Chloropyramine is known as a competitive reversibleH1 receptor antagonist (also known as an H1 inverse agonist), meaning that it exerts its pharmacological action by competing withhistamine for the H1 subtype histamine receptor. By blocking the effects of histamine, the drug inhibits the vasodilation, increased vascular permeability, and tissue edema associated with histamine release in the tissue. The H1 antagonistic properties of chloropyramine can be used by researchers for the purposes of blocking the effects ofhistamine on cells and tissues. In addition, chloropyramine has someanticholinergic properties.[1]
In children, it can induce agitation, and in many adult patients,dizziness may be observed. Because of the pronouncedsedative effect, the preparation should be prescribed cautiously in drivers and people working with machines.[citation needed]
A large study on people 65 years old or older linked the development ofAlzheimer's disease and other forms of dementia to the "higher cumulative" use of first-generation antihistamines, due to theiranticholinergic properties.[3]
In cases of severeallergic reactions, chloropyramine can be injectedintramuscularly orintravenously.Oral administration: In adults, 25 mg can be taken 3 to 4 times daily (up to 150 mg); in children over 5 years old, 25 mg can be taken 2 to 3 times daily. For external application, the skin or the eye conjunctiva can be treated up to several times a day by applying a thin layer of cream or ointment containing 1% chloropyramine hydrochloride.[citation needed]
The preparation begins with the condensation of 4-chlorobenzaldehyde with1,1-dimethyethylenediamine. The resultingSchiff base is reduced. The resulting amine is then further reacts with2-bromopyridine in the presence of sodamide.
^Vaughan JR, Anderson GW (March 1949). "Antihistamine agents; halogenated N,N-dimethyl-N-benzyl-N-(2-pyridyl)-ethylenediamines".The Journal of Organic Chemistry.14 (2):228–34.doi:10.1021/jo01154a006.PMID18117722.
^US granted 2569314, Kenneth HL, "N, n-dimethyl-n'-(4-halobenzyl)-n'-(2-pyridyl) ethylenediamines and preparation of the same", issued 1951, assigned to American Cyanamide
^US granted 2607778, Cates EM, Phillips RF, "Process of preparing n, n-dimethyln'-(p-chlorobenzyl)-n'-(2-pyridyl)-ethylenediamine", issued 1952, assigned to Merck & Co.
^CH granted 264754, "Verfahren zur Herstellung eines Äthylendiaminderivates.", issued 1950, assigned to J. R. Geigy AG
^CH granted 266234, "Verfahren zur Herstellung eines Äthylendiaminderivates.", issued 1950, assigned to J. R. Geigy AG
^CH granted 266235, "Verfahren zur Herstellung eines Äthylendiaminderivates.", issued 1950, assigned to J. R. Geigy AG
^GB granted 651596, "Manufacture of n-(2-pyridyl)-n-(p-chloro-benzyl)-n:n-dimethyl-ethylenediamine", issued 1951, assigned to J. R. Geigy AG
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