Buserelin-long FS - instructions for use, doses, side effects, contraindications

Active substanceBuserelinBuserelin

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Buserelin-long FS

lyophilizate w / m

NATIVA, LLC Russia

Dosage form: & nbsplyophilizate for the preparation of a suspension for intramuscular administration of prolonged action

Composition:Composition per 1 bottle:

*Active substance:*
Buserelina acetate	3.93 mg
in terms of buserelin	3.75 mg
Excipients:
DLmilk and glycolic acid copolymer	200.0 mg
D-Mannitol	85.0 mg
Carmellose sodium	30.0 mg
Polysorbate-80	2.0 mg

Solvent for suspension preparation:

Mannitol, a solution of 0.8%

Composition per ml:

D-Mannitol	8.0 mg
Water for injections	up to 1.0 ml

Description:

Lyophilized powder (brittle lyophilizate) or compressed into a tablet porous mass of white or white with a weak yellowish hue of color.

Solvent in ampoule: clear, colorless liquid.

Reduced suspension:when adding a solvent and stirring, a homogeneous suspension of white or white with a weak yellowish hue is formed; when standing, the suspension precipitates, but it is easily resuspended by shaking; the suspension must pass into the syringe freely through needle No. 0840.

Pharmacotherapeutic group:Antitumor agent - gonadotropin-releasing hormone analog

ATX: & nbsp

L.02.A.E.01 Buserelin

Pharmacodynamics:

Synthetic analogue of endogenous gonadotropin-releasing hormone (GnRH).

Buserelin competitively binds to the receptor cells of the anterior pituitary gland, causing a transient increase in levels of sex hormones in the blood plasma subsequently leads to complete reversible blockade gonadotropic pituitary function, inhibiting, thus selection luteinizing (LH) and follicle stimulating hormone (FSH). As a result of the suppression of the synthesis of sex hormones in the gonads, which is manifested decrease of estradiol concentration in blood plasma values to post-menopausal women and a reduction of testosterone to postkastratsioinogo levels in men.

After the first injection of Buserelin by 21 days in men, the concentration of testosterone decreases to the postastrational level (characteristic of the state of orchidectomy), i.e. called pharmacological castration. And in women, the concentration of estradiol is reduced to a level corresponding to ovariectomy or postmenopause.The concentration of testosterone and estradiol remains reduced throughout the treatment period, conducted every 28 days, which leads to inhibition of growth and the reverse development of hormone-dependent tumors. After discontinuation of treatment, the physiological secretion of hormones is restored.

Pharmacokinetics:

Bioavailability is high. The maximum concentration in plasma is achieved approximately 2-3 hours after intramuscular injection and remains at a level sufficient to inhibit the synthesis of gonadotropins by the pituitary gland for at least 4 weeks.

Indications:

- Hormone-dependent prostate cancer;

- mammary cancer;

- endometriosis (pre- and postoperative periods);

- myoma of the uterus;

- hyperplastic processes of the endometrium;

- treatment of infertility (when carrying out the program of in vitro fertilization (IVF)).

Contraindications:

- Pregnancy;

- lactation period;

- Hypersensitivity to the components of the drug.

Dosing and Administration:

With breast cancer and hormone-dependent prostate cancer Buserelin-long FS is administered at a dose of 3.75 mg (1 injection) intramuscularly (IM) every 4 weeks for a long time under the supervision of a doctor.

In the treatment of endometriosis, endometrial hyperplastic processes the drug is administered at a dose of 3.75 mg IM once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. The duration of treatment is 4-6 months.

In the treatment of uterine fibroids Buserelin-long FS is administered at a dose of 3.75 mg IM once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. Duration of treatment - before the operation 3 months, in the remaining cases - 6 months.

In the treatment of infertility by extracorporeal fertilization (IVF) Buserelin-long FS is administered at a dose of 3.75 mg (1 injection) IM once at the onset of folliculin (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21-24 days) of the menstrual cycle preceding stimulation. After blockade of the pituitary function, confirmed by a decrease in the concentration of estrogens in the blood serum, not less than 50% of the initial value (usually determined 12 to 15 days after Buserelin-long FS injection), in the absence of ovarian cysts (according to ultrasound), thickness of the endometrium no more than 5 mm, stimulation of superovulation by gonadotropic hormones under ultrasound monitoring and control of the concentration of estradiol in the serum begins.

