Tolvaptan

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Tolvaptan
Systematic (IUPAC) name
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
Identifiers
CAS number	150683-30-0
ATC code	?
PubChem	443894
Chemical data
Formula	C₂₆H₂₅Cl N₂O₃
Mol. mass	448.941 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic (CYP3A4-mediated)^[1]
Half life	6 to 8 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	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 [1] for treatment 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.^[2]

[edit] Notes

^ 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. PMID 16211205.
^ 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. PMID 15113814.

[edit] 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. PMID 12742979.