About: Flupirtine

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An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz:8890 associated with source document(s)

Attributes	Values
rdf:type	http://linked.opendata.cz/ontology/drugbank/Drug
http://linked.open...gbank/description	Flupirtine is a pyridine derivative that is in clinical use as a nonopioid analgesic. It was approved for the treatment of pain in 1984 in Europe. It is not approved for use in the U.S. or Canada, but is currently in phase II trials for the treatment of fibromyalgia. (en)
http://linked.open...generalReferences	# Muller WE, Laplanche JL, Ushijima H, Schroder HC: Novel approaches in diagnosis and therapy of Creutzfeldt-Jakob disease. Mech Ageing Dev. 2000 Jul 31;116(2-3):193-218. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10996019 # Dhar S, Bitting RL, Rylova SN, Jansen PJ, Lockhart E, Koeberl DD, Amalfitano A, Boustany RM: Flupirtine blocks apoptosis in batten patient lymphoblasts and in human postmitotic CLN3- and CLN2-deficient neurons. Ann Neurol. 2002 Apr;51(4):448-66. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11921051 # Swedberg MD, Shannon HE, Nickel B, Goldberg SR: Pharmacological mechanisms of action of flupirtine: a novel, centrally acting, nonopioid analgesic evaluated by its discriminative effects in the rat. J Pharmacol Exp Ther. 1988 Sep;246(3):1067-74. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/2901483 # Abrams SM, Baker LR, Crome P, White AS, Johnston A, Ankier SI, Warrington SJ, Turner P, Niebch G: Pharmacokinetics of flupirtine in elderly volunteers and in patients with moderate renal impairment. Postgrad Med J. 1988 May;64(751):361-3. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/3200777 # Narang PK, Tourville JF, Chatterji DC, Gallelli JF: Quantitation of flupirtine and its active acetylated metabolite by reversed-phase high-performance liquid chromatography using fluorometric detection. J Chromatogr. 1984 Jan 13;305(1):135-43. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/6707137 (en)
http://linked.open...gy/drugbank/group	approved (en) investigational (en)
http://linked.open...drugbank/halfLife	6.5 hrs (average), 11.2-16.8 hrs (average 14 hrs) (elderly), 8.7-10.9 hrs (average 9.8 hrs) (in those with moderate-level renal impairment). (en)
http://linked.open...ugbank/indication	Investigated for use/treatment in fibromyalgia. (en)
sameAs	Flupirtine
Title	Flupirtine (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB06623/identifier/chemspider/48119 http://linked.opendata.cz/resource/drugbank/drug/DB06623/identifier/drugbank/DB06623 http://linked.opendata.cz/resource/drugbank/drug/DB06623/identifier/kegg-drug/D07978 http://linked.opendata.cz/resource/drugbank/drug/DB06623/identifier/pubchem-compound/53276 http://linked.opendata.cz/resource/drugbank/drug/DB06623/identifier/wikipedia/Flupirtine
http://linked.open...mechanismOfAction	Flupirtine upregulates Bcl-2, increases glutathione levels, activates an inwardly rectifying potassium channel, and delays loss of intermitochondrial membrane calcium retention capacity. Flupirtine acts like a NMDA receptor antagonists, but does not bind to the receptor. One study concluded that the discriminative effects of flupirtine are neither of opioid nor of alpha-1 adrenergic type, but are primarily mediated through alpha-2 adrenergic mechanisms [PMID: 2901483]. (en)
http://linked.open...outeOfElimination	72% of flupirtine and its metabolites appear in urine and 18% appear in faeces. (en)
http://linked.open.../drugbank/synonym	Flupirtine (en) SID11111201 (en) SID124880149 (en) SID90341043 (en)
http://linked.open...drugbank/toxicity	Oral, mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50 = 980 mg/kg. (en)
http://linked.open...ogy/drugbank/salt	(en)
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http://linked.open...Molecular-Formula	http://linked.opendata.cz/resource/drugbank/property/271B4D8A-363D-11E5-9242-09173F13E4C5
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http://linked.open...l/drug/hasATCCode	Flupirtine
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http://linked.open...ugbank/absorption	Bioavailability: 90% (oral), 70% (rectal) (en)
http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	56995-20-1 (en)
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http://linked.open...-strongest-basic-	http://linked.opendata.cz/resource/drugbank/property/271B4D94-363D-11E5-9242-09173F13E4C5

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