Expiration date: 10/2026

The composition and form of issue:

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

buserelina acetate (in the form of a free peptide) 3.75 mg

auxiliary substances: copolymer of DL-lactic and glycolic acids — 200 mg D-mannitol — 85 mg carboxymethylcellulose sodium and 30 mg of Polysorbate-80 — 2 mg 

the solvent in the vial: D-mannitol — 16 mg water for injection 2 ml 

in the paper cartons 1 a bottle complete with the solvent in an ampoule 2 ml disposable syringe and 2 needles.

Description pharmaceutical form:

Dried powder white or with a faint yellowish tint.

The solvent in ampoule — colorless transparent liquid.

Feature:

A synthetic analogue of natural gonadotropin-releasing hormone.

Pharmacokinetics:

The bioavailability is high. After the/m introduction Cmax in plasma is approximately 2-3 hours and is maintained at a level sufficient to inhibit the synthesis of gonadotropins by the pituitary gland, at least 4 weeks.

Description pharmacological action:

Competitive binds to receptors on cells of the anterior pituitary, causing a transient increase in levels of sex hormones in the blood plasma. Further, the use of therapeutic dosages (average 12-14 days) to a full blockade of the gonadotropic function of the pituitary gland, thus inhibiting the secretion of LH and FSH. This eventually suppresses 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.

The concentration of testosterone during continuous treatment for 2-3 weeks is reduced to content, specific to the state of blindness, i.e., is called pharmacological castration.

Indications:

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

Contraindications:

• hypersensitivity to the drug
  
• pregnancy
  
• breast-feeding.
  

Application of pregnancy and breast-feeding:

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Side effects:

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

Women — typical symptoms hypoestrogenic state ("pharmacological climax"):

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

From the endocrine system: tides, sweating, vaginal dryness, reduced libido, lower abdominal pain, demineralization of the bones, rarely menstrualnopodobnoe bleeding (usually within the first weeks of treatment).

Men: in the treatment of prostate cancer, during the first 2-3 weeks after the first injection, you may develop fever and progression of the underlying disease, which is associated with the stimulation of the synthesis of gonadotropins and testosterone and gynecomastia, a transient increase in the concentration of androgens in the blood rarely, ossalgia, urinary retention, renal edema, muscle weakness in the lower extremities, lymphedema.

Other: in individual cases, a pulmonary embolism, diarrhoea events (causality not clearly established).

Drug interactions:

The simultaneous use with other drugs containing sex hormones (for example, the mode of induction of ovulation), may facilitate the occurrence of ovarian hyperstimulation syndrome.

While the use of buserelin can reduce the effectiveness of gipoglikemicakih funds.

Method of application and dose:

V/m.

Hormone-dependent prostate cancer 3.75 mg every 4 weeks.

Endometriosis, endometrial hyperplasia — 3.75 mg 1 every 4 weeks. Treatment should begin during the first 5 days of the menstrual cycle. The duration of treatment is 4-6 months.

Uterine fibroids — 3.75 mg 1 every 4 weeks. Treatment should begin during the first 5 days of the menstrual cycle. The duration of treatment before surgery is 3 months, in other cases — 6 months.

Treatment of infertility by in vitro fertilization — a 3.75 mg dose on the 2nd day of the menstrual cycle.

Rules for the preparation of the slurry and drug administration

The drug is introduced only to/m Suspension for the/m injection prepared with supplied solvent immediately before administration. The fence of the solvent from the vial and transfer it into the vial is carried out using the supplied needle with the pink pavilion (1,2×50 mm). The vial is gently shaken to obtain a homogeneous suspension. Suspension fully climbs into the syringe without inverting the vial. Needle with pink pavilion is replaced by a needle with a green pavilion (0,8×40 mm) and immediately done in/m injection.

Overdose:

Currently, the cases of drug overdose with the drug Buserelin-depo was not reported.

Precautions:

Use caution when prescribing the drug to patients engaged in potentially hazardous activities requiring increased attention and speed of mental and motor reactions.

Special instructions:

Women

Patients with any form of depression during treatment 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 the start of treatment is recommended to exclude the presence of pregnancy and to stop taking hormonal contraceptives, but within the first 2 months of use it is necessary to use other (non-hormonal) methods of contraception.

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 and for 2 weeks after it.