Oktreotid, 111In

General characteristics. Structure:

Active agent: Pentetreotid of 0,01 mg. 

Excipients: gentisic acid, sodium chloride, sodium citrate 5,5-water. 

Contains in 1 ml of ready solution: 

Active agents: MBK indium-111 111, 222, Pentetreotida of 0,01 mg. 

Excipients: gentisic acid, sodium chloride, sodium citrate, Acidum hydrochloricum, water. 

Description: Lyophilisate of white color.

Pharmacological properties:

Oktreotid, 111In – represents пентетреотид (DTPA-modifitsirovanny октреотид), marked indium-111 isotope (111In). 

Oktreotid - the synthetic octapeptide which is an analog of somatostatin and having pharmacological effects, similar to it, but considerable the bigger duration of action. Pharmacological activity of an oktreotid is caused by its ability to contact the receptors of somatostatin (S2 and S5) which are on a surface of cells. Oktreotid, 111In actively contacts the same receptors of somatostatin, as октреотид. 

Cells of a number of tumors and their metastasises have the high density of receptors of somatostatin significantly exceeding them density on cells of normal fabrics that allows to visualize these tumors using drug Oktreotid, 111In.

The maintenance of an oktreotid in drug is 10 times less, than in a single therapeutic dose in this connection Oktreotid, 111In has no the pharmakodinamichesky properties characteristic of an oktreotid. 

Pharmacokinetics. 

After intravenous administration drug quickly leaves a blood channel and in 10 minutes in blood remains ⅓ from the entered dose. 

Semi-removal time Oktreotid, 111In makes 6 hours of an organism. Removal is almost completely carried out through kidneys. A half of the entered dose of drug is removed with urine within 6 hours after an injection. Within 24 hours 85% of the entered dose Oktreotid, 111In are removed. 

Removal of drug through a liver is insignificant. In 3 days only 2% of the entered dose are defined in Calais. 

Oktreotid, 111In is brought generally in an invariable look. However to 10% of radioactivity it is removed in the form which is not connected with peptide.

Indications to use:

Drug is intended for radionuclide diagnosis of the tumors having the high density of somatostatinovy receptors (neuroendocrinal tumors, tumors of the central nervous system, a breast cancer, small-celled cancer of a lung) by method of a planar stsintigrafiya or a one-photon emission computer tomography (OFEKT). 

Drug can be also used for establishment of the receptor status of a tumor for the purpose of forecasting of clinical effect for treatment by Oktreotid.

Route of administration and doses:

Preparation Oktreotid, 111In 

To place a bottle with lyophilisate in the protective lead cylinder, to wipe a rubber bung with the tampon moistened with alcohol and to dry up in aseptic conditions, to transfer 1,0 ml of India-111 solution of chloride by means of a needle and the syringe which is in a case with lyophilisate to a bottle with lyophilisate. It is easy to stir up a bottle until all lyophilisate is not dissolved. To incubate the received solution within 30 min. at the room temperature (it is not higher than 25 ° C). After that solution has to be transparent, colourless and not contain mechanical inclusions. 

The received solution is counted on 1 patient and has to be used during 6 h after preparation. 

The drug is administered intravenously bolyusno in a dose 111mbk for a planar stsintsigrafiya and 222mbk for OFEKT.

Beam loadings.

Beam loads of bodies and all body of the patient at intravenous administration of drug.

Bodies                     Absorbed dose of mGy/MBK

Adrenal glands                7,58×10-5

Bladder               1,4×10-3

Skeleton                      5,6×10-5

Brain                 1,00×10-5

Mammary gland              1,21×10-5

Zhyolchny bubble              1,07×10-4

Stomach                     1,2×10-4

Small intestine              4,6×10-4

Upper part of a large intestine 3,3×10-4

Lower part of a large intestine 4×10-4

Heart                     2,6×10-3

Kidneys                      8,1×10-4

Liver                     7×10-5

Lungs                     2,4×10-5

Muscles                     5,18×10-5

Ovaries                     2,1×10-4

Seed plants                  7×10-5

Pancreas         7,78×10-5

Red marrow          6×10-5

Skin                       2,03×10-5

Spleen                   7,54×10-5

Thymus            1,63×10-5

Thyroid gland           1,38×10-5

Uterus                      2,73×10-4

Effective equivalent dose 1,9×10-1 mzv/MBK.

Features of use:

Work with drug has to be carried out according to the following normative documents:

- "The basic health regulations of ensuring radiation safety" (OSPORB-99),

- "Standards of radiation safety" (NRB-99),

- SanPiN 2. 61. 1281-3,

- MU 2. 6.1. 1892 – 04.

Use at pregnancy and feeding by a breast.

Use of drug at pregnancy is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit. 

In need of use of drug in the period of a lactation it is necessary to stop breastfeeding for the term of not less than 48 hours.

Side effects:

At clinical use of drug of undesirable reactions it is not revealed.

Interaction with other medicines:

Not to use together with synthetic analogs of somatostatin. 

Data on interaction with other medicines are absent.

Contraindications:

Hypersensitivity to drug or its components.

Overdose:

At use of drug in the diagnostic purposes and control of radioactivity of indium-111 the overdose is improbable, due to the lack at drug of pharmakodinamichesky properties.

Storage conditions:

The bottle with lyophilisate in packaging is stored in the dry, protected from light place, at a temperature from 2 °C to 8 °C. The deviation from temperature condition (18-25 °C) at transportation within 1 month is allowed. 

Ready drug is stored at a temperature not above 250 °C.

Issue conditions:

According to the recipe

Packaging:

Lyophilisate for preparation of solution for intravenous administration (bottles of dark glass) of 5 ml. 

Packaging 1. 

Bottle with lyophilisate, the syringe of single use, a sterile needle, 2 spirit tampons place in a blister strip packaging. 1 blister strip packaging together with the instruction for preparation and use is placed in a cardboard pack. 

Packaging 2. 

5 bottles with lyophilisate place in a blister strip packaging. The blister strip packaging with the instruction on a medical use is placed in a cardboard pack.