Chlorpheniramine maleate; aka
2-PYRIDINEPROPANAMINE,GAMMA-(4- CHLOROPHENYL)-N,N-DIMETHYL-,(2)-2- BUTENEDIOATE(1:1)
Chemical formula: C16-H19-Cl-N2.C4-H4-O4
Chlorpheniramine is an anticholinergic antihistamine. It also is
effective against nausea and motion sickness, with its primary
mechanism of action being its ability to reduce acetylcholine levels
in the brain. Acetylcholine is a neurotransmitter. In the brain,
acetylcholine and dopamine have antagonistic effects on each other, so
a proper balance is necessary for a healthy, functioning body
and mind. Many antihistamines (Benadryltm included) work the same way;
by reducing (or inhibiting the effects of) the level of acetylcholine in the brain, histamine levels
decrease throughout the body, alleviating the symptoms of an allergic
reaction. The decrease in acetylcholine gives the dopamine more
influence within the brain, which is why anticholinergic drugs are often
used to alleviate the symptoms of Parkinson's Disease. Anticholinergics
also tend to promote urine retention via temporary swelling of the Prostate,
making them useful as anti-incontinence drugs.
Chlorpheniramine is sold under the brand name Chlor-Trimetontm,
but it can also be obtained in a far less expensive generic form. I
prefer it by itself; it is often included in a cocktail of drugs
like acetaminophen and the recently-banned stimulant phenylpropylalamine.
Like just about any antihistamine, the side effects include drowsiness
or excitability (neurotransmitter action can seem paradoxical to
the observer). In my experience, Benadryl (diphenhydramine hydrochloride)
is the strongest when it comes to producing these generally undesirable
effects. Because of this, most over-the-counter sleep aids contain
a small dose of diphenhydramine. Pseudoephedrine gives me a detached feeling
and makes me drowsy also, but Chlorpheniramine is just right. I don't
notice it one bit.
That doesn't mean it works for everybody. People over 60 are
especially likely to suffer from side effects. It's a good idea not
to mix Chlorpheniramine with alcohol or any other drug that produces
a drowsy effect. This includes sedatives such as Valium, and opiates.
This hasn't stopped the pharmaceutical industry from marketing a blend
of Chlorpheniramine and Hydrocodone (codeine) for particularily severe
Because it is an anticholinergic, it should not be mixed with any
other drugs that are anticholinergics also. If you do, expect
side effects like dry mouth and heart palpitations, which are no fun.
Some popular anticholinergics are Atropine, Benadryl, the herb
Henbane, and the anti-motion-sickness drug Dramamine. Atropine
is obtained from the Deadly Nightshade (Belladonna) plant. Its close cousin,
Scopolamine, has similar effects (used officially as a patch to treat motion
sickness). The anticholinergic effect of Scopolamine is what gives
Jimsonweed, Belladonna, and Datura their powerful, psychoactive deliriant effects.
I wouldn't recommend taking a mega-dose of Chlorpheniramine for recreational
uses, but I have heard of people using Benadryl in such a manner.
Chlorpheniramine with recreational drugs is not a good idea either,
simply because it is yet another drug dicking around with the neurotransmitters
in your brain. The well-known "This is your brain on dissociatives"
FAQ warns that anticholinergics can increase the likelihood of
developing Olney's Lesions in the brain when combined with dissociatives
like Ketamine, Nitrous Oxide, or Dextromethorphan.
And one last thing -- DO NOT combine Chlorpheniramine with MAOIs, either! MAO inhibitors can drastically prolong and intensify the side effects, which isn't desirable. Some common MAOIs include St. John's Wort, Passionflower (to a lesser degree), Harmala, and Yohimbe / Yohimbine, which is incidentally one of the more powerful and potentially lethal sources.
Update (07-30-02) -- Chlorpheniramine initially didn't bother me, but I began noticing side effects (including a racing heart) and eventually moved on to the nasal steroid Beconase.