Conivaptan hydrochloride

What is Conivaptan hydrochloride?

Conivaptan hydrochloride (Vaprisol) is a vasopressin receptor antagonist used to raise serum sodium in hospitalized patients with euvolemic and hypervolemic hyponatremia.

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Conivaptan structure

Conivaptan-3D-balls

What are the uses of this medicine?

• Conivaptan hydrochloride (Vaprisol) is used to raise serum sodium in hospitalized patients with euvolemic and hypervolemic hyponatremia.

Limitations of Use:

• VAPRISOL has not been shown to be effective for the treatment of the signs and symptoms of heart failure.
• It has not been established that raising serum sodium with VAPRISOL provides a symptomatic benefit to patients.

How does this medicine work?

• Conivaptan hydrochloride is a dual arginine vasopressin (AVP) antagonist.
• The level of AVP in circulating blood is critical for the regulation of water and electrolyte balance and is usually elevated in both euvolemic and hypervolemic hyponatremia.
• The AVP effect is mediated through V2 receptors, which are functionally coupled to aquaporin channels in the apical membrane of the collecting ducts of the kidney.
• These receptors help to maintain plasma osmolality within the normal range.
• The predominant pharmacodynamic effect of conivaptan hydrochloride in the treatment of hyponatremia is through its V2 antagonism of AVP in the renal collecting ducts, an effect that results in aquaresis, or excretion of free water.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• hypovolemic hyponatremia.
• Coadministration with potent CYP3A inhibitors such as ketoconazole, itraconazole, clarithromycin, ritonavir, and indinavir.
• Anuria

What drug interactions can this medicine cause?

• Coadministration with strong CYP3A inhibitors (e.g. ketoconazole, itraconazole, clarithromycin, ritonavir and indinavir) increases conivaptan exposure and is contraindicated.
• Coadministration with CYP3A substrates results in increased exposure of the other drug.
• Exposure to coadministered digoxin may be increased and digoxin levels should be monitored.

Is this medicine FDA approved?

• It was approved in 2004 for hyponatremia (low blood sodium levels).
• The compound was discovered by Astellas and marked in 2006.
• The drug is now marketed by Cumberland Pharmaceuticals, Inc. Conivaptan inhibits two of the three subtypes of the vasopressin receptor (V1a and V2).

How should this medicine be used?

Recommended dosage:

• Loading Dose: 20 mg IV administered over 30 minutes , followed by:
• Continuous infusion: 20 mg/day over 24 hours, for 2 to 4 days.
• Following initial day of treatment, dosage may be increased to 40 mg/day continuous infusion as needed to raise serum sodium.
• Monitor volume status and serum sodium frequently and discontinue if patient develops hypovolemia, hypotension or undesirable rapid rate of increase in serum sodium.

Hepatic impairment:

• Decrease the dose in patients with moderate or severe hepatic impairment.

Administration:

• VAPRISOL is for intravenous use only.
• VAPRISOL is for use in hospitalized patients
• Administer VAPRISOL through large veins and change of the infusion site every 24 hours to minimize the risk of vascular irritation.
• The total duration of infusion of VAPRISOL (after the loading dose) should not exceed four days.
• Patients receiving VAPRISOL must have frequent monitoring of serum sodium and volume status.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Intravenous injection solution: conivaptan hydrochloride 20 mg/100 mL premixed in 5% Dextrose

This medicine is available in fallowing brand namesː

• VAPRISOL

What side effects can this medication cause?

The most common side effects of this medicine include:

• infusion site reactions (including phlebitis)
• pyrexia
• hypokalemia
• headache
• orthostatic hypotension

What special precautions should I follow?

• The amount of safety data on the use of VAPRISOL in patients with hypervolemic hyponatremia associated with heart failure is limited. VAPRISOL should be used to raise serum sodium in such patients only after consideration of other treatment options.
• For patients who develop hypovolemia or hypotension while receiving VAPRISOL, VAPRISOL should be discontinued, and volume status and vital signs should be frequently monitored. Once the patient is again euvolemic and is no longer hypotensive, VAPRISOL may be resumed at a reduced dose if the patient remains hyponatremic.
• Infusion site reactions are common and can include serious reactions, even with proper infusion rates . Administer VAPRISOL via large veins, and rotate the infusion site every 24 hours.
• Osmotic demyelination syndrome is a risk associated with overly rapid correction of hyponatremia. Monitor serum sodium and neurologic status as serious neurologic sequelae can result from over rapid correction of serum sodium.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hypotension and thirst

Management of overdosage:

• In case of overdose, based on expected exaggerated pharmacological activity, symptomatic treatment with frequent monitoring of vital signs and close observation of the patient is recommended.

Can this medicine be used in pregnancy?

• There are no available data with VAPRISOL in pregnant women to inform a drug-associated risk for major birth defects and miscarriage.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• conivaptan hydrochloride

Inactive ingredients:

• dextrose
• lactic acid

Who manufactures and distributes this medicine?

Marketed by:

• Cumberland Pharmaceuticals Inc.
• Nashville TN

• VAPRISOL is a registered trademark of Cumberland Pharmaceuticals Inc.

What should I know about storage and disposal of this medication?

• VAPRISOL in INTRAVIA Plastic Containers should be stored at 25°C (77°F); however, brief exposure up to 40°C (104°F) does not adversely affect the product.
• Avoid excessive heat.
• Protect from freezing.
• Protect from light until ready to use.

• Dailymed label info on Conivaptan hydrochloride
• FDA Conivaptan hydrochloride

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