M-iodobenzylguanidine, 123-I (M-iodbenzylguanidin, 123-I)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceJoenguang [123I]Joenguang [123I]
Dosage form: & nbspsolution for intravenous administration
Composition:

In 1 ml of the drug contains:

active substances: Yoda-123 - not less than 100 MBq, M-iodobenzylguanidine sulfate 0.3 mg;

Excipients: Mr.atria chloride, sulfations (in the form of ammonium sulfate), water for injection.

Description:A clear, colorless liquid.
Pharmacotherapeutic group:Radiopharmaceutical diagnostic tool
ATX: & nbsp

V.09   Diagnostic radiopharmaceuticals

Pharmacodynamics:

Physicochemical characteristics

M-iodobenzylguanidine 123I - radiopharmaceutical diagnostic preparation, is an aqueous solution of meta-iodobenzylguanidine sulfate, labeled with iodine-123. The radiochemical purity of the preparation is 95%.

Volumetric activity of at least 100 MBq / ml at the date and time of preparation. The radioactive iodine-123 isotope decays with a half-life of 13.31 hours, by trapping the orbital electron and emitting monochromatic 159-keV gamma radiation (83.4%).

The drug is sterile and pyrogen-free, pH 5.0-6.5.

Pharmacodynamics

Radiopharmaceutical (RFP) "M-iodobenzylguanidine,123I"Has a similar molecular structure with an adrenergic hormone called norepinephrine. The kinetics and distribution of RFPs are similar to the kinetics and distribution of norepinephrine. Accumulating in the endings of postsynaptic sympathetic neurons and competing with norepinephrine, the drug, however, does not have the mediator properties of norepinephrine, it does not have a pharmacological effect on the activity of the sympathetic nervous system and does not cause a hemodynamic effect.

RFP "M-iodobenzylguanidine, 123I "is an indicator used as a diagnostic tool for visualization of the state of the sympathetic nervous system and with the help of which the integrity and functional state of the adrenergic nerve endings of various organs and tissues are evaluated.

The accumulation of "M-iodobenzylguanidine, 123I"In adrenergic nerve endings of various organs and tissues are described by two mechanisms:

1 - energy-dependent - sodium-dependent pathway;

2 - non-volatile - by mechanical diffusion.

In radionuclide diagnostics, the administered doses are so small that the capture mechanism dominates - the sodium-dependent pathway.

After entering the cell, most of the "M-iodobenzylguanidine, 123I"With neuroblastomas remains in the cytoplasm in a free form; with pheochromocytoma and paragangliome, the drug is actively transported into granules of catecholamines, but not metabolized by enzymes that metabolize catecholamines.

Pharmacokinetics:

After intravenous administration, the highest increase in the concentration of RFP is observed in the liver, heart, salivary glands, lungs. The preparation is excreted by the kidneys 40-55% in 24 hours and 70-90% in 96 hours, mostly unchanged.

Tissue Concentration % doses / g:

liver-0.76,

heart - 0.64,

lungs-0.17,

muscles - 0.02,

blood - 0.02.

The drug is excreted by the kidneys 40-55% for 24 hours and 70-90% for 96 hours, mostly unchanged.

Indications:

"M-iodobenzylguanidine,123I"is used to assess the functional state of the sympathetic nervous system of the heart and diagnose catecholamine tumors.

"M-iodobenzylguanidine, 123I "is accumulated by cells of neuroendocrine sympathomedular tumors of various localizations.This drug is used for diagnosis of primary neuroblastomas, pheochromocytomas, apudas (carcinoids), sympathetic paragangliomas, medullary thyroid cancer, as well as their metastases and bone marrow infiltration in neuroblastomas.

The accumulation of "M-iodobenzylguanidine,123I "in the myocardium depends on the state of the sympathetic nervous system of the heart. This drug is used to diagnose violations of sympathetic innervation of the myocardium in various cardiac pathologies: arrhythmias, heart failure, cardiomyopathies of various origins, including diabetic, ischemic and stress damage to the myocardium.

