Buserelin depot, lyophilizate 3.75mg

Pharmacodynamics

Antitumor drug, a synthetic analog of GnRH. Buserelin competitively binds to receptors of cells in the anterior pituitary lobe, causing a transient increase in plasma levels of sex hormones.

On average after 12-14 days the use of the drug in therapeutic doses leads to a complete blockade of the gonadotropic function of the pituitary gland, thus inhibiting the release of LH and FSH. As a result, suppression of sex hormone synthesis in gonads is observed, which is manifested by decrease of estradiol concentration in blood plasma to postmenopausal values in women and decrease of testosterone to post-castration level in men.

The concentration of testosterone during continuous treatment for 2-3 weeks decreases to the content characteristic of the orchiectomy state, i.e. the drug causes pharmacological castration.

Pharmacokinetics

The bioavailability is high. C_max in plasma is reached approximately 2 to 3 h after i.v. administration and remains at a level sufficient to inhibit pituitary gonadotropin synthesis for at least 4 weeks.

Indications

Hormone-dependent prostate cancer;
breast cancer;
endometriosis (pre- and postoperative periods);
uterine fibroids;
hyperplastic processes of the endometrium;
infertility treatment (during an in vitro fertilization program).

Pharmacological effect

Pharmacodynamics

Antitumor drug, synthetic analogue of 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.

On average, after 12-14 days, use of the drug in therapeutic doses leads 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 testosterone content to a post-castration level in men.

The concentration of testosterone with continuous treatment for 2-3 weeks decreases to the level characteristic of the orchiectomy state, i.e. the drug causes pharmacological castration.

Pharmacokinetics

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

Special instructions

Women

Patients with any form of depression during treatment with Buserelin-depot 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 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.

Men

In order to effectively prevent possible side effects in the first phase of the drug’s action, it is necessary to use antiandrogens 2 weeks before the first injection of Buserelin-depot and for 2 weeks after the first injection.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration

Caution should be exercised when prescribing the drug to patients engaged in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Active ingredient

Buserelin

Composition

Active ingredients:

buserelin acetate 3.93 mg, which corresponds to the content of buserelin 3.75 mg

Excipients:

copolymer of DL-lactic and glycolic acids – 200 mg,

mannitol – 85 mg,

carmellose sodium – 30 mg,

polysorbate 80 – 2 mg.

Solvent:

solution of mannitol 0.8% d/i – 2 ml.

Pregnancy

Use during pregnancy and lactation is contraindicated.

Contraindications

Pregnancy;
lactation period;
hypersensitivity to the components of the drug.

Side Effects

Allergic reactions: urticaria, skin hyperemia; rarely – angioedema.

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

From the musculoskeletal system: bone demineralization, which is a 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-like bleeding (usually during the first weeks of treatment).

In men during the treatment of prostate cancer – during the first 2-3 weeks after the first injection, exacerbation and progression of the underlying disease is possible (which is associated with stimulation of the synthesis of gonadotropins and, accordingly, testosterone), gynecomastia, possible “hot flashes”, increased sweating and decreased potency (rarely requires a change in 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. When patients with prostate cancer begin treatment, they may experience 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 noted.

Other: in isolated cases (the cause-and-effect relationship has not been clearly established) – pulmonary embolism, dyspeptic symptoms.

Interaction

The simultaneous use of 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, buserelin may reduce the effectiveness of hypoglycemic agents.

Overdose

Currently, no cases of overdose with Buserelin-depot have been reported.

Storage conditions

In a dry place, protected from light, at a temperature of 8–20 °C

Shelf life

2 years

Manufacturer

Pharm-Sintez, Russia