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Mechanism of Action

Targets AVP and excess water to raise serum sodium concentration1,2

In patients with hyponatremia, the neurohormone arginine vasopressin (AVP) binds to the V2 receptors in the collecting ducts of the kidneys, resulting in free water reabsorption.3-5

  • VAPRISOL is an aquaretic2
  • By blocking AVP at the V2 receptor, VAPRISOL promotes free water clearance and raises serum sodium concentration to regulate the water/sodium balance1

This video brings the role of AVP in hyponatremia to life:

REFERENCES: 1. Vaprisol® [Package Insert] Cumberland Pharmaceuticals Inc. Nashville, TN 2016 2. Verbalis JG, Goldsmith SR, Greenberg A, Schrier RW, Sterns RH. Hyponatremia treatment guidelines 2007: expert panel recommendations. Am J Med. 2007;120(11A):S1-S21. 3. Verbalis JG. Disorders of body water homeostasis. Best Pract Res Clin Endocrinol Metab. 2003;17:471-503. 4. Janicic N, Verbalis JG. Evaluation and management of hypo-osmolality in hospitalized patients. Endocrinol Metab Clin North Am. 2003;32:459-481. 5. Tahara A, Tomura Y, Wada K-I, et al. Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo. J Pharmacol Exp Ther. 1997;282:301-308.

Indication: VAPRISOL is indicated to raise serum sodium in hospitalized patients with euvolemic and hypervolemic hyponatremia.
Important Limitations: VAPRISOL has not been shown to be effective for the treatment of the signs and symptoms of heart failure and is not approved for this indication. It has not been established that raising serum sodium with VAPRISOL provides a symptomatic benefit to patients.


VAPRISOL is contraindicated in patients with hypovolemic hyponatremia. The coadministration of VAPRISOL with potent CYP3A inhibitors, such as ketoconazole, itraconazole, clarithromycin, ritonavir, and indinavir, is contraindicated. In addition, no benefit can be expected in patients unable to make urine.

Hyponatremia associated with heart failure: Safety data on the use of VAPRISOL in these patients are limited. Consider other treatment options.
Overly rapid correction of serum sodium: Monitor serum sodium, volume and neurologic status and if the patient develops an undesirably rapid rate of rise of serum, VAPRISOL should be discontinued. If serum sodium concentration continues to rise, VAPRISOL should not be resumed. Serious neurologic sequelae, including osmotic demyelination syndrome, can result from over rapid correction of serum sodium. In susceptible patients, including those with severe malnutrition, alcoholism or advanced liver disease, slower rates of correction should be used.
Hypovolemia or Hypotension: For patients who develop hypovolemia or hypotension while receiving VAPRISOL, VAPRISOL should be discontinued, and volume status and vital signs should be monitored.
Infusion site reactions: Serious reactions have occurred. Administer through large veins and change infusion site every 24 hours.

The most common adverse reactions (incidence ≥10%) reported in clinical trials were infusion site reactions (including phlebitis), pyrexia, hypokalemia, headache and orthostatic hypotension.

Potent CYP3A inhibitors may increase the exposure of conivaptan and are contraindicated. Generally avoid CYP3A substrates. Exposure to coadministered digoxin may be increased and digoxin levels should be monitored.

Use in Patients with Hepatic Impairment
In patients with moderate to severe hepatic impairment, initiate VAPRISOL with a loading dose of 10 mg over 30 minutes followed by 10 mg/day as a continuous infusion for 2 to 4 days. If no rise in serum sodium, VAPRISOL may be titrated upward to 20 mg/day.