2D structure of histamine
3D structure of histamine
|Synonyms||5-imidazoleethylamine, eramin, ergamine, ergotidine and theramine|
|Brand names|| Ceplene, Histatrol
|Routes|| Inhalation, ID, IV, SC
|ATC code||L03AX14 (2HCl), V04CG03 (2H3PO4)|
|Licensing data|| EU EMA: link.|
US FDA: link.
In the CNS it acts via the H1 and H3 receptors, H1 is excitatory while H3 is an inhibitory auto- and hetero- receptor. H1 receptor activation improves wakefulness, whereas blocking this receptor is responsible for the sedating effect of many drugs, especially the first antihistamines to be developed.
In the periphery it acts via H1, H2 and H4 receptors. H1 receptors play a crucial role in mediating allergic responses in the body, it is via blocking this receptor that the family of drugs, the antihistamines, achieve their anti-allergy effects. H2 receptors, on the other hand, is secreted by the cells of the stomach in order to induce the release of stomach acid. Consequently H2 antagonists produce inhibitory effects on the release of stomach acid and are used to treat stomach ulcers and related conditions. H4 receptors are expressed primarily in immune cells and appears to play a role in immune responses, similarly to the H1 receptor.
Medical use of histamineEdit
Exogenous histamine, that is histamine that comes from sources other than the body produces smooth muscle stimulation, leading to bronchoconstriction (that is, the airways close up) and reduced blood pressure (due to dilation of the blood vessels). When it comes into contact with the skin it leads to a hypersensitivity reaction similar to allergic reactions (including red dots of skin that are raised and swollen and discomfort; usually used as a test for leprosy-induced nerve damage). In the European Union it is also approved for use, in combination with a low-dose of aldesleukin, as post-consolidation therapy (to prevent future relapse) in people with acute myeloid leukaemia.
- NCBI Bookshelf provides free book resources on this topic.
- PubMed provides review articles from the past five years (limit to free review articles or to systematic reviews)
- The TRIP database provides clinical publications about evidence-based medicine.
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 Walter, M; Stark, H (January 2012). "Histamine receptor subtypes: a century of rational drug design.". Frontiers in Bioscience 4: 461–88. PMID 22202071.
- ↑ 2.0 2.1 Brayfield, A, ed. (30 January 2013). "Histamine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 13 September 2014.
- ↑ "Ceplene : EPAR - Product Information". European Medicines Agency. Solna, Sweden: Meda AB. 10 April 2014. Retrieved 5 December 2014.
- ↑ Yang, LP; Perry, CM (1 January 2011). "Histamine dihydrochloride: in the management of acute myeloid leukaemia.". Drugs 71 (1): 109–22. PMID 21175244. doi:10.2165/11206410-000000000-00000.
- ↑ Schlenk, RF (November 2014). "Post-remission therapy for acute myeloid leukemia.". Haematologica 99 (11): 1663–1670. PMC 4222459. PMID 25420282. doi:10.3324/haematol.2014.114611.