Methyprylon: Difference between revisions

Jump to navigation Jump to search
VisualWikitext
m (Robot: Automated text replacement (-{{SIB}} + & -{{EH}} + & -{{EJ}} + & -{{Editor Help}} + & -{{Editor Join}} +))
No edit summary
 
Line 1: Line 1:
{{drugbox
{{Drugbox
| IUPAC_name = 3,3-diethyl-5-methyl-piperidine-2,4-dione
| Verifiedfields = changed
| image = Methyprylon.png
| verifiedrevid = 457635672
| width = 130
| IUPAC_name = (''RS'')-3,3-diethyl-5-methylpiperidine-2,4-dione
| image = Methypyron Wiki Str.png
 
| width = 150
| drug_name = Methyprylon
 
<!--Clinical data-->
| tradename =  Dimerin, Methyprylone, Noctan, Noludar
| Drugs.com =
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US = <!-- A / B / C / D / X -->
| pregnancy_category = 
| legal_AU = <!-- Unscheduled / S2 / S4 / S8 -->
| legal_UK = <!-- GSL / P / POM / CD -->
| legal_US = Schedule III<!-- OTC / Rx-only -->
| legal_status = 
| routes_of_administration = oral
 
<!--Pharmacokinetic data-->
| bioavailability = 
| protein_bound = 60%
| metabolism = 
| elimination_half-life = 6-16 hours
| excretion = 
 
<!--Identifiers-->
| CASNo_Ref = {{cascite|correct|CAS}}
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 125-64-4
| CAS_number = 125-64-4
| ATC_prefix = N05
| ATC_prefix = N05
| ATC_suffix = CE02
| ATC_suffix = CE02
| ATC_supplemental =  
| ATC_supplemental =
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C10H17NO2/c1-4-10(5-2)8(12)7(3)6-11-9(10)13/h7H,4-6H2,1-3H3,(H,11,13)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = SIDLZWOQUZRBRU-UHFFFAOYSA-N
| PubChem = 4162
| PubChem = 4162
| DrugBank = APRD00734
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| C=10 | H=17 | N=1 | O=2
| DrugBank = DB01107
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 4018
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = CUT48I42ON
| KEGG_Ref = {{keggcite|changed|kegg}}
| KEGG = D01150
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 1200790
 
<!--Chemical data-->
| C=10 | H=17 | N=1 | O=2  
| molecular_weight = 183.248 g/mol
| molecular_weight = 183.248 g/mol
| bioavailability =
| protein_bound = 60%
| metabolism =
| elimination_half-life = 6-16 hours
| excretion =
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US = <!-- A / B / C / D / X -->
| pregnancy_category =
| legal_AU = <!-- Unscheduled / S2 / S4 / S8 -->
| legal_UK = <!-- GSL / P / POM / CD -->
| legal_US = <!-- OTC / Rx-only -->
| legal_status =
| routes_of_administration =
}}
}}
'''Methyprylon''' (Noludar) is a [[sedative]] of the [[piperidinedione]] derivative family developed by Hoffmann-La Roche.<ref>
{{ cite patent
| country = US
| status  = patent
| number  = 2680116
| title  = Piperidiones and Process for the Manufacture thereof
| gdate  = 1954-06-01
| invent1 = Frick, H.
| invent2 = Lutz, A. H.
| assign1 = Hoffmann-La Roche
}}
__NOTOC__
{{SI}}
{{CMG}}
== Overview ==


{{SI}}
</ref>
This medicine was used for treating [[insomnia]], but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as [[benzodiazepines]].<ref>{{ cite pmid | 16792 }}</ref>
Methyprylon was withdrawn from the US market in June 1989 and the Canadian market in September 1990.
Some other trade names are Noctan and Dimerin.


'''Methyprylon''' is a [[sedative]] of the [[piperidinedione]] derivative family. This medicine was used for treating [[insomnia]], but is now rarely used as it has been replaced by newer drugs with less side effects, such as [[benzodiazepines]]. Methyprylon was withdrawn from the US market in June 1965 and the Canadian market in September 1990.  
==Adverse effects==
Side effects can include skin rash, fever, depression, ulcers or sores in mouth or throat, unusual bleeding or bruising, confusion, fast heartbeat, respiratory depression, swelling of feet or lower legs, dizziness, drowsiness, headache, double vision, clumsiness, constipation, diarrhea, nausea, vomiting, unusual weakness.{{Citation needed|date=October 2011}}


Side effects can include: Skin rash, fever, depression, ulcers or sores in mouth or throat, unusual bleeding or bruising, confusion, fast heartbeat, respiratory depression, swelling of feet or lower legs, dizziness, drowsiness, headache, double vision, clumsiness, constipation, diarrhea, nausea, vomiting, unusual weakness
==Pharmacokinetics==
A study of single oral doses of 300&nbsp;mg in healthy volunteers found that the zero-order absorption model fit the data best. Mean (+/- SD) values for the half-life (9.2 +/- 2.2 h), apparent clearance, (11.91 +/- 4.42 mL/h/kg) and apparent steady-state volume of distribution, (0.97 +/- 0.33 L/kg) were found.<ref>{{ cite pmid | 2866242 }}</ref>


