Buserelin - Long lyophilisate for preparation of suspension for i / m administration 3.75mg, No. 1

Buserelin - Long lyophilisate for preparation of suspension for i / m administration 3.75mg, No. 1; 'Hormone-dependent prostate cancer, breast cancer, endometriosis (pre- and postoperative periods), uterine fibroids, endometrial hyperplastic processes, treatment of infertility (when conducting an in vitro fertilization program).

Individual, depending on the indications and treatment regimen.

buserelin acetate (as free peptide)

Pregnancy, lactation, hypersensitivity to buserelin.

pharmachologic effect

Synthetic analogue of natural GnRH. Buserelin competitively binds to the receptors of the cells of the anterior lobe of the g and pophysis, causing a short-term increase in the level of sex hormones in the blood plasma. Application in therapeutic doses for 12-14 days leads to a complete blockade of the gonadotropic function of the pituitary gland, thus inhibiting the release of LH and FSH. As a result, the synthesis of sex hormones is suppressed, which is manifested by a decrease in the concentration of estradiol in the blood plasma to postmenopausal values ??in women and a decrease in testosterone content to the post-castration level in men. The concentration of testosterone with continuous use of buserelin for 14-21 days decreases to the level characteristic of the state of orchiectomy, i.e. causes pharmacological castration.

Pharmacokinetics

After subcutaneous administration, buserelin is completely absorbed from the gastrointestinal tract, in plasma it is observed 1 hour after administration. It accumulates in the liver, kidneys, and also in the anterior lobe of the pituitary gland. Metabolized by tissue peptidases. It is excreted in the urine and bile unchanged and in the form of metabolites. T1 / 2 is about 80 min.

Side effect

Possibly: urticaria, skin flushing; in women - frequent mood swings, sleep disturbances, depression, headache, hot flashes, increased sweating, vaginal dryness, decreased libido, lower abdominal pain, bone demineralization; in men, gynecomastia. Rarely: angioedema; in women - menstrual bleeding; in men - ossalgia, urinary retention, renal edema, muscle weakness in the lower extremities, lymphostasis. In isolated cases: a causal relationship has not been established - thrombosis, dyspeptic symptoms.

Application during pregnancy and lactation

Contraindicated during pregnancy, lactation.

special instructions

Patients with depression require special medical supervision during treatment. At the beginning of treatment, the development of an ovarian cyst is possible. In men, in order to prevent the side effects of buserelin, it is necessary to use antiandrogens according to the appropriate scheme.

Influence on the ability to drive vehicles and mechanisms

Buserelin should be used with caution in patients engaged in potentially hazardous activities that require increased attention and high speed of psychomotor reactions.