Buserelin

General characteristics. Structure:

Active agent: a buserelina acetate - 2,100 g. 

Auxiliary veestvo: a benzalkoniya chloride - 0,100 g, water for injections to 1,0 l.

The nasal spray suppressing synthesis of sex hormones in ovaries and reducing concentration of oestradiol in a blood plasma to postclimacteric values. 

Pharmacological properties:

Pharmacodynamics. Drug is a synthetic analog natural a 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 an ovary and decrease in concentration of oestradiol (E2) in a blood plasma to postclimacteric values is as a result observed. 

Pharmacokinetics. At intranasal use drug is completely soaked up through a mucous membrane of a nose. In insignificant quantities it is allocated with breast milk. The elimination half-life makes about 3 h. 

Indications to use:

The hormonedependent pathology of reproductive system caused by an absolute or relative giperestrogeniya: endometriosis (before - and postoperative the periods), a hysteromyoma, hyperplastic processes of an endometria, treatment of infertility (when carrying out the program of extracorporal fertilization (EKO)). 

Route of administration and doses:

At treatment of endometriosis, a hysteromyoma, hyperplastic processes of an endometria: the drug is administered in the nasal courses after their clarification in a dose 900 mkg a day. The single dose of drug by full pressing of a pomp makes 150 mkg. The daily dose of drug is entered in the equal portions on one injection into each nostril by 3 times a day at regular intervals (6-8) hours in the morning, in the afternoon and in the evening. Treatment by drug Buserelin should be begun in the first or second day of a menstrual cycle. 

At treatment of infertility by method of extracorporal fertilization (EKO): Drug is appointed on 600 mkg a day, i.e. on one injection of 150 mkg in the nasal course by 4 times a day at regular intervals. The drug is administered from the middle of a lyuteinovy phase of a menstrual cycle (about 21-24 days of a cycle) about day of introduction of an ovulatory dose of a chorionic gonadotrophin. On this background at achievement of blockade of synthesis of oestradiol (E2) from 2-5 in the afternoon of menstrualnopodobny bleeding according to standard schemes stimulation is carried out by drugs of gonadotrophins. At the expressed blockade of reproductive system and the "weak" response of ovaries to stimulation of an ovulation drugs of gonadotrophins Buserelin it is necessary to reduce a daily dose of drug to 2 injections a day or to increase a dose of gonadotrophins. The repeated course of treatment is carried out only on doctor's orders and after medical examination under dynamic control of a hormonal profile and ultrasonic monitoring.

Features of use:

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. The repeated course of treatment should be begun only after careful assessment of a ratio of the expected advantage and potential risk of development of osteoporosis. At the patients using contact lenses emergence of signs of irritation of eyes is possible. 

Considering an intranasal route of administration, the irritation of a mucous membrane of a nose, sometimes nasal bleeding is possible. Drug can be used at rhinitis, however before its use it is necessary to clear the nasal courses. Drug use Buserelin in a combination with surgical treatment at endometriosis reduces the sizes of the pathological centers and their blood supply, inflammatory manifestations and, therefore, reduces operation time, and postoperative therapy improves results, reducing the frequency of a postoperative recurrence and reducing formation of commissures. 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.

Side effects:

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). 

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

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:

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:

In bottles on 17,5 ml with a plastic pomp doser.