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20-September-2008 09:55:57 - Astemizole Astemizole Systematic IUPAC name 1-4-fluorophenylmethyl- N-1-2-4-methoxyphenylethyl- 4-piperidylbenzoimidazol-2-amine Identifiers CAS number 68844-77-9 ATC code R06AX11 PubChem 2247 DrugBank APRD00585 Chemical data Formula C28H31FN4O Mol. mass 458.571 Pharmacokinetic data Bioavailability ? Metabolism Hepatic Half life 24 hours Excretion Fecal Therapeutic considerations Pregnancy cat. C USA Legal status Unscheduled Routes Oral Astemizole marketed under the brand name Hismanal is a second generation antihistamine drug which 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 It has been withdrawn from the market in most countries because of rare but potentially fatal interactions with CYP3A4 enzyme inhibitors e.g. erythromycin, grapefruit juice. Contents 1 Pharmacology 2 Toxicity 3 Research 4 External links 5 Footnotes Pharmacology Astemizole is an histamine H1-receptor antagonist. It is structurally similar to terfenadine and haloperidol a butyrophenone antipsychotic. It has anticholinergic and antipruritic effects. 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 does not cross the blood-brain barrier, and H1 receptor binding is mostly in the peripheral rather than central nervous system CNS depression is thus minimal. 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%. Toxicity Astemizole has an oral LD50 of approximately 2052mg/kg in mice. Research It has been reported that this drug might prevent 97% of the muscle wasting atrophy that occurs in immobile, bedridden patients.1 Testing upon mice showed that it blocked the activity of a protein present in the muscle that is involved in muscle atrophy.2 Recent studies have also suggested anti-malarial properties of astemizole. However the concerns for the drug's longterm effects on the heart preclude its routine use in humans for this indication. Astemizole has recently been found to be a potent treatment for malaria. It has a mechanism of action similar to chloroquine but has activity even in chloroquine-resistant parasites.3 External links RxList.com - Astemizole Statement on Astemizole from Health Canada Footnotes ^ Drug 'could stop muscle wasting', NetDoctor.co.uk 2006-05-25. Retrieved on 2006-05-27. ^ Wang X, Hockerman GH, Green Iii HW, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL May24 2006. Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway. FASEB J 20: 1531. doi:10.1096/fj.05-5350fje. PMID 16723379. ^ Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ 2006. A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol 2: 415-16. doi:10.1038/nchembio806. PMID 16816845. v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratidine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 Burimamide Ciproxifan Clobenpropit Conessine Impentamine Iodophenpropit Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 Retrieved from http://en..org/wiki/Astemizole Categories: Antihistamines | Withdrawn drugs Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Español Polski ไทย This page was last modified on 31 July 2008, at 10:30
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