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SNRIs | Antidepressant Topic Index | MAOIs

1.  Three Ring Circus

Defined by their three-ring chemical structure, almost all tricyclic antidepressants (TCAs) work in pretty much the same way: norepinephrine reuptake inhibition, alpha-1, H1, and M1 antagonism, and sodium voltage channel blocking. Most also do enough serotonin reuptake inhibition to make a difference, and some are also 5HT2A and 5HT2C antagonists. TCAs discussed on this site include:


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2.  But Wait, There’s Four

Tetracyclic - having four rings - antidepressants like Remeron and amoxapine are usually lumped in with TCAs even they don’t really work enough like TCAs to warrant that. Enough places and papers refer to Remeron (mirtazapine), etc. as TCAs anyway, so we may as well put them on the same page.1 However, Asendin (amoxapine) is unofficially classified as an atypical antipsychotic by Stahl and other pharmacologists, based upon its efficacy in treating schizophrenia and mechanism of action, while all the others have a similar mechanism of action that is completely different than amoxapine, and are grouped as noradrenergic and specific serotonergic antidepressants (NaSSAs). All it takes is one more to be approved in the US and they’re getting their own Crazymeds class.

3.  TCA Dosage Equivalents

As far as tricylic ADs are concerned you’d think it would be fairly easy to put together, as there are three essential components of a TCA’s mechanism of action that make it an effective antidepressant: norepinephrine and serotonin reuptake inhibition, and alpha-1 norepinephrine antagonism. Some of them do more, but those are the main three for AD action. Turns out only three are roughly equivalent as far as raw potency is concerned - desipramine, my dear friend protriptyline, and nortriptyline. So while 25mg of desipramine = 25mg of nortriptyline, and it’s close enough to 1:1 until you hit 100mg, protriptyline’s pharmacokinetics are so loopy that I wouldn’t put any money on one 20mg dose of protriptyline being equivalent to two 10mg doses of protriptyline. Then we start getting into some meds being the active metabolites of others and a hell of a lot of other complexities.

3.1  By the Numbers

Take a look for yourself. These are measures of potency, and potency is not the same as how well a drug works. It isn’t even the same as the effect a drug will have in your brain. Why? These are the base substances, and not the various salts (hydrochloride (HCl), mesylate, pamoate, etc.) that are the active ingredients in many meds. That usually makes a difference in how well a substance is absorbed and distributed throughout your system. According to the results shown on the first table, clomipramine is exactly ten times as potent when it comes to making norepinephrine hang around your synapses than loxapine is, but if the formulations of two drugs resulted in five times as much loxapine per milligram getting to your brain and staying there than was the case with clomipramine, then the clomipramine would be only twice as potent2.

The lower the number, the greater the strength.
SERT: Serotonin transport
NET: Norepinephrine transport
DAT: Dopamine transport
“transport” is another way of referring to reuptake.
These tables are sortable. Just click on a column header to sort the table by that column. Clicking on the same header more than once toggles between ascending and descending.

Binding Profiles of Selected Tricyclic and Tetracyclic Antidepressants

Med (generic)SERTNETDAT5-HT1A5-HT2Aα1α2D2H1Musc
amitriptyline4.30353,25032024268151,2301.0313.8
clomipramine0.28382,1907,00027383,2001903137
desipramine17.60.833,1906,7003151156,3503,40085132
dosulepin8.6465,3102,3002584702,400?3.625
doxepin6829.512,10028326241,1851,3800.2152
imipramine1.40378,5007,650115613,1501,3102468
lofepramine705.418,0004,6002001002,7002,00036067
nortriptyline184.371,14030243582,2651,8858.294
protriptyline19.61.412,1003,800701306,6002,3002525
trimipramine1492,4503,7808,00032246801800.2758
amoxapine5816.04,3102200.6502,600160251,000
loxapine2,4003809,0002,9001.7282,400704.9450
maprotiline5,80011.11,00012,000120909,4003502.0570
mianserin4,0001019,4001904.3744.32,1971.7820
mirtazapine>100,0001,640>100,000?6960819>5,4541.6794

.

From Tricyclic antidepressant pharmacology and therapeutic drug interactions updated Receptor profile, Ki (nmol/l), of TCAs and comparator drugs: uptake inhibition and receptor antagonism (HCR data)


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Mixed with the NSRI reboxetine for comparison.

generic name5-HTNAH1α1Musc5-HT2A
mirtazapine>10,0004,6000.1450067016
mianserin>4,000710.40348207
doxepin6829.50.24248325
amitriptyline20501271829
imipramine76040324680
clomipramine0.145415322535
nortriptyline100106.3553744
dothiepin7870440038260
desipramine180.83110100100280
reboxetine587.2310>1000>1000>1000

.

If you like these kind of data, see the page on SSRI dosage equivalents.

We also have a forum for TCAs on Crazymeds Talk, and Remeron has its own forum, so if this page and the pages for individual TCAs aren’t enough for you, take a look at that part of this site.



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SNRIs | AD Topic Index | MAOIs


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1 That the acronym TeCA hasn't caught on doesn't help much either.

2 I made that up just to have an example using TCAs. A real case is Paxil vs. Prozac. Paroxetine is 14 times as potent as fluoxetine in serotonin reuptake inhibition, but Paxil (paroxetine HCl) is only twice as potent as Prozac (fluoxetine HCl).


Tricyclic & Tetracyclic Antidepressants (TCAs) by Jerod Poore is copyright © 2010 Jerod Poore

Last modified on Sunday, 01 June, 2014 at 11:16:27 by JerodPoorePage Author: Jerod PooreDate created: 26 November 2010

All drug names are the trademarks of someone else. Look on the appropriate PI sheets or ask Google who the owners are. The way pharmaceutical companies buy each other and swap products like Monopoly™ real estate, the ownership of any trademarks may have changed without my noticing.





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1 While there are plenty of books to help you with hypochondria, for some reason there’s not much in the way of websites. Then again, staying off of the Internet is a large part of curing/managing the disorder.

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