Composition, form of production and packaging
Lyophilizate for the preparation of a solution for intravenous administration of white or almost white color, in the form of a cake or individual aggregates, or powder; The prepared solution is a colorless transparent liquid.
zoledronic acid 1.5 mg
[PRING] tin dichloride anhydrous - 0.33 mg.
In 1 ml of the prepared solution contains:
technetium 99m 185-740 MBq
zoledronic acid 300 Ојg
Excipients: tin dichloride anhydrous - 0.66 mg, sodium chloride - 9 mg, water d / and - up to 1 ml.
1.83 mg - bottles of dark glass with a volume of 10 ml (1) complete with a disposable syringe, sterile needle and alcohol sponges (2 pcs.) - packings of cellular contour (1) - packs of cardboard.
1.83 mg - bottles of dark glass with a volume of 10 ml (5) - packings of cellular contour (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Radiopharmaceutical diagnostic drug.
Zoledronic acid, labeled with 99m Tc, has a high tropism for bone tissue.
The basic substance of the lyophilizate is bisphosphonate - zoledronic acid, which has the maximum affinity for sites of increased metabolism and accelerated resorption in bone tissue.
Studies of the pharmacokinetics of zoledronic acid labeled with 99m Tc have shown that its distribution is characterized by pronounced osteotropism against the background of a high rate of excretion from organs, tissues and the whole body. C max of the drug in the main organs and tissues, including the kidneys, is observed 10 min after administration. In the bladder, C max is noted 1 h after the administration. The maximum accumulation of the drug in the skeleton (up to 40% of the injected activity) is observed 1 to 2 hours after administration. High accumulation of the drug in the skeleton persists up to 8-12 hours of observation.
Zoledronic acid, labeled with 99m Tc, is characterized by a high rate of excretion. The level of activity in the blood after administration does not exceed 1% and is reduced to trace values вЂ‹вЂ‹by 4-5 min. 1 hour after the introduction, up to 20% of the drug is excreted from the body with urine, there is a significant decrease in the level of the isotope in the kidneys, liver, skeletal muscles and throughout the body.
The peculiarities of the pharmacokinetics of zoledronic acid labeled with 99m Tc, distinguished by the rapid elimination rate, against the background of high affinity for sites of increased metabolism and accelerated resorption in bone tissue, explain the possibility of performing osteoscintigraphy as early as one hour after administration, providing a qualitative visualization of the skeleton.
To identify the foci of pathological resorption and areas of increased metabolism in bone tissue with various pathological processes in the skeleton:
- to identify and identify lytic, mixed and blast metastases in the skeleton in malignant tumors of various origin and prevalence;
- with osteomyelitis, osteoarticular tuberculosis, osteoporosis, various osteoarticular degenerative processes, incl. with arthritis and arthrosis of various origin;
- for the selection of specific therapy for bone lesions with zoledronic acid preparations and for monitoring the effectiveness of treatment.
The drug is administered iv. Dosage is carried out in accordance with the objectives of the study and the nature of the methods performed, as well as the technical characteristics of the equipment used. As a rule, the administered dose is 5 MBq per 1 kg of body weight.
Rules of preparation preparation Resoscan, 99m Tc
- 5 ml of the eluate from the technetium-99m generator with volumetric activity of 185-740 MBq / ml under aseptic conditions are injected with a syringe into a vial of lyophilizate, piercing the rubber stopper with a needle;
- If necessary, dilute the eluate with an isotonic solution of sodium chloride before the required volume activity;
- the contents of the vial are mixed by shaking until the lyophilizate is completely dissolved;
- the preparation is ready for use 20 minutes after preparation;
- A ready-made preparation prepared on the basis of a lyophilizate contained in one bottle can be used to study 5 patients.
Methodology of the survey
The study is performed with the help of a gamma camera using whole-body scintigraphy in the anterior and posterior projections 1-2 hours after the administration of the drug with mandatory pre-emptying of the bladder.
Interpretation of the results of the study is carried out by estimating the distribution of the drug in the skeleton. Zones of pathological changes in bone tissue are characterized by foci of hyperfixation of the drug Resoscan, 99m Tc.
Radiation loads on the organs and whole body of the patient when using the drug Resoscan, 99m Tc
Organs Dose (rad / MBq)
Stomach 1.5 Г— 10 -4
Lightweight 3.8 Г— 10 -4
Red bone marrow 1.0? 10 -3
Ovaries 3.6 Г— 10 -4
Testes 2.4 Г— 10 -4
The upper part of the large intestine is 2.1 Г— 10 -4
The lower part of the large intestine is 3.8 Г— 10 -4
The bladder is 2.3 Г— 10 -2
The liver is 2.3 Г— 10 -4
Thyroid gland 1.5 Г— 10 -4
Mammary gland 8.5? 10 -5
Bones of 7.0? 10 -3
Leather 1.0? 10 -4
Small intestine 2.4? 10 -4
The kidneys are 1.4 Г— 10 -4
Skeletal Muscle 2.1 Г— 10 -4
The pancreas is 2.1 Г— 10 -4
Spleen 1.9 Г— 10 -4
The whole body (remains) of 2.5 Г— 10 -4
Heart 2.4? 10 -4
Adrenal glands 2.8 Г— 10 -4
The brain is 1.7 Г— 10 -4
The gall bladder is 1.9 Г— 10 -4
Thymus gland 1.3 Г— 10 -4
Uterus 6.1 Г— 10 -4
Effective dose (mSv / MBq) - 0.0016
Possible: allergic reactions.
- children and adolescence under 18;
- Hypersensitivity to the drug or its components.
PREGNANCY AND LACTATION
The drug is contraindicated in pregnancy.
Nursing mothers should refrain from breastfeeding the baby within 24 hours after drug administration.
APPLICATION FOR CHILDREN
Contraindication: children and adolescence under 18 years.
Work with the drug should be carried out in accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99), the "Norms of Radiation Safety" (NRB-99) and the guidelines "Hygienic requirements for ensuring radiation safety during radionuclide diagnostics using radiopharmaceuticals" (MU 22.214.171.1242-04).
Overdose of the drug is unlikely in connection with the careful control of the injected activity in the conditions of a specialized hospital.
In the doses used, interaction with other drugs was not noted.
TERMS OF RELEASE FROM PHARMACY
The drug is not subject to sale through the pharmacy network, it is released only upon application to specialized radioisotope laboratories (departments) of medical diagnostic facilities.
TERMS AND CONDITIONS OF STORAGE
The lyophilizate should be stored in a dry, dark place at a temperature of 2 В° to 10 В° C. The drug should be stored in accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99). Shelf life of the lyophilisate is 1 year, the finished product is 5 hours from the time of preparation. Do not use after expiry date.