词条 | Otilonium bromide |
释义 |
}}{{Drugbox | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 408354493 | IUPAC_name = N,N-Diethyl-N-methyl-2-(4-[2-(octyloxy)benzamido]benzoyloxy)ethanaminium bromide | image = Otilonium bromide.png | tradename = Spasmoctyl 40, Doralin | Drugs.com = {{drugs.com|international|otilonium-bromide}} | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = | ATC_prefix = A03 | ATC_suffix = AB06 | PubChem = 72092 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | UNII_Ref = {{fdacite|changed|FDA}} | UNII = 21HN3N72PV | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D07083 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 65077 | C=29 | H=43 | Br=1 | N=2 | O=4 | molecular_weight = 563.57 g/mol | smiles = CCCCCCCCOC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)OCC[N+](C)(CC)CC.[Br-] | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C29H42N2O4.BrH/c1-5-8-9-10-11-14-22-34-27-16-13-12-15-26(27)28(32)30-25-19-17-24(18-20-25)29(33)35-23-21-31(4,6-2)7-3;/h12-13,15-20H,5-11,14,21-23H2,1-4H3;1H | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = VWZPIJGXYWHBOW-UHFFFAOYSA-N }}Otilonium bromide is an antimuscarinic and calcium channel blocker used to relieve spasmodic pain of the gut, especially in irritable bowel syndrome.[1] Medical usesA pooled analysis of three clinical trials suggest that otilonium is more effective than placebo for the treatment of irritable bowel syndrome.[2] PharmacologyOtilinium binds to both muscarinic receptors and tachykinin NK2 receptors.[3] It has been shown to inhibit L-type and T-type calcium channels, actions which may contribute to or determine its effects in the gut.[4][5] When taken orally, very little of the drug is absorbed into the rest of the body,[6] which means that most of its actions remain confined to the gastrointestinal system. References1. ^{{cite web|archiveurl=https://web.archive.org/web/20160304071357/http://www.grupounipharm.com/sites/default/files/DISMOX+Inserto+CORREGIDO+2011.+Ingl%C3%A9s.pdf|url=http://www.grupounipharm.com/sites/default/files/DISMOX+Inserto+CORREGIDO+2011.+Ingl%C3%A9s.pdf|title=Dismox|archivedate=4 March 2016|publisher=}} {{Drugs for functional gastrointestinal disorders}}{{Muscarinic acetylcholine receptor modulators}}{{gastrointestinal-drug-stub}}2. ^{{cite journal|last1=Clavé|first1=P|last2=Tack|first2=J|title=Efficacy of otilonium bromide in irritable bowel syndrome: a pooled analysis.|journal=Therapeutic advances in gastroenterology|date=March 2017|volume=10|issue=3|pages=311–322|doi=10.1177/1756283X16681708|pmid=28246548|pmc=5305018}} 3. ^{{cite journal|last1=Evangelista|first1=S|title=Otilonium bromide: a selective spasmolytic for the gastrointestinal tract.|journal=The Journal of international medical research|date=1999|volume=27|issue=5|pages=207–22|doi=10.1177/030006059902700501|pmid=10689627}} 4. ^{{cite journal|last1=Martin|first1=MT|last2=Hove-Madsen|first2=L|last3=Jimenez|first3=M|title=Otilonium bromide inhibits muscle contractions via L-type calcium channels in the rat colon.|journal=Neurogastroenterology & Motility|date=April 2004|volume=16|issue=2|pages=175–83|doi=10.1111/j.1365-2982.2004.00518.x|pmid=15086871}} 5. ^{{cite journal|last1=Strege|first1=PR|last2=Sha|first2=L|last3=Beyder|first3=A|last4=Bernard|first4=CE|last5=Perez-Reyes|first5=E|last6=Evangelista|first6=S|last7=Gibbons|first7=SJ|last8=Szurszewski|first8=JH|last9=Farrugia|first9=G|title=T-type Ca(2+) channel modulation by otilonium bromide.|journal=American Journal of Physiology. Gastrointestinal and Liver Physiology|date=May 2010|volume=298|issue=5|pages=G706-13|doi=10.1152/ajpgi.00437.2009|pmid=20203058|pmc=2867415}} 6. ^{{cite journal|last1=Shin|first1=BS|last2=Kim|first2=JJ|last3=Kim|first3=J|last4=Hu|first4=SK|last5=Kim|first5=HJ|last6=Hong|first6=SH|last7=Kim|first7=HK|last8=Lee|first8=HS|last9=Yoo|first9=SD|title=Oral bioavailability and enterohepatic recirculation of otilonium bromide in rats.|journal=Archives of Pharmacal Research|date=January 2008|volume=31|issue=1|pages=117–24|pmid=18277617|doi=10.1007/s12272-008-1129-2}} 6 : Muscarinic antagonists|Quaternary ammonium compounds|Phenol ethers|Benzanilides|Benzoates|Bromides |
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