Sodium iodide Na131I - instructions for use, dose, side effects, contraindications

Components	amount
Active substance:
Sodium iodide Na¹³¹I	37-740 MBq
Excipients:
Sodium carbonate	0.49 mg
Sodium bicarbonate	2.75 mg
Sodium thiosulfate pentahydrate	0.245 mg
Sodium chloride	0.7 mg
Water for injections	up to 1 ml

Description:A clear, colorless solution.

Pharmacotherapeutic group:Radiopharmaceutical diagnostic and therapeutic agent

ATX: & nbsp

V.09.F.X Other radiopharmaceuticals for diagnosing thyroid diseases

Pharmacodynamics:Physicochemical characteristics

Sodium iodide, ¹³¹I, a solution for intravenous administration is a solution of sodium iodide with iodine-131 in a buffer solution, pH - 7,0-10,0, radiochemical purity 97.0%, volumetric activity - 37 - 740 MBq / ml for drug manufacturing date . Iodine-131 is characterized by a half-life of 8.02 days; The most intense component of gamma radiation has an energy of 0.365 MeV (81.7%); beta radiation - 606 keV.

The radiation dose administered to patients by iodine-131, depending on the absorption of the thyroid gland, is presented in ICRP 53: Annals of the ICRP, the irradiation dose for patients from radiopharmaceuticals, Pergamon Press 1987.

Blocked thyroid gland, absorption when using thyreostatics - 0%

Organ	Absorbed dose per unit of injected activity [mGy / MBq]
Organ	Adults	15 years		10 years	5 years	1 year
Adrenal glands	0,037	0,042		0,067	0,110	0,200
The wall of the bladder	0,610	0,750		1,100	1,800	3,400
Surface of bone	0,032	0,038		0,061	0,097	0,190
Breast	0,033	0,033		0,052	0,085	0,170
Gastrointestinal tract:
The wall of the stomach	0,034	0,040		0,064	0,100	0,190
Small intestine	0,038	0,047		0,075	0,120	0,220
The wall of the upper part of the large intestine	0,037	0,045		0,070	0,120	0,210
The wall of the lower part of the large intestine	0,043	0,052		0,082	0,130	0,230
Kidneys	0,065	0,080		0,120	0,170	0,310
Liver	0,033	0,040		0,065	0,100	0,200
Lungs	0,031	0,038		0,060	0,096	0,190
Ovaries	0,042	0,054		0,084	0,130	0,240
Pancreas	0,035	0,043		0,069	0,110	0,210
Red marrow	0,035	0,042		0,065	0,100	0,190
Spleen	0,034	0,040		0,065	0,100	0,200
Eggs	0,037	0,045		0,075	0,120	0,230
Thyroid	0,029	0,038		0,063	0,100	0,200
Ureter	0,054	0,067		0,110	0,170	0,300
Other fabrics	0,032	0,039		0,062	0,100	0,190
The effective equivalent dose (mSv / MBq)	0,072	0,088		0,140	0,210	0,400
Up to 50.8% of the effective equivalent dose falls on the wall of the bladder. Incomplete locking: Effective dose (mSv / MBq) with a slight absorption by the thyroid gland.
Absorption of 0.5%	0,300		0,450	0,690	1,500	2,800
Absorption 1.0%	0,520		0,810	1,200	2,700	5,300
Absorption 2.0%	0,970		1,500	2,400	5,300	10,00

Absorption of the thyroid gland 15%

Organ	Absorbed dose per unit of injected activity [mGy / MBq]
Organ	Adults	15 years	10 years	5 years	1 year
Adrenal glands	0,036	0,043	0,071	0,110	0,220
The wall of the bladder	0,520	0,640	0,980	1,500	2,900
Surface of bone	0,047	0,067	0,094	0,140	0,240
Breast	0,043	0,043	0,081	0,130	0,250
Lcd path
The wall of the stomach	0,460	0,580	0,840	1,500	2,900
Small intestine	0,280	0,350	0,620	1,000	2,000
The wall of the upper part of the large intestine	0,059	0,065	0,100	0,160	0,280
The wall of the lower part of the large intestine	0,042	0,053	0,082	0,130	0,230
Kidneys	0,060	0,075	0,110	0,170	0,290
Liver	0,032	0,041	0,068	0,110	0,220
Lungs	0,053	0,071	0,120	0,190	0,330
Ovaries	0,043	0,059	0,092	0,140	0,260
Pancreas	0,052	0,062	0,100	0,150	0,270
Red marrow	0,054	0,074	0,099	0,140	0,240
Spleen	0,042	0,051	0,081	0,120	0,230
Eggs	0,028	0,035	0,058	0,094	0,180
Thyroid	210,0	340,0	510,0	1100,0	2000,0
Uterus	0,054	0,068	0,110	0,170	0,310
Other fabrics	0,065	0,089	0,140	0,220	0,400
The effective dose (mSv / MBq)	6,600	10,00	15,00	34,00	62,00

