Tolvaptan
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| Image:Tolvaptan.svg | |
| 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 | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C26H25ClN2O3 |
| 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.[1]
Notes
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.
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Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
