Buserelin Fsintez

General characteristics. Structure:

Active ingredient: 157,5 mkg of a buserelin of acetate in 1 dose (150 mkg in terms of бусерелин).

Auxiliary veshchstvo: a bezalkoniya chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Buserelin synthetic analog endogenous gonadotrophin-rileasing of hormone (GNRG). Competitively contacts receptors of cells of a front share of a hypophysis and causes short-term increase in level of sex hormones in a blood plasma. Further use of medical doses of drug (on average in 12-14 days) leads to a total block of gonadotropic function of a hypophysis and reduces 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 бусерелин it is completely soaked up through a mucous membrane of a nose. The elimination half-life makes about 3 h. In insignificant quantities drug is emitted with breast milk.

Indications to use:

The hormonedependent pathology of reproductive system caused by an absolute or relative giperestrogeniya: 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:

The single dose of drug by full pressing of a pomp makes 150 mkg. Co of a glass bottle with drug to remove the plastic screw-on cover (at the same time there has to be a click of control of the first opening) and to screw the dosing plastic stopper pomp. Holding with fingers a wide rim of a stopper pomp to remove a protective cap. To direct a bottle with solution vertically up and sharply to press 3-5 times a rim for trial production of solution in air (it is necessary for filling of a raspylitelny head with medicinal mix). Drug is ready to use. Buserelin Fsintez enter into the nasal courses after their clarification.

     

At treatment of endometriosis, a hysteromyoma, hyperplastic processes of an endometria: the recommended daily dose of the drug "Buserelin Fsintez" of 900 mkg a day. The daily dose of drug is entered in the equal portions on one injection (150 mkg) into each nostril by 3 times a day at regular intervals (8 hours) in the morning, in the afternoon and in the evening. Treatment busereliny should be begun in the first or second day of a menstrual cycle, administration of drug continuous throughout all course of treatment. Course of treatment of 4-6 months.

At treatment of infertility by method of extracorporal fertilization (EKO): the recommended daily dose of the drug "Buserelin Fsintez" of 600 mkg. The drug is administered intranazalno on one injection (150 mkg) in one nostril 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 it is necessary to reduce a daily dose of the drug "Buserelin Fsintez" 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:

Prior to treatment by Buserelin Fsintez it is recommended 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.

During treatment by the patient's drug with any form of a depression have to be under observation of the doctor.

Use of the drug "Buserelin Fsintez" before surgical treatment at endometriosis reduces the sizes of the pathological centers, 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.

The repeated course of treatment should be begun only after careful assessment of a ratio of the expected advantage and potential risk.

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.

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.

Influence on ability упарвлять car and other mechanisms. It is necessary to be careful at purpose of drug to patients during the driving of motor transport and occupation potentially dangerous types of activity requiring special attention and speed of mental and motor reactions.

Side effects:

Allergic reactions: a small tortoiseshell, a dermahemia, a skin itch, it is very rare - an acute anaphylaxis, a Quincke's disease.

From TsNS: dizziness, headache, frequent change of mood, sleep disorder, nervousness, fatigue, decrease in memory and ability to concentration of attention, depression.

From cardiovascular system: a heart consciousness, increase in the ABP (at patients with an arterial hypertension).

From a GIT: nausea, vomiting, diarrhea, lock, appetite disturbance, thirst.

Others: pains in the bottom of a stomach, dryness of a vagina, decrease in a libido; seldom – menstrualnopodobny bleeding (as a rule, within the first weeks of treatment); in isolated cases – nasal bleedings; thromboembolism of a pulmonary artery; hypostases in anklebones and feet; dorsodynia, joints.

From laboratory indicators: decrease in tolerance to glucose, a hyperglycemia; changes in a lipidic range; increase in activity of serumal transaminases, hyperbilirubinemia; thrombocytopenia or leukopenia.

Local reactions – irritation of a mucous membrane of a nose, dryness and a rhinalgia.

Interaction with other medicines:

Simultaneous use of the drug "Buserelin Fsintez" 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 a diabetes mellitus 1 and 2 types Buserelin Fsintez can reduce efficiency of hypoglycemic means.

Contraindications:

- hypersensitivity to drug components;
- pregnancy;
- lactation.

With care: to apply at arterial hypertension, a diabetes mellitus, a depression.

Overdose:

Now about overdose cases by drug it was not reported.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C, in places unavailable to children. A period of validity - 2 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Spray nasal dosed 150 mkg / a dose: on 17,5 ml (nominal quantity not less than 187 doses) drug in the bottles of dark glass corked by covers plastic screwing on with a ring of control of the first opening. On 1 bottle complete with the dosing plastic stopper pomp and the application instruction place in a cardboard pack.