Tolvaptan phosphate: Difference between revisions

Latest revision as of 05:34, 16 February 2025

Tolvaptan[edit]

Tolvaptan is a vasopressin receptor antagonist used primarily in the treatment of hyponatremia and autosomal dominant polycystic kidney disease (ADPKD). It is a selective V2 receptor antagonist that works by increasing the excretion of free water, thereby correcting the imbalance of water and sodium in the body.

Mechanism of Action[edit]

Tolvaptan acts by selectively binding to the V2 receptors in the kidneys, which are responsible for the antidiuretic effects of vasopressin. By blocking these receptors, Tolvaptan prevents the action of vasopressin, leading to an increase in the excretion of free water without the loss of electrolytes. This results in an increase in serum sodium concentration, making it effective in treating hyponatremia.

Clinical Uses[edit]

Tolvaptan is primarily used in the management of:

Hyponatremia: Particularly in cases associated with the syndrome of inappropriate antidiuretic hormone secretion (SIADH).
Autosomal dominant polycystic kidney disease (ADPKD): Tolvaptan slows the progression of kidney cyst development and renal insufficiency in patients with ADPKD.

Side Effects[edit]

Common side effects of Tolvaptan include:

Increased thirst
Dry mouth
Polyuria
Fatigue

Serious side effects may include:

Liver injury
Hypernatremia

Contraindications[edit]

Tolvaptan is contraindicated in patients with:

Anuria
Hypovolemic hyponatremia
Urgent need to raise serum sodium acutely
Inability to sense or respond to thirst

Pharmacokinetics[edit]

Tolvaptan is well absorbed after oral administration, with a bioavailability of approximately 56%. It is extensively metabolized in the liver, primarily by the cytochrome P450 enzyme CYP3A4. The elimination half-life of Tolvaptan is about 3 to 4 hours.

Related Pages[edit]

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-'''Tolvaptan phosphate''' is a [[pharmaceutical drug]] used primarily in the treatment of [[hyponatremia]] (low blood sodium levels) associated with [[congestive heart failure]], [[cirrhosis]], and the [[syndrome of inappropriate antidiuretic hormone]] (SIADH). It is a selective [[vasopressin receptor 2]] antagonist that increases the excretion of water without affecting the excretion of electrolytes.
+== Tolvaptan ==
+[[File:Tolvaptan_phosphate.svg|thumb|right|Chemical structure of Tolvaptan]]
+'''Tolvaptan''' is a [[vasopressin receptor antagonist]] used primarily in the treatment of [[hyponatremia]] and [[autosomal dominant polycystic kidney disease]] (ADPKD). It is a selective V2 receptor antagonist that works by increasing the excretion of free water, thereby correcting the imbalance of water and sodium in the body.
 == Mechanism of Action ==
-Tolvaptan phosphate works by blocking the action of [[vasopressin]], a hormone that regulates the balance of water and sodium in the body. By inhibiting the vasopressin receptor 2, tolvaptan phosphate increases the excretion of water in the urine, thereby increasing the concentration of sodium in the blood.
-== Clinical Use ==
+Tolvaptan acts by selectively binding to the V2 receptors in the [[kidney]]s, which are responsible for the antidiuretic effects of [[vasopressin]]. By blocking these receptors, Tolvaptan prevents the action of vasopressin, leading to an increase in the excretion of free water without the loss of electrolytes. This results in an increase in serum sodium concentration, making it effective in treating hyponatremia.
-Tolvaptan phosphate is used in the management of hyponatremia in patients with congestive heart failure, cirrhosis, and SIADH. It is also used in the treatment of [[autosomal dominant polycystic kidney disease]] (ADPKD), a genetic disorder characterized by the growth of numerous cysts in the kidneys.
+== Clinical Uses ==
+Tolvaptan is primarily used in the management of:
+* [[Hyponatremia]]: Particularly in cases associated with the syndrome of inappropriate antidiuretic hormone secretion (SIADH).
+* [[Autosomal dominant polycystic kidney disease]] (ADPKD): Tolvaptan slows the progression of kidney cyst development and renal insufficiency in patients with ADPKD.
 == Side Effects ==
-Common side effects of tolvaptan phosphate include thirst, dry mouth, and increased urination. Serious side effects may include liver damage, low blood sodium levels, and dehydration.
+Common side effects of Tolvaptan include:
+* Increased thirst
+* Dry mouth
+* Polyuria
+* Fatigue
+Serious side effects may include:
+* Liver injury
+* Hypernatremia
 == Contraindications ==
-Tolvaptan phosphate is contraindicated in patients with hypersensitivity to the drug or any of its components. It is also contraindicated in patients with anuria (inability to urinate), hypovolemic hyponatremia, and in patients who cannot sense or respond to thirst.
-== Drug Interactions ==
+Tolvaptan is contraindicated in patients with:
-Tolvaptan phosphate may interact with other drugs such as [[CYP3A4]] inhibitors, which can increase the concentration of tolvaptan in the blood and potentially increase the risk of side effects.
+* Anuria
+* Hypovolemic hyponatremia
+* Urgent need to raise serum sodium acutely
+* Inability to sense or respond to thirst
+== Pharmacokinetics ==
+Tolvaptan is well absorbed after oral administration, with a bioavailability of approximately 56%. It is extensively metabolized in the liver, primarily by the [[cytochrome P450]] enzyme CYP3A4. The elimination half-life of Tolvaptan is about 3 to 4 hours.
+== Related Pages ==
-== Dosage and Administration ==
+* [[Vasopressin receptor antagonist]]
-The dosage of tolvaptan phosphate is individualized based on the patient's condition and response to treatment. It is usually taken orally once daily.
+* [[Hyponatremia]]
+* [[Autosomal dominant polycystic kidney disease]]
+* [[Kidney]]
-[[Category:Pharmaceutical drugs]]
 [[Category:Vasopressin receptor antagonists]]
-{{Pharma-stub}}
+[[Category:Diuretics]]
+[[Category:Kidney disease treatments]]