Conivaptan
Conivaptan Brand names, Conivaptan Analogs
Conivaptan Brand Names Mixture
- No information avaliable
Conivaptan Chemical_Formula
C32H26N4O2
Conivaptan RX_link
No information avaliable
Conivaptan fda sheet
Conivaptan msds (material safety sheet)
Conivaptan Synthesis Reference
No information avaliable
Conivaptan Molecular Weight
498.575 g/mol
Conivaptan Melting Point
No information avaliable
Conivaptan H2O Solubility
Very slightly soluble (0.15 mg/mL at 23oC)
Conivaptan State
Solid
Conivaptan LogP
5.955
Conivaptan Dosage Forms
Liquid (ampule containing 20 mg conivaptan hydrochloride)
Conivaptan Indication
For the treatment of euvolemic 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.
Conivaptan Pharmacology
Conivaptan is a nonpeptide, dual antagonist of arginine vasopressin (AVP) V1A and V2 receptors. 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 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. The pharmacodynamic effects of conivaptan include increased free water excretion (i.e., effective water clearance [EWC]) generally accompanied by increased net fluid loss, increased urine output, and decreased urine osmolality.
Conivaptan Absorption
No information avaliable
Conivaptan side effects and 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.
Conivaptan Patient Information
No information avaliable
Conivaptan Organisms Affected
Humans and other mammals