Thyroid absorption 35%

Organ	Absorbed dose per unit of injected activity [mGy / MBq]
Organ	Adults	15 years	10 years	5 years	1 year
Adrenal glands	0,042	0,050	0,087	0,140	0,280
The wall of the bladder	0,400	0,500	0,760	1,200	2,300
Surface of bone	0,076	0,120	0,160	0,230	0,350
Breast	0,067	0,066	0,130	0,220	0,400
Lcd path
The wall of the stomach	0,460	0,590	0,850	1,500	3,000
Small intestine	0,280	0,350	0,620	1,000	2,000
The wall of the upper part of the large intestine	0,058	0,065	0,100	0,170	0,300
The wall of the lower part of the large intestine	0,040	0,051	0,080	0,130	0,240
Kidneys	0,056	0,072	0,110	0,170	0,290
Liver	0,037	0,049	0,082	0,140	0,270
Lungs	0,090	0,120	0,210	0,330	0,560
Ovaries	0,042	0,057	0,090	0,140	0,270
Pancreas	0,054	0,069	0,110	0,180	0,320
Red marrow	0,086	0,120	0,160	0,220	0,350
Spleen	0,046	0,059	0,096	0,150	0,280
Eggs	0,026	0,032	0,054	0,089	0,180
Thyroid	500,0	790,0	1200,0	2600,0	4700,0
Uterus	0,050	0,063	0,100	0,160	0,300
Other fabrics	0,110	0,160	0,260	0,410	0,710
The effective dose (mSv / MBq)	15,00	24,00	36,00	78,00	140,00

absorption by the thyroid gland 55%

organ	absorbed dose per unit of injected activity [mg / mb \|
	adults	15 years	10 years	5 years	1 year
adrenal glands	0,049	0,058	0,110	0,170	0,340
bladder wall	0,290	0,360	0,540	0,850	1,600
bone surface	0,110	0,170	0,220	0,320	0,480
breast	0,091	0,089	0,190	0,310	0,560
L / C path
gastric wall	0,460	0,590	0,860	1,500	3,000
small intestine	0,280	0,350	0,620	1,000	2,000
upper wall of large intestine	0,058	0,067	0,110	0,180	0,320
the wall of the lower part of the large intestine	0,039	0,049	0,078	0,130	0,240
kidneys	0,051	0,068	0,100	0,170	0,290
liver	0,043	0,058	0,097	0,170	0,330
lungs	0,130	0,180	0,300	0,480	0,800
ovaries	0,041	0,056	0,090	0,150	0,270
pancreas	0,058	0,076	0,130	0,210	0,380
red marrow	0,120	0,180	0,220	0,290	0,460
spleen	0,051	0,068	0,110	0,170	0,330
testicles	0,026	0,031	0,052	0,087	0,170
thyroid	790,0	1200,0	1900,0	4100,0	7400,0
uterus	0,046	0,060	0,099	0,160	0,300
other tissues	0,160	0,240	0,370	0,590	1,000
effective dose (mV / mb)	24,00	37,00	56,00	120,00	220,00

Pharmacokinetics:

Selective accumulation of iodine-131 in the thyroid gland allows the use of the drug for therapeutic purposes to treat thyrotoxicosis, as well as thyroid cancer and its metastases.

Radioactive isotope of iodine ¹³¹I, when introduced into the body, it accumulates mainly in the thyroid gland. Absorption kinetics ¹³¹I thyroid gland (relative to the administered amount) is on average: after 2 hours - 14%, after 4 hours - 19%, after 24 hours - 27%. It is excreted in urine and feces (60% within 24 hours).

