Active substanceExametasimExametasim
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  • Teoksim, 99mTc
    lyophilizate in / in 
    DIAMED, LLC     Russia
  • Ceretec®
    lyophilizate in / in 
    JI Halskea Limited     United Kingdom
  • Dosage form: & nbsplyophilizate for the preparation of a solution for intravenous administration
    Composition:

    Lyophilizate:

    Active substances: -

    Excipients:

    d, 1-hexamethylpropyleneamino oxime (Exametamazine) 0.5 mg

    Tin dichloride anhydrous 5.1 μg

    Tartaric acid 15.0 μg

    Sodium chloride 4.5 mg

    Mannitol (Mannitol) 5.0 mg

    - 1 bottle

    Ready product:

    Active substances:

    Technetium-99m 37 - 148 MBq

    Excipients:

    d, 1-hexamethylpropyleneamino oxime (Exametamazine) 0.1 mg

    Tin dichloride anhydrous 1.0 μg

    Tartaric acid 3.0 mcg

    Sodium chloride 9.9 mg

    Mannitol (Mannitol) 1.0 mg

    Water for injection q.s. - 1 ml

    Description:

    Lyophilizate is white.

    The finished product is a colorless, clear liquid.

    Pharmacotherapeutic group:radiopharmaceutical diagnostic tool
    ATX: & nbsp

    V.09.A.A.01   99m Tc-Technetium-exametazime

    Pharmacodynamics:

    "Teoksim, 99mTc "- radiopharmaceutical preparation is prepared from lyophilizate and sodium pertechnetate solution, 99mTc from the technetium-99m generator.

    Isotope 99mTc has a half-life of 6.04 hours. Upon decay 99mTc emits gamma quanta with an energy of 140 KeV and a yield of 90%.

    Diagnostic tool for evaluation of cerebral blood flow and preparation in vitro labeled 99mTc of leukocytes.

    The property of Teoksima, 99mTc accumulate in brain tissues, depending on the state of cerebral blood flow, allows one to identify brain diseases associated with vascularization impairment using single-photon emission computed tomography (SPECT).

    Known tropicity Teoksima, 99mTc to leukocytes is used to insert a label into the blood elements. In turn, the labeled 99mTc autologous leukocytes allow to use them for visualization of inflammatory foci of different localization, in connection with pronounced leukocyte infiltration of lesions.

    Pharmacokinetics:

    Already from the first minutes after intravenous administration and during the first hour there is a rapid transition of the drug from the bloodstream into the brain tissue where Teoksim, 99mTc binds firmly to specific proteins and other biostructures of brain tissue. The drug penetrates well through the blood-brain barrier and accumulates in the brain in proportion to the level of cerebral blood flow, stable level of drug concentration persists long enough.

    The accumulation level of Teoksima, 99mTc in the brain is 3.5-4.5% of the injected activity.Only after 2 hours there are the first signs of a slow removal of the isotope from the blood with a half-life of 16 hours. So after 24 hours it is more than 70% of the maximum value.

    Having lipophilic properties that limit the passage of the complex through the glomerular system of the kidneys, Teoksim, 99mTc is excreted from the body by the hepatobiliary system with a half-life of 24 hours.

    The appearance of technetium-99m in urine during the second hour after the administration of the drug is due to the presence of a second complex that does not possess encephalotropic activity, but also does not affect the stable content during this period of the basic lipophilic complex in the brain tissue
    Indications:

    For the diagnosis of brain diseases associated with impaired cerebral circulation: with transient ischemia of the brain, stroke, epilepsy, migraine, dementia, tumors.

    For visualization of inflammatory foci of different localization and origin by the method of labeling with the drug Teoksim, 99mTc in vitro leukocytes and granulocytes.

    Contraindications:

    Pregnancy, hypersensitivity to the drug, age to 18 years.

    Pregnancy and lactation:

    If it is necessary to administer the drug during lactation, breastfeeding should be discontinued within 24 hours after the study.

    Dosing and Administration:

    Enter intravenously.

    To study the blood circulation of the brain.

    Preparation of the preparation.

    The preparation is prepared immediately before use by adding 5.0 ml of sodium pertechnetate, 99mTc from a technetium-99m generator into a vial of lyophilizate. The following conditions must be observed:

    - A solution of sodium pertechnetate, 99mTc should be obtained no later than 24 hours after the previous elution of the technetium-99m generator.

    - The resulting solution of sodium pertechnetate, 99mTc should be used to prepare the drug Teoksim, 99mTc for 2 hours. The finished product can be stored for no more than 30 minutes.

    After the addition of the eluate from the technetium generator and thorough mixing, the contents of the vial are administered intravenously.

    Entered dose: 0.5 mg d, 1-HMPAO isomer labeled 185-740 MBq of technetium-99 m. SPECT is used for evaluation. Plane tomography is performed in four projections. SPECT is carried out according to a known method in 10-15 minutes. after the administration of the drug.

    Identification of foci of inflammation.

    Preparation of labeled leukocytes:

    Required Reagents:

    1. Dextrose citrate (DC):

    - sodium citrate - 22 g

    - citric acid - 8 g

    - dextran 500 - 22.4 g

    - water for injection-up to 1L

    The solution is sterilized through a millipore filter (0.2 r).

    2. 2% solution of methyl cellulose in physiological solution, for which dissolve 2 g Methocell E50 Premium (Dow) in 100 ml sterile, apyrogenic physiological solution, mix until completely dissolved. The solution is filtered through a 0.45 p filter. Store the solution at 2-4 ° C.

