Dimetindene Explained

Dimetindene, also sold under the brand name Fenistil, is an antihistamine/anticholinergic. It is a first generation[1] selective H1 antagonist.[2] Dimetindene is an atypical first generation H1 antagonist as it only minimally[3] passes across the blood–brain barrier.

Dimetindene is also an M2 receptor antagonist.[4]

It was patented in 1958 and came into medical use in 1960.[5]

Medical use

Dimetindene is used orally and topically as an antipruritic.[6] It is used topically to treat skin irritations, such as insect bites. Dimetindene is also administered orally to treat allergies, such as hay fever.

It is commonly formulated as its maleic acid salt, dimethindene maleate.

Names

It is sold under the brand name Fenistil among others.

Notes and References

  1. Fromer LM, Ortiz GR, Dowdee AM . Assessment of Patient Attitudes About Mometasone Furoate Nasal Spray: The Ease-of-Use Patient Survey . The World Allergy Organization Journal . 1 . 9 . 156–159 . September 2008 . 23282579 . 3651039 . 10.1186/1939-4551-1-9-145 . free .
  2. Web site: Dimetindene. Drugs.com.
  3. Noguchi S, Inukai T, Kuno T, Tanaka C . The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking . Physiology & Behavior . 51 . 6 . 1123–1127 . June 1992 . 1353628 . 10.1016/0031-9384(92)90297-f . 29562845 .
  4. Matsumoto Y, Miyazato M, Furuta A, Torimoto K, Hirao Y, Chancellor MB, Yoshimura N . Differential roles of M2 and M3 muscarinic receptor subtypes in modulation of bladder afferent activity in rats . Urology . 75 . 4 . 862–867 . April 2010 . 20156651 . 2871158 . 10.1016/j.urology.2009.12.013 .
  5. Book: Fischer J, Ganellin CR . Analogue-based Drug Discovery . 2006 . John Wiley & Sons . 9783527607495 . 547 . en.
  6. Wexler L . A clinical evaluation of dimethindene . Current Therapeutic Research, Clinical and Experimental . 4 . 306–309 . June 1962 . 14006402 .