Expiration date: 05/2025

The composition and form of issue:

Lyophilisate for preparation of suspension for intramuscular introduction of the prolonged action. 1 vial contains:

buserelina acetate 3,93 mg

in terms of buserelin — 3.75 mg 

other ingredients:dl-lactic and glycolic acids copolymer, 200 mg of d-mannitol — carmellose 85 mg of sodium and 30 mg of Polysorbate-80 — 2 mg 

solvent: mannitol, a solution of 0.8% (1 ml: d-mannitol — 8.0 mg water for injection to 1.0 ml) 

in dark glass bottles of 10 ml (complete with the solvent in vials of neutral glass 2 ml syringe 5 ml, sterile needle 0,8 x 40 mm 1.2 x 50 mm, with alcohol wipes) in the package contour cell 1 set in cardboard pack 1 pack.

Description pharmaceutical form:

Active substance: lyophilized powder (lyophilisate brittle) or compacted into a tablet of a porous mass of white or white with weak yellowish tint.

Solvent: clear, colorless liquid.

The recovered slurry: when adding solvent and shaking forms a homogeneous suspension of white or white with weak yellowish color upon standing, the slurry is deposited, but it is easy resuspendiruetsa by shaking the suspension needs to move freely in the syringe through a needle of No. 0840.

Pharmacokinetics:

The bioavailability is high. Cmax in plasma is about 2-3 h after the/m introduction and remains at a level sufficient to inhibit the synthesis of gonadotropins by the pituitary gland at least 4 weeks.

Description pharmacological action:

A synthetic analog of endogenous GnRH. Competitive buserelin binds to receptors on cells of the anterior pituitary, causing a transient increase in levels of sex hormones in blood plasma, in the future leads to reversible blockade of the gonadotropic function of the pituitary gland, inhibiting, thus, the secretion of LH and FSH. The result is a suppression of the synthesis of sex hormones in the gonads that is manifested by a decrease in the concentration of estradiol in the blood plasma to post-menopausal values in women and reduced testosterone to post-castration levels in men. After the first administration buserelina to 21 th day in men decreases testosterone concentration to post-castration levels (characteristic of the state of orchidectomy), i.e., is called pharmacological castration. And women the concentration of estradiol decreases to the level corresponding to ovariectomy or menopause.

The concentration of testosterone and estradiol remains reduced during the entire treatment period conducted every 28 days, which leads to inhibition of growth and reverse the development of hormone-dependent tumors. After stopping treatment restores the physiological secretion of hormones.

Indications:

• hormone-dependent prostate cancer
  
• breast cancer
  
• endometriosis (pre - and postoperative periods)
  
• uterine fibroids
  
• hyperplastic processes of the endometrium
  
• infertility treatment (during the in vitro fertilization (IVF).
  

Contraindications:

• hypersensitivity to the drug
  
• pregnancy
  
• lactation.
  

Application of pregnancy and breast-feeding:

Contraindicated in pregnancy.

Side effects:

Allergic reactions: urticaria, hyperemia of skin, rarely — angioedema.

CNS: frequent change of mood, sleep disturbance, depression, headache.

From the side of musculoskeletal system: long-term use — bone demineralization with risk of osteoporosis.

In women — headache, depression, sweating and change in libido, dryness of the vaginal mucosa, abdominal pain, rarely — menstrualnopodobnoe bleeding (within the first weeks of treatment).

In men, the treatment of prostate cancer — within the first 2-3 weeks after the first injection of buserelin can cause the exacerbation and progression of the underlying disease (associated with the stimulation of the synthesis of gonadotropins and, consequently, of testosterone), gynecomastia, possible tides blood to a person sweating and lower potency (rarely requires removal of therapy), 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 may experience temporary increased pain in the bones, in this case, symptomatic therapy. Reported separate cases of obstruction of the ureter and compression of the spinal cord.

Other: in single cases (causal relationship is not clearly established) — pulmonary embolism, dyspeptic disorders.

Drug interactions:

The simultaneous use of the drug Buserelin-long FS with preparations containing sex hormones (for example, the mode of induction of ovulation), may facilitate the occurrence of ovarian hyperstimulation syndrome.

While the use of Buserelin-long FS can reduce the effectiveness of gipoglikemicakih funds.

Method of application and dose:

V/m.

When hormone-dependent prostate cancer Buserelin-long FS injected I/m in a dose of 3.75 mg (1 injection) every 4 weeks.

In the treatment of endometriosis, endometrial hyperplastic processes, the drug is administered at a dose of 3.75 mg I/m once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. Duration of treatment is 4-6 months.

In the treatment of uterine fibroids Buserelin-long FS administered at a dose of 3.75 mg I/m once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. The duration of treatment before surgery 3 months, in other cases — 6 months.

In the treatment of infertility by IVF Buserelin-long FS 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 mid-luteal phase (21-24 days) of the menstrual cycle preceding stimulation. After a blockade of pituitary function, as evidenced by a decrease in the concentration of estrogens in blood serum not less than 50% of 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 more than 5 mm starts stimulation of superovulation gonadotropin hormones under ultrasound monitoring and estradiol level in serum.

Overdose:

Currently, the cases of drug overdose were reported.

Special instructions:

In women. Patients with any form of depression during treatment with the drug should be under close medical supervision.

Ovulation induction should be done under strict medical supervision.

In the initial stage of treatment may develop ovarian cyst.

Before treatment to exclude pregnancy and to stop taking a hormonal contraceptive, but during the first two months of the application it is necessary to use other (non-hormonal) methods of contraception.

After cessation of treatment, ovarian function is restored. Menstruation resumed after 3 months.

In men. For the effective prevention of possible side effects in the first phase of drug action requires the use of antiandrogens for 2 weeks prior to the first injection of Buserelin-long FS and for 2 weeks after the first injection.

Effects on ability to drive and other mechanisms. Use caution when prescribing the drug to patients engaged in potentially hazardous activities requiring increased attention and speed of mental and motor reactions.