Author(s):
Anna Paul, Lakshmi R
Email(s):
lakshmir@aims.amrita.edu
DOI:
10.52711/0974-360X.2021.00601
Address:
Anna Paul, Lakshmi R
Department of Pharmacy Practice, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, Kerala, India.
*Corresponding Author
Published In:
Volume - 14,
Issue - 6,
Year - 2021
ABSTRACT:
Tolvaptan is the first orally active vasopressin receptor 2 antagonist approved by FDA in 2009 for the treatment of clinically significant hypervolemic and euvolemic hyponatremia associated with heart failure, syndrome of inappropriate antidiuretic hormone secretion, liver cirrhosis. Binding of vasopressin to V2 receptors which are located on renal collecting duct cells were competitively inhibited by Tolvaptan thus prevents vasopressin-mediated activation of these receptors and leads to an increase in the water permeability of the collecting duct causing an increase in the concentration of urine, results in an increase in free water clearance, a decrease in urine osmolality and a fall in serum sodium concentration. Tolvaptan is different from other conventional diuretics because it does not stimulate the sodium channel and increases free water excretion without affecting urinary sodium and potassium excretion. It is metabolized principally via the cytochrome P 450 (CYP 3A) isoenzymes and is eliminated by routes other than renal. Concurrent administration of tolvaptan with ketoconazole or other strong CYP 3A inhibitor decrease the total clearance of tolvaptan and increases tolvaptan concentrations. Urine sodium potassium ratio, weight loss, soluble CD14, urinary aquaporin 2 levels are known predictors of tolvaptan response. Tolvaptan is associated with decreased cost and high effectiveness.
Cite this article:
Anna Paul, Lakshmi R. Tolvaptan in Hyponatremia – A Pharmacologic approach. Research Journal of Pharmacy and Technology. 2021; 14(6):3455-0. doi: 10.52711/0974-360X.2021.00601
Cite(Electronic):
Anna Paul, Lakshmi R. Tolvaptan in Hyponatremia – A Pharmacologic approach. Research Journal of Pharmacy and Technology. 2021; 14(6):3455-0. doi: 10.52711/0974-360X.2021.00601 Available on: https://rjptonline.org/AbstractView.aspx?PID=2021-14-6-91
REFERENCE:
1. Ohnishi A, Orita Y, Okahara R, et al. Potent aquaretic agent. A novel nonpeptide selective vasopressin 2 antagonist (OPC-31260) in men. Journal of Clinical Investigation. 1993;92: 2653–2659.
2. Serradeil-Le C, Wagnon J, Garcia C, et al. Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors. Journal of Clinical Investigation. 1993;92: 224–231.
3. Freidinger RM, Pettibone DJ. Small molecule ligands for oxytocin and vasopressin receptors. Medicinal Research Reviews. 1997;17: 1–16.
4. Tahara A, Tomura Y, Wada KI, et al. Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo. Journal of Pharmacology and Experimental Therapeutics. 1997;282: 301–308.
5. Yamamura Y, Nakamura S, Itoh S, et al. OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosingin rats. Journal of Pharmacology and Experimental Therapeutics. 1998;287: 860–867.
6. Samsca (tolvaptan) [prescribing Information]. Tokyo, Japan: Otsuka Pharmaceutical Co, Ltd. 2009. http://www.samsca.com/pdf/samscaPI. pdf. Accessed May 2, 2010.
7. Zimmerman EA, Nilaver G, Hou-Yu A, et al. Vasopressinergic and oxytocinergic pathways in the central nervous system. Federation Proceedings. 1984;43: 91–96.
8. Goldsmith SR. Baroreceptor-mediated suppression of osmotically stimulated vasopressin in normal humans. Journal of Applied Physiology. 1988;65: 1226–1230.
9. Treschan TA, Peters J. The vasopressin system: physiology and clinical strategies. Anaesthesiology. 2006;105: 599–612.
