| Revision as of 13:38, 23 November 2011 editBeetstra (talk | contribs)Edit filter managers, Administrators172,031 edits Saving copy of the {{drugbox}} taken from revid 457107129 of page Medazepam for the Chem/Drugbox validation project (updated: 'DrugBank', 'CAS_number'). |
Latest revision as of 23:36, 27 March 2024 edit Kimen8 (talk | contribs)Extended confirmed users5,112 editsm →Pharmacology: ce caps |
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{{Short description|Benzodiazepine drug}} |
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{{ambox | text = This page contains a copy of the infobox ({{tl|drugbox}}) taken from revid of page ] with values updated to verified values.}} |
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{{Drugbox |
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{{Drugbox |
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| Verifiedfields = changed |
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| Verifiedfields = changed |
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| Watchedfields = changed |
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| verifiedrevid = 408583871 |
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| verifiedrevid = 462101416 |
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| IUPAC_name = 9-chloro-2-methyl-6-phenyl-2,5-diazabicycloundeca-5,8,10,12-tetraene |
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| IUPAC_name = 7-chloro-1-methyl-5-phenyl-2,3-dihydro-1,4-benzodiazepine |
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| image = Medazepam skeletal.svg |
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| width = 120 |
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| image = Medazepam.svg |
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| width = 170 |
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| image2 = Medazepam3d.png |
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| image2 = Medazepam ball-and-stick model.png |
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<!--Clinical data--> |
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<!--Clinical data--> |
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| tradename = |
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| tradename = Rudotel |
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| Drugs.com = {{drugs.com|international|medazepam}} |
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| Drugs.com = {{drugs.com|international|medazepam}} |
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| pregnancy_category = ? |
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| pregnancy_category = |
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| legal_BR = B1 |
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| legal_status = ](US) |
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| legal_BR_comment = <ref>{{Cite web |author=Anvisa |author-link=Brazilian Health Regulatory Agency |date=2023-03-31 |title=RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial |trans-title=Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control|url=https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |url-status=live |archive-url=https://web.archive.org/web/20230803143925/https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |archive-date=2023-08-03 |access-date=2023-08-16 |publisher=] |language=pt-BR |publication-date=2023-04-04}}</ref> |
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| legal_CA = Schedule IV |
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| legal_DE = Rx-only/Anlage III |
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| legal_US = Schedule IV |
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| routes_of_administration = Oral |
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| routes_of_administration = Oral |
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<!--Pharmacokinetic data--> |
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<!--Pharmacokinetic data--> |
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| bioavailability = ? |
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| bioavailability = 50–75% (С<sub>max</sub> = 1–2 hours) |
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| protein_bound = >99% |
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| metabolism = ] |
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| metabolism = ] |
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| elimination_half-life = 36-150 hours |
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| elimination_half-life = 2 hours, 36–150 hours (terminal) |
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| excretion = ] |
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| excretion = ] (63–85%), ] 15–37% |
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<!--Identifiers--> |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number_Ref = {{cascite|changed|??}} |
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| CAS_number = <!-- blanked - oldvalue: 2898-12-6 --> |
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| CAS_number = 2898-12-6 |
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| ATC_prefix = N05 |
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| ATC_prefix = N05 |
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| ATC_suffix = BA03 |
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| ATC_suffix = BA03 |
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| PubChem = 4041 |
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| PubChem = 4041 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank_Ref = {{drugbankcite|changed|drugbank}} |