Repeated studies conducted during and after treatment provide prompt information on the effectiveness of the measures taken, which allows us to timely change and optimize the tactics of treating the patient.

Contraindications:

- Dand sensitivity to the drug or its components;

- use during pregnancy and lactation.

Dosing and Administration:

The drug is administered intravenously in the patient's position while lying or sitting.

Mandatory preliminary blockade of the thyroid gland with sodium iodide (100 mg per day) 3 days before the study and 2 days after the study.

Recommended doses: adult patients - 110-300 MBq;

If necessary, the drug can be diluted with 0.9% sodium chloride solution.

As the diagnostic equipment, a gamma camera is used, planar or rotary (SPECT), with a round (not less than 400 mm in diameter) or a rectangular crystal.

Adjustment of the amplitude analyzer 0.159 MeV, 20% window. The collimator should be used for energy above 0.150 MeV, since the X-ray radiation produced by the scattering of gamma quanta on the collimator material is not absorbed by the walls of the channels of the standard technetium collimator and the image becomes very noisy. Data collection and processing system - any of the existing data acquisition matrices is not less than 128x128 elements.

Myocardial scintigraphy is carried out in 20-30 minutes and 4 hours after intravenous administration of RFP in planar or rotational regimens. The image processing on the computer includes background subtraction, 9-point smoothing or filtering with an adequate filter, correction of the frame of the late study for iodine-123 decomposition and the determination of the parameters: heart / mediastinum ratio, the percentage of elution of RFP from the myocardium,an estimate of the nature of the RFP distribution with respect to the region of maximum accumulation.

Visualization of the adrenal glands and the whole body is carried out 24 hours after intravenous administration of the drug. After standard image processing, the presence of foci of hyperfixation of RFP and visualization of bone marrow is visually determined. The level of accumulation in the outbreak is estimated by a standard method by comparing symmetrical areas: the adrenal region with the level of accumulation in the liver (the normal accumulation limit is 120-125%).

Normally, the whole body is visualized as a shadow. Increased accumulation of RFP is observed in the salivary glands, in the heart, in the liver, in the bladder; poor accumulation in the intestine; the skeleton is not visualized. Visualization of the thyroid gland is carried out 10 minutes after the administration of RFPs on the gamma camera in the patient's position lying on his back in a standard procedure.

Radiation loads on the organs and tissues of the patient when using the drug "M-IODBENZILGUANIDIN, 123I"

Organs

Effective equivalent dose, mSv / MBq

bladder

0,0874

adrenal glands

0,0089

red marrow

0,0091

spleen

0,0072

whole body

0,0098

The critical organ of irradiation of the patient is the thyroid gland and the lower part of the large intestine.

Side effects:

With the use of the drug may develop allergic reactions.

Overdose:

Data on drug overdose are absent.

Interaction:

For 2 weeks before the study with the drug "M-iodobenzylguanidine,123I"should stop taking sympatholytic, antihypertensive drugs, blockers of" slow "calcium channels and beta-blockers, as these drugs reduce the level of accumulation of" M-iodobenzylguanidine,123I"in the myocardium and catecholamine tumors.

Special instructions:

Work with the drug should be carried out in accordance with the "Basic Sanitary Regulations for Radiation Safety" (OSPORB-99).

Form release / dosage:Solution for intravenous administration with activity of 400, 800 and 1000 MBq for the set date and time of delivery.
Packaging:

In bottles with a capacity of 10 ml, hermetically sealed with rubber stoppers and crimped with metal caps.

The bottle, passport and instructions for the medical use of the drug are placed in a packaging transport package for radioactive substances.

Storage conditions:

The drug is stored in accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99).

Shelf life:

10,0 hours from the date and time of manufacture.

Terms of leave from pharmacies:For hospitals
Registration number:P N000052 / 01
Date of registration:08.12.2008
Expiration Date:Unlimited
The owner of the registration certificate:Radium Institute. VGKhlopina NGO, State Unitary Enterprise Radium Institute. VGKhlopina NGO, State Unitary Enterprise Russia
Manufacturer: & nbsp
Information update date: & nbsp18.11.2017
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