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Principles of Heart Failure Pharmacotherapy
Published in Andreas P. Kalogeropoulos, Hal A. Skopicki, Javed Butler, Heart Failure, 2023
Erika L. Hellenbart, Stephanie Dwyer Kaluzna, Robert J. DiDomenico
Conivaptan is administered as a 20 mg IV loading dose followed by a continuous infusion of 20–40 mg/day (0.83–1.7 mg/hour).46,49 In contrast, tolvaptan is administered orally (15 mg once daily) and the dose may be increased every 24 hours to a maximum of 60 mg once daily.48,50 Both drugs are metabolized by CYP3A4, while conivaptan is also a strong inhibitor of CYP3A4.46,49,50 Therefore, conivaptan and tolvaptan are contraindicated in combination with strong CYP3A4 inhibitors, and conivaptan should be used cautiously in combination with drugs that are major substrates for CYP3A4.49,50 Although the half-life of conivaptan is ~5 hours, it exhibits nonlinear pharmacokinetics with a variable half-life due, in part, to inhibition of its own metabolism. 46,48,49 The half-life of tolvaptan is longer (12–24 hours), allowing for once daily dosing.48,50
Nutrition and Heart Failure
Published in David Heber, Zhaoping Li, Primary Care Nutrition, 2017
Tolvaptan has been shown in more than one clinical trial to raise sodium levels; however, mortality and rehospitalization were not improved (Felker et al. 2017). While tolvaptan is FDA approved for the treatment of euvolemic hyponatremia and hypervolemic hyponatremia, it has no place in the treatment of HF.
Station 1: Abdominal
Published in Saira Ghafur, Parminder K Judge, Richard Kitchen, Samuel Blows, Fiona Moss, The MRCP PACES Handbook, 2017
Saira Ghafur, Parminder K Judge, Richard Kitchen, Samuel Blows, Fiona Moss
Vasopressin antagonists – tolvaptan – inhibits binding of vasopressin to V2 receptors, reducing cell proliferation, cyst formation and fluid excretion. NICE recommends this if PKD with CKD stage 2 or 3 at the start of treatment with evidence of rapidly progressive disease
A cross-sectional survey of hospitalization and blood tests implementation status in patients who received tolvaptan under 75 years of age using a Japanese claims database
Published in Expert Opinion on Drug Safety, 2021
Shungo Imai, Kenji Momo, Hitoshi Kashiwagi, Yuki Sato, Takayuki Miyai, Mitsuru Sugawara, Yoh Takekuma
Tolvaptan is a nonpeptide orally selective antagonist of the vasopressin V2 receptor that increases dilute urine production in a dose-dependent manner [1]. Tolvaptan is used for the treatment of the following diseases under the Japanese medical insurance [2]: (1) fluid accumulation induced by chronic heart failure (FA-CHF), (2) fluid accumulation induced by liver cirrhosis (FA-LC), (3) autosomal dominant polycystic kidney disease (ADPKD), and (4) hyponatremia-induced syndrome of inappropriate antidiuretic hormone secretion (SIADH). In Japan, tolvaptan was first approved in October 2010 for FA-CHF. Then, it was additionally approved for treating FA-LC in September 2013. However, the use of tolvaptan for these indications is not approved in other countries and regions [2–8]. Further, tolvaptan is prescribed at lower doses (7.5 or 15 mg daily) for these indications than for ADPKD (60 mg daily).
Pharmacological management of portal hypertension and its complications in children: lessons from adults and opportunities for the future
Published in Expert Opinion on Pharmacotherapy, 2021
Sarah Henkel, Carol Vetterly, Robert Squires, Patrick McKiernan, James Squires
The vasopressin receptor (V2) antagonist tolvaptan, which increases the excretion of free water, has been shown to increase serum sodium at 4 and 30 day intervals in two double blind, placebo controlled phase 3 studies (SALT-1 and SALT-2) of patients with multiple different underlying diseases, including cirrhosis [55]. In cirrhotic patients with hyponatremia, tolvaptan has been shown to improve 6-month survival outcomes if normonatremia was achieved, and to improve ascites in patients with cirrhosis and normal serum sodium and renal function [56,57]. In pediatric patients, tolvaptan has been used in ADPKD and in SIADH without hepatic compromise, but data are otherwise limited in children [57]. In 2013, the U.S. Food and Drug Administration issued a safety alert for tolvaptan due to possible liver injury. The drug labeling was updated to include limiting treatment duration to 30 days, remove the indication for use in patients with cirrhosis, and discontinue use in patients with hepatic injury.
Utilization and budget impact of tolvaptan in the inpatient setting among patients with heart failure and hyponatremia
Published in Current Medical Research and Opinion, 2018
Alpesh N. Amin, Jesse D. Ortendahl, Amanda L. Harmon, Siddhesh A. Kamat, Robert A. Stellhorn, Sandra L. Chase, Shirin V. Sundar
Another potential therapy for HN in patients with HF is arginine vasopressin (AVP)-receptor antagonists or “vaptans”. AVP-receptor antagonists increase sodium levels and exhibit beneficial effects on hemodynamic variables, making their use promising in patients with HN13,17. Tolvaptan is the only oral, selective vasopressin V2-receptor antagonist18 available in the US. Tolvaptan is indicated for the treatment of clinically significant hypervolemic and euvolemic HN (serum sodium <125 mEq/L), or less marked HN that is symptomatic and has resisted correction with fluid restriction, including patients with HF and syndrome of inappropriate antidiuretic hormone (SIADH)18. While patients with HF and HN are being treated with tolvaptan, their sodium levels must be monitored to avoid an overly rapid correction. Therefore, the appropriate setting to initiate tolvaptan treatment is the hospital where sodium can be monitored. Tolvaptan treatment is discontinued when sodium has normalized.