10. Finley JJ 4th, Konstam MA, Udelson JE. Arginine vasopressin antagonists for the treatment of heart failure and hyponatremia. Circulation. 2008;118(4): 410–421.
11. Felker GM, Connor CM, Braunwald E. Heart Failure Clinical Research Network Investigators. Loop diuretics in acute decompensated heart failure. Circ Heart Fail 2009; 2: 56–62.
12. Torres AC, Wickham EP, Biskobing DM. Tolvaptan for the management of syndrome of inappropriate antidiuretic hormone secretion. Endocrine Practice 2011;17(4): 97-100.
13. Goldberg A, Hammerman H, Petcherski S, et al. Hyponatremia and long-term mortality in survivors of acute ST-elevation myocardial infarction. Arch Intern Med 2006;166: 781-786.
14. Londono MC, Guevara M, Rimola A, et al. Hyponatremia impairs early post transplantation outcome in patients with cirrhosis undergoing liver transplantation. Gastroenterology 2006;130: 1135-1143.
15. Bhardwaj A. Neurological impact of vasopressin dysregulation and hyponatremia. Annals of Neurology 2006;59: 229-236.
16. Renneboog B, Musch W, Vandemergel X, et al. Mild chronic hyponatremia is associated with falls, unsteadiness, and attention deficits. American Journal of Medicine 2006; 119:171.
17. Peri A, Pirozzi N, Parenti G, et al. Hyponatremia and the syndrome of inappropriate secretion of antidiuretic hormone (SIADH). Journal of Endocrinological Investigation. 2010; 33: 671–682.
18. Schrier RW, Gross P, Gheorghiade M, et al. Tolvaptan, a selective oral vasopressin V2-receptor antagonist, for hyponatremia. New England Journal of Medicine. 2006; 355(20): 2099–2112.
19. Wong VW, Chim AM, Wong GL, et al. Performance of the new MELD-Na score in predicting 3-month and 1-year mortality in Chinese patients with chronic hepatitis B. Liver Transplantation 2007; 13: 1228-1235.
20. 19.. Kim WR, Biggins SW, Kremers WK, et al. Hyponatremia and mortality among patients on the liver-transplant waiting list. New England Journal of Medicine 2008; 359: 1018-1026.
21. Runyon BA, Aasld. Introduction to the revised American Association for the Study of Liver Diseases Practice Guideline management of adult patients with ascites due to cirrhosis 2012. Hepatology 2013; 57: 1651-1653.
22. Wong F, Gines P, Watson H, et al. Effects of a selective vasopressin V2 receptor antagonist, satavaptan, on ascites recurrence after paracentesis in patients with cirrhosis. Journal of Hepatology 2010; 53: 283-90.
23. Spasovski G, Vanholder R, Allolio B, et al. Clinical practice guideline on diagnosis and treatment of hyponatraemia. Nephrology Dialysis Transplantation 2014; 29(2): 1-39.
24. European Association for the Study of the Liver. EASL clinical practice guidelines on the management of ascites, spontaneous bacterial peritonitis, and hepatorenal syndrome in cirrhosis. Journal of Hepatology 2010; 53: 397-417.
25. Sakaida I, Kawazoe S, Kajimura K, Saito T, Okuse C, Takaguchi K, Okada M, et al. Tolvaptan for improvement of hepatic edema: A phase 3, multicenter, randomized, double-blind, placebo-controlled trial. Hepatology Research 2014; 44: 73-82.
26. . Gine´s P, Berl T, Bernardi M, Bichet DG, Hamon G, Jime´nez W, et al. Hyponatremia in cirrhosis: from pathogenesis to treatment. Hepatology 1998; 28: 851-864
27. 26.Torres VE, Meijer E, Bae KT, et al. Rationale and design of the TEMPO (Tolvaptan Efficacy and Safety in management of Autosomal Dominant Polycystic Kidney Disease and its Outcomes)3/4 study. American Journal of Kidney Diseases 2011; 57: 692-699.
