Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties
Pharmacotherapeutic category: Iodated, X-ray contrast media: Water-soluble, nephrotropic, low osmolar X-ray contrast media.
ATC code: V08AB04
Iopamidol is a non-ionic radio-opaque hydrosoluble substance with strongly reduced toxicity and no teratogenic effects. Its use at doses 2 to 4 times higher than for clinical use provoked transient bradycardia and hypotension in dogs, followed by mild hypertension and increased respiratory frequency.
Base values were returned in 2-4 minutes.
The results of a prospective study with CT multilayer method indicate that the incidence of contrast nephropathy in patients with moderate or severe renal insufficiency (creatinine clearance between 10:59 mL/min/1.73m2) undergoing TC examination after intravenous administration of a dose equal to 40 g of iodine, was low and not significantly different with the nonionic monomer at low osmolality, iopamidol and with a nonionic iso-osmolar dimer. With iopamidol no cases of increased serum creatinine more than or equal to 0.5 mg/dL has been recorded, iopamidol and nonionic dimer caused increases in serum creatinine more than or equal to 25% of baseline values in the 3.9-4.0% of treated patients.
The incidence of contrast nephropathy in patients undergoing cardioangiographic investigations with iopamidol is similar to that observed after administration of a nonionic iso-osmolar dimer.

Pharmacokinetic Properties

5.2   Pharmacokinetic properties

Biotrasformation: In humans and animals iopamidol does not undergo detectable metabolic processes.
Elimination: the vast majority is via renal route.
In dogs, 93-95% of the administered dose was excreted renally and 0.5% through the biliary route in 7-10 hours.
In humans, more than 90% of the dose is excreted by the urinary route in 24 hours.
Blood half-life in the excretion phase (T ½ / B) is approximately 60 minutes in dogs and 90-120 minutes in humans.

For intrathecal administration it will pass into the bloodstream, with peak reached in 90-150 min.
and almost complete excretion in 24 hours.