Buserelin-Depo lyophilisate for preparation of suspension for injection 3.75mg, No. 1 + solvent, syringe, needle

• Hormone-dependent prostate cancer;

• Mammary cancer;

• Endometriosis (pre- and postoperative periods);

• Myoma of the uterus;

• Endometrial hyperplastic processes;

• Infertility treatment (when conducting an in vitro fertilization (IVF) program.

With hormone-dependent prostate cancer - 375 mg intramuscularly (IM) every 4 weeks;

In the treatment of endometriosis, hyperplastic processes of the endometrium - 375 mg / m once every 4 weeks. Treatment should be started in the first five days of the menstrual cycle. Duration of treatment - 4 - 6 months;

In the treatment of uterine fibroids - 375 mg / m once every 4 weeks.
Treatment should be started in the first five days of the menstrual cycle. Duration of treatment - 3 months before surgery, in other cases - 6 months;

In the treatment of infertility by in vitro fertilization (IVF) - 375 mg / m once at the beginning of the follicular (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21-24 days) of the menstrual cycle prior to stimulation. After blockade of the pituitary function, confirmed by a decrease in the concentration of estrogen in the blood serum by at least 50% of the initial level (usually determined 12-15 days after injection of Buserelin - depot) in the absence of ovarian cysts (according to ultrasound), the thickness of the endometrium is not more than 5 mm. stimulation of superovulation with gonadotropic hormones under ultrasound monitoring and control of the level of estradiol in the blood serum.

Rules for the preparation of the suspension and administration of the drug
- The drug is injected only intramuscularly - The
suspension for intramuscular injection is prepared using the supplied solvent immediately before administration.
-The drug should be prepared and administered only by specially trained medical personnel.
- Hold the bottle with Buserelin-Depot strictly vertically. By tapping lightly on the bottle, make sure that all the lyophilisate is at the bottom of the bottle.
-Open the syringe and attach a needle with a pink pavilion (12 x 50 mm) to it to collect the solvent.
-Open the ampoule and draw the entire contents of the solvent ampoule into the syringe and install the syringe. for a dose of 2 ml.
-Remove the plastic cap from the vial containing the lyophilisate. Disinfect the rubber stopper of the vial with an alcohol swab. Insert the needle into the vial with lyophilisate through the center of the rubber stopper and carefully inject the solvent along the inner wall of the vial without touching the contents of the vial with the needle. Remove the syringe from the vial.
-The vial should remain stationary until the lyophilisate is completely saturated with the solvent and a suspension is formed (about 3 - 5 minutes). After that, without turning the bottle over, check for the presence of dry lyophilisate at the walls and bottom of the bottle. If dry residues of the lyophilisate are found, leave the vial until it is completely saturated.
-After you have made sure that there are no residues of dry lyophilisate, the contents of the vial should be gently mixed in circular movements for 30-60 seconds until a homogeneous suspension is formed. Do not turn or shake the bottle as this can lead to flocculation and unsuitable suspension.
-Quickly insert the needle through the rubber stopper into the vial. Then the cut of the needle is lowered and by tilting the bottle at an angle of 45 degrees, slowly draw the suspension completely into the syringe. Do not overturn the bottle while dialing. A small amount of the drug may remain on the sides and bottom of the bottle. The consumption of the remainder on the walls and bottom of the bottle is taken into account.
-Immediately replace the pink pavilion needle with the green pavilion needle (08 x 40 mm) gently turn the syringe over and remove the air from the syringe.
-A suspension of Buserelin-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 pull the syringe plunger back slightly to make sure there is no damage to the vessel. Enter the suspension intramuscularly slowly with constant pressure on the syringe plunger. If the needles are clogged, replace it with another needle of the same diameter.

Precautions for use.

In women
Patients with any form of depression during the period of treatment with Buserelin-depot should be under close medical supervision.
Ovulation induction should be performed under strict medical supervision.
In the initial stage of drug treatment, the development of an ovarian cyst is possible.
Before starting 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.

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, sodium carmellose - 30 mg, polysorbate-80 - 2 mg.

