Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1    Pharmacodynamic properties
Pharmacotherapeutic group: X-ray contrast medium, iodinated
ATC code: V08A B09

The organically bound iodine absorbs radiation in the blood vessels/tissues when it is injected.

For most of the haemodynamic, clinical-chemical and coagulation parameters examined following intravenous injection of iodixanol in healthy volunteers, no significant deviation from preinjection values has been found. The few changes observed in the laboratory parameters were minor and considered to be of no clinical importance.

VISIPAQUE induces only minor effects on renal function in patients. In 64 diabetic patients with serum creatinine levels of 1.3– 3.5 mg/dl , VISIPAQUE use resulted in 3% of patients experiencing a rise in creatinine of  0.5 mg/dl and 0% of the patients with a rise of  1.0 mg/dl . The release of enzymes (alkaline phosphatase and N-acetyl-β-glucosaminidase) from the proximal tubular cells is less than after injections of non-ionic monomeric contrast media and the same trend is seen compared to ionic dimeric contrast media. VISIPAQUE is also well tolerated by the kidney.
Cardiovascular parameters such as LVEDP, LVSP, heart rate and QT‐time as well as femoral blood flow were less influenced⋅ after VISIPAQUE than after other contrast media, where measured.

Pharmacokinetic Properties

5.2    Pharmacokinetic properties

Iodixanol is rapidly distributed in the body with a mean distribution half-life of approximately 21 minutes. The apparent volume of distribution is of the same magnitude as the extracellular fluid (0.26 l/kg b.w.), indicating that iodixanol is distributed in the extra-cellular volume only.

No metabolites have been detected. The protein binding is less than 2%.
The mean elimination half-life is approximately 2 hours. Iodixanol is excreted mainly through the kidneys by glomerular filtration. Approximately 80% of the administered dose is recovered unmetabolized in the urine within 4 hours and 97% within 24 hours after intravenous injection in healthy volunteers. Only about 1.2% of the injected dose is excreted in faeces within 72 hours.
The maximum urinary concentration appears within approximately 1 hour after injection.

No dose dependent kinetics has been observed in the recommended dose range.

No specific pharmacokinetic studies have been performed for use in body cavities