Gadoteric acid (Acidum gadotericum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Magnetic resonance contrast media

Included in the formulation
  • Dothar
    solution in / in 
    Gerbe     France
    • АТХ:

    V.08.C.A   Paramagnetic contrast media

    Pharmacodynamics:The behavior of protons, placed in a strongly constant magnetic field, is converted by a magnetic resonance imager into an image. In a strong magnetic field, the protons go into an excited state, then with the disappearance of the field they again stabilize (the so-called relaxation of protons). The images are based on measuring the density and dynamics of the relaxation (spin-lattice (T1) or longitudinal and spin-spin (T2) or transverse times) of protons. When magnetic resonance imaging visualization of normal and pathological tissues of the brain partially depends on the differences in the intensity of the radio-frequency signal due to differences in the proton density, T1 and T2. Paramagnetic agents have more than one unpaired electron, which increases the proton relaxation rate in their molecular environment (the relaxing effect of the unpaired electron is 700 times higher than that of the proton). When placed in a magnetic field gadoteric acid shortens the relaxation time T1 and T2 tissues, which accumulate, enhancing the visualization in the central nervous system of normal tissues that do not have a blood-brain barrier (for example, the pituitary gland and membranes).
    Pharmacokinetics:Gadoteric acid does not penetrate the blood-brain barrier and does not accumulate in formations with an intact blood-brain barrier (cysts, formed post-operative scars). At the same time, pathological vascularization and violations of the blood-brain barrier of tumors, abscesses, subacute infarcts contribute to the accumulation of gadotera acid in them. After intravenous administration, it is mainly distributed in the extracellular fluid of the body. The half-life of the plasma is 90 minutes. Plasma clearance is lower in patients with impaired renal function. It does not bind to blood plasma proteins, does not penetrate the intact blood-brain barrier, and penetrates into breast milk in trace amounts. Slowly penetrates the placenta. Quickly excreted by glomerular filtration in the kidneys, unchanged. In small quantities is excreted with feces.
    Indications:Magnetic resonance imaging of the brain with contrast enhancement (in the presence of intracranial formations, presumably with an impaired blood-brain barrier).

    When magnetic resonance imaging CNS gadoteric acid comparable in effectiveness with gadodiomide and gadopentetova acid (all at a dose of 0.1 mmol / kg) with a frequency of adverse reactions 15.1; 11.6 and 14%, respectively, including moderate ones 8.3; 13.6 and 8.4% (the difference in both cases is not reliable).

    Magnetic resonance imaging spine with contrast enhancement (to visualize lesions of the spine and surrounding tissues).

    Magnetic resonance imaging torso with contrast enhancement (in the study of primary and secondary liver tumors, primary bone tumors and soft tissues).

    Magnetic resonance imaging of the whole body.

    Magnetic resonance angiography.

    When angiography of large branches of the aorta Magnetic resonance imaging with a contrast enhancement of gadotric acid provides a sensitivity of 96% and a specificity of 89-93%, in the study of the main arteries of the tibia - a specificity of 84%.

    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 6 years of age (safety and efficacy not studied).

    Presence of contraindications for carrying out magnetic resonance imaging (artificial pacemaker, coronary or vascular stenting for 6 weeks prior to manipulation, ferromagnetic implants, subarachnoid or epidural administration).

    Carefully:Severe renal dysfunction; severe cardiovascular diseases; low threshold of convulsive readiness.
    Pregnancy and lactation:The category of FDA recommendations is not defined. Qualitative and well-controlled studies on humans have not been conducted. Despite the lack of evidence that magnetic and electric fields affect human development, research in vitro and theoretical views raise concerns about their impact on the development of the embryo and fetus. To determine the safety of magnetic resonance imaging further studies are needed during pregnancy. FDA recommendations for other paramagnetic contrast agents in category C.

    Lactation: in trace amounts penetrates into breast milk. It is necessary to refrain from breastfeeding for 24 hours after magnetic resonance research.

    Dosing and Administration:Intravenously, 0.1 mmol / kg (0.2 ml / kg).If necessary, repeat the introduction until the total dose of 0.2 mmol / kg (0.4 ml / kg) is reached.

    Application in elderly patients

    Use in the elderly has not been systematically studied. As a rule, after age 65, there is an age-related decline in kidney function. In this group, it is necessary to assess the function of the kidneys before the MRI study (glomerular filtration rate, kidney ultrasound, biochemical analysis). For information on cases of nephrogenic systemic fibrosis, see "specific instructions" below.

    Use in children

    In children, the use is limited: magnetic resonance imaging of the brain and spinal cord, torso with contrast enhancement. Doses for children correspond to those for adults.

    Side effects:CNS: fainting, nausea, vomiting, headache, paresthesia, generalized convulsions, muscle cramps, muscle weakness.

    Local changes: pain in the injection site.

    Skin and mucous: eczema, skin rash, hypersensitivity, skin reactions (erythematous rash, itching).

    Allergies: anaphylactoid reactions (including severe, up to a lethal outcome) angioedema.

    From the cardiovascular system: collapse, cardiac arrest, lowering of blood pressure.

    Respiratory system: swelling of the larynx, broncho- or laryngospasm, pulmonary edema, shortness of breath, stridor, cough, itching, rhinitis, sneezing.

    Other reactions: conjunctivitis, abdominal pain, chest pain, urticaria, skin rash, anaphylactic shock, sensation of heat or cold, malaise, severe sweating, chilliness, pale skin.

    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:Pharmacologically incompatible with any medicines.
    Special instructions:There have been reported cases of development of nephrogenic systemic fibrosis due to the introduction of gadolinium-containing contrast agents, including gadoteric acid, to 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.

    As with the use of other contrast agents for intravenous administration, the use of gadoteric acid may be accompanied by manifestations of 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.

    There are a significant number of modes and techniques for using gadoteric acid for various indications. It is necessary to refer to special literature on the conduct of MRI studies.

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