Tolvaptan

drugbox
IUPAC_name = "N"-{4- [(6"R")-9-chloro-6-hydroxy-2-azabicyclo [5.4.0]
undeca-8,10,12-triene-2-carbonyl] -3-methyl-phenyl}-
2-methyl-benzamide

---

CAS_number = 150683-30-0
ATC_prefix = C03
ATC_suffix = XA01
ATC_supplemental = [cite web |url=http://www.whocc.no/atcddd/new_atc_ddd.html#ATCDDD_FINAL |title=ATC/DDD Classification (FINAL): New ATC 5th level codes |date=August 27, 2008 |author=WHO International Working Group for Drug Statistics Methodology |publisher=WHO Collaborating Centre for Drug Statistics Methodology |accessdate=2008-09-05]
PubChem = 443894
DrugBank =
C = 26 | H = 25 | Cl = 1 | N = 2 | O = 3
molecular_weight = 448.941 g/mol
bioavailability =
protein_bound =
metabolism = Hepatic (CYP3A4-mediated)cite journal | author = Shoaf S, Elizari M, Wang Z "et al."| title = Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias | journal = J Cardiovasc Pharmacol Ther | volume = 10 | issue = 3 | pages = 165–71 | year = 2005 | pmid = 16211205| doi = 10.1177/107424840501000304]
elimination_half-life = 6 to 8 hours
excretion =
pregnancy_AU =
pregnancy_US =
pregnancy_category =
legal_AU =
legal_CA =
legal_UK =
legal_US =
legal_status =
routes_of_administration = Oral

Tolvaptan (INN), also known as OPC-41061, is a selective, competitive arginine vasopressin receptor 2 antagonist under investigation as a potential treatment for fluid retention and hyponatremia (low blood sodium levels) associated with congestive heart failure.

Tolvaptan is also in fast-track clinical trials [ [http://www.medicalnewstoday.com/medicalnews.php?newsid=38392 Otsuka Maryland Research Institute, Inc.] ] for cure of 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.cite journal | author = Gheorghiade M, Gattis W, O'Connor C "et al."| title = Effects of tolvaptan, a vasopressin antagonist, in patients hospitalized with worsening heart failure: a randomized controlled trial | journal = JAMA | volume = 291 | issue = 16 | pages = 1963–71 | year = 2004 | pmid = 15113814| doi = 10.1001/jama.291.16.1963]

ee also

* Conivaptan
* Mozavaptan
* Satavaptan

Notes

References

*cite journal | author = Gheorghiade M, Niazi I, Ouyang J "et al."| title = Vasopressin V2-receptor blockade with tolvaptan in patients with chronic heart failure: results from a double-blind, randomized trial | journal = Circulation | volume = 107 | issue = 21 | pages = 2690–6 | year = 2003 | pmid = 12742979| doi = 10.1161/01.CIR.0000070422.41439.04