Samarium 153 Sm oxabifor

Radiopharmaceutical therapeutic drug Samarium, 153 sm Oxabiphor is developed and manufactured by Radiopreparat, which operates on the basis of the Institute of Nuclear Physics of the Academy of Sciences of the Republic of Uzbekistan.

Until recently, when diagnosing metastatic disease of bone tissue, only two drugs were on arms with the oncologist: ⁸⁹ Sr and ³² P, although the world experience of oncology practice uses isotopes of much more chemical elements in the treatment of this pathology. To date, a new drug that can come to the aid of the patient and ease his growing pain is Samarium, 153 sm Oxabiphor is a modern radiopharmaceutical. Pain syndrome with lesions of the bone system increases with the progression of the disease and becomes prerogative throughout the entire period of therapy. It is in this direction that the drug under consideration works. In parallel, the injected drug allows to slow down the development and spread of the metastasis process, which is important for a progressive oncological disease.
 

Indications of the samarium 153 Sm Oxabiphora

Preparations of this pharmacological group are developed for a narrowly targeted impact on the human body, that is, to address a particular pathological problem. Indications for the use of Samaria also have only one direction - this is a relief of pain symptoms, which invariably manifests itself in metastatic disease of bone tissue (in oncology practice). This medicine, as well as allows you to slow down the spread of metastases in the bones.

Another area of application of the drug Samaria is rheumatological practice. It is used in the pathology of the musculoskeletal system, which has passed into a chronic condition. The drug reduces the symptoms of arthralgia (the periodic occurrence of pain in joints, in the absence of characteristic signs and symptoms of their defeat), leading to a stable remission. Including pain relief symptoms of such diseases as deforming arthrosis, rheumatoid arthritis and other pathologies.

Release form

Based on the pharmacological orientation of the drug, as well as because of its belonging to radioisotope drugs, its release form is a drug solution that is used for intravenous administration.

Samaria is a transparent liquid that does not have color. 1 ml of the drug consists of several active chemical compounds, which determine the pharmacodynamics of the drug. This Samarium 153 ( ¹⁵³ Sm), which is present from 240 to 1500 MBq, also enters in the form of a tandem samarium oxabiphore, which is represented by an amount of 25 to 100 μg and sodium oxabibor in an amount of 15 to 25 mg.

There are also concomitant substances that allow to maintain therapeutic features of the drug at a high level - it is sodium chloride, as well as special pure water, which is used for injections and the injection of droppers.

Depending on the concentration of active active substances, the drug is delivered to the pharmacological market with 15 ml bottles, but different therapeutic effects: 500 MBq, 1000 MBq and 2000 MBq. A container containing a medicinal liquid is also packaged in a special kit designed to isolate radioactive substances.

Pharmacodynamics

Drugs belonging to this group, almost all work directed. Pharmacodynamics Samarium is caused by the accumulation in the bone tissues of a sick person isotope samarium-153. At the same time, his selectivity is determined by the fact that he begins to be cumulated directly in places affected by metastatic formations. Their sedimentation occurs in destructively inflammatory foci, which undergo changes in the bones of the human body.

The effect of the drug is due to the emission of beta particles emitted by the isotopes of Samarium-153 (153 is the mass number determined by Mendeleev and added to his table). It is these rays that affect the affected area, as well as the surrounding nerve endings. Samarium, thanks to its pharmacological characteristics, shows a high antiproliferative efficacy, and in parallel has an analgesic effect.

Samarium-153 isotopes emit hard gamma radiation, which makes it possible, using special medical equipment, such as a gamma camera, to fix the distribution zone and the level of cumulation of the drug.

After undergoing a course of therapy by Samaria, the osteoscintigraphy performed shows that the accumulation of the drug component in the affected tissues is two to three times higher than it settles in symmetric areas of the human body that is not affected by the disease, which confirms the selectivity of the effect of this medication.

A similar result of the survey is identical to the diagnostic indices that were performed on the basis of the osteotropic compounds of technetium-99m. This indicator allows us to give recommendations for its use in the status of selecting the method of radionuclide treatment with samarium-153 oxabiophore.

Pharmacokinetics

Pharmacokinetics Samarium shows that the clinical efficacy of drug administration begins to be noticeably manifested in at least a couple of weeks after the procedure for the introduction of radionuclide medicaments. The therapeutic effect itself is of a persistent nature and, depending on the individual characteristics of the patient, can last from three to six months.

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Dosing and administration

The drug in question is used in medical therapy as an intravenous injection. Due to its high radiation load, in order to protect the medical personnel working with the patient, during the procedure, Samaria, just before administration, is diluted with 0.9% sodium chloride solution (NaCl) taken in an amount of 50 to 100 ml.

1. In order to carry out the preliminary dilution procedure correctly, it is necessary to establish a system for intravenous infestation for work, insert the needle into the vein and proceed to the dropwise injection of the sodium chloride solution. 
2. After a short time, the drip system is closed using a special clip, all the necessary quantity of Samaria is introduced into the container containing NaCl by means of a medical syringe.
3. After this, intravenous infusion can be continued, but the patient will receive a diluted radionuclide preparation.

The method of administration and dose of the medicinal product is prescribed by the attending physician-oncologist. The recommended starting dosage of the drug is 1.5 mCi per kilogram of patient weight. In a specific clinical picture of the disease, the amount of active ingredient administered can be corrected for both smaller (1 mCi per kilogram of patient weight) and larger (2 1.5 per kilogram of patient weight) side.

