Gadopentetova acid - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Magnetic resonance contrast media

Included in the formulation

Gadopentetova acid-TL

solution in / in

TECHNOLOGY OF DRUGS, LTD. Russia

Magnevist®

solution in / in

Bayer AG Germany

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

АТХ:

V.08.C.A Paramagnetic contrast media

Pharmacodynamics:Gadopentetic acid is a paramagnetic contrast medium with a gadolinium chelate complex in its structure. The presence of paramagnetic properties allows gadopentetic acid to significantly enhance the contrast and "visibility" of different formations on MRI shots compared to those made without contrast.

Gadolinium ion shortens the relaxation time of excited atomic nuclei, which increases the intensity of the signal and thus increases the contrast of the image of certain tissues.

Hypopen- tate of dimeglumine practically does not bind to proteins and does not interact with the complement system, and therefore has an extremely low ability to induce anaphylactoid reactions.

Pharmacokinetics:The fate of the active substance (dimeglumina gadopentetata) in the body is similar to the fate of other highly hydrophilic biologically inert substances released by the kidneysmannitol or inulin). Pharmacokinetics of the drug does not depend on the dose administered.

After intravenous administration, the active substance quickly penetrates into the interstitial space. Hypopen-tate of dimeglumin does not pass through intact blood-brain and hematotestick barriers and penetrates through the placental barrier in trace amounts, it is rapidly excreted from the fetal organism.

In unchanged form is excreted by the kidneys by glomerular filtration: after 6 and 24 hours 83% and 91% of the administered dose are output, respectively.

With feces, about 1% of the administered amount of the drug is released.

Renal clearance of dimegluminum gadopentetate at a body surface of 1.73 m² is 120 ml / min.

Peculiarities of pharmacokinetics in patients with impaired hepatic and renal function

Half-life is slightly increased in patients with violations of liver function of any severity.

At moderate severity (creatinine clearance> 20 ml / min) renal failure directly increases the half-life of the drug. The extrarenal excretion does not increase. In patients with severe renal failure (creatinine clearance <20 ml / min) and a half-life of more than 30 hours, the drug can be removed by hemodialysis.

The volume of the distribution is 266 ml / kg. Optimum resolution (contrast) is observed within 45 minutes after the administration of the drug.

Indications:The drug is used:

- in MRI studies of the brain and spinal cord, as it accumulates in altered tissues when the blood-brain barrier (cyst, scar, glioblastoma, changes in the vasculature) is violated.

- to enhance the contrast in the conduct of magnetic resonance imaging whole body, namely:

detection of a tumor, inflammation, an affected vessel;

differential diagnosis of the structure of pathological formations;

differential diagnosis of tumors and scar tissue after a session of chemoradiotherapy and so on.

ICD-10

XXI.Z00-Z13.Z03.1 Observation for suspected malignant tumor

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

XX.Y40-Y59.Y57.6 Other diagnostic drugs

Contraindications:- hypersensitivity to the drug;

- Pregnancy and the period of breastfeeding. Clinical data in this age group is not enough, so the use of gadopennetic acid in pregnant and lactating mothers is not recommended, unless it is dictated by clinical necessity;

- severe renal failure (limited use).

Carefully:- epilepsy and low threshold of convulsive readiness;

- for violations of kidney function, gadopentetic acid should be used only after a thorough examination and an assessment of the relationship between benefit and risk to the patient;

- Clinical data on patients with cardiovascular diseases are limited. Some studies reported a transient increase in the QT interval without any adverse reactions;

- special caution is necessary when using gadopennetic acid in patients with a history of allergic anamnesis (in particular, reaction to contrast drugs in the past).

Pregnancy and lactation:FDA risk category - F

Clinical data in this age group is not enough, therefore, the use of gadopennetic acid in pregnant and lactating mothers is not recommended.

Well-controlled studies in humans have not been conducted. In animal experiments, the drug caused teratogenic and embryotoxic effects.

Lactation: Do not use the drug in lactation or stop breastfeeding for the period of treatment.There is evidence of the penetration of small amounts of the drug into breast milk in rats.

Dosing and Administration:The maximum single dose is 0.6 ml / kg (0.3 mol / kg) for adults and 0.4 ml / kg for children. Introduce intravenously bolus, in the patient's lying position, immediately before the beginning of the MRI study. The drug is not injected intramuscularly or into the membranes of the brain. For adults, children and newborns, a single dose is 0.1 mmol / kg body weight. The dose depends on the purpose of the study and the age of the patient.

Use in the elderly has not been systematically studied. There is no data on the need to reduce the dosage of the drug in patients in this group, although due to age-related changes in the cardiovascular, respiratory, central nervous and other systems, this may be relevant.

Side effects:Allergic reactions: possible anaphylactic shock.

From the digestive tract: rarely - nausea, vomiting, abdominal pain. Laboratory increase of serum transaminases.

Other: short-term change in taste after a very rapid administration of the drug.

Increase in laboratory indicators: rarely - an asymptomatic insignificant increase in the level of iron and serum bilirubin.

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 - no data. Do not mix gadopennetic acid with any drug.

Special instructions:When determining the iron content in the serum by complexometric methods, it is possible to obtain false values due to the free ligand of gadopentetic acid. Gadopentetic acid can be completely removed from the body during hemodialysis.

Instructions

Gadopentetic acid (Acidum gadopenteticum)