The value of the accumulation and removal rates of the drug from organs and tissues depends on the functional state of the thyroid gland, as well as on the age and sex of the patient.

Indications:

For medicinal purposes The drug is used to treat patients with toxic goiter, thyroid cancer and its metastases.

For diagnostic purposes - To assess the functional state of the thyroid gland, scan and scintigraphy of the thyroid gland in various diseases, including diagnosis of disteariosis, as well as A-cell thyroid cancer and metastases.

Contraindications:

Pregnancy, lactation.

Contraindication to the treatment of thyrotoxicosis with radioactive iodine is thyrotoxic adenoma, nodular goiter, retrosternal goiter, simple goiter without thyroid dysfunction, mild thyrotoxicosis, mixed toxic goiter, diffuse kidney damage, blood diseases, especially with violation of leukopoiesis and thrombocytopoiesis, severe hemorrhagic syndrome, hypersensitivity, age restriction - up to 20 years, gastric ulcer and duodenal ulcer in the stage of exacerbation.

Contraindication to the use of the drug for diagnostic purposes is hypersensitivity, children under 18 years.

Carefully:

The use of the drug with a therapeutic purpose in the age group of 20-40 years should only be carried out after a thorough assessment of the risk / benefit.

If you have one of the listed diseases / conditions, be sure to consult a doctor before starting therapy.

Pregnancy and lactation:

The use of the drug is contraindicated in pregnancy and during breastfeeding.

Dosing and Administration:

A solution with a specific radioactivity should be administered directly to patients intravenously.

Radioiodine therapy

In the treatment of thyrotoxicosis in diffuse and multi-site toxic goiter, treatment is carried out 3-4 weeks after thyroidectomy or withdrawal L-tiroxine 20 days before the administration of the drug. Patients are transferred to specialized wards equipped with an autonomous ventilation and sewerage system connected to special treatment facilities. Patients are withdrawn from the "closed" regime when the gamma radiation power is reduced to the permissible level of radiation safety (3 μSv / h).

In the treatment of thyrotoxicosis, the amount of the drug administered is individually selected in the range from 111 to 555 MBq.

The main condition for radioiodine therapy of cancer and metastases of the thyroid gland is thyroidectomy. The duration of treatment - no earlier than 4-6 weeks after surgery. The most optimal form for radioiodine therapy is the highly differentiated A-cellular thyroid cancer. Carrying out radioiodine therapy of metastases of B- and C-cell forms of thyroid cancer is inexpedient.

In the treatment of metastases of thyroid cancer, the drug is prescribed by mouth in an amount of 1850-3700 MBq once every 3 months. Before each re-appointment of the drug, studies of iodine-absorption activity of metastases are carried out. To do this, use the method of scintigraphy or radioisotope scanning after the administration of 37-74 MBq of the drug. The duration of therapy can be up to 2 years, and the total dose ¹³¹I - 18.5-25.9 MBq.

Currently, there are two most common methods for calculating the input activity of iodine-131.

Individual calculation based on the volume of the thyroid gland, the rate of iodine-131 capture during the diagnostic scan 24 hours after taking the drug and the specified activity per gram of tissue (range from 0.1 to 0.3 MBq / g) according to the formula:

Av = (As x V) / (C x 10), where

Az is the given activity, MBq / g;

V - volume of the thyroid gland, cm³;

C - iodine-131 capture rate after 24 hours after drug administration;

10 is the coefficient.

Purpose of the fixed activity of iodine-131:

190 MBq - small glands;

380 MBq - glands of medium size;

579 MB - large glands.

Before the start of treatment, a preliminary determination of the absorption of iodine-131 by the thyroid gland is necessary, which guarantees the correctness of treatment, excludes the possibility of an error associated with the use of fixed activity in a patient with a large but poorly absorbing iodine-131 gland.

In the therapeutic use of the drug, continuous monitoring of the peripheral blood condition is a prerequisite.

Radioiodiagnostics

Preparation of the patient. Research of the functional state of the thyroid gland should be conducted no earlier than 4-6 weeks after the abolition of the intake of stable iodine preparations, iodine and iodinated foods and multivitamin preparations containing iodine, iodine-containing radiopaque agents, fluoride, bromine, thiiodothyronine, thyroxine, thyroidin, 6-methylthiouracil and other similar antithyroid drugs, as well as glucocorticosteroids.