Rules for the preparation of suspension and drug administration

- The drug is administered only intramuscularly

- Suspension for intravenous injection is prepared immediately before administration with the help of the applied solvent.

- The drug should be prepared and administered only by specially trained medical personnel.

- Keep the bottle with Buserelin-long FS strictly vertically. Tapping lightly on the vial, make sure that all the lyophilizate is on the bottom of the vial.

- Open the syringe, attach a 1.2 mm x 50 mm needle to the solvent intake.

- Open the ampoule with the solvent and fill the contents of the ampoule into the syringe, install the syringe on a dose of 2 ml.

- Remove the plastic cap from the vial containing the lyophilizate. Disinfect the rubber stopper of the vial with an alcohol swab. Insert the needle into the vial with the lyophilizate through the center of the rubber stopper and carefully insert the solvent into the inner wall of the vial without touching the needle with the contents of the vial. Remove the syringe from the vial.

- The bottle must remain stationary until the solvent is completely saturated with the lyophilizate and the suspension is formed (about 3 to 5 minutes). After that, without turning the bottle, check the presence of dry lyophilizate at the walls and the bottom of the vial.If there are any dry residues of the lyophilizate, leave the vial until it is completely soaked.

- After you are convinced of the absence of residues of dry lyophilizate, carefully mix the contents of the vial in a circular motion for 30-60 seconds until a uniform suspension is formed. Do not overturn or shake the bottle.

- Quickly insert the needle through the rubber stopper into the vial. Then cut the needle cut down and, tilting the vial at an angle of 45 degrees, slowly put the suspension in the syringe completely. Do not flip the bottle when typing.

A small amount of the drug can remain on the walls and bottom of the vial. The consumption of the residue on the walls and the bottom of the vial is taken into account.

Immediately after the solution is removed, remove the needle. Replace with a 0.8 mm x 40 mm needle, gently flip the syringe and remove air from the syringe.

- Suspension Buserelin-long FS is administered immediately after preparation.

- Use an alcohol swab to disinfect the injection site.

Insert the needle deep into the gluteus muscle, then slightly 1 pull the syringe plunger backward to make sure that there is no damage to the vessel.

Insert the suspension slowly with constant pressure on the syringe plunger.

When clogging the needle, replace it with another needle of the same diameter.

- With repeated injections, the left and right sides should alternate.

Side effects:

Adverse reactions recorded more often than single observations are listed below for organs and systems, indicating the frequency of their occurrence.

The frequency of adverse reactions that may occur during therapy is given in the following gradation: very often (≥10%), often (≥1% and <10%), infrequently (≥0.1% and <1%), rarely (≥0.01% and <0.1%), very rarely (<0.01%), frequency unknown (individual reports of undesirable phenomena, in which setting the frequency is not always possible).

For men and women:

Disorders of the psyche: often - a frequent change of mood, depression.

Impaired nervous system: Often - sleep disorders, headache.

Vascular disorders: Often - "tides".

Disturbances from the skin and subcutaneous tissues: often - urticaria, skin hyperemia; rarely - angioedema.

Disturbances from the musculoskeletal and connective tissue: frequency unknown - with long-term use - demineralization of bones, which is a risk of osteoporosis.

Among women:

Heart Disease: often - palpitation.

Disorders from the liver and bile ducts: frequency unknown - increased activity of alanine aminotransferase in blood plasma, increased activity of aspartate aminotransferase in blood plasma.

Disturbances from the skin and subcutaneous tissues: infrequently - increased sweating.

Disturbances from the musculoskeletal and connective tissue: often - unpleasant sensations in the joints.

Violations of the genitals and breast: Often - changes in libido, dryness of the vaginal mucosa, menstrual bleeding (during the first weeks of treatment); often - pain in the lower abdomen.