Solvent in ampoule:

Mannitol injection 0.8%

Composition for 1 ampoule:

Mannitol - 16.0 mg,

Water for injection - up to 2 ml

• Pregnancy;

• Breastfeeding period;

• Hypersensitivity to the components of the drug.

Trade name of the drug

Buserelin-depot

International non-proprietary name

Buserelin

Dosage form

lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action

Composition

Composition for 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, sodium carmellose - 30 mg, polysorbate-80 - 2 mg.

Solvent in ampoule:

Mannitol injection 0.8%

Composition for 1 ampoule:

Mannitol - 16.0 mg,

Water for injection - up to 2 ml

Description

Lyophilized powder (brittle lyophilisate) of white or white color with a slight yellowish sheen.
Solvent in ampoule:
Clear, colorless solution.
Reconstituted suspension:
Shake the contents of the vial until a homogeneous suspension of white or white with a faint yellowish tinge is obtained; the suspension should not delaminate for at least 5 minutes. On standing, the suspension settles, but easily resuspended with shaking. The suspension must pass freely through the # 0804 needle.

Pharmacotherapeutic group

Antineoplastic agent, gonadotropin-releasing hormone (GnRH) analog

ATX code

L02AE01

Pharmacodynamics:

A synthetic analogue of natural gonadotropin-releasing hormone (GnRH). Buserelin competitively binds to the receptors of the cells of the anterior pituitary gland, 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 after 12-14 days) to a complete blockade of the gonadotropic function of the pituitary gland, 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 postmenopausal values ??in women and a decrease in testosterone content to the post-castration level in men.
The concentration of testosterone with continuous treatment for 2-3 weeks decreases to the content characteristic of the state of orchiectomy, i.e. pharmacological castration is caused.

Pharmacokinetics:

Bioavailability is high. The maximum plasma concentration is reached approximately 2-3 hours after intramuscular administration 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;

• Endometrial hyperplastic processes;

• Infertility treatment (when conducting an in vitro fertilization (IVF) program.

Contraindications:

• Pregnancy;

• Breastfeeding period;

• Hypersensitivity to the components of the drug.

Pregnancy and lactation:

The drug is contraindicated in pregnant and lactating women.

Method of administration and dosage:

With hormone-dependent prostate cancer - 375 mg intramuscularly (IM) every 4 weeks;

In the treatment of endometriosis, hyperplastic processes of the endometrium - 375 mg / m once every 4 weeks. Treatment should be started in the first five days of the menstrual cycle. Duration of treatment - 4 - 6 months;

In the treatment of uterine fibroids - 375 mg / m once every 4 weeks.
Treatment should be started in the first five days of the menstrual cycle. Duration of treatment - 3 months before surgery, in other cases - 6 months;

In the treatment of infertility by in vitro fertilization (IVF) - 375 mg / m once at the beginning of the follicular (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21-24 days) of the menstrual cycle prior to stimulation. After blockade of the pituitary function, confirmed by a decrease in the concentration of estrogen in the blood serum by at least 50% of the initial level (usually determined 12-15 days after injection of Buserelin - depot) in the absence of ovarian cysts (according to ultrasound), the thickness of the endometrium is not more than 5 mm. stimulation of superovulation with gonadotropic hormones under ultrasound monitoring and control of the level of estradiol in the blood serum.

