Buserelin

Buserelin – the antineoplastic drug which is an analog a hormone gonadotrophin-rileasing.

Form of release and structure

Drug is produced in shape:

• Spray nasal dosed (in bottles from dark glass on 17,5 ml with a dosing stopper pomp);
• Solution for hypodermic introduction of 0,1 mg/ml and 0,5 mg/ml (in ampoules on 1 ml packaged on 1, 5 or 7 pieces in packaging).

Active ingredient of Buserelin is the buserelina acetate.

Spray excipients:

• Benzalkoniya chloride;
• Water for injections.

Solution excipients:

• Sodium chloride;
• Water for injections.

Indications to use

Buserelin's use is reasonable at hormonal pathology of reproductive system which is caused by a relative or absolute giperestrogeniya:

• Hysteromyoma;
• Endometriosis (during the preoperative and postoperative periods);
• Hyperplastic processes of an endometria.

Drug can be appointed when carrying out the program of extracorporal fertilization at treatment of infertility.

Contraindications

Contraindications to Buserelin's use are:

• Period of pregnancy and lactation;
• Hypersensitivity to drug components.

With care drug is appointed at:

• Diabetes mellitus;
• Arterial hypertension;
• Depressions.

Route of administration and dosage

At spray use:

The drug is administered in previously cleared nasal passes.

At treatment of a hysteromyoma, endometriosis, hyperplastic processes of an endometria:

• Therapy is recommended to be begun in the 1st or 2nd day of a menstrual cycle, it is necessary to administer the drug continuously throughout all course of treatment;
• The daily dose of Buserelin makes 900 mkg. Full pressing of a pomp provides introduction of a single dose of drug which makes 150 mkg;
• The daily dose is entered in the equal portions (on 1 injection into each nasal pass) 3 times a day, at regular intervals (6-8 hours);
• Treatment duration – 4-6 months.

At treatment of infertility by means of a method of extracorporal fertilization:

• Therapy is recommended to be begun for the 2nd day (the beginning of a follikulinovy phase), or for 21-24 days (the middle of a lyuteinovy phase) of the menstrual cycle preceding stimulation;
• The daily dose of drug makes 900-1200 mkg. The drug is administered 3-4 times in knocks at regular intervals, on 1 injection (150 mkg) in each nasal pass;
• In 14-17 days of therapy at a thickness of endometria no more than 5 mm, decrease in level of oestradiol in blood serum not less than for 50% from initial, and also on condition of absence of cysts in ovaries, stimulation of a superovulation under ultrasonic monitoring and control of concentration of oestradiol in blood serum begins gonadotropic hormones;
• Buserelin's dose if necessary can be adjusted.

At solution use:

The drug is administered subcutaneously.

At treatment of female infertility by means of a method of extracorporal fertilization:

1. Therapy begins for the 21st day of the menstrual cycle preceding stimulation. Buserelin of 0,1 mg (1 ml) is entered daily until introduction of a chorionic gonadotrophin. Since 3rd day of a medical menstrual cycle, the drug of a menopauzny gonadotrophin is administered. The chorionic gonadotrophin is entered in 34-36 hours prior to the planned puncture of follicles;
2. Use of drug begins from 21 days of the menstrual cycle preceding stimulation – daily Buserelin is entered on 0,5 mg (1 ml) till 3rd day of a medical cycle. Further daily introduction of Buserelin on 0,1 mg (1 ml) which needs also to be applied until introduction of a chorionic gonadotrophin is appointed. From the 3rd day of the stimulating menstrual cycle the drug of a menopausal gonadotrophin is administered. The chorionic gonadotrophin is entered in 34-36 hours prior to the planned puncture of follicles;
3. From the 1st day of the stimulating cycle Buserelin is entered on 0,1 mg (1 ml) until introduction of a chorionic gonadotrophin. From the 2nd day of a medical cycle drug of a menopausal gonadotrophin is appointed. The chorionic gonadotrophin is entered in 34-36 hours prior to the planned puncture of follicles;

At treatment of endometriosis, a hysteromyoma:

• In the first 7 days of therapy of 1 times a day about 0,5 mg (1 ml) of Buserelin are entered;
• Further daily on 0,1 mg (1 ml) for maintenance of therapeutic effect.

It is necessary to change places of an injection.

Side effects

Buserelin's use can cause the following side effects:

• From endocrine system: the increased sweating, decrease in a libido, demineralization of bones, "inflows" of blood to an upper part of a thorax and face skin, dryness of a vagina, pain in the bottom of a stomach; seldom – menstrualnopodobny bleeding (it is noted in the first weeks of therapy);
• From the central nervous system: dizziness and headaches, fatigue, drowsiness, a sleep disorder, emotional lability, nervousness, decline in the ability to concentration of attention and memory, development of a depression or aggravation of its current;
• From the alimentary system: thirst, lock, diarrhea, nausea and vomiting, decrease or increase in body weight, appetite disturbance;
• From sense bodys: pressure sense on an eyeglobe, a sonitus, vision disorders (not clear vision) and hearing;
• From cardiovascular system: increase in arterial pressure (at the patients having arterial hypertension), heartbeat;
• From laboratory indicators: a hyperglycemia, decrease in tolerance to glucose, increase in activity of serumal transaminases, thrombocytopenia or a leukopenia, changes in a lipidic range, a hyperbilirubinemia;
• Allergic reactions: a skin itch, a small tortoiseshell, a dermahemia, it is very rare – acute or anaphylactoid anaphylaxis, a bronchospasm, a Quincke's disease;
• Others: in isolated cases – a thromboembolism of a pulmonary artery, acceleration or delay of processes of growth of hair on the head and a body, nasal bleedings, hypostases in the field of feet and anklebones, a joint pain, spin;
• Local reactions (at spray use): pain and dryness in a nose, irritation of a mucous membrane of a nasal cavity.

Special instructions

At the initial stages of treatment there is a risk of development of an oothecoma.

When carrying out induction of an ovulation strict medical observation is necessary.

The repeated course of therapy is possible only on condition of careful assessment of a ratio of potential risk of development of osteoporosis and the expected advantage.

Intranasal use of Buserelin at rhinitis is allowed, but in this case nasal passes have to be cleared before drug injection.

Treatment of the patients having a depression demands careful observation of the doctor.

In the course of therapy of endometriosis Buserelin's use in a combination with surgical treatment reduces blood supply of the pathological centers and their sizes, inflammatory manifestations and, as a result, reduces operation time. Postoperative therapy promotes decrease in frequency of a postoperative recurrence and reduces formation of commissures, thereby improving results of treatment.

In the course of therapy at the patients using contact lenses signs of irritation of eyes can be shown.

Before therapy it is necessary to exclude pregnancy and to cancel reception of hormonal contraceptives. Within the first 2 months of treatment it is recommended to apply non-hormonal methods of contraception.

In the course of therapy it is recommended to be careful at implementation of potentially dangerous types of activity demanding speed of psychomotor reactions and the increased concentration of attention including when driving the car.

Analogs

Buserelin's analog is Buserelin Fsintez.

Terms and storage conditions

Spray period of validity – 3 years, solution – 2 years. To store in protected from the sun, the place, unavailable to children, spray at a temperature of 8-25 °C, solution – 8-20 °C.