Buserelin-depot

General characteristics. Structure:

Active agent: a buserelina acetate of 3,75 mg in the form of free peptide. 

Excipients: copolymer DL of milk and glikoliyevy acids - 200 mg, a D-mannitol - 85 mg, sodium carboxymethylcellulose - 30 mg, polysorbate-80 - 2 mg. 

Description: The lyophilized powder white or with a weak yellowish shade of color. 

Solvent in an ampoule: The D-mannitol - 16 mg, water for injections - 2 ml. 

Description: Colourless transparent liquid. 

Pharmacological properties:

Pharmacodynamics. Synthetic analog natural gonadotrophin-rileasing of hormone (GNRG). Buserelin competitively contacts receptors of cells of a front share of a hypophysis, causing short-term increase in level of sex hormones in a blood plasma. Further use of medical doses of drug brings (on average in 12-14 days) to a total block of gonadotropic function of a hypophysis, inhibiting, thus, allocation of luteinizing (LG) and follicle-stimulating hormone (FSG). Suppression of synthesis of sex hormones in gonads is as a result observed that is shown by decrease in concentration of oestradiol in a blood plasma to postclimacteric values at women and decrease in content of testosterone to postkastratsionny level at men. 

Concentration of testosterone at continuous treatment within 2-3 weeks decreases before the contents characteristic of a condition of an orkhiektomiya, i.e. pharmacological castration is caused. 

Pharmacokinetics. Bioavailability is high. The maximum concentration in plasma is reached approximately in 2-3 hours after intramuscular introduction and remains at the level sufficient for inhibition of synthesis of gonadotrophins a hypophysis not less than 4 weeks. 

Indications to use:

- hormonedependent prostate cancer, 

- breast cancer, 

- endometriosis (before - and postoperative the periods), 

- hysteromyoma, 

- hyperplastic processes of an endometria, 

- treatment of infertility (when carrying out the program of extracorporal fertilization (EKO). 

Route of administration and doses:

At a hormonedependent prostate cancer: 3,75 mg intramusculary each 4 weeks (in oil). 

At treatment of endometriosis, hyperplastic processes of an endometria: To 3,75 mg there are each 4 weeks in oil once. Treatment is begun in the first five days of a menstrual cycle. Treatment duration – 4-6 months. 

At treatment of a hysteromyoma: To 3,75 mg there are each 4 weeks in oil once. Treatment is begun in the first five days of a menstrual cycle. Treatment duration – before operation 3 months, in other cases - 6 months. 

At treatment of infertility by method of extracorporal fertilization (EKO): 3,75 mg in oil once for the 2nd day of a menstrual cycle. 

Features of use:

At women. Patients with any form of a depression during treatment by drug Buserelin have to be under careful observation of the doctor. 

Induction of an ovulation should be carried out under strict medical observation. In an initial stage of treatment by drug development of an oothecoma is possible. Prior to treatment drug recommends to exclude pregnancy and to stop reception of hormonal contraceptives, however within the first two months of use of drug it is necessary to apply other (non-hormonal) methods of contraception. 

At men. For the purpose of effective prevention of possible side effects in the first phase of effect of drug use of anti-androgens in two weeks prior to the first injection of a buserelin – depot and on an extent of two weeks after the first injection is necessary. 

Side effects:

Allergic reactions: a small tortoiseshell, a dermahemia, it is rare - a Quincke's disease. 

At women - typical side reactions are manifestation of the reached gipoestrogennny state – "a pharmacological climax": 

From TsNS: frequent change of mood, sleep disorder, depression, headache. 

From the endocrinological status: "inflows", the increased sweating, dryness of a vagina, decrease in a libido, pain in the bottom of a stomach, demineralization of bones, it is rare – menstrualnopodobny bleeding (as a rule, within the first weeks of treatment). 

At men, at cancer therapy of a prostate - within the first 2-3 weeks after the first injection can cause an aggravation and progressing of a basic disease that is connected with stimulation of synthesis of gonadotrophins and, respectively, testosterone, a gynecomastia, passing increase in concentration of androgens in blood (it is rare – an ossalgiya, an urination delay, renal hypostases, muscular weakness in the lower extremities, a lymphostasis). 

Others: in isolated cases (relationship of cause and effect is accurately not established) - a thromboembolism of a pulmonary artery, dispepsichesky disturbances. 

Interaction with other medicines:

Simultaneous use of drug Buserelin with the drugs containing sex hormones (for example, in the mode of induction of an ovulation), can promote emergence of a syndrome of hyper stimulation of ovaries. 

At simultaneous use Buserelin can reduce efficiency of hypoglycemic means.  

Contraindications:

Pregnancy, the feeding period a breast, hypersensitivity to drug components. 

Overdose:

Now about overdose cases by drug Buserelin it was not reported.

Storage conditions:

The list B, in protected from light and the place, unavailable to children, at a temperature from 8 °C to 20 °C. 

Issue conditions:

According to the recipe

Packaging:

Bottle with lyophilisate in a strip packaging complete with solvent in an ampoule (2 ml), and the application instruction are located with the one-time syringe and two needles in a cardboard pack.