mg

According to the PET study, even 10mg of clomipramine demonstrated around 80% SERT occupancy. 20mg clomipramine occupied well above 80% of transporters.

I'm not claiming that 20mg of clomipramine is the optimal dose for severe depression, although it could well be sufficient to 'replace' an SSRI. Clomipramine's potent and selective noradrenergic metabolite may contribute to the overall antidepressant efficacy of clomipramine at higher doses. Also, the antihistamine, anticholinergic, and serotonin 5-HT2 antagonist properties of clomipramine will be more prominent at high doses.

In my opinion, psychiatry should completely discard the traditional idea that *all* TCAs (except nortriptyline) should be dosed at 100mg+ per day for optimal efficacy. This is clearly nonsense because the potency of the various TCAs at monoamine reuptake sites and receptors varies greatly. In addition, individual response to TCAs is extremely variable, both clinically and in terms of pharmacokinetics. In the absense of anything better, all we can really do at the moment is 'start low and go slow', avoiding the temptation to make any inflexible pre-treatment decisions about what the final therapeutic dose ought to be.

 

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URL: http://www.dr-bob.org/babble/20100628/msgs/953155.html