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Old 08-07-2010, 07:49 PM   #1 (permalink)
 
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Default chlorpheniramine maleate

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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Old 08-07-2010, 07:57 PM   #2 (permalink)
 
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WHOA. That's in cough medicine! brb

Seems like it could harmful in the long term. :/
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Old 08-07-2010, 08:03 PM   #3 (permalink)
 
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Originally Posted by PeopleAreStrange View Post
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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Old 08-07-2010, 08:15 PM   #4 (permalink)
 
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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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Old 08-07-2010, 08:28 PM   #5 (permalink)
 
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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.

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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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Old 08-07-2010, 08:32 PM   #6 (permalink)
 
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Originally Posted by UltraShy
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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Old 08-07-2010, 10:35 PM   #7 (permalink)
 
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Originally Posted by UltraShy View Post
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
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Drugs with clinically relevant serotonergic potency
From reference:--(36, 37)
Serotonin reuptake inhibitors (selective and non-selective)
  • Paroxetine sertraline fluoxetine fluvoxamine citalopram.
  • venlafaxine milnacipran duloxetine sibutramine.
  • clomipramine imipramine (but not other TCAs).
  • tramadol pethidine fentanil (and congeners) methadone dextromethorphan dextropropoxyphene pentazocine (but not other opioids).
  • chlorpheniramine brompheniramine (but not other anti-histamines).
Serotonin releasers
  • Amphetamine MDMA.
Monoamine oxidase inhibitors
  • Tranylcypromine phenelzine nialamid iproniazid isocarboxazid.
  • pargyline selegiline clorgyline.
  • moclobemide toloxatone.
  • furazolidone procarbazine linezolid.
  • Methylene Blue
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Old 08-08-2010, 02:19 AM   #8 (permalink)
 
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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
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Old 08-08-2010, 02:41 AM   #9 (permalink)
 
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Originally Posted by Arisa1536 View Post
Was this chlorpheniramine maleate the drug mentioned in the movie/novel Shutter island?
I guess that's chlorpromazine.
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Old 08-08-2010, 03:13 PM   #10 (permalink)
 
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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...

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Originally Posted by Arisa1536 View Post
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
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Old 08-08-2010, 06:25 PM   #11 (permalink)
 
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Quote:
Originally Posted by Medline View Post
I guess that's chlorpromazine.
Lol thats the one
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