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Namespace Prefixes

PrefixIRI
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n30http://linked.opendata.cz/resource/drugbank/drug/DB01011/identifier/pubchem-substance/
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n26http://wifo5-03.informatik.uni-mannheim.de/drugbank/resource/drugs/
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n28http://linked.opendata.cz/resource/atc/
n22http://linked.opendata.cz/resource/drugbank/drug/DB01011/identifier/wikipedia/

Statements

Subject Item
n2:DB01011
rdf:type
n3:Drug
n3:description
An inhibitor of the enzyme steroid 11-beta-monooxygenase. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of cushing syndrome. [PubChem]
n3:dosage
n8:271B50DE-363D-11E5-9242-09173F13E4C5
n3:group
approved
n3:halfLife
1.9 ±0.7 hours.
n3:indication
Used as a diagnostic drug for testing hypothalamic-pituitary ACTH function. Occasionally used in Cushing's syndrome.
n3:manufacturer
n21:271B50DC-363D-11E5-9242-09173F13E4C5
owl:sameAs
n26:DB01011 n29:DB01011
dcterms:title
Metyrapone
adms:identifier
n6:PA450486 n7:4174 n14:4030 n15:DB01011 n16:6911 n17:0078-0455-17 n18:MYT n19:C07205 n20:D00410 n22:Metyrapone n30:46504862
n3:mechanismOfAction
The pharmacological effect of Metopirone is to reduce cortisol and corticosterone production by inhibiting the 11-ß-hydroxylation reaction in the adrenal cortex. Removal of the strong inhibitory feedback mechanism exerted by cortisol results in an increase in adrenocorticotropic hormone (ACTH) production by the pituitary. With continued blockade of the enzymatic steps leading to production of cortisol and corticosterone, there is a marked increase in adrenocortical secretion of their immediate precursors, 11-desoxycortisol and desoxycorticosterone, which are weak suppressors of ACTH release, and a corresponding elevation of these steroids in the plasma and of their metabolites in the urine. These metabolites are readily determined by measuring urinary 17-hydroxycorticosteroids (17-OHCS) or 17-ketogenic steroids (17-KGS). Because of these actions, metopirone is used as a diagnostic test, with urinary 17-OHCS measured as an index of pituitary ACTH responsiveness. Metopirone may also suppress biosynthesis of aldosterone, resulting in a mild natriuresis.
n3:packager
n21:271B50DA-363D-11E5-9242-09173F13E4C5 n21:271B50DB-363D-11E5-9242-09173F13E4C5
n3:routeOfElimination
After administration of 4.5 g metyrapone (750 mg every 4 hours), an average of 5.3% of the dose was excreted in the urine in the form of metyrapone (9.2% free and 90.8% as glucuronide) and 38.5% in the form of metyrapol (8.1% free and 91.9% as glucuronide) within 72 hours after the first dose was given.
n3:synonym
Metopiron Metyraponum Metopirone Metyrapone Metirapona
n3:toxicity
Oral LD<sub>50</sub> in rats is 521 mg/kg. One case has been recorded in which a 6-year-old girl died after two doses of Metopirone, 2 g. Symptoms of overdose include cardiac arrhythmias, hypotension, dehydration, anxiety, confusion, weakness, impairment of consciousness, nausea, vomiting, epigastric pain, and diarrhea.
n23:hasConcept
n24:M0013712
foaf:page
n12:metopirone.htm n13:metyrapone.html
n3:IUPAC-Name
n4:271B50E3-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B50E9-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B50E8-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B50E5-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B50E6-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B50E7-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B50E1-363D-11E5-9242-09173F13E4C5 n4:271B50F8-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B50E2-363D-11E5-9242-09173F13E4C5 n4:271B50DF-363D-11E5-9242-09173F13E4C5 n4:271B50FA-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B50E0-363D-11E5-9242-09173F13E4C5
n27:hasATCCode
n28:V04CD01
n3:H-Bond-Acceptor-Count
n4:271B50EF-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B50F0-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B50EA-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B50EB-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B50ED-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B50EC-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B50EE-363D-11E5-9242-09173F13E4C5
n3:absorption
Absorbed rapidly and well when administered orally. Peak plasma concentrations are usually reached 1 hour after administration.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
54-36-4
n3:category
n3:containedIn
n10:271B50DD-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B50F4-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B50F6-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B50F7-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B50F9-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B50F3-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B50F2-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B50F5-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B50E4-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B50F1-363D-11E5-9242-09173F13E4C5