|Systematic (IUPAC) name|
|1-[(4-fluorophenyl)methyl]- N-[1-[2-(4-methoxyphenyl)ethyl]- 4-piperidyl]benzoimidazol-2-amine|
|14px (what is this?)|
Astemizole (R43512, marketed under the brand name Hismanal) was a second-generation antihistamine drug that has a long duration of action. Astemizole was discovered by Janssen Pharmaceutica in 1977. It has been withdrawn from the market in most countries because of rare but potentially fatal side effects (QTc interval prolongation and related arrhythmias due to hERG channel blockade).
Astemizole competitively binds to histamine H1-receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. This suppresses the formation of edema and pruritus (caused by histamine).
Astemizole may also act on histamine H3 receptors, thereby producing adverse effects.
Astemizole is rapidly absorbed from the gastrointestinal tract; protein binding is around 96 percent.
Astemizole may cause life-threatening arrhythmia.
Astemizole has an oral LD50 of approximately 2052 mg/kg (in mice).
It has been reported that this drug might prevent much of the muscle wasting (atrophy) that occurs in immobile, bedridden patients. An experiment on a small number of mice showed that astemizole blocked the activity of a protein present in muscle that is involved in muscle atrophy. However, the concerns for the drug's long-term effects on the heart preclude its routine use in humans for this indication.
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- "Purdue researchers find 'switch' for skeletal-muscle atrophy". Purdue University. 2006-05-24. Retrieved 2009-06-22.
- Wang X, Hockerman GH, Green Iii HW, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL (May 24, 2006). "Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway". FASEB J 20 (9): 1531–3. PMID 16723379. doi:10.1096/fj.05-5350fje.
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