V2 Receptor Antagonist; Tolvaptan

Abstract

Hyponatremia is the most common electrolyte disorder in hospitalized patients. Many studies documented that it was related to increased morbidity and mortality in patients with congestive heart failure, liver cirrhosis, and neurologic diseases. Although knowledge of hyponatremia has been cumulated, the optimal management of hyponatremia remains incompletely established in clinical practice because of the diversity of underlying disease states, and its multiple causes with differing pathophysiologic mechanisms. Since vasopressin receptor antagonists have unique aquaretic effect to selectively increase electrolytes-free water excretion, clinicians could apply a more effective method to treat hyponatremia. Tolvaptan has significant evidence that it improves serum sodium levels in patients with euvolemic or hypervolemic hyponatremia related with heart failure, cirrhosis or syndrome of inappropriate anti-diuretic hormone. Tolvaptan has acceptable safety and tolerability for long-term usage in chronic hyponatremia, and the beneficial effects on serum Na+ occurred in patients with both mild and marked hyponatremia.

Efficacy and safety of a 14-day administration of tolvaptan in the treatment of patients with ascites in hepatic oedema

“…[16][17][18] In addition to these indications, add-on therapy of tolvaptan to conventional diuretics is expected to be useful for the treatment of hepatic oedema, since tolvaptan induces the secretion of free water without sodium excretion (aquaresis). 19 In a pharmacokinetics/pharmacodynamics study, tolvaptan was shown to decrease body weight and ascites volume, and increase urine output, in a dose-dependent manner. 20 Additionally, a dose-finding study investigating the effect of a 7-day treatment with tolvaptan 7.5, 15, and 30 mg/day in hepatic oedema, determined that the optimal dose of tolvaptan was 7.5 mg/day, based on reductions in body weight and abdominal circumference.…”

Postoperative usage of tolvaptan in a patient with aortic valve stenosis complicated by Child-Pugh classification B liver cirrhosis and hepatic edema

“…d The chest X-ray at discharge demonstrated improved cardiomegaly with no sign of congestion Tolvaptan is also used postoperatively for heart surgery patients. The add-on treatment of tolvaptan to conventional diuretics is anticipated to be useful for hepatic edema because tolvaptan increases excess fluid excretion and improves blood sodium levels without causing sodium excretion [4]. The effectiveness of tolvaptan for hepatic edema has been reported [5].…”

Papel de los vaptanes en el tratamiento de la hiponatremia

“…Los vaptanes constituyen una familia con base fisiopatológica sólida y se han mostrado eficaces y seguros, y vienen a ocupar un hueco terapéutico, principalmente en el manejo de la hiponatremia euvolémica, donde las otras alternativas terapéuticas, escasas, se han demostrado insuficientes [90][91][92][93][94][95][96][97][98][99][100] . En EE.…”

“…Esta posibilidad no parece de importancia en el uso de estos fármacos en breves períodos de tiempo; sin embargo, el empleo a largo plazo no se conoce y puede requerir una monitorización estrecha cuando se emplean otros fármacos que se metabolizan por esa vía 96,99,100 . Esta posibilidad no parece de importancia en el uso de estos fármacos en breves períodos de tiempo; sin embargo, el empleo a largo plazo no se conoce y puede requerir una monitorización estrecha cuando se emplean otros fármacos que se metabolizan por esa vía 96,99,100 .…”

“…Con la experiencia acumulada hasta la actualidad, se pueden perfilar las recomendaciones más sobresalientes en su empleo [90][91][92][93][94][95][96][97][98][99][100] . Se recomienda iniciar tolvaptán en hiponatremias leves o moderadas secundarias a SIADH, por lo general con natremias iguales o superiores a 120 mmol/l.…”