If there is a therapeutic need, three months after the first procedure, the introduction of Samaria can be repeated.

Proceeding from the radioactivity of the applied mdikamenta, this procedure is carried out only in a specialized medical institution, which is equipped with an improved system of treatment facilities and filters. One of such places may be an oncological dispensary of regional subordination. After the patient has undergone this procedure for the first two days, the urine of the patient does not start immediately into the sewer system, but is maintained for some time for the procedure of splitting radionuclides.

Throughout the time of treatment, it is necessary to constantly monitor the formula and other indicators of the blood condition.

Samaria is not allowed to be administered to patients who have a history of malfunctioning of the liver and kidney due to severe impairment.

Use of the samarium 153 Sm Oxabiphora during pregnancy

Due to its radioactivity, the use of Samaria during pregnancy, as well as during the period when a young mother feeds her newborn baby with breast milk, is categorically contraindicated. If there is a clinical need to include this medication in the treatment protocol of a nursing woman, the baby should be weaned and transferred to artificial feeding.

Contraindications

Any pharmacological drug, due to its effect on the human body, has its limitations in the application and introduction of the protocol of treatment. There are also contraindications to the use of Samaria, which are represented by the following limitations:

1. Increased intolerance of the patient's body components of the drug.
2. Severe form of renal and / or hepatic dysfunction.
3. Thrombocytopenia is a reduced amount of platelets in the patient's blood plasma (less than 100.0 x ^{10 9} / L).
4. Leukopenia is a decreased amount of leukocytes in the blood plasma of the patient (less than 2,0х10 ⁹ / l).
5. Suppression of bone marrow hematopoiesis (hematopoiesis - the process of formation and development of blood cells).
6. Preventing Samaria from prescribing is also the fact that, shortly before this, the patient underwent massive myelosuppressive treatment.
7. And also if there is a real probability of compression fracture of the spine.
8. The drug is not allowed to be used in the treatment protocol for children and adolescents who at the time of treatment are under 18 years old. 

Side effects of the samarium 153 Sm Oxabiphora

Due to its pharmacological characteristics, the drug in question is quite aggressive and its administration can cause negative symptoms. Side effects of Samaria are quite trivial and conditioned by such a set:

• Nausea. This uncomfortable state can last for three days after the administration of the drug, after which its intensity gradually comes to naught. The second variant of its cupping is the introduction into maintenance therapy of one or two tablets of metoclopramide - an effective antiemetic, which perfectly removes and attacks of nausea.
• For two weeks, which proceed after the procedure, the patient feels increased pain. It arises from the radiation reaction of tissue cells, which are located in the area of pathological lesion. To stop this symptomatology is possible by entering into the protocol of treatment metamizole sodium (a drug group pyrazolones) - a drug that has in its characteristics, among other things, narcotic analgesic properties. Along with it, medicinal products related to the pharmacological group of non-steroidal anti-inflammatory drugs (NSAIDs) may also be prescribed.

Overdose

Samaria has recently entered the pharmacological market, therefore, to date, the overdose of the considered ma- dicate has not been described, in the absence of a sufficient research base.

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Interactions with other drugs

Any drug has its own limitations to admission, but this, above all, concerns the use of the considered drug in the conditions of monotherapy. When used in the treatment of complex therapy, it is necessary to know, in addition to the individual characteristics of each drug, the features of Samaria's interaction with other drugs in order to prevent deterioration of the patient's condition, weighting his anamnesis with additional pathological complications.

The specialist is obliged to know that the pharmacodynamics of radionuclide Samarium ¹⁵³ Sm Oxabiphor is therapeutically compatible with the chemotherapy using its drugs and hormone therapy, as well as with the technique of influencing malignant neoplasms and metastatic structures by remote radiation therapy.

It is necessary only to regularly monitor the patient's body condition, as well as monitor the main indicators of peripheral blood.

Storage conditions

This medicine does not go to free sale. The storage conditions of Samaria are subject to all the "Rules for the storage, recording and transport of radioactive substances, waste disposal".

They mainly focuses on the fact that the medicines of this radiopharmaceutical group should be stored in such a way that irradiation of the attendant medical personnel is not allowed, harming them. This radiation can also influence the level of accuracy of laboratory measurements and studies.

Within the laboratory, there must be as much amount of a document as is necessary for daily procedures, and no more.

Samarium, as a drug emitting active beta particles, as well as showing gamma radiation should be contained only in a special iron, in the presence of active gamma rays and with lead upholstery, a safe located in a laboratory room.

A careful daily monitoring of the use of drugs of this category is necessary.

Transportation of such drugs, including Samaria, is carried out in sealed containers to prevent the release of the drug. The personnel accompanying this cargo, as well as the environment, should be protected.

Utilization of radioactive sewage into absorbing pits, boreholes, ponds intended for breeding fish and waterfowl, as well as for water-irrigated fields, is strictly prohibited.

The place of disposal of radioactive substances should be appropriately equipped. Leakage is unacceptable.

Shelf life

This medicine is diluted directly in the process of intravenous infusion. Shelf life of the drug in question is quite organic and is only four days from the date of manufacture of Samaria. If the medicine was not in demand during the stipulated period, it is subject to disposal in compliance with all requirements detailed in the rules for storage, operation and disposal of radioactive substances and compounds.