Buserelin Depot - instructions for use, dose, side effects, contraindications

Active substanceBuserelinBuserelin

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Buserelin Depot

lyophilizate w / m

FARM-SYNTHESIS, CJSC Russia

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 one bottle:

Active substance: Buserelin acetate 3.93 mg

in terms of Buserelin 3.75 mg

Excipients:

DL-lactic and glycolic acid copolymer - 200 mg, Mannitol - 85 mg, carmellose sodium - 30 mg, polysorbate-80 - 2 mg.

Solvent in ampoule:

Mannitol injection 0.8%

Composition per 1 ampoule:

Mannitol - 16.0 mg,

Water for injection - up to 2 ml

Description:Lyophilized powder (brittle lyophilizate) white or white with a slight yellowish tint of color.
Solvent in ampoule:
A clear, colorless solution.
Reduced suspension:
Shake the contents of the vial to obtain a homogeneous suspension of white or white with a slight yellowish hue; the suspension should not be segregated for at least 5 minutes. When standing, the suspension precipitates, but it is easily resuspended by shaking. The suspension should be free to pass through needle No. 0804.

Pharmacotherapeutic group:An antineoplastic agent, gonadotropin-releasing hormone (GnRH) analog

ATX: & nbsp

L.02.A.E.01 Buserelin

Pharmacodynamics:Synthetic analogue of natural gonadotropin-releasing hormone (GnRH). Buserelin competitively binds to the receptors of the anterior pituitary cells, causing a short-term increase in the level of sex hormones in the blood plasma. Further use of therapeutic doses of the drug leads (on average 12-14 days) to complete blockade of the gonadotropic function of the pituitary, thus inhibiting the release of luteinizing (LH) and follicle-stimulating hormone (FSH). As a result, there is a suppression of the synthesis of sex hormones in the gonads, which is manifested by a decrease in the concentration of estradiol in the blood plasma to post-menopausal values in women and a decrease in the testosterone content to the post -astration level in men.
The concentration of testosterone in continuous treatment decreases by 2-3 weeks to the content typical for the state of orchiectomy, i.е. called pharmacological castration.

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;

Breastfeeding period;

Hypersensitivity to the components of the drug.

Pregnancy and lactation:

The drug is contraindicated in pregnant and lactating women.

Dosing and Administration:With hormone-dependent prostate cancer - 3.75 mg intramuscularly (IM) every 4 weeks;
In the treatment of endometriosis, endometrial hyperplastic processes - 3.75 mg IM once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. Duration of treatment - 4 - 6 months;
In the treatment of uterine fibroids - 3.75 mg IM once every 4 weeks.
Treatment should be started in the first five days of the menstrual cycle.Duration of treatment - before the operation 3 months, in other cases - 6 months;
In the treatment of infertility by extracorporeal fertilization (IVF) - 3.75 mg IM once at the beginning of the follicular (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21 to 24 days) of the menstrual cycle preceding stimulation. After blockade of the pituitary function, confirmed by a decrease in the serum level of estrogen in the blood serum, not less than 50% of the baseline level (usually determined 12-15 days after Buserelin-Depot injection), in the absence of ovarian cysts (according to ultrasound data), the thickness of the endometrium is not more than 5 mm, stimulation of superovulation by gonadotropic hormones under ultrasound monitoring and control of the level of estradiol in serum begins.
Rules for the preparation of suspension and drug administration
-The drug is administered only intramuscularly
- A suspension for an intravenous injection is prepared with the help of the applied solvent, just prior to administration.
-The preparation should be prepared and administered only by specially trained medical personnel.
-Wind the bottle with Buselinom-Depo strictly vertically.Tapping lightly on a vial, achieve that, all лиофилизат was on the bottom of a vial.
-Open the syringe, attach a needle with a pink pavilion (1.2 x 50 mm) to the solvent intake.
- Open the ampoule and put into the syringe all the contents of the ampoule with the solvent, install the syringe. for a dose of 2ml.
-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 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 a suspension is formed (about 3 to 5 minutes). After that, without turning the bottle, you should check the presence of dry lyophilizate at the walls and bottom of the vial. If a dry residue of the lyophilizate is found, leave the vial until it is completely soaked.
-After you are convinced of the absence of residues of dry lyophilizate, the contents of the vial should be gently stirred in a circular motion for 30-60 seconds until a uniform suspension is formed.Do not overturn or shake the bottle, this can lead to flocculation and the unfitness of the suspension.
- Quickly insert the needle through the rubber stopper into the vial. Then the cut, the needles are lowered 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 residue on the walls, and the bottom of the vial is taken into account.
- Just replace the needle with a pink pavilion on a needle with a green pavilion (0.8 x 40 mm), gently turn the syringe and remove air from the syringe.
- Suspension Buserelina-depot should be administered immediately - after preparation.
- Use an alcohol swab to disinfect the injection site. Insert the needle deep into the gluteus muscle, then gently pull the plunger of the syringe backward to make sure that there is no damage to the vessel. Insert the suspension intramuscularly slowly with constant pressure on the syringe plunger. When clogging the needle, replace it with another needle of the same diameter.
Precautions for use.
Among women
Patients with any form of depression during treatment with the drug "Buserelin-Depot" should be under the close supervision of a doctor.
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 beginning of treatment with the drug, 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.
In men
In order to effectively prevent possible side effects in the first phase of the drug's action, it is necessary to use antiandrogens two weeks before the first injection of Buserelin-Depot and for two weeks after the first injection.

