Butyrate, 11C (Butirat, 11C)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbspsolution for intravenous administration
Composition:

In 1 ml of solution contains:

Carbon-11

from 300 to 1600 MBq

Sodium bicarbonate

13.0 mg

Water for injections

up to 1.0 ml

* Preparation of the drug occurs in the process of continuous synthesis in a specialized module.

Note. Carbon-11 is obtained on the proton accelerator in the nuclear reaction 14N (p,α)11C when irradiating gaseous nitrogen with a natural isotope composition (GOST 9293-74). Carbon-11 in the preparation is in the chemical form of the sodium salt of 1- [11C] -butyric acid (sodium 1- (11C) -butyrate).

Description:

A clear, colorless liquid.

Pharmacotherapeutic group:Radiopharmaceutical diagnostic tool
ATX: & nbsp
  • Diagnostic radiopharmaceuticals
    • Pharmacodynamics:

    Physicochemical characteristics

    The preparation is an isotonic sodium bicarbonate solution containing carbon-11 in the chemical form of the sodium salt of 1- [11C] butyric acid (sodium 1- [11C] butyrate). The preparation is prepared without the addition of a carrier.

    Volumetric activity of the preparation from 300 to 1600 MBq / ml at the date and time of manufacture, pH from 8.0 to 9.5, radiochemical purity is not less than 95.0%.

    The half-life of carbon-11 is 20.38 minutes. The radionuclide decays in positron type with an average positron energy of 385 keV, the energy of annihilation gamma radiation is 511 keV.

    Pharmacological properties

    When administered intravenously, the preparation "Butyrate, 11C "is rapidly excreted from the blood.The maximum level of drug capture in the organs is observed in the second minute and remains for at least 20 minutes, which is sufficient for conducting positron emission tomography.The drug arrives and is distributed in organs in proportion to the level of perfusion and metabolic activity of transport proteins. cellular mitochondria occurs β-oxidation of fatty acid with the formation of 11C-Acetyl-CoA. In conditions of sufficient oxygenation 11C-Acetyl-CoA is metabolized in the Krebs cycle to carbon dioxide, carbon-11 and water. Under conditions of hypoxia, mainly labeled phospholipids and triglycerides. Phospholipids and triglycerides are retained in the cell, and under hypoxic conditions the proportion of formation of phospholipids and triglycerides increases in comparison with carbon dioxide.

    Since the introduction of the RFP "Butirate, 11C "there is a gradual removal of the radionuclide label through the lungs in the form of carbon dioxide, carbon 11. The radionuclide label is not excreted by the kidneys.

    "Butyrate, 11C "is a nonspecific tumorotropic radiopharmaceutical (RFP) .In its diagnostic properties RFP is suitable for conducting positron emission tomography for the diagnosis of tumors.

    The most informative is the study of malignant and hypervascular benign brain tumors, since the drug does not accumulate in the cerebral cortex, which does not prevent the visualization of tumors. It should also be noted the possibility of visualization of prostate cancer, so when the drug is injected intravenously, the radionuclide label does not enter the bladder.

    RFP "Butirate, 11C "is also a cardiotrophic agent and is suitable for the study of the metabolism of fatty acids in the myocardium." Normally with intravenous administration of "Butyrate, 11C "uniformly distributed in all regions of the left ventricular myocardium is proportional myocardial perfusion. Over the next 30 minutes the gradual uniform removal of radionuclide labels of infarction as metabolize the drug, the observed increased accumulation of carbon-11 in the lungs and exhaled air. When significant reduction in myocardial blood flow , leading to hypoxia, the level of capture and β-oxidation of fatty acids decrease, as a result of which the radionuclide label is retained in myocytes in the form of a sword s phospholipids and triglycerides.In areas of postinfarction cardiosclerosis there is persistent hypophysis of RFP, which indicates hypoperfusion and lack of metabolism

    Pharmacokinetics:

    After intravenous administration of RFP "Butirate, 11C "quickly leaves the bloodstream and within 1 minute its content in the blood does not exceed 4-5% of the injected.The current of the blood is delivered to the tissues, which is included in the metabolic processes according to the level of their perfusion.The maximum level of capture in organs and tissues is observed in (0.12 g%), the liver (0.1 g%), the spleen (0.06 g%), the myocardium (0.03 g%), the pancreas (0, 03 g%) In other organs, including the brain, lungs, muscles, skeleton and skin, the accumulation of the drug is a background. the metabolism of the drug is slowed down.At the same time, a rapid removal of the radionuclide is observed from the myocardium and kidneysNoah tags. FROM the moment of intravenous RFP, gradual excretion radionuclide label through the lungs in the form of carbon dioxide, carbon-11.

