medazepam
{{Short description|Benzodiazepine drug}}
{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 462101416
| IUPAC_name = 7-chloro-1-methyl-5-phenyl-2,3-dihydro-1,4-benzodiazepine
| image = Medazepam.svg
| image_class = skin-invert-image
| width = 170
| image2 = Medazepam ball-and-stick model.png
| tradename = Rudotel
| Drugs.com = {{drugs.com|international|medazepam}}
| pregnancy_category =
| legal_BR = B1
| legal_BR_comment = {{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=Diário Oficial da União |language=pt-BR |publication-date=2023-04-04}}
| legal_CA = Schedule IV
| legal_DE = Rx-only/Anlage III
| legal_US = Schedule IV
| routes_of_administration = Oral
| bioavailability = 50–75% (Сmax = 1–2 hours)
| protein_bound = >99%
| metabolism = Hepatic
| elimination_half-life = 2 hours, 36–150 hours (terminal)
| excretion = Renal (63–85%), Biliary 15–37%
| CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 2898-12-6
| ATC_prefix = N05
| ATC_suffix = BA03
| PubChem = 4041
| DrugBank_Ref = {{drugbankcite|changed|drugbank}}
| DrugBank = none
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 3901
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = P0J3387W3S
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D01292
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 28333
| C=16 | H=15 | Cl=1 | N=2
| smiles = ClC1=CC(C(C2=CC=CC=C2)=NCCN3C)=C3C=C1
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = YLCXGBZIZBEVPZ-UHFFFAOYSA-N
}}
Medazepam is a drug that is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam.{{cite encyclopedia | url = http://www.drug-encyclopedia.eu/DW_EN/benzodiazepines.shtml | encyclopedia = Encyclopedia of Drugs | title = Benzodiazepines }} Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours.{{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 }}
Pharmacology
Medazepam acts as a prodrug to nordazepam.
Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex by allosteric modulation of the GABA receptor.{{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 }} Benzodiazepines may also act via micromolar benzodiazepine-binding sites as Ca2+ 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.{{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 }} It has major active benzodiazepine metabolites, which gives it a more prolonged therapeutic effect after administration.{{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 }}
See also
References
{{reflist}}
External links
- [http://www.inchem.org/documents/pims/pharm/pim460.htm Inchem - Medazepam]
{{Benzodiazepines}}
{{Anxiolytics}}
{{GABAAR PAMs}}