Side effects:Allergic reactions: urticaria, skin hyperemia, rarely - angioedema.
From the side of the central nervous system: frequent mood swings, sleep disorders, depression, headache.
From the musculoskeletal system: at long application - demineralization of bones that is a risk of development of an osteoporosis
Among women - Headache, depression, sweating and changes in libido, dryness of the vaginal mucosa, pain in the lower abdomen, rarely - menstrual bleeding (during the first weeks of treatment).
In men, in the treatment of prostate cancer - within the first 2-3 weeks after the first injection buserelin may cause an exacerbation and progression of the underlying disease (associated with the stimulation of the synthesis of gonadotropins and, accordingly, testosterone), gynecomastia, possible "hot flashes", increased sweating and decreased potency (rarely requires a change of therapy), a transient increase in androgen concentration in the blood, urinary retention, kidney "edema - swelling of the face, eyelids, legs; 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. There have been isolated cases of development of obstruction of the ureters and compression of the spinal cord.
Other: in isolated cases (the cause-and-effect relationship is not clearly established) - pulmonary embolism, dyspepsia.

Overdose:

Currently, cases of overdose with the drug "Buserelin-Depot" were not reported.

Interaction:

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

With simultaneous application buserelin can reduce the effectiveness of hypoglycemic agents.

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:

Liofilizate for the preparation of suspension for intramuscular administration of prolonged action.

Packaging:

320,93 mg of lyophilizate containing 3.75 mg buserelin in bottles of dark glass with a capacity of 10 ml.

The vials are sealed with rubber stoppers and aluminum-plastic caps.

2 ml of solvent in neutral glass ampoules, having a tension ring or break point.

The following is placed in the contour cell package:

1 bottle with the drug;

1 ampoule with a solvent;

1 disposable syringe with a capacity of 5 ml;

1 sterile needle for injection, 0.8 mm x 40 mm in size, with a green pavilion complete with a syringe;

1 sterile solvent needle, 1.2 mm x 50 mm in size, with a pink pavilion;

2 alcohol tampons.

1, 2, 3 or 6 contour cell packs of the kit together with instructions for medical use are placed in a cardboard pack.

Storage conditions:In a dry, dark place at a temperature of 8 to 25 ° C. Keep out of the reach of children.
Special precautions for the destruction of unused medicinal product
A vial with a preparation, a syringe and needles destroy separately.

Shelf life:

Lyophilizate - 3 years.

Solvent - 5 years.

Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002378 / 01

Date of registration:11.04.2008 / 18.11.2016

Expiration Date:Unlimited

The owner of the registration certificate:FARM-SYNTHESIS, CJSC FARM-SYNTHESIS, CJSC Russia

Manufacturer: & nbsp

Company DEKO, LLC Russia

DIAMED, LLC Russia

Information update date: & nbsp13.03.2017

Illustrated instructions

Instructions

Buserelin Depot (Buserelin-depo)