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tolvaptan
EntityQ426132· pop 18· linked from 141 articles

Also known as OPC-41061, Samsca®

Tolvaptan, sold under the brand name Samsca among others, is an aquaretic drug that functions as a selective, competitive vasopressin receptor 2 (V2) antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan was approved by the U.S. Food and Drug Administration (FDA) on May 19, 2009, and is sold by Otsuka Pharmaceutical Co. under the trade name Samsca. Tolvaptan, as Jynarque, was granted approval for medical use in the United States in April 2018.

Key facts

Drug.Verifiedfields
changed
Drug.Watchedfields
changed
Drug.verifiedrevid
470611744
Drug.IUPAC_name
N-(4-{[(5R)-7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide
Drug.image
(RS)-Tolvaptan Structural Formula V1.svg
Drug.image_class
skin-invert-image
Drug.image2
Tolvaptan ball-and-stick model.png
Drug.image_class2
bg-transparent
Drug.tradename
Samsca, Jinarc, Jynarque, others
Drug.MedlinePlus
a609033
Drug.DailyMedID
Tolvaptan
Drug.pregnancy_category
UK: Contraindicated
Drug.routes_of_administration
By mouth
Drug.ATC_prefix
C03
Drug.ATC_suffix
XA01
Drug.legal_AU
S4
Drug.legal_UK
POM
Drug.legal_US
Rx-only

via Wikipedia infobox

Research

1,795 papers

via PubMed

~4 min read

Encyclopedic overview

7 sections
Contents
  • Medical uses
  • Side effects
  • Pharmacology
  • Chemistry
  • References
  • Further reading
  • External links

{{Infobox drug | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 470611744 | IUPAC_name = N-(4-{[(5R)-7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide | image = (RS)-Tolvaptan Structural Formula V1.svg | image_class = skin-invert-image | image2 = Tolvaptan ball-and-stick model.png | image_class2 = bg-transparent

| tradename = Samsca, Jinarc, Jynarque, others | Drugs.com = | MedlinePlus = a609033 | DailyMedID = Tolvaptan | pregnancy_AU = | pregnancy_category = UK: Contraindicated | routes_of_administration = By mouth | ATC_prefix = C03 | ATC_suffix = XA01 | ATC_supplemental = | legal_AU = S4 | legal_AU_comment = | legal_CA = | legal_UK = POM | legal_UK_comment = | legal_US = Rx-only | legal_US_comment = | legal_EU = Rx-only | legal_EU_comment = | legal_status = | protein_bound = 99% | metabolism = Liver (CYP3A4-mediated) | elimination_half-life = 12 hours (terminal) | excretion = | CAS_number_Ref = | CAS_number = 150683-30-0 | PubChem = 216237 | IUPHAR_ligand = 2226 | DrugBank_Ref = | DrugBank = DB06212 | ChemSpiderID_Ref = | ChemSpiderID = 187438 | UNII_Ref = | UNII = 21G72T1950 | ChEMBL_Ref = | ChEMBL = 344159 | ChEBI = 32246 | KEGG = D01213

Excerpted from Wikipedia’s “tolvaptan” article, available under the CC BY-SA 4.0 licence.

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