# chlorpheniramine maleate



## robotaffliction (Jul 24, 2009)

a lot of people have been looking for new medications for social anxiety, depression, etc... so i did some research on a VERY old drug (circa 1950, before TCAs and MAOIs!) and apparently many studies show chlorpheniramine (Chlor Trimeton in the US, an OTC antihistamine) to have anxiolytic effects as well as antidepressant effects. because its so old, no large-scale human trials were ever done, and it lost patent protection half a century ago most likely

it has strong affinity for the serotonin transporter (i.e., SSRI-like effect), and modest affinity for the dopamine transporter and norepinephrine transporter (more reuptake inhibition, and it will displace radiolabeled [3H]-cocaine from its binding sites in brain imaging studies), as well as having 5HT-2C antagonism (similar to remeron or agomelatin, two antidepressants with anxiolytic effects). and obviously it's an antihistamine so it would probably need to be taken at night. but it's sold as an over-the-counter time-released 12 hour+ form at a 12 mg dose, which is a recommended dose recognized as safe. it has a peculiar side-effect profile compared to other antihistamines, since *excitation*, not sedation is reported at higher doses, especially in children.. this is probably consistent with its broad spectrum pharmacological profile (i.e., all the reuptake inhibition and antagonism listed above)

anyone have any personal experiences with this? i'd imagine just taking it every night for a number of days for itching/allergies/etc. might have an antidepressant/anti-anxiety/pro-social effect for *some* people at least

cheers!

PS - not to be combined with an MAOI!!


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## PeopleAreStrange (Jun 4, 2009)

WHOA. That's in cough medicine! brb

Seems like it could harmful in the long term. :/


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## robotaffliction (Jul 24, 2009)

PeopleAreStrange said:


> WHOA. That's in cough medicine! brb
> 
> Seems like it could harmful in the long term. :/


well if you could point me to a study showing that it might be harmful in the long term when used daily as an antihistamine, then absolutely. but if its completely safe for that purpose, then why would it be dangerous for use in whatever purpose "off-label"?

obviously cough syrup is a different story, it has artificial sugar and other ingredients (cough suppressant, decongestants, etc)


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## robotaffliction (Jul 24, 2009)

oops, looks like theres already a much older thread on it here, tho they didnt seem to do as much research on it..


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## UltraShy (Nov 8, 2003)

Long ago I used that antihistamine when visiting people who had cats that I'm very allergic to. I used it simply because it was the absolute cheapest allergy pill around at $2.75 for a bottle of 100 pills.

Nothing special about it that I ever noticed. It's just an allergy pill.

Didn't really sedate me, but then I've yet to find any antihistamine to be noticeably sedating and I used allergy pills way back in ye olden days before the newer generation of "non-sedating" ones came to market.



> it has a peculiar side-effect profile compared to other antihistamines, since *excitation*, not sedation is reported at higher doses, *especially in children*..


I wouldn't make much of that, since paradoxical effects are most commonly seen in the very young and very old. Things like Benadryl that will sedate most making some kids hyper, or Valium being able to agitate someone who's 85 even though it's a chill pill to most.

I never noticed it to produce excitation either. Seemed like any other allergy pill to me, with price being the only factor favoring it. Keep in mind that when I used it a decade+ ago I was subject to no potential placebo effect, since I didn't expect it to do anything other than keep me from having an allergic reaction to cats (that are very cute, but secretly have an evil plot of make my eyes swell shut). I had to take in in amounts higher than recommended just to survive exposure to cats.

As for the comment about not mixing it with MAOIs, I've never heard of any antihistamine that was a problem with MAOIs before. Can anyone else confirm this? Typically MAOI problems come up when you have multi-ingredient meds for colds & allergies and one of those ingredients is typically psudoephedrine (Sudafed) that's tossed in to deal with nasal congestion that so often comes with allergies & colds.

As for long-term harm, there are people who take allergy meds daily forever, so if there was a risk one would think it would be readily apparent after over half a century of use.


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## robotaffliction (Jul 24, 2009)

UltraShy said:


> As for the comment about not mixing it with MAOIs, I've never heard of any antihistamine that was a problem with MAOIs before. Can anyone else confirm this? Typically MAOI problems come up when you have multi-ingredient meds for colds & allergies and one of those ingredients is typically psudoephedrine (Sudafed) that's tossed in to deal with nasal congestion that so often comes with allergies & colds.
> 
> As for long-term harm, there are people who take allergy meds daily forever, so if there was a risk one would think it would be readily apparent after over half a century of use.


it's written on the box, "Do not take with an MAOI inhibitor"  The brand I am looking at is Chlor-Tripolon (the Canadian version).

