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Conivaptan
- indication:For the treatment of euvolemic or hypervolemic hyponatremia (e.g. the syndrome of inappropriate secretion of antidiuretic hormone, or in the setting of hypothyroidism, adrenal insufficiency, pulmonary disorders, etc.) in hospitalized patients.
- pharmacologypharmacology:
- mechanism: Conivaptan is a dual AVP antagonist with nanomolar affinity for human arginine vasopressin V<sub>1A</sub> and V<sub>2</sub> receptors <i>in vitro</i>. This antagonism occurs in the renal collecting ducts, resulting in aquaresis, or excretion of free water.
- toxicity: Although no data on overdosage in humans are available, conivaptan has been administered as a 20 mg loading dose on Day 1 followed by continuous infusion of 80 mg/day for 4 days in hyponatremia patients and up to 120 mg/day for 2 days in CHF patients. No new toxicities were identified at these higher doses, but adverse events related to the pharmacologic activity of conivaptan, e.g. hypotension and thirst, occurred more frequently at these higher doses.
- absorprion:
- halflife: 5 hours
- roouteelimination:
- volumedistribution:
- clearance: