Rezoskan, 99mTc

General characteristics. Structure:

Active agent: zoledronovy acid - 1,5mg.

Excipients: Tin of dichloride anhydrous - 0,33mg, Technetium-99m - 185-740mbk, Zoledronovaya acid 0,3mg, Olova of dichloride anhydrous - 0,066mg, Sodium chloride - 9,0mg, water for injections to 1,0 ml.

Description. Lyophilisate: white or almost white lyophilisate in the form of flat cake or separate units, or in the form of powder. 

Ready solution: colourless transparent liquid.

Pharmacological properties:

Zoledronovy acid, marked 99mTc, possesses a high tropnost to a bone tissue. The main substance of lyophilisate – бисфосфонат - the zoledronovy acid having the maximum affinity to sites of the increased metabolism and the accelerated resorption in a bone tissue.

Pharmacokinetics.

Researches of pharmacokinetics of zoledronovy acid, marked 99mTc, showed that the expressed osteotropnost against the background of the high speed of removal from bodies, fabrics and all body is characteristic of its distribution. The peak of concentration of drug in the main bodies and fabrics, including kidneys, is observed in 10 min. after introduction. In a bladder the peak of concentration is noted in 1 hour after introduction. The maximum of accumulation of drug in a skeleton (to 40% of the entered activity) is observed in 1 - 2 hour after introduction. High accumulation of drug in a skeleton remains till 8 - 12 o'clock observation.

Zoledronovy acid, marked 99mTc, differs in the high speed of removal. Activity level in blood after introduction does not exceed 1% and for 4 – 5 min. decreases to trace values. In 1 hour after introduction, to 20% of drug it is brought out of an organism with urine, considerable decrease in level of isotope in kidneys, a liver, skeletal muscles and in all body is observed.

Features of pharmacokinetics of zoledronovy acid, marked 99mTc, against the background of high affinity to sites of the increased metabolism and the accelerated resorption in a bone tissue, explain with the different bystry speed of removal a possibility of carrying out an osteostsintigrafiya, in 1 hour after introduction, providing high-quality visualization of a skeleton.

Indications to use:

Drug Rezoskan, 99mTc is used for identification of the centers of a pathological resorption and sites of the increased metabolism in a bone tissue at various pathological processes in a skeleton: for identification and identification of the lytic, mixed and blast metastasises in a skeleton, at malignant tumors of various origin and prevalence, at osteomyelitis, bone and joint tuberculosis, osteoporosis, various bone and joint degenerative processes, including at arthritises and arthroses of various origin, for the choice of specific therapy of bone defeats by drugs of zoledronovy acid and control of efficiency of treatment.

Route of administration and doses:

The drug is administered intravenously. The dosage is carried out according to research problems and character of the carried-out methods, and also technical characteristics of the used equipment. As a rule, the entered dose makes 5 MBK on 1 kg of body weight.

Drug preparation Rezoskan, 99mTc:

- 5 ml of eluate from the technetium-99m generator with volume activity of 185 - 740 MBK/ml in aseptic conditions enter by means of the syringe into a bottle with lyophilisate, puncturing a rubber bung with a needle;

- if necessary previously carry out eluate dilution by isotonic solution of sodium of chloride up to the required size of volume activity;

- contents of a bottle are mixed stirring before full dissolution of lyophilisate;

- drug is ready to use in 20 min. after preparation;

- the ready drug prepared on the basis of the lyophilisate which is contained rolled into one can be used for a research of 5 patients.

Technique of carrying out inspection.

The research is conducted by means of the gamma camera by method of a stsintigrafiya of all body in front and back projections in 1 - 2 hour after administration of drug with obligatory preliminary bladder emptying.

Interpretation of results of a research is carried out by assessment of distribution of drug in a skeleton. Zones of pathological changes in a bone tissue are characterized by the drug hyper fixing centers Rezoskan, 99mTc.

Beam loads of bodies and all body of the patient when using drug Rezoskan 99mTc:

Organa Doz's No.                         (MBK is glad/)

1 Stomach                         1.5х10-4

2 Lungs                         3.8х10-4

3 Territory кост. brain                     1.0х10-3

4 Ovaries                         3.6х10-4

5 Seed plants                       2.4х10-4

6 Upper part of a large intestine         2.1х10-4

7 Lower part of a large intestine         3.8х10-4

8 Bladder                   2.3х10-2

9 Liver                          2.3х10-4

10 Thyroid gland               1.5х10-4

11 Mammary gland                 8.5х10-5

12 Bones                          7.0х10-3

13 Skin                           1.0х10-4

14 Small bowel                    2.4х10-4

15 Kidneys                          1.4х10-3

16 Skeletal muscles                 2.1х10-4

17 Pancreas             2.1х10-4

18 Spleen                       1.9х10-4

19 All body (remains)                 2.5х10-4

20 Heart                         2.4х10-4

21 Adrenal glands                    2.8х10-4

22 Brain                    1.7х10-4

23 Gall bladder                  1.9х10-4

24 Thymus                1.3х10-4

25 Uterus                          6.1х10-4

Effective dose (mzv/MBK) – 0,0016.

Features of use:

Work with drug has to be carried out according to "The basic health regulations of ensuring radiation safety" (OSPORB-99), "Standards of radiation safety" (NRB-99) and the methodical instructions "Hygienic Requirements on Ensuring Radiation Safety when Carrying Out Radionuclide Diagnosis by means of Radiopharmaceuticals" (MU 2.6.1.1892-04).

Side effects:

Allergic reactions are possible.

Interaction with other medicines:

In the used dosages interaction with other medicines was not noted.

Contraindications:

Are not described.

Overdose:

The overdose of drug is improbable in connection with careful control of the entered activity in the conditions of a specialized hospital.

Storage conditions:

Lyophilisate is stored in the dry, protected from light place at a temperature from 2 to 10 °C.

Drug is stored according to "The basic health regulations of ensuring radiation safety" (OSPORB-99).

Issue conditions:

According to the recipe

Packaging:

Lyophilisate for preparation of solution for intravenous administration. On 1,83 mg of lyophilisate in bottles of dark the volume of 10 ml, corked by traffic jams from rubber and caps aluminum-plastic flew down. 

Packaging 1. 

1 bottle with lyophilisate, 1 syringe of single use, a sterile needle, 2 spirit tampons, pack into a blister strip packaging 

1 blister strip packaging (set) together with the application instruction is placed in a cardboard pack. 

Packaging 2. 

5 bottles with lyophilisate pack in planimetric cell upakovku.1 a blister strip packaging together with the application instruction place in a cardboard pack.