Bromazine Explained

Bromazine, sold under the brand names Ambodryl, Ambrodil, and Deserol among others, also known as bromodiphenhydramine, is an antihistamine and anticholinergic medication of the ethanolamine class.^{[1] [2] [3] [4] [5]} It is an analogue of diphenhydramine with a bromine substitution on one of the phenyl rings.

Synthesis

Grignard reaction between phenylmagnesium bromide and para-bromobenzaldehyde [1122-91-4] (1) gives p-bromobenzhydrol [29334-16-5] (2). Halogenation with acetyl bromide in benzene solvent gives p-bromo-benzhydrylbromide [18066-89-2] (3). Finally, etherification with deanol completed the synthesis of Bromazine (4).

Side effects

Continuous and/or cumulative use of anticholinergic medications, including first-generation antihistamines, is associated with higher risk for cognitive decline and dementia in elderly people.^{[6] [7]}

Notes and References

1. Book: Elks J . 14 November 2014 . The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies . Springer . 177– . 978-1-4757-2085-3 . 1058412474 .
2. Book: Swiss Pharmaceutical Society . Swiss Pharmaceutical Society . 2000 . Index Nominum 2000: International Drug Directory . Taylor & Francis . 134– . 978-3-88763-075-1 .
3. Book: Baker CE . Physicians' Desk Reference. 1974. Medical Economics Company. Oradell, NJ 07649. 1076, 1081. 28th.
4. Kalpaklioglu F, Baccioglu A . Efficacy and safety of H1-antihistamines: an update . Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry . 11 . 3 . 230–237 . 2012 . 23173575 . 10.2174/1871523011202030230 .
5. Maclaren WR, Bruff WC, Eisenberg BC, Weiner H, Martin WH . A clinical comparison of carbinoxamine maleate, tripelennamine hydrochloride, and bromodiphenhydramine hydrochloride in treating allergic symptoms . Annals of Allergy . 13 . 3 . 307–312 . 1955 . 14377226 .
6. Gray SL, Anderson ML, Dublin S, Hanlon JT, Hubbard R, Walker R, Yu O, Crane PK, Larson EB . 6 . Cumulative use of strong anticholinergics and incident dementia: a prospective cohort study . JAMA Internal Medicine . 175 . 3 . 401–407 . March 2015 . 25621434 . 4358759 . 10.1001/jamainternmed.2014.7663 . Rebecca Hubbard .
7. Carrière I, Fourrier-Reglat A, Dartigues JF, Rouaud O, Pasquier F, Ritchie K, Ancelin ML . Drugs with anticholinergic properties, cognitive decline, and dementia in an elderly general population: the 3-city study . Archives of Internal Medicine . 169 . 14 . 1317–1324 . July 2009 . 19636034 . 2933398 . 10.1001/archinternmed.2009.229 .