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Important Safety Information Full Prescribing Information

This information is intended for US healthcare professionals

A Unique MOA

The Role of AVP in Hyponatremia

Arginine vasopressin (AVP) is a neurohormone that is synthesized in the hypothalamus, stored in the pituitary gland, and plays a key role in balancing sodium and water in the body.¹ Its release from the pituitary is triggered by changes in the osmotic pressure of extracellular fluid.² Once released, it binds to the V₂ receptors in the collecting ducts of the kidneys.^1,3 The effects of AVP are mediated by three receptor subtypes: V_1A, V_1B (or V₃), and V₂.^4,5 However, the V₂ receptors are responsible for free water reabsorption.^4,5

Antagonism of the V₂ receptors leads to²:

Increases in free water clearance and effective water clearance
Increases in net fluid loss
Increases in urine output
Decreases in urine osmolality

NEXT: Video Presentation—The Role of AVP in Dilutional Hyponatremia

References: 1. Verbalis JG. Disorders of body water homeostasis. Best Pract Res Clin Endocrinol Metab. 2003;17:471-503. 2. Goldsmith SR. Current treatments and novel pharmacologic treatments for hyponatremia in congestive heart failure. Am J Cardiol. 2005;95(suppl):14B-23B. 3. Janicic N, Verbalis JG. Evaluation and management of hypo-osmolality in hospitalized patients. Endocrinol Metab Clin North Am. 2003;32:459-481. 4. Tahara A, Tomura Y, Wada KI, et al. Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V_1A and V₂ receptor antagonist, in vitro and in vivo. J Pharmacol Exp Ther. 1997;282:301-308. 5. Wong LL, Verbalis JG. Vasopressin V2 receptor antagonists. Cardiovasc Res. 2001;51:391-402.

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Vaprisol Works Differently—Find Out How

Learn more about how first-in-class Vaprisol targets AVP to lower serum [Na⁺].

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Vaprisol Provides Proven Efficacy

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Indication

Vaprisol is indicated for the treatment of euvolemic and hypervolemic hyponatremia in hospitalized patients
Vaprisol is not indicated for the treatment of congestive heart failure. It should only be used for the treatment of hyponatremia in patients with underlying heart failure when the expected benefit of raising serum sodium outweighs the increased risk of adverse events

Important Safety Information

Vaprisol is contraindicated in patients with hypovolemic hyponatremia. In addition, coadministration of Vaprisol with potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, clarithromycin, ritonavir, and indinavir, is contraindicated
Serum sodium, volume, and neurological status must be monitored frequently because Vaprisol potentially can cause overly rapid correction of sodium leading to serious sequelae
The use of Vaprisol in patients with hepatic impairment (including ascites, cirrhosis, or portal hypertension) or renal impairment has not been systematically evaluated. Use caution when administering Vaprisol to these patients
The most common adverse reactions reported were infusion site reactions (incidence of 73% and 63% for 20 mg/day and 40 mg/day, respectively) which were also the most common type of adverse reaction leading to discontinuation of Vaprisol. Discontinuations from treatment due to infusion site reactions were more common among Vaprisol-treated patients (3%) than among placebo-treated patients (0%). Other common adverse reactions were headaches (8%, 10%), hypokalemia (22%, 10%), orthostatic hypotension (14%, 6%), and pyrexia (11%, 5%) for Vaprisol 20 mg/day and 40 mg/day, respectively