Talk:Tolvaptan
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JAMA
[edit]Oops, not quite effective in heart failure, but some short-term benefits observed. JFW | T@lk 14:27, 25 March 2007 (UTC)
If anyone knows of a study, in the US, for this drug---please send information to me! I have SIADH and my nails are disappearing due to long term use of Demeclocycline. I really want to be switched to this new med.
My email is [email protected]
Thank you67.42.178.80 (talk) 01:54, 25 March 2008 (UTC)
Racemic drug
[edit]Tolvaptan is a racemic small molecule drug (Molecular Weight of 448.9 g.mol-1) and is a lipophilic drug, is essentially insoluble in water, and has fair oral absorption (>40% bioavailable). Tolvaptan hsa a plasma half-life of around 12 hours, a volume of distribution of 3L/kg, and has high plasma protein binding at 99%. Tolvaptan is extensively metabolised by 3A4, and therefore has many concommitent interactions with 3A4 substrates, inhibitors and inducers. Reportedly, Tolvaptan metabolites show no appreciable pharmacology against the vasopressin receptors. Interestingly, Tolvaptan is a racemic drug, with the two enantiomers showing differing PK/PD. Typical daily dosing is 30mg (or ~67µmol), or 60mg if insufficient efficacy is observed.
The compound shown is not Tolvaptan based on this information —Preceding unsigned comment added by ChemSpiderMan (talk • contribs) 13:40, 8 June 2009 (UTC)
- Confirmed, based on Merck Index 14th Ed, entry 9540, Tolvaptan is a racemic compound and so the structure image for this record needs revising. --The chemistds (talk) 13:48, 9 January 2012 (UTC)
Broken link
[edit]Link 2 is broken: http://www.medicalnewstoday.com/medicalnews.php?newsid=38392 apers0n (talk) 17:42, 23 February 2014 (UTC)
Moved from article
[edit]I have moved the following content here because it lacks context/explanation. If anyone wants to use it to improve the article, here it is. -- Ed (Edgar181) 15:04, 7 December 2017 (UTC)
- [[File:Tolvaptan.png|700px|center|thumb|Tolvaptan synthesis:<ref>{{Cite journal | doi = 10.1016/S0968-0896(99)00101-7| title = 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): A potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist| journal = Bioorganic & Medicinal Chemistry| volume = 7| issue = 8| pages = 1743| year = 1999| last1 = Kondo | first1 = K. | last2 = Ogawa | first2 = H. | last3 = Yamashita | first3 = H. | last4 = Miyamoto | first4 = H. | last5 = Tanaka | first5 = M. | last6 = Nakaya | first6 = K. | last7 = Kitano | first7 = K. | last8 = Yamamura | first8 = Y. | last9 = Nakamura | first9 = S. | last10 = Onogawa | first10 = T. | last11 = Mori | first11 = T. | last12 = Tominaga | first12 = M. }}</ref>]]
Polycystic Kidney Disease
[edit]I have removed the primary literature on this subject. It would be good to add some tertiary literature on this topic, e.g. from here. ―Biochemistry🙴❤ 20:21, 3 May 2019 (UTC)