Universal reference book for medicines
Name of the preparation: OCTREOIDIDE, 111 In (OCTREOTIDE, 111 In)

Active substance: pentetreotide

Type: Radioisotope diagnostic preparation

Manufacturer: FARM-SYNTHESIS (Russia)
Composition, form of production and packaging
Lyophilizate for the preparation of a solution for intravenous administration in

1 f.

pentetreotide 10 μg

Excipients: gentisic acid, sodium chloride, sodium citrate pentasecylhydrate.

In 1 ml of the prepared solution contains:

Active substances:

indium-111 111 MBq / 222 MBq

pentetreotide 10 μg

Excipients: gentisic acid, sodium chloride, sodium citrate, hydrochloric acid, water d / u.

Vials of dark glass with a volume of 10 ml (1) complete with a disposable syringe, sterile needle and alcohol sponges (2) - packings of cellular contour (1) - cardboard packs.

Vials of dark glass in volume of 10 ml (5) - packings cellular planimetric (1) - packs cardboard.


Description of the drug approved by the manufacturer for the printed edition of 2014.


Octreotide, 111 In - radiopharmaceutical preparation, is prepared from lyophilizate and indium-111 chloride solution.

The isotope Indium-111 has a half-life of 67.37 hours. Upon decay, Indium-111 emits gamma quanta with an energy of 0.173 MeV (89%), 0.247 (94%).

Octreotide, 111 In - is a pentetreotide (DTTP-modified octreotide), labeled with the isotope indium-111 ( 111 In).

Octreotide is a synthetic octapeptide, which is an analog of somatostatin and possesses similar pharmacological effects, but a much longer duration of action.
The pharmacological activity of octreotide is due to its ability to bind to somatostatin receptors (S 2 and S 5 ) located on the surface of cells. Octreotide, 111 In actively binds to the same somatostatin receptors as octreotide.
Cells of a number of tumors and their metastases have a high density of somatostatin receptors, significantly exceeding their density on cells of normal tissues, which makes it possible to visualize these tumors using Octreotide, 111 In preparation.

The content of octreotide in the preparation is 10 times less than in a single therapeutic dose, so Octreotide, 111 In does not possess the pharmacodynamic properties characteristic of octreotide.


After intravenous administration, the drug quickly leaves the bloodstream and after 10 minutes in the blood remains 1/3 of the administered dose.

T 1/2 Octreotide, 111 In from the body is 6 hours. The excretion is almost entirely through the kidneys.
Half of the administered dose of the drug is excreted in the urine within 6 hours after the injection. Within 24 hours 85% of the administered dose of Octreotide, 111 In. Is withdrawn.
Excretion of the drug through the liver is insignificant.
After 3 days only 2% of the administered dose is determined in the stool.
Octreotide, 111 In is displayed basically unchanged.
However, up to 10% of radioactivity is excreted in the form unbound to the peptide.

- for radionuclide diagnostics of tumors with a high somatostatin receptor density (neuroendocrine tumors, CNS tumors, breast cancer, small cell lung cancer) using planar scintigraphy and single-photon emission computed tomography (SPECT);

- to establish the receptor status of the tumor in order to predict the clinical effect on treatment with octreotide.


The drug is administered iv bolus in a dose of 111 MBq for planar scintigraphy and 222 MBq for SPECT.

Radiation loads on the organs and the entire body of the patient with Octreotide, 111 In:

The absorbed dose of mGy / MBq

Adrenal glands 7.58 × 10 -5

The bladder is 1.4 × 10 -3

Skeleton 5.6? 10 -5

The brain 1.00? 10 -5

The mammary gland is 1.21 × 10 -5

Gallbladder 1.07? 10 -4

Stomach 1.2 × 10 -4

Small intestine 4.6 × 10 -4

The upper part of the large intestine is 3.3 × 10 -4

The lower part of the large intestine is 4 × 10 -4

Heart 2.6? 10 -3

The kidneys 8.1 × 10 -4

Liver 7 × 10 -5

Lightweight 2.4? 10 -5

Muscles 5.18 × 10 -5

Ovaries 2.1 × 10 -4

Testes 7? 10 -5

The pancreas is 7.78 × 10 -5

Red bone marrow 6? 10 -5

Leather 2.03? 10 -5

The spleen is 7.54 × 10 -5

Thymus gland 1.63 × 10 -5

Thyroid gland 1.38 × 10 -5

Uterus 2.73 × 10 -4

The effective equivalent dose of 1.9 × 10 -1 mSv / MBq

Rules for the preparation Octreotide, 111 In

Place the vial with the lyophilizate in a protective lead cylinder, wipe the rubber plug with a swab dipped in alcohol and dry it under aseptic conditions, transfer 1 ml of India-111 chloride solution with a needle and a syringe in the lyophilizate pencil case to the lyophilisate vial.
It is easy to shake the bottle until all the lyophilisate is dissolved. Incubate the resulting solution for 30 minutes at room temperature (not above 25 ° C). After that, the solution should be clear, colorless and contain no mechanical inclusions.
The resulting solution is designed for 1 patient and should be used within 6 hours after preparation.


At clinical use of the preparation of undesirable reactions it is not revealed.


- hypersensitivity to the drug or its components.


Use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

If you need to use the drug during lactation, you should stop breastfeeding for at least 48 hours.


Do not use the drug in conjunction with synthetic analogues of somatostatin.

Work with the drug should be carried out in accordance with the following regulatory documents: "Basic Sanitary Rules for Ensuring Radiation Safety" (OSPORB-99), "Radiation Safety Standards" (NRB-99), SanPin 2. 61. 1281-3, MU 2. 6.1. .

When using the drug for diagnostic purposes and controlling the radioactivity of indium-111, an overdose is unlikely in connection with the lack of pharmacodynamic properties in the preparation.


Data on interactions with other drugs are not available.


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.


The bottle with lyophilizate in the package should be stored in a dry, dark place at a temperature of 2 ° to 8 ° C.
Shelf life - 1 year. It is allowed to deviate from the temperature regime (18-25 ° C) during transportation for 1 month.
The finished solution is stored at a temperature of no higher than 25 ° C.
The finished product is usable for no more than 6 hours. Do not use after the expiration date.
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