To study the function of the thyroid gland by the amount of iodine-131 accumulation, it is sufficient to enter 0.037-0.074 MBq of the drug, when scanning the thyroid gland, determining protein-bound iodine and studying the whole body radiometry method - 0,111-0,185 MBq.

Methods of research

Functional state of the thyroid gland can be estimated by:

- the amount of iodine-131 accumulation in the gland after 2, 4, 24 hours and at a later time after application of the drug;

- the level of protein-bound iodine in plasma;

- results of radiometry of the whole body.

Amount of accumulation ¹³¹I in the thyroid gland is the total index of the state of the inorganic and organic phases of iodine metabolism in this organ. The determination is made using a radiometer, placing the end of the sensor at a distance of 30 cm from the front surface of the neck. Radiometry standard, which is used as a ¹³¹I in an amount equal to the administered patient, is carried out under the same geometric conditions.

The percentage of radionuclide accumulation in the thyroid gland (A) is calculated by the formula:

A = [B-N_f/ C-N_f] x 100% where:

C - content ¹³¹I in iron, imp / min;

C - content ¹³¹I in the standard, imp / min;

N_f - background, imp / min.

In healthy people, in the thyroid gland, after 2 hours, an average of 14% of the introduced amount of isotope accumulates, after 4 hours - 19%, after 24 hours - 27%.

In order to determine level of protein-bound iodine in a patient after 48 hours, a blood sample (8-10 ml) is taken from the ulnar vein. After centrifugation, 4 to 5 ml of blood plasma is transferred to a test tube and the protein is separated by adding 3% of 10% trichloroacetic acid solution in a volume equal to the volume of the blood plasma to be analyzed, followed by centrifugation at 2000 rpm for 10 minutes. The resulting precipitate is dissolved in a 2M solution of caustic sodium or caustic potassium, leading to the original volume of blood plasma, and radiometric in the well counter in parallel with the standard. As the latter, a solution ¹³¹I, diluted in a ratio of 1: 500; the volume of the standard should be equal to the volume of plasma taken for radiometry.

The percentage of protein-bound iodine (A) is calculated by the formula:

A = (AT - N_f) х 1000 х 100 /C x (D - N_f) х 500% / l, where:

C - content ¹³¹I in iron, imp / min;

C - volume of blood plasma taken for analysis, ml;

D - content ¹³¹I in the standard, imp / min;

N_f - background, imp / min.

The normal level of protein-bound iodine is no more than 0.3% per liter.

Radiometry of the whole body allows to evaluate the peripheral stage of thyroid hormone exchange and is carried out in the following way: 2 hours after taking 1.0 MBq of the drug, during which the patient is asked not to empty the bladder, a first measurement in geometry providing the necessary accuracy; the results of this first radiometry are taken as 100%; in the subsequent radiometry is repeated after 24, 72, 120 and 192 hours; The registration is performed every time both with shielding of the neck (thyroid) region with a lead plate 4-5 cm thick, and without screening. Radiometry results are used to calculate the content ¹³¹I in subsequent terms in the thyroid gland and in the entire body, except for the thyroid gland, as a percentage of the administered amount.

Content ¹³¹I normal in the human body (without taking into account the thyroid gland) after 1 day is 10-25%, after 3 days - 9.7-15%, after 8 days - 2-12%.

The method of radionuclide diagnosis of A-cell cancer and thyroid metastases involves scanning or scintigraphy of the entire body 24 and 48 hours after intravenous administration 111-165 MBq of the preparation.

Side effects:

In the treatment of hyperthyroidism and metastatic thyroid possible aggravation of hyperthyroidism cancer occurrence hypothyroidism and myxedema, the appearance or amplification exophthalmos, radiotireoidity, nausea, vomiting, thrombocytopenia, leukopenia, acute gastritis, amenorrhea, ulcerative cystitis, mumps, alopecia, reactive skin changes in thyroid glands, mucous pharynx and larynx. Allergic reactions are possible. Treatment of these complications is symptomatic.

