Instruction for use: Buserelin-depo

ATX Code L02AE01 Buserelin

Pharmacological group

Antitumor agent, gonadotropin-releasing hormone analog (GnRH) [Hormones of the hypothalamus, pituitary gland, gonadotropins and their antagonists]

Antineoplastic agent, gonadotropin-releasing hormone analog (GnRH) [Antitumor hormonal agents and hormone antagonists]

Nosological classification (ICD-10)

C50 Malignant neoplasm of breast

Cancer of the nipple and areola of the breast, Breast carcinoma, The hormone-dependent form of recurrent breast cancer in women in menopause, Hormone-dependent breast cancer, Disseminated breast carcinoma, Disseminated Breast Cancer, Malignant breast cancer, Malignant neoplasm of breast, Contralateral breast cancer, Locally advanced or metastatic breast cancer,Locally-distributed breast cancer, Locally-recurring breast cancer, Metastatic breast carcinoma, Metastasis of breast tumors, Metastatic breast carcinoma, Inoperable breast carcinoma, Incompatible breast cancer, Breast cancer in women with metastases, Breast cancer in men with metastases, Breast Cancer, Breast cancer in men, Mammary cancer, Breast cancer with distant metastases, Breast cancer in postmenopausal women, Breast cancer hormone-dependent, Breast cancer with local metastases, Breast cancer with metastases, Breast cancer with regional metastases,Breast cancer with metastases, Common hormone-dependent forms of breast cancer, Common Breast Cancer, Recurrent Breast Cancer, Recurrence of breast tumors, Breast cancer, Estrogen-dependent breast cancer, Estrogen-Dependent Breast Cancer, Disseminated breast cancer with overexpression of HER2, Tumors of the mammary glands

C61 Malignant neoplasm of prostate

Adenocarcinoma of the prostate, Hormone-dependent prostate cancer, Hormone-Resistant Prostate Cancer, Malignant tumor of prostate, Malignant neoplasm of prostate, Carcinoma of the prostate, Locally-distributed non-metastatic prostate cancer, Locally advanced prostate cancer, Locally spread prostate cancer, Metastatic prostatic carcinoma, Metastatic prostate cancer, Metastatic hormone-resistant prostate cancer, Non-metastatic prostate cancer, Incompatible prostate cancer, Prostate Cancer, Prostate cancer, Common prostate cancer, Testosterone-Depot Prostate Cancer

D25 Leiomyoma of the uterus

Fibroids of the uterus

D26 Other benign neoplasms of the uterus

Fibromyoma of the uterus, Myoma, Uterine fibroids, Fibromyoma, Myoma of the uterus, Fibrrios, Meigs syndrome, Tumors of the uterus

N85.0 Endometrial glandular hyperplasia

Hyperplastic processes of the endometrium, Cystic glandular hyperplasia of the endometrium

N85.1 Adenomatous endometrial hyperplasia

N97 Female infertility

Female infertility in anovulation, Hyperprolactinemic infertility, Hyperprolactinaemia with infertility, Endocrine infertility, Infertility due to hypothalamic-pituitary dysfunction, Infertility infertility, Infertility, Infertility on the background of hyperprolactinaemia, Functional infertility, Marriage is infertile, Infertility of ovarian genesis, Stimulation of the growth of a single follicle

N31.1 Reflex neuropathic bladder, not elsewhere classified

hyperreflexia, Overactive Bladder, detrusor hyperreflexia, detrusor hyperreflexia

N31.2 neurogenic bladder weakness, not elsewhere classified

Urinary incontinence in a stressful situation, Atony of bladder, Atony of the bladder (the sphincter) (neurogenic), Impaired function of the sphincter of the bladder, Neurogenic bladder disorders, Neurogenic bladder disorder, Neurogenic bladder, Functional insufficiency of the sphincter of the bladder, Imperative incontinence

Composition

Liofilizate for the preparation of a suspension for intramuscular administration of prolonged action 1 fl.

active substance:

Buserelina acetate 3.93 mg

(In terms of Buserelin - 3.75 mg)

Auxiliary substances: DL-lactic and glycolic acid copolymer - 200 mg; Mannitol - 85 mg; Carmellose sodium - 30 mg; Polysorbate 80 - 2 mg

Solvent (mannitol, solution for injection 0.8%), composition at 1 amp:

Mannitol 16 mg

Water for injection up to 2 ml

Description of dosage form

Lyophilized powder (brittle lyophilizate) white or white with a slight yellowish tint of color.

Solvent: Clear colorless solution.

Restored 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 separate for at least 5 minutes. When standing, the suspension precipitates, but it is easily resuspended by shaking. The suspension must pass through the needle # 084 freely.

pharmachologic effect

Pharmacological action - antiandrogenic, antitumor, antigonadotropic, antiestrogenic.

Pharmacodynamics

Synthetic analogue of natural 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 gland, thus inhibiting the release of LH and 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 with continuous treatment for 2-3 weeks decreases to a content characteristic of the state of orchiectomy, i.e. Called pharmacological castration.

Pharmacokinetics

Bioavailability is high. Cmax in the plasma is achieved approximately 2-3 hours after the / m administration and is maintained at a level sufficient to inhibit the synthesis of gonadotropins by the pituitary for at least 4 weeks.

indications

Hormone-dependent prostate cancer;

mammary cancer;

Endometriosis (pre- and postoperative periods);

Uterine myoma;

Hyperplastic processes of the endometrium;

Treatment of infertility (during the IVF program).

