OptiMark

Country: Australia

Language: English

Source: Department of Health (Therapeutic Goods Administration)

Active ingredient:

Gadoversetamide

Available from:

Mallinckrodt Australia Pty Ltd

Class:

Medicine Registered

Summary of Product characteristics

P
HARMACOKINETICS
The pharmacokinetics of intravenously administered gadoversetamide
in 
normal subjects conforms to a two-compartment open-model with mean 
distribution and elimination half-lives (reported as mean ± SD) of
about 13.3 
± 6.8 and 103.6 ± 19.5 minutes.
D
ISTRIBUTION
Gadoversetamide does not undergo protein binding _in vitro_. The
volume of 
distribution at steady state of gadoversetamide in normal subjects is
162 
± 25 mL/kg, roughly equivalent to that of extracellular water.
[See U
SE

IN

P
REGNANCY
]
M
ETABOLISM
Metabolism of gadoversetamide was not demonstrated in clinical
studies.
E
LIMINATION
Gadoversetamide injection (0.1 mmol/kg) is eliminated primarily
in the urine 
with 95.5 ± 17.4% (mean ± SD) of the administered dose eliminated by
24 
hours. The renal and plasma clearance rates of gadoversetamide are 
essentially identical (69 ± 15.4 and 72 ± 16.3 mL/hr/kg,
respectively) in 
normal subjects indicating that the drug is essentially cleared
through the 
kidneys via glomerular filtration. There was no systematic difference
in any 
of the kinetic parameters as a function of dose level (0.1 to 0.7
mmol/kg). 
Therefore, within this dose range the kinetics of gadoversetamide
appear to 
be linear.
S
PECIAL
 P
OPULATIONS
Impaired Renal Function: A single intravenous dose of 0.1 mmol/kg of 
OptiMARK
TM
 Injection was administered to 28 subjects with impaired renal 
function (17 men and 11 women). Sixteen patients had concurrent CNS
or 
liver pathology. Renal impairment was demonstrated to delay the
elimination 
of gadoversetamide (see Table 2). The mean cumulative urinary
excretion of 
gadoversetamide at 72 hours was approximately 93.5% for renal
impaired 
patients and 95.8% for subjects with normal renal function.
Impaired Hepatic Function: A single intravenous dose of 0.1 mmol/kg 
of OptiMARK
TM
 Injection was administered to 5 subjects with impaired 
hepatic function (3 men and 2 women). Two patients had concurrent
renal 
impairment. There was no differ