User:Mr. Ibrahem/Tolvaptan

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Mr. Ibrahem/Tolvaptan
Clinical data
Trade namesSamsca, Jinarc, Jynarque, others
Other namesOPC-41061
AHFS/Drugs.comMonograph
MedlinePlusa609033
License data
Pregnancy
category
  • UK: Contraindicated
Routes of
administration		By mouth
Drug classVasopressin-2 receptor (V2) antagonist[1]
Legal status
Legal status
Pharmacokinetic data
BioavailabilityUnknown (40% absorbed)
Protein binding99%
MetabolismLiver (CYP3A4-mediated)[7]
Elimination half-life12 hours (terminal)
Identifiers
  • N-(4-{[(5R)-7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide
Chemical and physical data
FormulaC26H25ClN2O3
Molar mass448.95 g·mol−1
3D model (JSmol)
  • Cc1ccccc1C(=O)Nc2cc(C)c(cc2)C(=O)N3c4ccc(Cl)cc4[C@H](O)CCC3
  • InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31) checkY
  • Key:GYHCTFXIZSNGJT-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Tolvaptan, sold under the brand name Samsca among others, is a medication used to treat low sodium due to heart failure or syndrome of inappropriate antidiuretic hormone (SIADH).[8] It is also used for autosomal dominant polycystic kidney disease (ADPKD).[9] It is taken by mouth.[9] Effects begin within 4 hours.[8]

Common side effects include thirst, nausea, and rapid increase in sodium.[1] Other complications may include osmotic demyelination syndrome, liver failure, and high potassium.[8] It is a vasopressin-2 receptor (V2) antagonist which works by increasing urine production.[1]

Tolvaptan was approved for medical use in the United States and Europe in 2009.[1][8] A generic version was approved in 2020, though was not available commercially as of 2021.[10] In the United States 10 tablets of 30 mg costs about 3,800 USD as of 2021.[11] This amount in the United Kingdom costs the NHS about £750.[9]

References[edit]

  1. ^ a b c d e f "Samsca EPAR". European Medicines Agency (EMA). Archived from the original on 6 January 2021. Retrieved 14 December 2020.
  2. ^ "Samsca 15 mg tablets - Summary of Product Characteristics (SmPC)". (emc). Archived from the original on 24 January 2021. Retrieved 14 December 2020.
  3. ^ "Jinarc 15 mg tablets - Summary of Product Characteristics (SmPC)". (emc). 21 April 2020. Archived from the original on 17 January 2021. Retrieved 14 December 2020.
  4. ^ "Jynarque- tolvaptan kit Jynarque- tolvaptan tablet". DailyMed. 31 March 2020. Archived from the original on 19 October 2020. Retrieved 14 December 2020.
  5. ^ "Samsca- tolvaptan tablet". DailyMed. 26 October 2020. Archived from the original on 18 January 2021. Retrieved 14 December 2020.
  6. ^ "Jinarc EPAR". European Medicines Agency (EMA). Archived from the original on 7 January 2021. Retrieved 14 December 2020.
  7. ^ Shoaf S, Elizari M, Wang Z, et al. (2005). "Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias". J Cardiovasc Pharmacol Ther. 10 (3): 165–71. doi:10.1177/107424840501000304. PMID 16211205. S2CID 39158242.
  8. ^ a b c d e f "Tolvaptan Monograph for Professionals". Drugs.com. Archived from the original on 17 August 2019. Retrieved 8 October 2021.
  9. ^ a b c d BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 706. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  10. ^ "Drugs@FDA: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 20 October 2020. Retrieved 15 August 2020.
  11. ^ "Tolvaptan Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 8 October 2021.
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