    Area under the curve "concentration / time" (AUC) accumulation and elimination of RFP "Butirate, 11C "for the cardiac muscle is bi-exponential and is characterized by a phase of rapid accumulation of RFP in the myocardium, followed by a phase of rapid elimination of the radionuclide label (reflects the process of β-oxidation of fatty acid), and a phase of slow elimination of the radionuclide label (reflects the formation of labeled phospholipids and triglycerides). achieve maximum concentration (TCmOh) drug in a healthy myocardium - 1-2 minutes, half-life (T1/2) - 20-22 min. Normally, 30 minutes after the RFP administration, 60-80% of the radionuclide label is removed from the myocardium into the lungs in the form of carbon dioxide-11. In the conditions of cardiac muscle hypoxia, the rate of accumulation and removal of the radionuclide label from the myocardium is slowing.

    TCmOh for Butyrate, 11C "in tumor cells - 2-6 minutes The ratio of tumor / normal tissue, sufficient for visualization of malignant and hypervascular benign tumors, remains for another 20 minutes.

    Indications:

    The drug "Butyrate, 11C "is used as a diagnostic tool for positron emission tomography (PET) .The main indications for the study are:

    in oncology:

    - diagnostics and differential diagnosis of malignant and benign neoplasms;

    - control the effectiveness of treatment of malignant neoplasms, including when revealing the continued growth of malignant tumors in the postoperative zone.

    in cardiology:

    - assessment of the viability of the dysfunctioning myocardium, including in patients with complete blockage of the left bundle of the bundle;

    - Diagnosis of coronary heart disease (CHD), in particular, the degree of hypoxia of the heart muscle;

    - Evaluation of the effectiveness of ongoing treatment of IHD.
    Contraindications:

    Using RFP "Butirate, 11C "is contraindicated in pregnancy, lactation and for research in children, as clinical trials were conducted only in adults.

    Hypersensitivity reactions are possible.

    Dosing and Administration:

    The drug in the form of a sterile solution is administered to the patient intravenously. Before use in the bottle with RFP "Butyrate, 11C "is added a 10% solution of placental albumin in a ratio of 1: 1 to the volume of RFP.The mixture is filtered through a sterilizing filter with a pore size of 0.22 microns .The finished sterile solution should be clear.In the case of a patient with a history of allergic reaction to the protein RFP "Butyrate, 11C "can be administered without albumin.

    Dynamic PET studies of patients are optimally started immediately after injection of RFP "Butyrate, 11C "and carry out in a dynamic mode for 30 minutes.There is no special preparation for cancer patients.The study of cardiac patients is performed on an empty stomach (the last meal is evening meal).

    The diagnostic dose of the drug for dynamic study is 200 MBq per 1 m2 the patient's body surface. The surface area of ​​the body is determined from the nomogram on the basis of the growth and weight of the patient. Usually, from 250 to 400 MBq of the drug is used for one examination, which is injected intravenously in a volume of 0.5 to 2.5 ml.

    Effective dose

    Dose coefficients for calculating effective doses to patients when using the RFP "Butirate, 11FROM"

    Compound

    Dose factors, mSv / MBq

    Adults

    "Butyrate,11 FROM"

    0,0035

    The dose coefficient for intravenous administration of "Butyrate, 11C "in adults is 3.5x10-3 mSv / MBq. When the diagnostic dose of the drug is administered (from 250 to 400 MBq), the effective dose is from 0.87 to 1.4 mSv.

    Side effects:

    When using the drug in accordance with the instructions and in the recommended doses of side effects were not noted.

    Overdose:

    Overdose of the drug is unlikely in connection with the careful control of administered radioactivity in a specialized hospital.

    Interaction:

    Data on drug interaction are absent.

    Special instructions:

    Work with the drug is carried out in accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99) and the Guidelines "Hygienic Requirements for Ensuring Radiation Safety in the Conduct of Radionuclide Diagnostics by Radiopharmaceuticals" (MU-2.6.1.1892-04).

    Form release / dosage:

    Solution for intravenous administration (with volumetric radioactivity from 300 to 1600 MBq / ml).

    Packaging:

    Produced in batches with activity from 750 to 4000 MBq for the set date and time of manufacture, they are placed in a sterile glass bottle for medicinal products with a capacity of 10 ml, hermetically sealed with a rubber medical plug of type 1-1, or UL-1A and crimped with an aluminum cap.

    Each vial is placed in a transport container for radioactive substances such as KT1-20, a medical instruction and a passport are attached to the vial.

    Storage conditions:

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

    Shelf life:

    40 minutes from the date and time of manufacture.

    Do not use after expiry date.

    Terms of leave from pharmacies:For hospitals
    Registration number:P N001367 / 01
    Date of registration:04.10.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:FGU Russian Scientific Center for Radiology and Surgical TechnologiesFGU Russian Scientific Center for Radiology and Surgical Technologies Russia
    Manufacturer: & nbsp
    Information update date: & nbsp13.03.2017
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