Components:
Treatment option:
Medically reviewed by Militian Inessa Mesropovna, PharmD. Last updated on 21.03.2022
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hormone-dependent prostate cancer,
breast cancer,
endometriosis (pre-and postoperative periods),
uterine fibroids,
endometrial hyperplastic processes,
infertility treatment (during the IVF program).
The drug is administered only in/m.
In breast cancer and hormone-dependent prostate cancer - 3.75 mg / m every 4 weeks for a long time under the supervision of a doctor.
In the treatment of endometriosis, endometrial hyperplastic processes - 3.75 mg / m 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 - 3.75 mg / m once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. The duration of treatment before surgery is 3 months, in other cases-6 months.
In the treatment of infertility by IVF - 3.75 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 preceding stimulation. After the blockade of the pituitary function, confirmed by a decrease in the concentration of estrogens in the blood serum by at least 50% from the initial level (usually determined 12-15 days after the injection of the drug 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 gonadotropins begins under ultrasound monitoring and control of the level of estradiol in the blood serum.
Rules for the preparation of suspension and administration of the drug
The drug is administered only in/m.
The suspension for intravenous injection is prepared with the supplied solvent immediately before administration.
The drug should be prepared and administered only by specially trained medical personnel.
The bottle with the drug Buserelin-depot must be kept strictly vertical. By tapping lightly on the bottle, it is necessary to ensure that all the lyophilizate is at the bottom of the bottle.
Open the syringe, attach a needle with a pink pavilion (1.2×50 mm) to it for collecting the solvent.
Open the ampoule and fill the syringe with all the contents of the ampoule with solvent, set the syringe to a dose of 2 ml.
Remove the plastic cap from the bottle containing the lyophilizate. Disinfect the rubber stopper of the bottle with an alcohol swab. Insert the needle into the bottle of lyophilizate through the center of the rubber stopper and carefully insert the solvent along the inner wall of the bottle, without touching the contents of the bottle with the needle. Remove the syringe from the bottle.
The bottle should remain stationary until the lyophilizate is completely soaked with the solvent and a suspension is formed (approximately 3-5 minutes). After that, without turning the bottle, you should check for the presence of dry lyophilizate at the walls and at the bottom of the bottle. If dry residues of lyophilizate are detected, leave the bottle until it is completely soaked.
After the medical worker has made sure that there are no dry lyophilizate residues, the contents of the bottle should be carefully mixed in circular movements for 30-60 seconds until a homogeneous suspension is formed. Do not turn or shake the bottle, as this may cause flakes to fall out and the suspension to become unusable.
Quickly insert the needle through the rubber stopper into the bottle. Then lower the needle section down and, tilting the bottle at an angle of 45°, slowly dial the suspension completely into the syringe. Do not turn the bottle over when typing. A small amount of the drug may remain on the walls and bottom of the bottle. The consumption of the residue on the walls and bottom of the bottle is taken into account.
Immediately replace the needle with a pink pavilion with a needle with a green pavilion (0.8×40 mm), carefully turn the syringe over and remove the air from the syringe.
The suspension of the drug Buserelin-depot should be administered immediately after preparation.
Use an alcohol swab to disinfect the injection site. Insert the needle deep into the gluteal muscle, then pull the plunger of the syringe slightly back to make sure that there is no damage to the vessel. Enter the suspension in / m slowly with constant pressure on the plunger of the syringe. If the needle is clogged, replace it with another needle of the same diameter.
hypersensitivity to the components of the drug,
pregnancy,
breast-feeding period.
Allergic reactions: urticaria, hyperemia of the skin, rarely-angioedema.
From the central nervous system: frequent mood changes, sleep disorders, depression, headache.
From the musculoskeletal system: with prolonged use-demineralization of bones with the risk of developing osteoporosis.
In 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).
For men, in the treatment of prostate cancer — during the first 2-3 weeks after the first injection, buserelin can cause exacerbation and progression of the underlying disease (associated with stimulating 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 the concentration of androgens in the blood, urinary retention, renal edema-swelling of the face, eyelids, legs, muscle weakness in the lower extremities. At the beginning of treatment of patients with prostate cancer, there may be 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
Other: in isolated cases (the causal relationship is not clearly established) - pulmonary embolism, dyspeptic disorders.