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| DrugBank = <!-- blanked - oldvalue: none --> |
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| DrugBank = none |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = 3901 |
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| ChemSpiderID = 3901 |
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| UNII_Ref = {{fdacite|changed|FDA}} |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = P0J3387W3S |
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| UNII = P0J3387W3S |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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<!--Chemical data--> |
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<!--Chemical data--> |
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| C=16 | H=15 | Cl=1 | N=2 |
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| C=16 | H=15 | Cl=1 | N=2 |
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| smiles = ClC1=CC(C(C2=CC=CC=C2)=NCCN3C)=C3C=C1 |
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| molecular_weight = 270.8 |
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| smiles = Clc3ccc1c(\C(=N/CCN1C)c2ccccc2)c3 |
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| InChI = 1/C16H15ClN2/c1-19-10-9-18-16(12-5-3-2-4-6-12)14-11-13(17)7-8-15(14)19/h2-8,11H,9-10H2,1H3 |
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| InChIKey = YLCXGBZIZBEVPZ-UHFFFAOYAU |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI = 1S/C16H15ClN2/c1-19-10-9-18-16(12-5-3-2-4-6-12)14-11-13(17)7-8-15(14)19/h2-8,11H,9-10H2,1H3 |
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| StdInChI = 1S/C16H15ClN2/c1-19-10-9-18-16(12-5-3-2-4-6-12)14-11-13(17)7-8-15(14)19/h2-8,11H,9-10H2,1H3 |
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| StdInChIKey = YLCXGBZIZBEVPZ-UHFFFAOYSA-N |
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| StdInChIKey = YLCXGBZIZBEVPZ-UHFFFAOYSA-N |
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}} |
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}} |
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'''Medazepam''' is a drug that is a ] derivative. It possesses ], ], ], and ] properties. It is known by the following brand names: '''Azepamid''', '''Nobrium''', '''Tranquirax''' (mixed with ]), '''Rudotel''', '''Raporan''', '''Ansilan''' and '''Mezapam'''.<ref>{{cite encyclopedia | url = http://www.drug-encyclopedia.eu/DW_EN/benzodiazepines.shtml | encyclopedia = Encyclopedia of Drugs | title = Benzodiazepines }}</ref> Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours.<ref>{{cite web | url = http://www.bcnc.org.uk/equivalence.html | date = April 2007 | title = Benzodiazepine Equivalency Table | access-date = September 23, 2007 | first = Heather | last = Ashton | name-list-style = vanc | work = Benzodiazepines Co-operation Not Confrontation (BCNC) | archive-date = September 28, 2007 | archive-url = https://web.archive.org/web/20070928121055/http://www.bcnc.org.uk/equivalence.html | url-status = dead }}</ref> |
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==Pharmacology== |
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Medazepam acts as a ] to ]. |
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Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex by allosteric modulation of the GABA receptor.<ref>{{cite journal | vauthors = Zakusov VV, Ostrovskaya RU, Kozhechkin SN, Markovich VV, Molodavkin GM, Voronina TA | title = Further evidence for GABA-ergic mechanisms in the action of benzodiazepines | journal = Archives Internationales de Pharmacodynamie et de Therapie | volume = 229 | issue = 2 | pages = 313–26 | date = October 1977 | pmid = 23084 }}</ref> Benzodiazepines may also act via ] benzodiazepine-binding sites as ] channel blockers and significantly inhibited depolarization-sensitive calcium uptake in experiments with cell components from rat brains. This has been conjectured as a mechanism for high dose effects against seizures in a study.<ref>{{cite journal | vauthors = Taft WC, DeLorenzo RJ | title = Micromolar-affinity benzodiazepine receptors regulate voltage-sensitive calcium channels in nerve terminal preparations | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 81 | issue = 10 | pages = 3118–22 | date = May 1984 | pmid = 6328498 | pmc = 345232 | doi = 10.1073/pnas.81.10.3118 | url = http://www.pnas.org/cgi/reprint/81/10/3118.pdf | type = PDF | bibcode = 1984PNAS...81.3118T | doi-access = free }}</ref> It has major active benzodiazepine metabolites, which gives it a more prolonged therapeutic effect after administration.<ref>{{cite journal | vauthors = Jochemsen R, Breimer DD | title = Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles | journal = Current Medical Research and Opinion | volume = 8 Suppl 4 | pages = 60–79 | year = 1984 | pmid = 6144464 | doi = 10.1185/03007998409109545 }}</ref> |
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== See also == |
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*] |
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*] |
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*] |
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== References == |
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{{reflist}} |
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== External links == |
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* |
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{{Benzodiazepines}} |
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{{Anxiolytics}} |
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{{GABAAR PAMs}} |
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] |
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] |