Yes with the long-term harm, that was my point too, can't go wrong with old tried and true medicine..


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## jim_morrison (Aug 17, 2008)

UltraShy said:


> As for the comment about not mixing it with MAOIs, I've never heard of any antihistamine that was a problem with MAOIs before. Can anyone else confirm this?


It's most likely because Chlorpheniramine has a strong affinity for the serotonin transporter.

Chlorpheniramine and Brompheniramine seem to be the only antihistamines with SRI properties.

Anyway here's conformation; http://www.psychotropical.com/1_st_intro.shtml


> *Drugs with clinically relevant serotonergic potency*
> From reference:--(36, 37)
> *Serotonin reuptake inhibitors (selective and non-selective)*
> 
> ...


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## Arisa1536 (Dec 8, 2009)

Was this chlorpheniramine maleate the drug mentioned in the movie/novel Shutter island? 
the drug has been around since the early 1950's
Sounds very potent and dangerous to me

*robotaffliction* Are you on this medication?
I did not know they even still prescribed it
:afr:afr:afr


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## Medline (Sep 23, 2008)

Arisa1536 said:


> Was this chlorpheniramine maleate the drug mentioned in the movie/novel Shutter island?


I guess that's chlorpromazine.


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## robotaffliction (Jul 24, 2009)

yea i think that's something else, maybe chlorpromazine  this is just an over-the-counter antihistamine you can buy at the pharmacy in any country, possibly around even earlier than the 1950's, but still on the shelves and has no dangers...



Arisa1536 said:


> Was this chlorpheniramine maleate the drug mentioned in the movie/novel Shutter island?
> the drug has been around since the early 1950's
> Sounds very potent and dangerous to me
> 
> ...


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## Arisa1536 (Dec 8, 2009)

Medline said:


> I guess that's chlorpromazine.


Lol thats the one :idea


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## Caedmon (Dec 14, 2003)

Going to resurrect this old thread because I've been researching chlorpheniramine a bit and find it a very interesting med. 

From what I've read it seems to be a mildly sedating med (not unlike Paxil or Remeron in regards to antihistamine activity) with serotonin reuptake inhibition, 5HT2c antagonism, 5HT1a agonism, and subtle dopamine reuptake inhibition. Does cause a bit of alpha1 antagonism which may contribute to sedation; also a 2D6 inhibitor, in terms of enzyme interactions.

In theory a decent med for mixed anxiety/depression. At least as good as anything else out there, and available over the counter (you can get giant 500-count bottles on Amazon).


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## Cincomom (Oct 18, 2015)

This is the only antihistamine that works for me. I have been delighted to find it also has a "calming" effect. It slows my overanxious mind to a pleasant serene-ness. I have also noted loss of appetite. I have considered taking it on a daily basis for anti-anxiety. Prescribed anti-anxiety, antidepressants have unwanted side effects for me so I have not been able to find anything I would be willing to take regularly. Today while I am coming off a 2 week cold, I am going to try taking a half dose (2 mg) of the chlorpheniramine maleate (4 mg at full dose) to determine if it helps with the running nose and drip down my throat as well as the anxiety part.


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## UltraShy (Nov 8, 2003)

I never noticed it to help any with psych issues. Long ago I'd take huge amounts of it to deal with a cat owner who evidently didn't know what a vacuum cleaner was for.


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## MigraineMom (May 2, 2018)

As a veterinarian who is somewhat allergic to cats I have consumed a great deal of chlorpheniramine over several decades. I selected chlorpheniramine as my antihistamine of choice because of its incredibly long safety record as an OTC drug. It became obvious that this antihistamine had a calming effect on me regardless of how hectic my workday was. I initially believed this was due to sedation and drowsiness, but with continued use these unwanted effects diminished while the calming, anxiolytic effects of the drug remained. At that point I researched psychiatric effects of chlorpheniramine, which had not been my intended usage, and found that it was indeed a serotonergic drug with anxiolytic and antidepressant properties. My question is why, then, are patients with anxiety and depression not told to try this extremely safe and ridiculously inexpensive OTC drug by their GPs and psychiatrists first, before any of the newer psychiatric drugs? Would it not be best for a patient to be controlled with a simple, safe, cheap OTC drug with no need for insurance approvals and copays? Additionally, the stigma of being a psych patient is minimized if one is treated with an OTC antihistamine rather than a psychiatric-specific drug. That alone can make a difference to this class of patients in particular. 
There is certainly no harm in trying chlorpheniramine before the big guns. I hope GPs and mental health practitioners will consider this treatment first rather than following the recommendations of their pharmaceutical reps.


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