When using the drug for therapeutic purposes, oppression of bone marrow hematopoiesis is possible, restoration of which is carried out by the following means: leukogen, lenograstim, dioxomethyltetrahydropyrimidine, mogratostim, epoetin alfa.

When using the drug with a diagnostic purpose, allergic reactions are possible.

Overdose:

Overdose of the drug is unlikely in connection with the careful control of the injected activity in the conditions of a specialized hospital.

Interaction:

In the dosages used, no interaction with other drugs was noted.

Special instructions:

The work with the drug should be carried out in accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99/2010), "Radiation Safety Standards" (NRB-99/2009), Guidelines "Hygienic requirements for ensuring radiation safety during radionuclide diagnostics with the help of radiopharmaceuticals "(MU - 2.6.1.1892-04).

Patients exposed to high doses ¹³¹I, require hospitalization in connection with high radiological risk in a specialized hospital, whose chambers are equipped with an autonomous ventilation and sewage system connected to special treatment facilities.

Prior to the administration of sodium iodide ¹³¹I it is necessary to stop taking the following medicines: antithyroid drugs (incl. propylthiouracil, potassium perchlorate) for 2-5 days; salicylates, steroids, sodium nitroprusside, anticoagulants, antihistamines, anthelmintic, penicillins, sulfonamides, tolbutamide, sodium thiopental - for 1 week; phenylbutazone - for 1-2 weeks; expectorants and vitamins containing iodine - about 2 weeks; hormonal drugs of the thyroid gland - 2-6 weeks; amiodarone, benzodiazepines and lithium preparations - about 4 weeks; preparations for topical use containing in their composition iodine - 1-9 months; iodine-containing radiocontrast agents - up to 12 months. Due to the long half-life of amiodarone, the absorption of iodine by the thyroid tissue can be reduced for several months.

Contraception should be used in men and women within 12 months after radioiodine therapy of thyroid cancer and 6 months after treatment of thyrotoxicosis (in patients with benign thyroid diseases).

Effect on the ability to drive transp. cf. and fur:

The radiopharmaceutical does not affect the ability to drive and operate machinery.

Form release / dosage:Solution for intravenous administration with activity 40, 120, 200, 400, 1000, 2000, 4000, 6000, 7400 MBq for the set delivery date.

Packaging:

The activity of packing of the preparation at 40, 120, 200, 400, 1000, 2000, 4000, 6000, 7400 MBq for the set delivery date for volumetric activity from 37 to 740 MBq / ml at the date of manufacture in bottles of neutral glass (type I , Eur. F.) with a capacity of 10 ml, hermetically sealed with rubber stoppers and crimped with aluminum caps.With volumetric activity closer to the lower limit (37MBk / ml), nominal - 40, 120, 200, 400 MBq; with volume activity closer to the upper limit (740 MBq / ml), nominal - 1000, 2000, 4000, 6000, 7400 MBq.

A label is attached to the vial. The vial with radioactive contents is placed in a plastic pencil, which is placed in the plastic socket of the protective container type P-30. The container consists of a steel casing and a cork, which is fixed to the casing with screws. The inner cavities of the body and the plugs are filled with lead. Above and below the bottle is covered with absorbent inserts. A label is attached to the container. The protective container is placed in a sealed tin can and fixed in it with a styrofoam insert, the jar, together with the instruction for use, is placed in a cardboard box on which a label is affixed.

Storage conditions:

In the original packaging, at a temperature of no higher than 25 ° C.

In accordance with the "Basic Sanitary Rules for Ensuring Radiation Safety (OSPORB-99 / 20Yu)" and "Norms of Radiation Safety" (NRB - 99/2009).

Shelf life:

28 days from the date of manufacture.

Do not use after expiry date.

Terms of leave from pharmacies:For hospitals

Registration number:LP-003687

Date of registration:20.06.2016

Expiration Date:20.06.2021

The owner of the registration certificate:National Center for Nuclear ResearchNational Center for Nuclear Research Poland

Manufacturer: & nbsp

National Center for Nuclear Research Poland

Representation: & nbspNational Center for Nuclear ResearchNational Center for Nuclear ResearchPoland

Information update date: & nbsp26.05.2018

Illustrated instructions

Instructions

Sodium iodide Na131I (Sodium iodide, 131I)