Contraindications

Hypersensitivity to the components of the drug;

pregnancy;

Period of lactation.

pregnancy and lactation

The drug is contraindicated in pregnant and lactating women.

Side effects

Allergic reactions: urticaria, skin hyperemia; Rarely - angioedema.

From the side of the central nervous system: frequent mood changes, sleep disturbances, depression, headache.

From the musculoskeletal system: with prolonged use - demineralization of bones with the risk of osteoporosis.

Women - headache, depression, sweating and changes in libido, dryness of the vaginal mucosa, pain in the lower abdomen, rarely - menstrual like 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 the stimulation of the synthesis of gonadotropins and testosterone, respectively), gynecomastia, tides, increased sweating and decreased potency (Rarely requires a change of therapy), a transient increase in the concentration of androgens in the blood, urinary retention, renal edema - swelling of the face, eyelids, legs; Muscle weakness in the lower limbs. At the beginning of treatment of patients with prostate cancer, temporary pain in the bones may develop temporarily; In this case, symptomatic therapy should be performed. Some cases of development of obstruction of the ureters and compression of the spinal cord were noted.

Other: in isolated cases (the cause-and-effect relationship is not clearly established) - pulmonary embolism, dyspeptic disorders.

Interaction

The simultaneous use of Busherelin Depo with preparations containing sex hormones (for example, in the induction of ovulation) may contribute to the emergence of the ovarian hyperstimulation syndrome.

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

Dosing and Administration

The drug is administered only in / m.

In breast cancer and hormone-dependent prostate cancer - 3.75 mg IM every 4 weeks.

In the treatment of endometriosis, endometrial hyperplastic processes are 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.

When treating uterine fibroids - 3.75 mg IM once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. The duration of treatment before the operation is 3 months, in the remaining cases - 6 months.

In the treatment of infertility by IVF, 3.75 mg 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 serum estrogen concentration by at least 50% of the baseline (usually determined 12-15 days after injection of Buserelin-Depot), in the absence of ovarian cysts (according to ultrasound data), the thickness of the endometrium is not More than 5 mm, stimulation of superovulation with gonadotropic hormones begins under ultrasound monitoring and control of the level of estradiol in serum.

Rules for preparation of suspension and drug administration

The drug is administered only in / m.

The suspension for the intravenous injection is prepared using the supplied solvent immediately before administration.

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

The bottle with the drug Busherelin Depo must be kept strictly vertically. Tapping lightly on a vial, it is necessary to achieve, that all ëèîôèëèçàò was on the bottom of a vial.

Open the syringe, attach a needle with a pink pavilion (1.2 × 50 mm) to it to take the solvent.

Open the ampoule and draw into the syringe all the contents of the ampoule with the solvent, install the syringe to a dose of 2 ml.

Remove the plastic cap from the vial containing the lyophilizate. Disinfect the rubber stopper of the bottle with an alcohol swab. Insert the needle into the vial with lyophilizate through the center of the rubber stopper and gently 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 3-5 minutes). After that, without turning the bottle, you should check the presence of dry lyophilizate at the walls and at the bottom of the vial. If a dry residue of the lyophilizate is found, leave the vial until it is completely soaked.

After the health worker is 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 and shake the bottle, this can lead to flocculation and unsuitability of the suspension.

Quickly insert the needle through the rubber stopper into the vial. Then cut the needle cut down and, tilting the bottle at an angle of 45 °, slowly fill 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.

Immediately replace the needle with a pink pavilion on a needle with a green pavilion (0.8 × 40 mm), gently turn the syringe and remove air from the syringe.

Suspension of the drug Buserelin Depot should be administered immediately after preparation.

Using an alcohol tampon, disinfect the injection site. Insert the needle deep into the gluteus muscle, then slightly pull the syringe plunger backward to make sure that there is no damage to the vessel. Introduce the suspension in / m slowly with constant pressure on the syringe plunger. When clogging the needle, replace it with another needle of the same diameter.

Overdose

At present, no cases of an overdose of Busherelin Depo have been reported.

special instructions

Precautions for use

Among women. Patients with any form of depression during the treatment with Buselelin Depot 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 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, it is necessary to use antiandrogens two weeks before the first injection of Buserelin Depot and for two weeks after the first injection.

Effect on the ability to drive and other mechanisms. Caution should be exercised when prescribing the drug to patients engaged in potentially hazardous activities requiring increased attention and speed of mental and motor reactions.

Special precautions for the destruction of unused medicinal product. A vial with a preparation, a syringe and needles destroy separately.

Form of issue

Lyophilizate for the preparation of suspension for intramuscular administration of prolonged action. 320,93 mg of lyophilizate containing 3.75 mg buserelin, in dark glass bottles with a capacity of 10 ml. The vials are sealed with rubber stoppers and aluminum-plastic caps. For 2 ml of solvent in ampoules of neutral glass, having a tension ring or a break point.

In the contour cell pack, put 1 fl. With the drug; 1 amp. With a solvent; 1 disposable syringe with a capacity of 5 ml; 1 sterile injection needle, 0.8 mm × 40 mm in size, with a green pavilion complete with a syringe; 1 sterile solvent needle, 1.2 mm × 50 mm in size, with a pink pavilion; 2 alcohol tampons.

1, 2, 3, or 6 contour mesh packages of the kit are placed in a cardboard pack.

Terms of leave from pharmacies

On prescription.

storage Conditions

In a dry, the dark place at a temperature of 8 to 25 ° C.

Keep out of the reach of children.

Shelf life

3 years. Solvent - 5 years.

Do not use after the expiry date printed on the package.