In men, in the treatment of prostate cancer: during the first 2-3 weeks after the first injection buserelin can cause an exacerbation and progression of the underlying disease (associated with the stimulation of the synthesis of gonadotropins and, accordingly, testosterone), a transient increase in the concentration of androgens in the blood.

Violations from the blood and lymphatic system: in isolated cases (the cause-and-effect relationship is not clearly established) - pulmonary embolism.

Disorders from the gastrointestinal tract: in isolated cases (the cause-and-effect relationship is not clearly established) - dyspeptic disorders.

Disturbances from the skin and subcutaneous tissues: frequency unknown - increased sweating.

Disturbances from the musculoskeletal and connective tissue: frequency unknown - muscle weakness in the lower limbs. At the beginning of treatment for patients with prostate cancer, temporary pain in the bones may develop temporarily; In this case, symptomatic therapy should be performed.

Disorders from the kidneys and urinary tract: infrequently - delay urination. There have been isolated cases of development of obstruction of the ureters and compression of the spinal cord.

Violations of the genitals and mammary gland: Often - decreased potency (rarely requires withdrawal of therapy), often - gynecomastia.

General disorders and disorders at the site of administration: often - "Renal edema" - swelling of the face, eyelids, legs.

Overdose:

At present, no cases of overdose have been reported.

Interaction:

Simultaneous use of the drug "Buserelin-long FS" with drugs containing sex hormones (for example,in the induction of ovulation), may contribute to the emergence of the ovarian hyperstimulation syndrome.

With the simultaneous use of Buserelin-long FS may reduce the effectiveness of hypoglycemic agents.

Special instructions:

Among women

Patients with any form of depression during drug treatment should be under close medical supervision.

Induction of ovulation should be carried out under strict medical supervision.

In the initial stage of treatment with the drug, the development of ovarian cysts is possible.

Before the start of treatment it is recommended to exclude pregnancy and stop taking hormonal contraceptives, however, during the first two months of using the drug, it is necessary to use other (non-hormonal) methods of contraception.

After cessation of treatment, the function of the ovaries is restored. The first menstruation resumes after 3 months.

In men

In order to effectively prevent possible side effects in the first phase of the drug, it is necessary to use antiandrogens two weeks before the first injection of Buserelin-long FS and for two weeks after the first injection.

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

Caution should be exercised in prescribing patients to potentially dangerous activities requiring increased attention and speed of mental and motor reactions.

Form release / dosage:

Lyophilizate for the preparation of a suspension for intramuscular administration of prolonged action, 3.75 mg.

Packaging:

Lyophilizate containing 3.75 mg buserelin, in bottles of dark glass with a capacity of 10 ml. For 2 ml of solvent (mannitol injection 0.8%) into ampoules of neutral glass.

When manufacturing on "Nativa", Russia:

The following is placed in the contour cell package:

1 a vial or flask with a preparation;

1 ampoule with solvent;

1 disposable syringe with a capacity of 5 ml, packed in an individual contour mesh package;

1 sterile injection needle, 0.8 mm x 40 mm in size packed in a contour mesh package complete with a syringe;

1 sterile solvent needle, 1.2 mm x 50 mm, packed in a contour mesh package;

1 a knife for opening ampoules or 1 scarifier;

2 alcohol wipes, packed in individual packaging.

When you pack the solvent in imported ampoules that have rings for opening or a break point, the ampoule scapegrator or the opener for opening the ampoules is not put.

1 or 2 contour mesh packages together with the instruction for use are placed in a cardboard pack.

Or, when manufacturing at Pharmstandard-UfaVITA, Russia:

The following is placed in the contour cell package:

1 bottle with the drug;

1 ampoule with solvent;

1 disposable syringe,

with a capacity of 5 ml, complete with 1 sterile injection needle, 0.8 mm x 40 mm, packed in a contoured package;

1 a sterile solvent needle, 1.2 mm x 50 mm in size, packed in an individual contoured package;

2 alcohol wipes packed in individual packaging.

1 or 2 contour mesh packages together with the instruction for use are placed in a cardboard pack.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.