Quinupramine

{{short description|Tricyclic antidepressant}} {{Drugbox | IUPAC_name = (''±'')-11-quinuclidin-3-yl-5,6-dihydrobenzo[b][1]benzazepine | image = Quinupramine.svg | image_class = skin-invert-image

<!--Clinical data--> | tradename = | pregnancy_category = | legal_status = Rx-only | routes_of_administration = Oral

<!--Pharmacokinetic data--> | bioavailability = | metabolism = | elimination_half-life = 33 hours | excretion =

<!--Identifiers--> | CAS_number = 31721-17-2 | ATC_prefix = N06 | ATC_suffix = AA23 | PubChem = 93154 | ChemSpiderID = 84098 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 29O61HFF4L | KEGG = D07336

<!--Chemical data--> | C=21 | H=24 | N=2 }}

'''Quinupramine''' (brand names '''Kevopril''', '''Kinupril''', '''Adeprim''', '''Quinuprine''') is a tricyclic antidepressant (TCA) used in Europe for the treatment of depression.<ref name="isbn3-88763-075-0">{{cite book | author = Swiss Pharmaceutical Society | title = Index Nominum 2000: International Drug Directory (Book with CD-ROM) | publisher = Medpharm Scientific Publishers | location = Boca Raton | year = 2000 | page = 908 | isbn = 3-88763-075-0 | url = https://books.google.com/books?id=5GpcTQD_L2oC&q=quinupramine&pg=PA908}}</ref><ref name="isbn3-527-31058-4">{{cite book | vauthors = Vela JM, Buschmann H, Holenz J, Párraga A, Torrens A | title = Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application | publisher = Wiley-VCH | location = Weinheim | year = 2007 | page = 248 | isbn = 978-3-527-31058-6 | url = https://books.google.com/books?id=yXD4QA-Y_Z0C&q=quinupramine&pg=PA248}}</ref>

Pharmacologically, quinupramine acts ''in vitro'' as a strong muscarinic acetylcholine receptor antagonist (anticholinergic) and H₁ receptor antagonist (antihistamine), moderate 5-HT₂ receptor antagonist, and weak serotonin and norepinephrine reuptake inhibitor.<ref name="pmid6098759">{{cite journal | vauthors = Sakamoto H, Yokoyama N, Kohno S, Ohata K | title = Receptor binding profile of quinupramine, a new tricyclic antidepressant | journal = Japanese Journal of Pharmacology | volume = 36 | issue = 4 | pages = 455–460 | date = December 1984 | pmid = 6098759 | doi = 10.1254/jjp.36.455 | doi-access = free }}</ref> It has negligible affinity for the α₁-adrenergic, α₂-adrenergic, β-adrenergic, or D₂ receptor.<ref name="pmid6098759"/>

Clinically, quinupramine is reported to be stimulating similarly to imipramine, desipramine, and demexiptiline.<ref name="isbn0-306-47406-9">{{cite book | vauthors = Kent A, Billiard M | title = Sleep: physiology, investigations, and medicine | publisher = Kluwer Academic/Plenum | location = New York | year = 2003 | page = 233 | isbn = 0-306-47406-9 | url = https://books.google.com/books?id=IorPrIY6dOYC&q=quinupramine&pg=PA233}}</ref> It can be inferred that its ''in vivo'' metabolites may have stronger effects on the reuptake of norepinephrine and/or serotonin than quinupramine itself.{{Citation needed|date=October 2014}}

== References == {{Reflist|2}}

{{Antidepressants}} {{Navboxes | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 = {{Adrenergic receptor modulators}} {{Histamine receptor modulators}} {{Monoamine reuptake inhibitors}} {{Muscarinic acetylcholine receptor modulators}} {{Serotonin receptor modulators}} }} {{Tricyclics}}

Category:Dibenzazepines Category:Muscarinic antagonists Category:Quinuclidines Category:Tricyclic antidepressants

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