Tolvaptan

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Tolvaptan
File:Tolvaptan.svg
Systematic (IUPAC) name
N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration		 Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability Unknown (40% absorbed)
Protein binding 99%
Metabolism Hepatic (CYP3A4-mediated)[1]
Biological half-life 12 hours (terminal)
Identifiers
CAS Number 150683-30-0
ATC code C03XA01 (WHO) [2]
PubChem CID 443894
Synonyms N-{4-[(6R)-9-chloro-6-hydroxy-2-azabicyclo[5.4.0]undeca-8,10,12-triene-2-carbonyl]-3-methyl-phenyl}-2-methyl-benzamide
Chemical data
Formula C26H25ClN2O3
Molar mass 448.941 g/mol[[Script error: No such module "String".]]
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Tolvaptan (INN), also known as OPC-41061, is a selective, competitive arginine vasopressin receptor 2 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 on May 19, 2009, and is sold by Otsuka Pharmaceutical Co. under the trade name Samsca.

Tolvaptan is also in fast-track clinical trials[3] for polycystic kidney disease. In a 2004 trial, tolvaptan, when administered with traditional diuretics, was noted to increase excretion of excess fluids and improve blood sodium levels in patients with heart failure without producing side effects such as hypotension (low blood pressure) or hypokalemia (decreased blood levels of potassium) and without having an adverse effect on kidney function.[4]

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Kondo, K.; Ogawa, H.; Yamashita, H.; Miyamoto, H.; Tanaka, M.; Nakaya, K.; Kitano, K.; Yamamura, Y.; Nakamura, S.; Onogawa, T.; et al.; Bioor. Med. Chem. 1999, 7, 1743.

Notes

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References

  • Gheorghiade M, Niazi I, Ouyang J; et al. (2003). "Vasopressin V2-receptor blockade with tolvaptan in patients with chronic heart failure: results from a double-blind, randomized trial". Circulation. 107 (21): 2690–6. doi:10.1161/01.CIR.0000070422.41439.04. PMID 12742979. 


Sulfonamides
(except EA)
Thiazide-likes (primarily DCT)
Potassium-sparing (at CD)
Osmotic diuretics (PT, DL)
VAs (DCT and CD)
Other
Hypothalamic
Agonists: Lanreotide · Octreotide
Anterior pituitary
Agonists: Thyrotropin
Posterior pituitary
Agonists: Carbetocin · Demoxytocin
Antagonists: Atosiban


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  1. ↑ 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. 
  2. ↑ WHO International Working Group for Drug Statistics Methodology (August 27, 2008). "ATC/DDD Classification (FINAL): New ATC 5th level codes". WHO Collaborating Centre for Drug Statistics Methodology. Retrieved 2008-09-05. 
  3. ↑ Otsuka Maryland Research Institute, Inc.
  4. ↑ Gheorghiade M, Gattis W, O'Connor C; et al. (2004). "Effects of tolvaptan, a vasopressin antagonist, in patients hospitalized with worsening heart failure: a randomized controlled trial". JAMA. 291 (16): 1963–71. doi:10.1001/jama.291.16.1963. PMID 15113814. 
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