From Wikipedia, the free encyclopedia
First generation antihistamine
Mepyramine , also known as pyrilamine , is a
first generation antihistamine , targeting the
H1 receptor as an
inverse agonist .
[1] Mepyramine rapidly permeates the brain, often causing
drowsiness .
[2] It is often sold as a
maleate salt, pyrilamine maleate .
The medication has negligible
anticholinergic activity, with 130,000-fold
selectivity for the
histamine
H1 receptor over the
muscarinic acetylcholine receptors (for comparison,
diphenhydramine had 20-fold selectivity for the H1 receptor).
[3]
It was patented in 1943 and came into medical use in 1949.
[4]
It was marketed under the names Histadyl, Histalon, Neo-Antergan, Neo-Pyramine, and Nisaval.
[5] In the 1960s and 70s it was a very common component in over-the-counter sleep aids such as Alva-Tranquil, Dormin, Sedacaps,
Sominex , Nytol, and many others.
[5] The US
FDA included it in the list of chemicals and compounds barred from use in
over-the-counter nighttime sleep aid products in 1989.
[6]
It is used in over-the-counter combination products to treat the common cold and menstrual symptoms such as
Midol Complete .
[7] It is also the active ingredient of the topical antihistamine creams Anthisan
[8] and Neoantergan
[1] sold for the treatment of insect bites, stings, and nettle rash.
See also
References
^
a
b Parsons, Mike E.; Ganellin, C. Robin (January 2006).
"Histamine and its receptors" .
British Journal of Pharmacology . 147 (Suppl 1) (published 2 February 2009): S127–S135.
doi :
10.1038/sj.bjp.0706440 .
PMC
1760721 .
PMID
16402096 .
^
"Mepyramine" . drugbank.com . Retrieved 8 May 2021 .
^ Kubo, Nobuo; Shirakawa, Osamu; Kuno, Takayoshi; Tanaka, Chikako (March 1987).
"Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay" . Japanese Journal of Pharmacology . 43 (3): 277–282.
doi :
10.1254/jjp.43.277 .
PMID
2884340 .
^ Fischer, János; Gannelin, C. Robin, eds. (2006).
Analogue-based Drug Discovery . John Wiley & Sons. p. 545.
ISBN
9783527607495 .
^
a
b Thornton, William E. (September 1977). "Sleep aids and sedatives".
Journal of the American College of Emergency Physicians . 6 (9): 408–412.
doi :
10.1016/S0361-1124(77)80006-3 .
PMID
330911 .
^ 54
FR
6826
^
"Active Ingredients for Midol Complete" .
Bayer HealthCare LLC . Archived from
the original on 2 December 2009. Retrieved 8 December 2009 .
^
"Anthisan Cream - Patient Information Leaflet (PIL)" . Medicines.org .
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