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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB00861
rdf:type
n3:Drug
n3:description
Diflunisal, a salicylate derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with pharmacologic actions similar to other prototypical NSAIAs. Diflunisal possesses anti-inflammatory, analgesic and antipyretic activity. Though its mechanism of action has not been clearly established, most of its actions appear to be associated with inhibition of prostaglandin synthesis via the arachidonic acid pathway. Diflunisal is used to relieve pain accompanied with inflammation and in the symptomatic treatment of rheumatoid arthritis and osteoarthritis.
n3:dosage
n13:271B508B-363D-11E5-9242-09173F13E4C5 n13:271B508C-363D-11E5-9242-09173F13E4C5 n13:271B508D-363D-11E5-9242-09173F13E4C5
n3:group
approved
n3:halfLife
8 to 12 hours
n3:indication
For symptomatic treatment of mild to moderate pain accompanied by inflammation (e.g. musculoskeletal trauma, post-dental extraction, post-episiotomy), osteoarthritis, and rheumatoid arthritis.
n3:manufacturer
n14:271B5082-363D-11E5-9242-09173F13E4C5 n14:271B5083-363D-11E5-9242-09173F13E4C5 n14:271B5080-363D-11E5-9242-09173F13E4C5 n14:271B5081-363D-11E5-9242-09173F13E4C5 n14:271B5084-363D-11E5-9242-09173F13E4C5 n14:271B5085-363D-11E5-9242-09173F13E4C5
owl:sameAs
n6:DB00861 n29:DB00861
dcterms:title
Diflunisal
adms:identifier
n18:2951 n19:DB00861 n20:39669 n21:D00130 n22:54868-3049-3 n23:C01691 n24:Diflunisal n25:3059 n26:46507807 n27:FHI n28:PA449313
n3:mechanismOfAction
The precise mechanism of the analgesic and anti-inflammatory actions of diflunisal is not known. Diflunisal is a prostaglandin synthetase inhibitor. In animals, prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain. Since prostaglandins are known to be among the mediators of pain and inflammation, the mode of action of diflunisal may be due to a decrease of prostaglandins in peripheral tissues.
n3:packager
n14:271B507E-363D-11E5-9242-09173F13E4C5 n14:271B507F-363D-11E5-9242-09173F13E4C5 n14:271B507C-363D-11E5-9242-09173F13E4C5 n14:271B507D-363D-11E5-9242-09173F13E4C5 n14:271B507A-363D-11E5-9242-09173F13E4C5 n14:271B507B-363D-11E5-9242-09173F13E4C5 n14:271B5078-363D-11E5-9242-09173F13E4C5 n14:271B5079-363D-11E5-9242-09173F13E4C5 n14:271B5076-363D-11E5-9242-09173F13E4C5 n14:271B5077-363D-11E5-9242-09173F13E4C5 n14:271B5074-363D-11E5-9242-09173F13E4C5 n14:271B5075-363D-11E5-9242-09173F13E4C5 n14:271B5072-363D-11E5-9242-09173F13E4C5 n14:271B5073-363D-11E5-9242-09173F13E4C5 n14:271B5070-363D-11E5-9242-09173F13E4C5 n14:271B5071-363D-11E5-9242-09173F13E4C5 n14:271B506E-363D-11E5-9242-09173F13E4C5 n14:271B506F-363D-11E5-9242-09173F13E4C5 n14:271B506C-363D-11E5-9242-09173F13E4C5 n14:271B506D-363D-11E5-9242-09173F13E4C5
n3:routeOfElimination
The drug is excreted in the urine as two soluble glucuronide conjugates accounting for about 90% of the administered dose. Little or no diflunisal is excreted in the feces.
n3:synonym
2-(Hydroxy)-5-(2,4-difluorophenyl)benzoic acid Dolobid 2',4'-Difluoro-4-hydroxy-3-biphenylcarboxylic acid Diflunisal Diflunisalum 5-(2,4-Difluorophenyl)salicylic acid
n3:toxicity
Oral LD<sub>50</sub> in rat, mouse, and rabbit is 392 mg/kg, 439 mg/kg, and 603 mg/kg, respectively. Symptoms of overdose include drowsiness, nausea, vomiting, diarrhea, hyperventilation, tachycardia, sweating, tinnitus, disorientation, stupor, and coma. The lowest dose without the presence of other medicines which caused death was 15 grams. <p>Selective COX-2 inhibitors have been associated with increased risk of serious cardiovascular events (e.g. myocardial infarction, stroke) in some patients. Current data is insufficient to assess the cardiovascular risk of diflunisal. Short-term use does not appear to be associated with increased cardiovascular risk (except when used immediately following coronary artery bypass graft (CABG) surgery). Risk of GI toxicity including bleeding, ulceration and perforation. Risk of direct renal injury, including renal papillary necrosis. Severe hepatic reactions, including cholestasis and/or jaundice, have been reported. May cause rash or hypersensitivity syndrome.</p>
n10:hasAHFSCode
n16:28-08-04-92
n3:foodInteraction
Food slightly delays rate of absorption with no effect on extent of absorption. Take with food to reduce gastric irritation. Avoid alcohol.
n3:proteinBinding
At least 98 to 99% of diflunisal in plasma is bound to proteins.
n3:synthesisReference
Ruyle, W.V., Jarett, L.H. and Matzuk, A.R. ; U S . Patent 3,714,226; January 30, 1973; assigned to Merck & Co., Inc.
foaf:page
n8:diflunisal.htm n12:diflunisal.html n30:dol1145.shtml
n3:IUPAC-Name
n9:271B5092-363D-11E5-9242-09173F13E4C5
n3:InChI
n9:271B5098-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n9:271B5097-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n9:271B5094-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n9:271B5095-363D-11E5-9242-09173F13E4C5
n3:SMILES
n9:271B5096-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n9:271B50A8-363D-11E5-9242-09173F13E4C5 n9:271B5090-363D-11E5-9242-09173F13E4C5
n3:logP
n9:271B50AA-363D-11E5-9242-09173F13E4C5 n9:271B508E-363D-11E5-9242-09173F13E4C5 n9:271B5091-363D-11E5-9242-09173F13E4C5
n3:logS
n9:271B508F-363D-11E5-9242-09173F13E4C5
n10:hasATCCode
n11:N02BA11
n3:H-Bond-Acceptor-Count
n9:271B509E-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n9:271B509F-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n9:271B5099-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n9:271B509A-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n9:271B509C-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n9:271B509B-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n9:271B509D-363D-11E5-9242-09173F13E4C5
n3:absorption
Rapidly and completely absorbed following oral administration, with a bioavailability of 80-90%. Peak plasma concentrations are achieved 2 - 3 hours following oral administration.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
22494-42-4
n3:category
n3:containedIn
n4:271B5086-363D-11E5-9242-09173F13E4C5 n4:271B5087-363D-11E5-9242-09173F13E4C5 n4:271B508A-363D-11E5-9242-09173F13E4C5 n4:271B5088-363D-11E5-9242-09173F13E4C5 n4:271B5089-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n9:271B50A4-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n9:271B50A6-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n9:271B50A7-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n9:271B50A9-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n9:271B50A3-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n9:271B50A2-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n9:271B50A5-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n9:271B5093-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n9:271B50A0-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n9:271B50A1-363D-11E5-9242-09173F13E4C5