Buserelin - instructions for use, analogs, reviews and release forms (nasal spray Depo, injections in ampoules for injection Long FS 3.75 mg) of a drug for the treatment of endometriosis and infertility in women, including during pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Buserelin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Buserelin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Buserelin in the presence of existing structural analogues.Use for the treatment of endometriosis, uterine fibroids and infertility in women, including during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Buserelin - synthetic analogue of natural GnRH. Competitively binds to the receptors of the anterior pituitary cells, causing a short-term increase in the level of sex hormones in the blood plasma.

The use of the drug in therapeutic doses leads (on average 12-14 days) to 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 in the ovaries is suppressed and the concentration of estradiol (E2) in the blood plasma is reduced to post-menopausal values.

Composition

Buserelina acetate + excipients.

Pharmacokinetics

After subcutaneous administration, Buserelinum is completely absorbed from the digestive tract, plasma is observed 1 h after administration. Cumulates in the liver, kidneys, as well as in the anterior pituitary. It is metabolized by tissue peptidases. It is excreted in the urine and bile in unchanged form and in the form of metabolites.

With intranasal application, the drug is completely absorbed through the nasal mucosa. In small amounts excreted in breast milk.

Indications

The hormone-dependent pathology of the reproductive system, caused by absolute or relative hyperestrogenism:

• endometriosis (pre- and postoperative periods);
• uterine myoma;
• hyperplastic processes of the endometrium;
• treatment of infertility (when carrying out the program of in vitro fertilization);
• hormone-dependent prostate cancer;
• mammary cancer.

Forms of release

Spray nasal dosed (Buserelin Depot).

Lyophilizate for the preparation of a suspension of prolonged release for intramuscular and subcutaneous injection 3.75 mg (injections in ampoules for injections) (Buserelin Long FS).

Instructions for use and reception scheme

Spray nasal

In the treatment of endometriosis, uterine fibroids, endometrial hyperplastic processes, the drug is injected into the nasal passages after purification at a dose of 900 μg per day. A single dose of the drug with a full pressure pump is 150 mcg. The daily dose of the drug is administered in equal portions for one injection in each nostril 3 times a day at regular intervals (6-8 hours) in the morning, afternoon and evening. Treatment with Buselelin should be started on the first or second day of the menstrual cycle, administered continuously throughout the course of treatment.The course of treatment is 4-6 months.

In the treatment of infertility by in vitro fertilization, the drug is injected intranasally with one injection (150 μg) into each nostril 3-4 times a day at regular intervals. The daily dose of 900-1200 mcg. Buserelin is prescribed at the beginning of the follicular (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21-24 days) of the menstrual cycle preceding stimulation. After 14-17 days with a decrease in estradiol in the serum of patients not less than 50% of the baseline level, absence of cysts in the ovaries, thickness of the endometrium is not more than 5 mm, stimulation of superovulation by gonadotropic hormones under ultrasound monitoring and control of estradiol levels in serum begins. If necessary, dose adjustment may be carried out by Buserelin.

Ampoules Buserelin Depot

With hormone-dependent prostate cancer - 3.75 mg intramuscularly every 4 weeks.

In the treatment of endometriosis, endometrial hyperplastic processes are 3.75 mg IM once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. Duration of treatment is 4-6 months.

When treating uterine fibroids - 3.75 mg IM once every 4 weeks.Treatment should begin in the first five days of the menstrual cycle. Duration of treatment - before the operation 3 months, in the remaining cases - 6 months.

In the treatment of infertility by in vitro fertilization, 3.75 mg IM once at the beginning of the follicular (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21-24 days) of the menstrual cycle preceding stimulation. After blockade of the pituitary function, confirmed by a decrease in the serum level of estrogen in the blood serum, not less than 50% of the baseline (usually determined 12-15 days after Buserelin Depot injection), in the absence of cysts in the ovaries (according to ultrasound), the thickness of the endometrium is not more than 5 mm, stimulation of superovulation by gonadotropic hormones under ultrasound monitoring and control of the level of estradiol in serum begins.

Rules for the preparation of suspension and drug administration

The drug is administered only intramuscularly. The suspension for the IM injection is prepared with the help of the applied solvent immediately before administration. The drug should be prepared and administered only by specially trained medical personnel.

The vial with Buselinen Depot should be kept strictly vertically.Tapping lightly on a vial, it is necessary to achieve that all лиофилизат was on the bottom of a vial.

Open the syringe, attach a needle with a pink pavilion (1.2 × 50 mm) to the solvent intake.

Open the ampoule and dial into the syringe all the contents of the ampoule with the solvent, install the syringe to a dose of 2 ml.

Remove the plastic cap from the vial containing the lyophilizate. Disinfect the rubber stopper of the bottle with an alcohol swab. Insert the needle into the vial with lyophilizate through the center of the rubber stopper and carefully insert the solvent into the inner wall of the vial without touching the needle with the contents of the vial. Remove the syringe from the vial.