28. Gheorghiade M, Konstam MA, Burnett JC Jr., Grinfeld L, Maggioni AP, Swedberg K, et al. Short-term clinical effects of tolvaptan, an oral vasopressin antagonist, in patients hospitalized for heart failure: the EVEREST Clinical Status Trials. Journal of American Medical Association. 2007; 297(12): 1332–1343.
29. Soupart A, Gross P, Legros JJ, et al. Successful long-term treatment of hyponatremia in syndrome of inappropriate antidiuretic hormone secretion with satavaptan (SR121463B), an orally active nonpeptide vasopressin V2- receptor antagonist. Clinical Journal of the American Society of Nephrology 2006; 1: 1154–1160.
30. Ellison DH, Berl T: Clinical practice: The syndrome of inappropriate antidiuresis. New England Journal of Medicine 2007;356: 2064–2072.
31. Miyazaki T, Fujiki H, Yamamura Y, et al. Tolvaptan, an orally active vasopressin V(2)-receptor antagonist—pharmacology and clinical trials. Cardiovascular Drug Reviews. 2007; 25(1): 1–13.
32. Shoaf SE, Wang Z, Bricmont P, Mallikaarjun S. Pharmacokinetics, pharmacodynamics, and safety of tolvaptan, a nonpeptide AVP antagonist, during ascending single-dose studies in healthy subjects. Journal of Clinical Pharmacology. 2007;47(12):1498–1507.Plosker GL. Tolvaptan. Drugs. 2010; 70(4): 443–454.
33. Kawaratani H, Fukui H, Moriya K, et al. Predictive parameter of tolvaptan effectiveness in cirrhotic ascites. Hepatology Research. 2017; 47: 854-861.
34. Frey EA, Miller DS, Jahr TG et al. Soluble CD14 participates in the response of cells to lipopolysaccharide. Journal of Experimental Medicine.1992;176: 1665-1671.
35. Imamura T, Kinugawa K, Fujino T, et al. Increased Urine Aquaporin-2 Relative to Plasma Arginine Vasopressin Is a Novel Marker of Response to Tolvaptan in Patients with Decompensated Heart Failure. Circulation Journal. 2014; 78: 2240-2249.
36. Imamura T, Kinugawa K, Minatsuki S, et al. Urine Osmolality Estimated Using Urine Urea Nitrogen, Sodium and Creatinine Can Effectively Predict Response to Tolvaptan in Decompensated Heart Failure Patients. Circulation Journal. 2013; 77: 1208-1213.
37. Komiyama Y, Kurosaki M, Nakanishi H, et al. Prediction of diuretic response to tolvaptan by a simple, readily available spot urine Na/K ratio. PLOS One. 2017;12: e0174649.
38. Remya R, PC, S., Das, et al. A study on safety and efficacy of tolvaptan in hyponatremic patients with urinary sodium loss. International Journal of Pharmaceutical Sciences Review and Research. 2016; 38: 115-119.
39. Torres VE, Chapman AB, Devuyst O, et al. TEMPO 3:4 Trial Investigators. Tolvaptan in patients with autosomal dominant polycystic kidney disease. New England Journal of Medicine. 2012; 367: 2407-2418.
40. Berl T, Quittnat-Pelletier F, Verbalis JG, et al. Oral tolvaptan is safe and effective in chronic hyponatremia. Journal of the American Society of Nephrology. 2010; 21(4): 705–712.
41. Callahan MA, Do HT, Caplan DW, et al. Economic impact of hyponatremia in hospitalized patients: a retrospective cohort study. Postgraduate Medical Journal. 2009; 121: 186–191.
42. Cyr PL, Slawsky KA, Olchanski N, et al. Effect of serum sodium concentration and tolvaptan treatment on length of hospitalization in patients with heart failure. American Journal of Health System Pharmacy. 2011; 68: 328–333.