Drug intelligence / Profile preview

spironolactone + conivaptan

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of two small molecule drugs, spironolactone and conivaptan. Spironolactone is a potassium-sparing diuretic and mineralocorticoid receptor antagonist used primarily for heart failure, hypertension, edema associated with liver cirrhosis or nephrotic syndrome, primary hyperaldosteronism, and off-label for conditions like hirsutism and acne. It works by competitively inhibiting aldosterone at the mineralocorticoid receptor in the distal renal tubule, promoting sodium excretion while retaining potassium[1][8]. Conivaptan is a non-peptide dual vasopressin V1a/V2 receptor antagonist approved for raising serum sodium in euvolemic or hypervolemic hyponatremia (such as SIADH). By blocking these receptors, it induces aquaresis—excretion of free water without significant electrolyte loss—and reduces fluid overload[2][5][6]. The combination may be considered in cases of refractory volume overload or heart failure where both aldosterone-mediated sodium retention and vasopressin-mediated water retention are contributing factors; however, there are no established fixed-dose products combining these agents. Caution is warranted due to increased risk of adverse effects when used together[4].

Brand names
VaprisolAldactone
Other names
conivaptan hydrochloridespironolactone
02

Targets

AR (Adrenergic receptors)PR (Progesterone receptor)MR (Mineralocorticoid receptor)ER (Estrogen receptor)GR (Glucocorticoid receptor)AVPR2 (Arginine vasopressin V2 receptor)AVPR1A (Arginine vasopressin receptor 1A)

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