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Namespace Prefixes

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Statements

Subject Item
n2:DB04924
rdf:type
n5:Drug
n5:description
Itopride is a dopamine D2 antagonist with acetylcholinesterase inhibitory actions.
n5:generalReferences
# Mushiroda T, Douya R, Takahara E, Nagata O: The involvement of flavin-containing monooxygenase but not CYP3A4 in metabolism of itopride hydrochloride, a gastroprokinetic agent: comparison with cisapride and mosapride citrate. Drug Metab Dispos. 2000 Oct;28(10):1231-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10997945 # Holtmann G, Talley NJ, Liebregts T, Adam B, Parow C: A placebo-controlled trial of itopride in functional dyspepsia. N Engl J Med. 2006 Feb 23;354(8):832-40. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16495395 # Choung RS, Talley NJ, Peterson J, Camilleri M, Burton D, Harmsen WS, Zinsmeister AR: A double-blind, randomized, placebo-controlled trial of itopride (100 and 200 mg three times daily) on gastric motor and sensory function in healthy volunteers. Neurogastroenterol Motil. 2007 Mar;19(3):180-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17300287 # Chiba T, Tokunaga Y, Ikeda K, Takagi R, Chishima R, Terui T, Kudara N, Endo M, Inomata M, Orii S, Suzuki K: Effects of itopride hydrochloride and ranitidine in patients with functional dyspepsia: comparison between prokinetic and acid suppression therapies. Hepatogastroenterology. 2007 Sep;54(78):1878-81. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18019739 # Kim YS, Kim TH, Choi CS, Shon YW, Kim SW, Seo GS, Nah YH, Choi MG, Choi SC: Effect of itopride, a new prokinetic, in patients with mild GERD: a pilot study. World J Gastroenterol. 2005 Jul 21;11(27):4210-4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16015691 # Talley NJ, Tack J, Ptak T, Gupta R, Giguere M: Itopride in functional dyspepsia: Results of two phase III multicenter, randomized, double-blind, placebo-controlled trials. Gut. 2007 Oct 26;. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17965059
n5:group
investigational
n5:indication
Investigated for use/treatment in gastrointestinal diseases and disorders (miscellaneous).
owl:sameAs
n10:DB04924
dcterms:title
Itopride
adms:identifier
n4:14803321 n7:DB04924 n8:PA152432599 n13:3660 n15:3792
n5:mechanismOfAction
Itopride has anticholinesterase (AchE) activity as well as dopamine D2 receptor antagonistic activity. It is well established that M3 receptors exist on the smooth muscle layer throughout the gut and acetylcholine (ACh) released from enteric nerve endings stimulates the contraction of smooth muscle through M3 receptors. The enzyme AChE hydrolyses the released ACh, inactivates it and thus inhibits the gastric motility leading to various digestive disorders. Besides ACh, dopamine is present in significant amounts in the gastrointestinal tract and has several inhibitory effects on gastrointestinal motility, including reduction of lower esophageal sphincter and intragastric pressure. These effects appear to result from suppression of ACh release from the myenteric motor neurons and are mediated by the D2 subtype of dopamine receptors. Itopride, by virtue of its dopamine D2 receptor antagonism, removes the inhibitory effects on Ach release. It also inhibits the enzyme AchE which prevents the degradation of ACh. The net effect is an increase in ACh concentration, which in turn, promotes gastric motility, increases the lower esophageal sphincter pressure, accelerates gastric emptying and improves gastro-duodenal coordination. This dual mode of action of Itopride is unique and different from the actions of other prokinetic agents available in the market.
n5:synonym
N-(p-(2-(Dimethylamino)ethoxy)benzyl)veratramide
n5:IUPAC-Name
n6:271B5F3E-363D-11E5-9242-09173F13E4C5
n5:InChI
n6:271B5F44-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula
n6:271B5F43-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight
n6:271B5F40-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight
n6:271B5F41-363D-11E5-9242-09173F13E4C5
n5:SMILES
n6:271B5F42-363D-11E5-9242-09173F13E4C5
n5:Water-Solubility
n6:271B5F3C-363D-11E5-9242-09173F13E4C5
n5:logP
n6:271B5F3A-363D-11E5-9242-09173F13E4C5 n6:271B5F3D-363D-11E5-9242-09173F13E4C5
n5:logS
n6:271B5F3B-363D-11E5-9242-09173F13E4C5
n11:hasATCCode
n12:A03FA07
n5:H-Bond-Acceptor-Count
n6:271B5F4A-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count
n6:271B5F4B-363D-11E5-9242-09173F13E4C5
n5:InChIKey
n6:271B5F45-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-
n6:271B5F46-363D-11E5-9242-09173F13E4C5
n5:Polarizability
n6:271B5F48-363D-11E5-9242-09173F13E4C5
n5:Refractivity
n6:271B5F47-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count
n6:271B5F49-363D-11E5-9242-09173F13E4C5
n5:affectedOrganism
Humans and other mammals
n5:casRegistryNumber
122898-67-3
n5:Bioavailability
n6:271B5F50-363D-11E5-9242-09173F13E4C5
n5:Ghose-Filter
n6:271B5F52-363D-11E5-9242-09173F13E4C5
n5:MDDR-Like-Rule
n6:271B5F53-363D-11E5-9242-09173F13E4C5
n5:Number-of-Rings
n6:271B5F4F-363D-11E5-9242-09173F13E4C5
n5:Physiological-Charge
n6:271B5F4E-363D-11E5-9242-09173F13E4C5
n5:Rule-of-Five
n6:271B5F51-363D-11E5-9242-09173F13E4C5
n5:Traditional-IUPAC-Name
n6:271B5F3F-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-acidic-
n6:271B5F4C-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-basic-
n6:271B5F4D-363D-11E5-9242-09173F13E4C5