Gadoteridol - instructions for use, dose, side effects, contraindications

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АТХ:

V.08.C.A Paramagnetic contrast media

Pharmacodynamics:The first contrastive paramagnetic drug registered in the United States for magnetic resonance imaging of the central nervous system. Gadoteridol is a paramagnetic contrast medium with a gadolinium chelate complex in its structure. Like all preparations of this group, gadoteridol is highly hydrophilic and accumulates in areas of increased blood supply, for example in tumors, hemangiomas, hematomas and others. When placed in a magnetic field, the drug reduces T₁ and T₂ the relaxation time, which greatly increases the signal power in the tissues of accumulation. This visually enhances the contrast and "visibility" of different formations on MRI shots compared to those made without contrast.

Pharmacokinetics:Within 24 hours, 94.4 ± 4.8% of the administered dose of gadoterol is excreted from the body, mainly with urine. Biotransformation and decomposition of gadoterol in vivo not studied. Plasma and renal clearance are 1.41 ± 0.33 ml / min / kg and 1.50 ± 0.35 ml / min / kg, respectively, indicating a nearly complete excretion of the drug through the kidneys. The apparent volume of distribution is 204 ± 58 ml / kg, equal to the volume of distribution of extracellular fluid. The binding of gadoteridol with plasma proteins has not been studied.

Indications:Gadoteridol is indicated as a contrast agent for use in magnetic resonance imaging in adults and children older than 2 years to visualize foci of abnormal vascularization in the brain (intracranial foci), as well as the spinal cord and adjacent tissues.

ICD-10

XXI.Z00-Z13.Z03 Medical surveillance and evaluation in case of suspected disease or pathological condition

Contraindications:Hypersensitivity to the drug; pregnancy and the period of breastfeeding; children under 2 years of age (safety and efficacy not studied).

Carefully:Mild and moderate renal dysfunction, especially acute; The dosage regimen for patients in this group is not defined.

Earlier episodes of an allergy to a contrast substance with gadolinium; adverse allergic anamnesis.

Repeated studies involving gadoterol. The safety of such studies has not been specifically studied.

Pregnancy and lactation:The risk category for the fetus is the FDA - C. Data on clinical studies of the use of gadotheridol in pregnancy are absent.Therefore, the drug should not be administered to pregnant women unless it is clearly necessary. In experiments on rats and rabbits gadoteridol caused an increase in the frequency of miscarriages with the introduction of an eight-fold dosage shown to a person.

Lactation: after the introduction of the drug, refrain from breastfeeding for 24 hours.

Dosing and Administration:The recommended single dose for adults and children over 2 years is 0.1 mmol / kg body weight (0.2 ml / kg body weight).

The drug is administered rapidly (10 ml / min-60 ml / min) or bolus (> 60 ml / min).

A maintenance dose of 0.2 mmol / kg can be administered to patients with normal renal function when scant contrasts are detected.

Immediately after the administration of the drug, it is necessary to administer 5 ml of sodium chloride 0.9% intravenously through the same catheter to ensure the administration of drug residues into the bloodstream.

The procedure for magnetic resonance imaging should be completed within 1 hour after the administration of the drug.

Application in elderly patients

Of the 2,263 adults participating in the clinical study of gadotheridol, 22% were 65 years of age or older. Between elderly patients and other adult participants, no differences in kinetics and drug safety were found.However, due to the age-related decline in kidney function, careful monitoring of patients over 65 years of age, especially the following groups, is necessary:

- with the presence of severe renal failure;

- a dubious allergological anamnesis.

Use in children

Safety and efficacy in children under 2 years of age have not been systematically studied. The efficacy and safety of consecutive and repeated use of gadoterol in children has not been studied. In children older than 2 years, the drug can be applied once in a dose not exceeding 0.1 mmol / kg. This dose is administered intravenously bolus (<60 ml / min).

Side effects:Nephrogenic systemic fibrosis; allergic reactions. The most common observed side effects at the stage of clinical trials of gadoterol were nausea, taste disorders. The frequency was 1.4%, the severity of manifestations is from mild to moderate.

Overdose:There were no cases of overdose. The goals of therapy with a possible overdose are maintenance of vital functions, rapid administration of symptomatic therapy. The drug can be removed from the body by hemodialysis.

Interaction:Clinically significant interactions have not been studied. Pharmacologically incompatible with any other drugs.

Special instructions:There have been reports of cases of development of nephrogenic systemic fibrosis due to the introduction of gadolinium-containing contrast agents, including the drug gadoteridol, patients with the following diseases / conditions:

- acute or chronic renal failure (glomerular filtration rate <30 ml / min / 1.73 m²);

- Acute renal failure of any severity caused by hepatorenal syndrome, or in the period before and after liver transplantation.

In all cases, it is necessary to prescribe a minimum sufficient dose, in order to avoid such cases.

As with the use of other contrast agents for intravenous administration, the use of gadoterol may be accompanied by hypersensitivity, idiosyncrasy. Severe clinical conditions, including shock, can develop.

The risk is higher in cases when the reaction to a contrast agent developed earlier, with bronchial asthma and allergies in the anamnesis. Most of these reactions develop within 0.5-1 hour after administration.Careful monitoring with conditions for intensive care and resuscitation is necessary.

Instructions

Gadoteridol (Gadoteridolum)