Tolsama 30mg is an aquaretic drug which functions as a selective, competitivevasopressin receptor 2 (V2) antagonist will prevent hyponatremia (low blood sodium levels) along with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH)
Tolsama 30mg decrease the level of a hormone which manage the balance of water and salt (sodium) in the body. High levels of this hormone can cause an imbalance that causes low sodium levels and fluid retention.
Tolsama 30mg is used for the treatment of clinically important hypervolemic and euvolemic hyponatremia contains patients with heart failure and Syndrome of Inappropriate Antidiuretic Hormone (SIADH).
Tolvaptan is a type of selective and competitive arginine vasopressin receptor 2 antagonist. Vasopressin show action on the V2 receptors found in the walls of the vasculature and luminal membranes of renal collecting ducts. By stopping V2 receptors in the renal collecting ducts, aquaporins do not enter themselves into the walls hence inhibiting water absorption. This activity basically results in a rise in urine volume, reduce urine osmolality, and increase electrolyte-free water clearance to decrease intravascular volume and a higher serum sodium level. Tolvaptan is specifically required for heart failure patients as they have higher serum levels of vasopressin.
Time to peak plasma concentration of Tolsama is 2-4 hours and the absolute bioavailability is unknown. Food will not affect the bioavailability of Tolsama.
The plasma protein bounding of Tolsama is 99% and Volume of distribution in healthy subjects is 3L/kg.
Tolsama is metabolism occurs by CYP3A4 enzyme in the liver.
< 1% is excreted in the urine (unchanged form) and through fecal is very small amount of renal elimination.
In oral dose, half-life of Tolsama is 12 hours
The recommended starting dose for Tolsama is 15 mg administered once daily without food. The dose is increased to 30 mg once daily, after at least 24 hours, to a maximum of 60 mg once daily, as required to achieve the desired level of serum sodium.
Do not administer Tolsama for more than 30 days to minimize the risk of liver injury.
Following discontinuation from Tolsama, advised the patients to resume fluid restriction and should be observed for changes in serum sodium and volume status.
Administration of Tolsama should be without food
Grape juice should be avoided during therapy with Tolsama
Administrating monotherapy oral doses up to 480 mg and multiple doses up to 300 mg once in a day for 5 days have been well accepted in studies in healthy subjects. There is no essential antitoxin for Tolsama intoxication. The signs and symptoms of an acute overdose can be expected to be those of extra pharmacologic effect: a increase in serum sodium concentration, polyuria, thirst, and dehydration/hypovolemia.
- The conditions like Hypernatremia, hypovolemia, and/or dehydration; provoke patient to drink whenever thirsty
- Risk of potassium level increased
- Tolsama 15mg produce Osmotic demyelination syndrome is a harm along with too-fast correction of hyponatremia
- Tolsama 15mg can develops serious and likely fatal liver injury; acute liver failure needed liver transplantation reported; discontinue if laboratory abnormalities or signs or symptoms of liver injury are apparent.