Rules for the preparation of the suspension and administration of the drug
- The drug is injected only intramuscularly - The
suspension for intramuscular injection is prepared using the supplied solvent immediately before administration.
-The drug should be prepared and administered only by specially trained medical personnel.
- Hold the bottle with Buserelin-Depot strictly vertically. By tapping lightly on the bottle, make sure that all the lyophilisate is at the bottom of the bottle.
-Open the syringe and attach a needle with a pink pavilion (12 x 50 mm) to it to collect the solvent.
-Open the ampoule and draw the entire contents of the solvent ampoule into the syringe and install the syringe. for a dose of 2 ml.
-Remove the plastic cap from the vial containing the lyophilisate. Disinfect the rubber stopper of the vial with an alcohol swab. Insert the needle into the vial with lyophilisate through the center of the rubber stopper and carefully inject the solvent along the inner wall of the vial without touching the contents of the vial with the needle. Remove the syringe from the vial.
-The vial should remain stationary until the lyophilisate is completely saturated with the solvent and a suspension is formed (about 3 - 5 minutes). After that, without turning the bottle over, check for the presence of dry lyophilisate at the walls and bottom of the bottle. If dry residues of the lyophilisate are found, leave the vial until it is completely saturated.
-After you have made sure that there are no residues of dry lyophilisate, the contents of the vial should be gently mixed in circular movements for 30-60 seconds until a homogeneous suspension is formed. Do not turn or shake the bottle as this can lead to flocculation and unsuitable suspension.
-Quickly insert the needle through the rubber stopper into the vial. Then the cut of the needle is lowered and by tilting the bottle at an angle of 45 degrees, slowly draw the suspension completely into the syringe. Do not overturn the bottle while dialing. A small amount of the drug may remain on the sides and bottom of the bottle. The consumption of the remainder on the walls and bottom of the bottle is taken into account.
-Immediately replace the pink pavilion needle with the green pavilion needle (08 x 40 mm) gently turn the syringe over and remove the air from the syringe.
-A suspension of Buserelin-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 pull the syringe plunger back slightly to make sure there is no damage to the vessel. Enter the suspension intramuscularly slowly with constant pressure on the syringe plunger. If the needles are clogged, replace it with another needle of the same diameter.

Precautions for use.

In women
Patients with any form of depression during the period of treatment with Buserelin-depot should be under close medical supervision.
Ovulation induction should be performed under strict medical supervision.
In the initial stage of drug treatment, the development of an ovarian cyst is possible.
Before starting 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, flushing of the skin, rarely - angioedema.
From the side of the central nervous system: frequent mood swings; sleep disorders; depression; headache.
On the part of the musculoskeletal system: with prolonged use - demineralization of bones, which is a risk of osteoporosis
In women - headache depression sweating and changes in libido dryness of the vaginal mucosa lower abdominal pain rarely - menstrual bleeding (during the first weeks of treatment).
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 stimulation of the synthesis of gonadotropins and, accordingly, testosterone) gynecomastia; blood urinary retention 'renal' edema - edema of the face of the eyelids of the legs; muscle weakness in the lower limbs. At the beginning of treatment, patients with prostate cancer may experience a temporary increase in bone pain; in this case, symptomatic therapy should be carried out. There were isolated cases of ureteral obstruction and spinal cord compression.
Others:in isolated cases (the causal relationship is not clearly established) - pulmonary embolism, dyspeptic disorders.

Overdose:

Currently, no cases of overdose with Buserelin-depot have been reported.

Interaction:

The simultaneous use of the drug 'Buserelin-depot' with drugs containing sex hormones (for example, in the ovulation induction mode) may contribute to the occurrence of ovarian hyperstimulation syndrome.

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

Impact on the ability to drive vehicles. Wed and fur .:

Care should be taken when prescribing the drug to patients engaged in potentially hazardous activities requiring increased attention and speed of mental and motor reactions.

Release form / dosage:

Lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action.

Packaging:

32093 mg of lyophilisate containing 375 mg of buserelin in dark glass vials with a capacity of 10 ml.

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

2 ml of solvent in neutral glass ampoules with a tension ring or breaking point.

Place in a blister strip:

1 bottle with the drug;

1 ampoule with solvent;

1 disposable syringe with a capacity of 5 ml;

1 sterile injection needle measuring 08 mm x 40 mm with a green pavilion, complete with a syringe;

1 sterile solvent needle 12 mm x 50 mm with pink pavilion;

2 alcohol swabs.

1 2 3 or 6 blisters of the kit together with instructions for medical use are placed in a cardboard box.

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 disposal of unused medicinal product Dispose of the
syringe and needles separately.

Shelf life:

Lyophilisate - 3 years.

Solvent - 5 years.

Do not use after the expiration date indicated on the package.

Vacation conditions

On prescription.