Buserelin-Long

hormone-dependent prostate cancer,

breast cancer,

endometriosis (pre-and postoperative periods),

uterine fibroids,

endometrial hyperplastic processes,

infertility treatment (during the in vitro fertilization (IVF) program.

In/m.

In breast cancer and hormone-dependent prostate cancer Buserelin-long FS is administered at a dose of 3.75 mg (1 injection) in / m every 4 weeks. long - term 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 / 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 Buserelin-long FS is administered at a dose of 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 Buserelin-long FS is administered at a dose of 3.75 mg (1 injection) I / 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 Buserelin-long FS), 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

1. The drug is administered only intramuscularly.

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

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

4. The bottle with Buserelin-long FS should be held strictly vertically. Easily tapping on the bottle, ensure that all the lyophilizate is at the bottom of the bottle (Fig. 1).

Figure 1. Correct position of the drug bottle.

5. Open the syringe, attach a 1.2 x 50 mm needle to it to take the solvent.

6. Open the ampoule with solvent and fill the syringe with all the contents of the ampoule, set the syringe to a dose of 2 ml (Fig. 2, 3, 4).

Figure 2. Opening the ampoule with solvent.

Figure 3. Procedure for taking the contents of the ampoule into the syringe.

Figure 4. Rules for setting the required amount of liquid in the syringe.

7. Remove the plastic cap from the bottle containing the lyophilizate. Disinfect the rubber stopper of the bottle with an alcohol swab (Fig. 5).

Figure 5. Preparation and disinfection of the bottle cap with the drug.

8. 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 (Fig. 6).

Figure 6. Introduction of the solvent into the vial with the drug.

9. The bottle should remain stationary until the lyophilizate is completely soaked with the solvent and a suspension is formed (for about 3-5 minutes). Then, without turning the bottle, check for the presence of dry lyophilizate at the walls and bottom of the bottle. If dry residues of lyophilizate are detected, leave the bottle until completely soaked (Fig. 7).

Figure 7. Checking the presence of dry residue in the bottle.

10. After the dry lyophilizate remains have disappeared, the contents of the bottle should be carefully mixed in a circular motion for 30-60 seconds until a homogeneous suspension is formed. Do not turn or shake the bottle (Fig. 8).

Figure 8. Preparation of a homogeneous suspension (slow rotation of the bottle).

11. 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 (Fig. 9).

Figure 9. The procedure for taking the drug into the syringe.

12. 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 for the residue on the walls and bottom of the bottle is taken into account (Fig. 10).

Figure 10. The correct position of the bottle when taking the drug into the syringe.

13. Immediately after the solution set, remove the needle. Replace with a 0.8×40 mm needle, carefully turn the syringe over and remove the air from the syringe (Fig. 11).

Figure 11. Method of removing air from the syringe.

14. Buserelin-long FS suspension should be administered immediately after preparation.

15. 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 slowly, with constant pressure on the plunger of the syringe. If the needle is clogged, replace it with another needle of the same diameter.

16. For repeated injections, the left and right sides should be alternated.

hypersensitivity to the components of the drug,

pregnancy,

lactation period.

Allergic reactions: urticaria, hyperemia of the skin, rarely-angioedema.

From the central nervous system: frequent mood swings, sleep disturbances, 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).

In 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 flushes of blood to the face, increased sweating and decreased potency (rarely requires discontinuation of therapy), a transient increase in the concentration of androgens in the blood, urinary retention, renal edema-edema 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. Isolated cases of ureteral obstruction and spinal cord compression have been recorded

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

No overdose cases have been reported at this time.

Synthetic analog of endogenous 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, which later leads to a complete reversible 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. After the first administration of buserelin by the 21st day in men, the concentration of testosterone decreases to the post-castration level (characteristic of the state of orchidectomy), t.e. pharmacological castration is called. And in women, the concentration of estradiol decreases to the level corresponding to ovariectomy or postmenopause

The concentration of testosterone and estradiol remains reduced during the entire period of treatment, carried out 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.

Bioavailability is high. C_max 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 analog (GnRH) [Hormones of the hypothalamus, pituitary gland, gonadotropins and their antagonists]
• Antitumor agent, gonadotropin-releasing hormone analog (GnRH) [Antitumor hormonal agents and hormone antagonists]

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

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

In a place protected from light, at a temperature not exceeding 25 °C.

Keep out of reach of children.

lyophilizate for the preparation of a suspension for intramuscular administration of prolonged action 3.75 mg — 2 years. Solvent — 3 years.

lyophilizate for the preparation of a suspension for intramuscular administration of prolonged action 3.75 mg — 2 years. Solvent — 3 years.

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

Lyophilizate for the preparation of a suspension for intramuscular administration of prolonged action, containing 3.75 mg of buserelin. In dark glass bottles with a capacity of 10 ml. 2 ml of solvent (mannitol, 0.8% solution) in an ampoule of neutral glass.

In the contour cell packaging, place: 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, 1 sterile needle for solvent, with a size of 1.2 mm × 50 mm, 1 knife for opening ampoules or 1 scarifier, 2 alcohol wipes.

When packing the solvent in imported ampoules that have rings for opening or a break point, the ampoule scarifier or a knife for opening ampoules is not inserted. 1 the contour cell package of the kit is placed in a cardboard pack.

Contraindicated in pregnancy.

By prescription.

In women. Patients with any form of depression during treatment with the drug 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, it is recommended to exclude pregnancy and stop taking hormonal contraceptives, but during the first two months of using the drug, other (non-hormonal) methods of contraception should be used.

After discontinuation of treatment, ovarian function 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 2 weeks before the first injection of Buserelin-long FS and for 2 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.

L02AE01 Buserelin

Active substance: lyophilized powder (brittle lyophilizate) or compacted into a tablet, a porous mass of white or white with a faint yellowish tinge of color.

Solvent: clear, colorless liquid.

Reduced suspension: when the solvent is added and shaken, a homogeneous suspension of white or white with a faint yellowish tinge of color is formed, when standing, the suspension is precipitated, but easily resuspended when shaken, the suspension should pass freely into the syringe through needle No. 0840.