Conivaptan Hydrochloride

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Cat Number

API0232082

CAS Number

168626-94-6

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Product Detail Description Scientific Support Customer Q&A

CAS Number

168626-94-6

EINECS

111-171-7

Synonyms

Vaprisol; YM087; CI-1025

Molecular Formula

C32H27ClN4O2

Molecular Weight

535.04

Smiles

CC1=NC2=C(N1)CCN(C3=CC=CC=C32)C(=O)C4=CC=C(C=C4)NC(=O)C5=CC=CC=C5C6=CC=CC=C6.Cl

Appearance

White to off-white powder

Boiling Point

751.2ºC

General Description

Conivaptan hydrochloride is a nonpeptide, dual antagonist of arginine vasopressin receptors approved for intravenous use in hospitalized patients. As the hydrochloride salt formulation, it was initially approved by the FDA in 2005 for raising serum sodium levels in euvolemic and hypervolemic hyponatremia.

Mechanism of Action

Conivaptan exerts its pharmacological effects by competitively and reversibly antagonizing both V1A and V2 vasopressin receptor subtypes with high affinity. Blockade of V2 receptors in the renal collecting ducts inhibits antidiuretic hormone-mediated water reabsorption, producing electrolyte-sparing aquaresis—excretion of free water without sodium loss.

Application

Conivaptan hydrochloride is indicated to raise serum sodium in hospitalized patients with euvolemic or hypervolemic hyponatremia associated with conditions such as syndrome of inappropriate antidiuretic hormone secretion, heart failure, or cirrhosis. The drug is contraindicated in hypovolemic hyponatremia, anuria, and with potent CYP3A inhibitors, and its use is limited to short-term inpatient management.

Marbury T, et al. assessed the pharmacokinetics, protein binding, and safety of a 48-hour intravenous conivaptan infusion in eight subjects with severe hepatic impairment (Child-Pugh score 10–15) compared with nine subjects with normal liver function. Following a 20 mg loading dose and two consecutive 20 mg daily infusions, individuals with severe hepatic impairment exhibited approximately 60% higher overall drug exposure (AUC_INF), a longer terminal elimination half-life (12 vs. 9 hours), and 65% lower clearance compared to subjects with normal liver function. Although well tolerated, the significant pharmacokinetic differences led the authors to recommend a 50% dose reduction for conivaptan in patients with severe hepatic impairment to ensure safe and effective treatment for hyponatremia.

Fig. 1 Mean plasma conivaptan clearance versus baseline laboratory values. (Marbury T, et al., 2017)

References

Marbury T, et al. Pharmacokinetics of conivaptan use in patients with severe hepatic impairment. Drug Des Devel Ther. 2017;11:373-382.

Does Conivaptan Hydrochloride require light protection during long-term storage?

Yes, it is photosensitive. We recommend storage in light-resistant, amber-colored containers or in the original opaque packaging to prevent photolytic degradation.

What is the recommended storage temperature for Conivaptan Hydrochloride?

It should be stored at controlled room temperature, ideally between 15°C and 30°C. Refrigeration is not required but may be beneficial for extended storage periods.

Is Conivaptan Hydrochloride prone to hygroscopicity?

It exhibits low to moderate hygroscopicity. Nevertheless, we package it with silica gel desiccant in double polyethylene-lined fiber drums to ensure complete moisture protection.

How is the enantiomeric purity of Conivaptan Hydrochloride maintained over time?

We use chiral chromatography during release and stability testing to confirm that no racemization occurs, ensuring consistent pharmacological activity.