    Necessary equipment:

    - Plastic non-heparinized syringe with a volume of 60 ml - 2 pcs.

    - Plastic centrifuge tubes with lids sterile with a capacity of 25 - 30 ml (hereinafter referred to as centrifuge tubes) - 7 pcs.

    The procedure for the isolation and labeling of leukocytes is carried out under sterile conditions, for which it is necessary:

    - Add 9 ml of DC to each of 2 60 ml of plastic non-heparinized syringes.

    - Select 51 ml of patient's blood in each syringe using a needle 19G (butterfly). Close the syringes with sterile stoppers. Carefully mix blood and DC.

    - Add 2 ml of a 2% solution of methyl cellulose to each of the 4 centrifuge tubes.

    - Add 20 ml of blood from syringes without needles to 4 prepared centrifuge tubes, gently stir and cover with caps. Leave for sedimentation of red blood cells for 1 hour at room temperature.

    - The remaining 20 ml of blood is added to a clean centrifuge tube.

    Centrifuge the test tube with blood for 10 minutes. at 2000g. The resulting pure plasma is used for labeling and injection. Keep the plasma at room temperature. Apply the label "A" to the test tube.

    - After the sedimentation of erythrocytes, carefully transfer the platelet-rich and leukocyte-rich supernatant to a clean centrifuge tube. Centrifuge for 5 min. at 150g. The resulting sediment contains leukocytes.

    - Remove as much plasma as possible into a clean centrifuge tube and centrifuge for 10 minutes. at 2000g , to obtain a plasma containing methylcellulose. This plasma is used for washing cells after labeling. Apply the label "B" to the test tube.

    - Resuspend the leukocyte sediment by lightly shaking the test tube. Add 1 ml of clean plasma from the tube "A".

    - To determine the viability of the isolated leukocytes with the help of lifetime staining with trypan blue.For labeling, leucon coconut is suitable, containing at least 90% of viable cells.

    - In a standard reagent bottle add 340 - 550 MBq pertechnetate in a volume of 2-3 ml and mix thoroughly for 3 minutes. Thus it is necessary to observe the following:

    - solution of sodium pertechnetate, 99mTc should be obtained not later than 24 hours after the previous elution of the technetium-99m generator

    - the obtained solution of sodium pertechnetate, 99mTc should be used to prepare the drug Teoksim, 99mTc for 2 hours. The finished product can be stored for no more than 30 minutes.

    - The finished product is added to the cell suspension and incubated at room temperature for 10 min. At the end of the incubation, free GMPA, 99mTc block by adding 10 ml of plasma from the tube "B". Centrifuge for 5 min. at 150g.

    - Remove the entire supernatant, gently resuspend the labeled leukocytes in 5 ml of plasma from tube "A". The resulting preparation is ready for intravenous administration to the patient and should be used immediately after preparation.

    Diagnosis of inflammatory foci:

    The intravenous activity is 370 - 450 MBq.The study is conducted 1 hour and 4 hours after the administration. The received scintigrams are evaluated visually.

    Radiation loads on the organs and entire body of the patient when used drug Teoksim, 99mTc

    Absorbed dose, mGy / MBq

    Organs and Systems

    When evaluating the state of perfusion of the brain

    After intravenous administration of labeled leukocytes

    Tear glands

    0,069

    -

    Gallbladder

    0,055

    -

    Spleen

    -

    0,157

    Kidneys

    0,037

    -

    Thyroid

    0,030

    -

    The superior part of the large intestine

    0,027

    -

    Liver

    0,018

    0,024

    Red marrow

    -

    0,005

    Small intestine

    0,016

    -

    Lower part of large intestine

    0,012

    -

    Bladder

    0,011

    0,006

    Brain

    0,008

    -

    Ovaries

    0,006

    0,004

    Testes

    0,001

    -

    Effective equivalent dose, mSv / MBq

    0,0178

    0,0165

    Side effects:

    There were no any side effects when using the drug for diagnostic purposes. Allergic reactions are possible.

    Overdose:

    With a single administration, an overdose is unlikely, due to the lack of pharmacodynamic properties in the preparation.

    Interaction:

    When conducting diagnostic studies, interactions with other drugs were not noted.

    Special instructions:Work with the drug should be carried out in accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99),"Norms of radiation safety" (NRB-99) and guidelines "Hygienic requirements for radiation safety during radionuclide diagnostics using radiopharmaceuticals" (MU 2.6.1.1892-04)
    Form release / dosage:

    Lyophilizate for the preparation of a solution for intravenous administration (10 ml bottles).

    Packaging:

    For 5 vials with instructions for medical use of the drug in a box of cardboard.

    Storage conditions:

    Lyophilizate stored at a temperature of 2 ° C to 10 ° C. It is allowed to deviate from the temperature regime (18-25 ° C) during transportation for 1 month.

    Ready product stored in accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99).

    Shelf life:

    Lyophilizate for the preparation of a solution for intravenous administration - 1 year from the date of manufacture.

    The drug Teoksim, 99mTc - 30 minutes from the date of preparation.

    Terms of leave from pharmacies:For hospitals
    Registration number:P N003270 / 01
    Date of registration:09.12.2009
    The owner of the registration certificate:DIAMED, LLC DIAMED, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp20.10.2015
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