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CARDIOVASCULAR SYSTEM › DIURETICS › OTHER DIURETICS › Vasopressin antagonists
conivaptan
C03XA02
Forms & Strengths
- Intravenous Solution: 20 mg/4 mL
Adult Dosing
- Euvolemic and Hypervolemic Hyponatremia: Initial 20 mg IV infusion over 30 minutes, followed by 20 mg/day continuous IV infusion for 2 to 4 days (up to 7 days if necessary).
- Maximum daily dose: 40 mg/day via continuous infusion after the initial dose.
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established.
Indications
- Euvolemic hyponatremia (SIADH, hypothyroidism, adrenal insufficiency)
- Hypervolemic hyponatremia (heart failure, cirrhosis)
Mechanism of Action
- Dual vasopressin V1A and V2 receptor antagonist.
- Promotes free water excretion (aquaresis) without significant sodium and potassium loss by blocking renal V2 receptors in the collecting ducts.
- Causes vasodilation by blocking V1A receptors in vascular smooth muscle.
Contraindications
- Hypovolemic hyponatremia
- Concurrent administration of strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir)
- Anuria
- Hypersensitivity to conivaptan or any of its components
Adverse Reactions
- Infusion site reactions (phlebitis, erythema, pain)
- Orthostatic hypotension
- Hypokalemia
- Headache
- Pyrexia
- Constipation
- Vomiting
- Osmotic demyelination syndrome (rapid overcorrection of sodium)
Drug Interactions
- Strong CYP3A inhibitors significantly increase conivaptan plasma concentrations and are contraindicated.
- Moderate CYP3A inhibitors (e.g., erythromycin, fluconazole, diltiazem) increase conivaptan levels; use with caution.
- CYP3A substrates (e.g., midazolam, simvastatin, amlodipine) may have increased concentrations when co-administered with conivaptan.
- Diuretics may potentiate the risk of severe hypovolemia and hyponatremia overcorrection.
Curated Content: Needs Vetting Before Put to Clinical Use