Tolvaptan

Tolvaptan

Tolvaptan

Chemical compound

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.[9] Tolvaptan, as Jynarque, was granted approval for medical use in the United States in April 2018.[10]

Quick Facts Clinical data, Trade names ...

The U.S. Food and Drug Administration (FDA) granted tolvaptan a fast track designation for clinical trials investigating its use for the treatment of polycystic kidney disease.[11] The FDA granted Jynarque an orphan drug designation in April 2012, for the treatment of autosomal dominant polycystic kidney disease.[12]

Tolvaptan is available as a generic medication.[13][14]

Medical uses

Tolvaptan (Samsca) is indicated for the treatment of clinically significant hypervolemic and euvolemic hyponatremia.[15]

Tolvaptan (Jynarque) is indicated for slow kidney-function decline in adults at risk of rapidly progressing autosomal dominant polycystic kidney disease (ADPKD).[16]

Tolvaptan phosphate is a prodrug of tolvaptan, developed for intravenous administration. Tolvaptan phosphate is converted into the active drug tolvaptan in the human body following administration.[17]

Side effects

The FDA has determined that tolvaptan should not be used for longer than 30 days and should not be used in patients with underlying liver disease because it can cause liver injury, potentially leading to liver failure.[18] When using to treat hyponatremia, it may cause too rapid correction of hyponatremia resulting in fatal osmotic demyelination syndrome.[19]

Pharmacology

Tolvaptan is a selective vasopressin V2 receptor antagonist.[15][16]

Chemistry

Tolvaptan is a racemate, a 1:1 mixture of the following two enantiomers:[20]

More information Enantiomers of tolvaptan ...

References

  1. [1]
    "Samsca 15 mg tablets - Summary of Product Characteristics (SmPC)". (emc). Retrieved 14 December 2020.
  2. [2]
    "Jinarc 15 mg tablets - Summary of Product Characteristics (SmPC)". (emc). 21 April 2020. Retrieved 14 December 2020.
  3. [3]
    "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
  4. [4]
    "Jynarque- tolvaptan kit Jynarque- tolvaptan tablet". DailyMed. 31 March 2020. Retrieved 14 December 2020.
  5. [5]
    "Samsca- tolvaptan tablet". DailyMed. 26 October 2020. Retrieved 14 December 2020.
  6. [6]
    "Samsca EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 14 December 2020.
  7. [7]
    "Jinarc EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 14 December 2020.
  8. [8]
    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.
  9. [9]
    "Drug Approval Package: Samsca (Tolvaptan) Tablets NDA #022275". U.S. Food and Drug Administration (FDA). 21 July 2009. Retrieved 15 August 2020.
  10. [10]
    "Drug Approval Package: Jynarque (tolvaptan)". U.S. Food and Drug Administration (FDA). 8 June 2018. Retrieved 15 August 2020.
  11. [11]
    "Otsuka Maryland Research Institute, Inc. Granted Fast Track Designation For Tolvaptan In PKD". Medical News Today. Healthline Media UK Ltd. Retrieved 6 December 2018.
  12. [12]
    "Tolvaptan Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 6 April 2012. Retrieved 15 August 2020.
  13. [13]
    "Drugs@FDA: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 15 August 2020.
  14. [14]
    "Tolvaptan Accord: Pending EC decision". European Medicines Agency (EMA). 26 January 2023. Retrieved 28 January 2023.
  15. [15]
    "Samsca- tolvaptan tablet". DailyMed. 28 May 2019. Retrieved 15 August 2020.
  16. [16]
    "Jynarque- tolvaptan kit Jynarque- tolvaptan tablet". DailyMed. 31 March 2020. Retrieved 15 August 2020.
  17. [17]
    "Otsuka Obtains Approval in Japan for SAMTASU® for I.V. Infusion, a V2 -Receptor Antagonist for the Treatment of Cardiac Edema" (Press release). March 28, 2022. Retrieved June 11, 2022.
  18. [18]
    "U.S. Food and Drug Administration." Samsca (Tolvaptan): Drug Safety Communication. N.p., 30 Apr. 2013. Web. 1 June 2014. <http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm350185.htm>[dead link]
  19. [19]
    Goodman & Gilman's the pharmacological basis of therapeutics. Brunton, Laurence L, Knollmann, Björn C, Hilal-Dandan, Randa (Thirteenth ed.). New York. 5 December 2017. ISBN 9781259584732. OCLC 994570810.{{cite book}}: CS1 maint: location missing publisher (link) CS1 maint: others (link)
  20. [20]
    Rote Liste Service GmbH (Hrsg.): Rote Liste 2017 - Arzneimittelverzeichnis für Deutschland (einschließlich EU-Zulassungen und bestimmter Medizinprodukte). Rote Liste Service GmbH, Frankfurt/Main, 2017, Aufl. 57, ISBN 978-3-946057-10-9, S. 222.

Further reading

  • "Tolvaptan". Drug Information Portal. U.S. National Library of Medicine.
Share this article:

This article uses material from the Wikipedia article Tolvaptan, and is written by contributors. Text is available under a CC BY-SA 4.0 International License; additional terms may apply. Images, videos and audio are available under their respective licenses.