Universal reference book for medicines
Product name: BUTYRAT, 11 C (BUTIRAT, 11 C)

Active substance: nonappropriate

Type: Radioisotope diagnostic preparation

Producer: RUSSIAN SCIENTIFIC CENTER OF RADIOLOGY AND SURGICAL TECHNOLOGIES (Russia)
Composition, form of production and packaging
The solution for intravenous administration is
clear, colorless.

1 ml

carbon-11 300-1600 MBq

Excipients: sodium bicarbonate - 13 mg, water d / and up to 1 ml.

750 - 4000 MBq - vials (1) - transport containers for radioactive substances.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

With intravenous administration, Butirate, 11 C is rapidly excreted from the blood.
The maximum level of capture of the drug in the organs is observed in the second minute and at least 20 more are stored, which is enough for conducting positron emission tomography. The drug arrives and is distributed in the organs in proportion to the level of perfusion and metabolic activity of the protein-transporter. In cellular mitochondria, α-oxidation of fatty acid takes place with the formation of 11 C-Acetyl-CoA. Under conditions of sufficient oxygenation, 11 C-acetyl-CoA is metabolized in the Krebs cycle to carbon dioxide, carbon-11 and water. In conditions of hypoxia, mainly labeled phospholipids and triglycerides are formed. 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 RFP Butyrate, 11 C, a gradual elimination of the radionuclide label through the lungs in the form of carbon dioxide, carbon-11 is observed.The radionuclide label is not displayed by the kidneys.

Butyrate, 11 C is a nonspecific tumorotropic radiopharmaceutical (RFP).
On its diagnostic properties RFP is suitable for conducting positron emission tomography for the purpose of diagnosing 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 avenge the possibility of visualization of prostate cancer, so when the drug is injected intravenously, the radionuclide label does not enter the bladder.
RFP Butyrate, 11 C is also a cardiotropic agent and is suitable for studying the metabolism of fatty acids in the myocardium.
Normally, with intravenous administration of Butyrate, 11 C is evenly distributed in all parts of the left ventricle of the myocardium in proportion to myocardial perfusion. In the next 30 minutes there is a gradual uniform elimination of the radonuclide mark from the myocardium as the drug is metabolized, with an increased accumulation of carbon-11 in the lungs and exhaled air. With a significant decrease 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 labeled phospholipids and triglycerides. In areas of postinfarction cardiosclerosis there is persistent hypophyse of RFP, which indicates hypoperfusion and lack of metabolism.
PHARMACOKINETICS

After intravenous RFP Butyrate, 11 C quickly leaves the blood rust and after 1 minute its content in the blood does not exceed 4-5% of the injected.
With the blood current, the drug is delivered to tissues, where it is included in the metabolic processes according to the level of their perfusion. The maximum level of capture in organs and tissues is observed at 1 minute. RFP is accumulated in increased amounts in the kidneys (0.12 g%), liver (0.1 g%), spleen (0.06 g%), myocardium (0.03 g%), pancreas (0.03 g%). In other organs, including the brain, lungs, muscles, the skeleton to the skin is the accumulation of the drug background. In the liver, spleen and glands, the metabolism of the drug is slowed down. At the same time, a rapid removal of the radionuclide label is normal from the myocardium and kidneys. Since the intravenous administration of RFP, a gradual removal of the radionuclide label through the lungs in the form of carbon dioxide, carbon-11 is noted.
The area under the concentration / time (AUC) curve of accumulation and excretion of RFP Butyrate, 11 C for 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 α-oxidation of fatty acid) and the phase of slow elimination of the radonuclide label (reflects the formation of labeled phospholipids and triglycerides).
The time to reach the maximum concentration (TC max ) of the drug in a healthy myocardium is 1-2 minutes, the half-life (T 1/2 ) is 20-22 minutes. 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.
TC max ) for Butyrate, 11 C in tumor cells - 2-6
min. The tumor / normal tissue ratio sufficient for the visualization of malignant and hypervascular benign tumors is maintained for another 20 minutes.
INDICATIONS

As a diagnostic tool for positron emission tomography (PET).
The main indications for the study are:
in oncology:

- Diagnosis and differential diagnosis of malignant and benign neoplasms;

- control of 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 leg 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.

DOSING MODE

The drug in the form of a sterile solution is administered to the patient intravenously.
Before use in a bottle with RFP Butyrate, 11 C add 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 μm. The finished sterile solution should be clear. If a patient has a history of an allergic reaction to the protein RFP Butyrate, 11 C can be administered without albumin.
Dynamic PET studies of patients are optimal to begin immediately after the injection of RFP Butyrate, 11 C and run in a dynamic mode for 30 minutes.
Special preparation of cancer patients is not required. The study of cardiac patients is performed on an empty stomach (the last meal is evening).
The diagnostic dose of the drug for dynamic study is 200 MBq per 1 m 2 of the body surface of the patient.
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 calculation of effective radiation doses for patients using the RFP preparation Butyrate, 11 С

Dose ratio, mSv / MBq

Adults

Butyrate, 11 C 0.0035

The dose-related coefficient for intravenous administration of Butyrate, 11 C in adults is 3.5 × 10 -3 mSp / MPK.
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 EFFECT

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

CONTRAINDICATIONS

- during pregnancy;

- during lactation;

- for study in children, as clinical trials were conducted only in adults.

Hypersensitivity reactions are possible.

PREGNANCY AND LACTATION

Contraindicated in pregnancy and lactation


APPLICATION FOR CHILDREN

Contraindicated for study in children, as clinical trials were conducted only in adults.

SPECIAL INSTRUCTIONS

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

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

DRUG INTERACTION

Data on drug interaction are absent.

TERMS OF RELEASE FROM PHARMACY

The drug sales through the pharmacy network is not
subject.
TERMS AND CONDITIONS OF STORAGE

The drug is stored in accordance with the requirements of the "Basic Sanitary Regulations for Radiation Safety (OSPORB-99).
Shelf life - 40 minutes from the date and time of manufacture. Do not use after expiry date.
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