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