Tolvaptan tablets (Tolvaptan) efficacy and role

The active ingredient in Tolvaptan tablets is tolvaptan, which is a selective and competitive arginine vasopressin receptor2 antagonist. Vasopressin acts on V2 receptors found in the walls of the vasculature and in the luminal membrane of the renal collecting ducts. By blocking V2 receptors in the renal collecting duct, aquaporins do not insert themselves into the kidney wall, preventing water absorption.

This effect ultimately results in increased urine output, decreased urinary osmolality, and increased clearance of electrolyte-free water, thereby reducing intravascular volume and increasing serum sodium levels. Tolvaptan is particularly useful in patients with heart failure because of their higher serum vasopressin levels. The pharmacokinetic properties of tolvaptan are stereospecific, with a steady-state ratio of S-(-) and R-(+) enantiomers of approximately 3. The absolute bioavailability of tolvaptan is unknown. At least 40% of the dose is absorbed as tolvaptan or metabolites. Food does not affect the bioavailability of tolvaptan. In the placebo-controlled trial of ADPKD and its open-label extension study, three cases of severe liver injury caused by tolvaptan were observed, indicating that the drug may cause liver injury that can progress to liver failure.

Tolvaptan tablets have been marketed in China and have entered the scope of Class B medical insurance. The price paid by medical insurance is relatively cheap, but the reimbursement ratio is different in different regions, and the price after reimbursement will be different. Domestic pharmacies or hospitals will sell this drug, and the original drug of tolvaptan tablets is also on the market overseas. There are also generic tolvaptan tablets produced in other countries. The price of Indian pharmaceutical factory production specifications15mg*4 tablets per box is around RMB 800 (the price may fluctuate due to the exchange rate). The ingredients of foreign generic drugs are basically the same as those of domestic and foreign original drugs.