HEXABRIX � ioxaglate meglumine and ioxaglate sodium injection
Guerbet LLC
Guerbet LLC
NOT FOR INTRATHECAL USE
DESCRIPTION
HEXABRIX is a sterile, non-pyrogenic, aqueous solution intended for use as a diagnostic radiopaque medium. HEXABRIX contains 39.3% w/v N-(2-hydroxyethyl)-2,4,6-triiodo-5-[2-[2,4,6-triiodo-3-(N-methylacetamido)-5-(methylcarbamoyl) benzamido] acetamido]-isophthalamic acid, compounded with 1-deoxy-1-(methylamino)-D-glucitol (1:1) and 19.6% w/v sodium N-(2-hydroxyethyl)-2,4,6 triiodo-5-[2-[2,4,6-triiodo-3-(N-methylacetamido)-5-(methylcarbamoyl) benzamido] acetamido]-isophthalamate.
The two salts have the following structural formulae:
Chemical StructureChemical Structure
Each milliliter contains 393 mg of ioxaglate meglumine, 196 mg of ioxaglate sodium and 0.10 mg edetate calcium disodium as a stabilizer. The solution contains 3.48 mg (0.15 mEq) sodium in each milliliter and provides 32% (320 mg/mL) organically bound iodine.
Solutions of ioxaglate (HEXABRIX) provide six iodine atoms for each two dissociated ions. HEXABRIX is an ionic contrast agent. HEXABRIX has an osmolarity of approximately 460 mOsmol/L, an osmolality of approximately 600 mOsmol/kg of water and is, therefore, hypertonic under conditions of use.
HEXABRIX has a viscosity (cps) of 15.7 at 20�C and 7.5 at 37�C. The pH has been adjusted to 6.0 to 7.6 with meglumine, sodium hydroxide or ioxaglic acid.
HEXABRIX is a clear, colorless to pale yellow solution containing no undissolved solids. Crystallization does not occur at normal room temperatures. It is supplied in containers from which the air has been displaced by nitrogen.
CLINICAL PHARMACOLOGY
Intravascular injection of a radiopaque diagnostic agent opacifies those vessels in the path of the flow of the contrast medium, permitting radiographic visualization of the internal structures of the human body until significant hemodilution occurs.
Following intravascular injection, HEXABRIX is rapidly transported through the circulatory system to the kidneys and is excreted unchanged in the urine. The pharmacokinetics of intravascularly administered radiopaque contrast media are usually best described by a two compartment model with a rapid alpha phase for drug distribution and a slower beta phase for drug elimination. In 10 patients with normal renal function, the alpha and beta half-lives of HEXABRIX were 12 (4-17) and 92 (61-140) minutes, respectively. Following the intravenous administration of 50 mL of HEXABRIX in 10 normal volunteers, the mean peak plasma concentration occurred at two (1-3) minutes, reaching a concentration of 2.1 (1.8-2.8) mg/mL. Approximately 50 (42-67) percent of the intravenously administered dose was recovered in the urine at two hours, and 90 (68-105) percent was recovered at 24 hours.