==External links==
A case report found that the pharmacokinetics of methyprylon were not concentration dependent in an overdose case; explanations included saturation or inhibition of metabolic pathways. The generally accepted half-life for a therapeutic dose was not found appropriate in intoxicated patients and would underestimate the time required to reach a safe concentration of the drug.<ref>{{ cite pmid | 1686463 }}</ref>
* {{cite journal | author = Contos D, Dixon K, Guthrie R, Gerber N, Mays D | title = Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration. | journal = J Pharm Sci | volume = 80 | issue = 8 | pages = 768-71 | year = 1991 | id = PMID 1686463}}
* {{cite journal | author = Gwilt P, Pankaskie M, Thornburg J, Zustiak R, Shoenthal D | title = Pharmacokinetics of methyprylon following a single oral dose. | journal = J Pharm Sci | volume = 74 | issue = 9 | pages = 1001-3 | year = 1985 | id = PMID 2866242}}
* {{cite journal | author = Lomen P, Linet O | title = Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients. | journal = J Int Med Res | volume = 4 | issue = 1 | pages = 55-8 | year = 1976 | id = PMID 16792}}


{{Sedative}}
==See also==
{{Colbegin|2}}
*[[Pyrithyldione]]
*[[Piperidione]]
*[[Bemegride]]
*[[Thalidomide]]
*[[Glutethimide]]
*[[Phenglutarimide]]
{{Colend}}


==References==
{{reflist|2}}


[[Category: Drugs]]
{{Sedatives}}
[[Category: Sedatives]]
{{GABAAR PAMs}}


{{WH}}
[[Category:drug]]
{{WikiDoc Sources}}
[[Category:Piperidines]]
[[Category:Lactams]]
[[Category:Ketones]]
[[Category:GABAA receptor positive allosteric modulators]]

Latest revision as of 17:38, 13 April 2015

Methyprylon
Clinical data
Trade namesDimerin, Methyprylone, Noctan, Noludar
Routes of
administration		oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding60%
Elimination half-life6-16 hours
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC10H17NO2
Molar mass183.248 g/mol
 ☒N☑Y (what is this?)  (verify)

Methyprylon (Noludar) is a sedative of the piperidinedione derivative family developed by Hoffmann-La Roche.[1] This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines.[2] Methyprylon was withdrawn from the US market in June 1989 and the Canadian market in September 1990. Some other trade names are Noctan and Dimerin.

Adverse effects

Side effects can include skin rash, fever, depression, ulcers or sores in mouth or throat, unusual bleeding or bruising, confusion, fast heartbeat, respiratory depression, swelling of feet or lower legs, dizziness, drowsiness, headache, double vision, clumsiness, constipation, diarrhea, nausea, vomiting, unusual weakness.[citation needed]

Pharmacokinetics

A study of single oral doses of 300 mg in healthy volunteers found that the zero-order absorption model fit the data best. Mean (+/- SD) values for the half-life (9.2 +/- 2.2 h), apparent clearance, (11.91 +/- 4.42 mL/h/kg) and apparent steady-state volume of distribution, (0.97 +/- 0.33 L/kg) were found.[3]

A case report found that the pharmacokinetics of methyprylon were not concentration dependent in an overdose case; explanations included saturation or inhibition of metabolic pathways. The generally accepted half-life for a therapeutic dose was not found appropriate in intoxicated patients and would underestimate the time required to reach a safe concentration of the drug.[4]

See also

References

  1. ↑ US patent 2680116, Frick, H. & Lutz, A. H., "Piperidiones and Process for the Manufacture thereof", issued 1954-06-01, assigned to Hoffmann-La Roche 

    WikiDoc Resources for Methyprylon

    Articles

    Most recent articles on Methyprylon

    Most cited articles on Methyprylon

    Review articles on Methyprylon

    Articles on Methyprylon in N Eng J Med, Lancet, BMJ

    Media

    Powerpoint slides on Methyprylon

    Images of Methyprylon

    Photos of Methyprylon

    Podcasts & MP3s on Methyprylon

    Videos on Methyprylon

    Evidence Based Medicine

    Cochrane Collaboration on Methyprylon

    Bandolier on Methyprylon

    TRIP on Methyprylon

    Clinical Trials

    Ongoing Trials on Methyprylon at Clinical Trials.gov

    Trial results on Methyprylon

    Clinical Trials on Methyprylon at Google

    Guidelines / Policies / Govt

    US National Guidelines Clearinghouse on Methyprylon

    NICE Guidance on Methyprylon

    NHS PRODIGY Guidance

    FDA on Methyprylon

    CDC on Methyprylon

    Books

    Books on Methyprylon

    News

    Methyprylon in the news

    Be alerted to news on Methyprylon

    News trends on Methyprylon

    Commentary

    Blogs on Methyprylon

    Definitions

    Definitions of Methyprylon

    Patient Resources / Community

    Patient resources on Methyprylon

    Discussion groups on Methyprylon

    Patient Handouts on Methyprylon

    Directions to Hospitals Treating Methyprylon

    Risk calculators and risk factors for Methyprylon

    Healthcare Provider Resources

    Symptoms of Methyprylon

    Causes & Risk Factors for Methyprylon

    Diagnostic studies for Methyprylon

    Treatment of Methyprylon

    Continuing Medical Education (CME)

    CME Programs on Methyprylon

    International

    Methyprylon en Espanol

    Methyprylon en Francais

    Business

    Methyprylon in the Marketplace

    Patents on Methyprylon

    Experimental / Informatics

    List of terms related to Methyprylon

    Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1] == Overview ==

  2. ↑ PMID 16792 (PMID 16792)
    Citation will be completed automatically in a few minutes. Jump the queue or expand by hand
  3. ↑ PMID 2866242 (PMID 2866242)
    Citation will be completed automatically in a few minutes. Jump the queue or expand by hand
  4. ↑ PMID 1686463 (PMID 1686463)
    Citation will be completed automatically in a few minutes. Jump the queue or expand by hand

Template:Sedatives Template:GABAAR PAMs

Retrieved from "https://www.wikidoc.org/index.php?title=Methyprylon&oldid=1086905"