The bottle must remain stationary until the solvent is completely saturated with the lyophilizate and the suspension is formed (for about 3-5 minutes). After that, without turning the bottle, you should check the presence of dry lyophilizate at the walls and bottom of the vial. If a dry residue of the lyophilizate is found, leave the vial until it is completely soaked.

After the remaining dry lyophilizate is not left, the contents of the vial should be gently stirred in a circular motion for 30-60 seconds until a uniform suspension is formed.Do not overturn and shake the bottle, this can lead to the loss of flakes and the unfitness of the suspension.

It is necessary to quickly insert the needle through the rubber stopper into the vial. Then cut the needle cut down and, tilting the vial at an angle of 45 degrees, slowly fill the syringe completely. Do not flip the bottle when typing. A small amount of the drug can remain on the walls and bottom of the vial. The consumption of the residue on the walls and the bottom of the vial is taken into account.

Immediately replace the needle with a pink pavilion on a needle with a green pavilion (0.8 × 40 mm), gently turn the syringe and remove air from the syringe.

Suspension Buselelina Depot should be administered immediately after preparation.

Using an alcohol sponge, you need to disinfect the injection site. Insert the needle deep into the gluteus muscle, then gently pull the plunger of the syringe backward to make sure that there is no damage to the vessel. Administer the suspension intramuscularly slowly with constant pressure on the syringe plunger. When the needle is clogged, it is replaced with another needle of the same diameter.

Side effect

• headache;
• dizziness;
• nervousness;
• fatigue;
• sleep disturbance;
• drowsiness;
• decreased memory and ability to concentrate;
• emotional lability;
• development of depression or worsening of its course;
• noise in ears;
• hearing and vision impairment (vague vision);
• a feeling of pressure on the eyeball;
• "tides" of blood to the skin of the face and upper chest;
• increased sweating;
• dryness of the vagina;
• decreased libido;
• pain in the lower abdomen;
• demineralization of bones;
• menstrualnopodobnoe bleeding (usually during the first weeks of treatment);
• palpitation;
• increased blood pressure (in patients with hypertension);
• hives;
• itching;
• hyperemia of the skin;
• bronchospasm;
• anaphylactic and / or anaphylactoid shock;
• angioedema;
• nausea, vomiting;
• diarrhea;
• constipation;
• a violation of appetite;
• increase or decrease in body weight;
• hyperglycemia;
• changes in the lipid spectrum;
• thrombocytopenia or leukopenia;
• nasal bleeding;
• pulmonary embolism;
• edema in the ankles and feet;
• weakening or strengthening of hair growth on the head and on the body;
• pain in the back, joints;
• irritation of the nasal mucosa;
• dryness and pain in the nose.

Contraindications

• pregnancy;
• lactation period;
• hypersensitivity to the components of the drug.

Application in pregnancy and lactation

Contraindicated use of the drug during pregnancy and lactation.

special instructions

Patients with any form of depression during the treatment with Buselelin should be under close medical supervision.

Induction of ovulation should be carried out under strict medical supervision.

In the initial stage of treatment with the drug, the development of ovarian cysts is possible.

Repeated treatment should be started only after a thorough assessment of the relationship between the expected benefit and the potential risk of osteoporosis.

Patients who use contact lenses may develop signs of eye irritation.

Given the intranasal (spray in the nose) way of use, there may be irritation of the nasal mucosa, sometimes - nosebleeds. The drug can be used in rhinitis, but before using it, the nasal passages should be cleared.

The use of Busherelin in combination with surgical treatment for endometriosis reduces the size of pathological foci and their blood supply, inflammatory manifestations and, consequently, shortens the operation time, and postoperative therapy improves results, reducing the frequency of postoperative relapses and reducing the formation of adhesions.

Before the beginning of treatment with the drug, it is recommended to exclude pregnancy and stop taking hormonal contraceptives, however, during the first two months of using the drug, it is necessary to use other (non-hormonal) methods of contraception.

The menstrual cycle and recovery of menstruation is observed within 1-2 months after the end of the drug Bucerelin. At the same time, you can start planning a pregnancy.

In case of drinking alcohol together with the drug Buserelin, consult your doctor.

To treat prostate cancer should not be prescribed to patients after an orchiectomy. At the beginning of prostate cancer treatment, an exacerbation of the disease (usually less than 10 days) associated with an initial transient increase in androgen concentration in the blood ("flash phenomenon") is possible. In this case, severe pain in the bones or in the location of the tumor, exacerbation of symptoms (including dysuria) is possible. The intensification of neurological disorders in patients with metastases in the spine can lead to temporary weakness and paresthesia in the lower extremities. It is necessary to warn the patient about the need to continue therapy, despite the side effects, which in the course of further treatment decrease or disappear.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Simultaneous use of Buserelin with other drugs containing sex hormones (for example, in the induction of ovulation), can contribute to the emergence of the syndrome of ovarian hyperstimulation.

With simultaneous application of Buserelin can reduce the effectiveness of hypoglycemic agents.

Analogues of the drug Buserelin

Structural analogs for the active substance:

• Buserelin FSintez;
• Buserelin depot;
• Buserelin Long FS;
• Buserelina acetate;
• Suprefact;
• Suprefact of the depot.

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