Anexate
Anexate Brand names, Anexate Analogs
Anexate Brand Names Mixture
- No information avaliable
Anexate Chemical_Formula
C32H26N4O2
Anexate RX_link
No information avaliable
Anexate fda sheet
Anexate msds (material safety sheet)
Anexate Synthesis Reference
No information avaliable
Anexate Molecular Weight
498.575 g/mol
Anexate Melting Point
No information avaliable
Anexate H2O Solubility
Very slightly soluble (0.15 mg/mL at 23oC)
Anexate State
Solid
Anexate LogP
5.955
Anexate Dosage Forms
Liquid (ampule containing 20 mg conivaptan hydrochloride)
Anexate 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.
Anexate 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.
Anexate Absorption
No information avaliable
Anexate 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.
Anexate Patient Information
No information avaliable
Anexate Organisms Affected
Humans and other mammals