Currently, cases of overdose of the drug Buserelin-depo have not been reported.
A synthetic analogue of natural 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 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 content of testosterone 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.
Bioavailability is high. Cmax in plasma, it is reached approximately 2-3 hours after intravenous administration and remains at a level sufficient to inhibit the synthesis of gonadotropins by the pituitary gland for at least 4 weeks.
- Antitumor agent, gonadotropin-releasing hormone (GnRH) analog [Hormones of the hypothalamus, pituitary gland, gonadotropins and their antagonists]
- Antitumor agent, gonadotropin-releasing hormone (GnRH) analog [Antitumor hormonal agents and Hormone antagonists]
Concomitant use of the drug Buserelin-depot with drugs containing sex hormones (for example, in the mode of ovulation induction) may contribute to the occurrence of ovarian hyperstimulation syndrome.
With simultaneous use of buserelin may reduce the effectiveness of hypoglycemic agents.
In a dry place, protected from light, at a temperature of 8 to 25 °C.
Keep out of reach of children.
Shelf life of the drug Buserelin-depot3 года. Растворитель — 5 лет.Do not use after the expiration date indicated on the package.
| Lyophilizate for the preparation of a suspension for intramuscular administration of prolonged action | 1 fl. |
| active substance: | |
| buserelin acetate | 3.93 mg |
| (in terms of buserelin-3.75 mg) | |
| excipients: DL-lactic and glycolic acids copolymer-200 mg, mannitol-85 mg, carmellose sodium-30 mg, polysorbate 80-2 mg | |
| solvent (mannitol, 0.8% injection solution), composition per 1 amp.: | |
| mannitol | 16 mg |
| water for injection | up to 2 ml |
Lyophilizate for the preparation of a suspension for intramuscular administration of prolonged action. 320.93 mg of lyophilizate containing 3.75 mg of buserelin, in dark glass vials with a capacity of 10 ml. The bottles are hermetically sealed with rubber stoppers and aluminum-plastic caps. 2 ml of solvent in ampoules of neutral glass, having a tension ring or a break point.
In the contour cell packaging, 1 fl. with the drug, 1 amp. with the solvent, 1 single-use syringe, with a capacity of 5 ml, 1 sterile needle for injection, with a size of 0.8 mm × 40 mm, with a green pavilion complete with a syringe, 1 sterile needle for solvent, with a size of 1.2 mm × 50 mm, with a pink pavilion, 2 alcohol swabs.
1, 2, 3, or 6 contour cell packages of the set are placed in a cardboard pack.
The drug is contraindicated in pregnant and lactating women.
By prescription.
Precautions for use
In women. Patients with any form of depression during treatment with Buserelin-depo should be under close medical supervision.
Ovulation induction should be performed under strict medical supervision.
In the initial stage of treatment with the drug, 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, but 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 the drug Buserelin-depot and for two weeks after the first injection.
Influence on the ability to drive a car and other mechanisms. Caution should be exercised when prescribing the drug to patients engaged in potentially dangerous activities that require increased attention and speed of mental and motor reactions.
Special precautions for the disposal of unused medicinal products. The bottle with the drug, the syringe and the needles are destroyed separately.
L02AE01 Buserelin
- C50 Malignant neoplasms of the breast
- C61 Malignant neoplasm of the prostate gland
- D25 Uterine leiomyoma
- D26 Other benign neoplasms of the uterus
- N85. 0 Glandular endometrial hyperplasia
- N85. 1 Endometrial adenomatous hyperplasia
- N97 Female infertility
- Z31. 1 Artificial insemination
- Z31. 2 In vitro fertilization
Lyophilized powder (brittle lyophilizate) white or white with a faint yellowish tinge of color.
Solvent: clear, colorless solution.
Reduced suspension: shake the contents of the bottle until a homogeneous suspension of white or white with a faint yellowish tinge of color is obtained, the suspension should not be stratified for at least 5 minutes. When standing, the suspension is precipitated, but it is easily resuspended when shaken. The suspension must pass freely through needle No. 0804.
