Buserelin

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Buserelin: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Drug interactions
10. Analogs
11. Terms and conditions of storage
12. Terms of dispensing from pharmacies
13. Reviews
14. Price in pharmacies

Latin name: Buserelin

ATX code: L02AE01

Active ingredient: buserelin (buserelin)

Manufacturer: CJSC "Pharm-Sintez" (Russia)

Description and photo update: 2019-14-08

Prices in pharmacies: from 482 rubles.

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Buserelin is an antineoplastic drug analogous to the gonadotropin-releasing hormone.

Release form and composition

The drug is available in the form:

Dosed nasal spray (in 17.5 ml dark glass vials with a dosing pump stopper);
Solution for subcutaneous administration of 0.1 mg / ml and 0.5 mg / ml (in 1 ml ampoules, packaged in 1, 5 or 7 pieces per package).

Buserelin's active ingredient is buserelin acetate.

Spray auxiliary substances:

Benzalkonium chloride;
Water for injections.

Excipients of the solution:

Sodium chloride;
Water for injections.

Pharmacological properties

Buserelin is characterized by antigonadotropic, antiandrogenic and antiestrogenic effects.

Pharmacodynamics

The drug is a synthetic analogue of the natural gonadotropin-releasing hormone (GnRH). The action of buserelin consists in competitive binding to receptors of cells localized in the anterior lobe of the pituitary gland, which causes a short-term increase in the concentration of sex hormones in the blood plasma. Further use of therapeutic doses of the drug on average after 12-14 days becomes the cause of the complete blockade of the gonadotropic function of the pituitary gland. Thus, the production of follicle-stimulating (FSH) and luteinizing (LH) hormones is inhibited. As a result, there is an inhibition of the production of sex hormones in the ovaries and a decrease in the content of estradiol in the blood plasma to postmenopausal parameters.

Pharmacokinetics

With intranasal administration, buserelin is completely absorbed through the mucous membrane of the nasal sinuses. The substance passes into breast milk in small amounts. The half-life of buserelin is approximately 3 hours.

Indications for use

According to the instructions, Buserelin is used for hormonal pathology of the reproductive system, which is caused by relative or absolute hyperestrogenism:

Myoma of the uterus;
Endometriosis (in the preoperative and postoperative periods);
Endometrial hyperplastic processes.

The drug can be prescribed during an in vitro fertilization program for the treatment of infertility.

Contraindications

Contraindications to the use of Buserelin are:

Pregnancy and lactation period;
Hypersensitivity to drug components.

The drug is prescribed with caution when:

Diabetes mellitus;
Arterial hypertension;
Depression.

Instructions for the use of Buserelin: method and dosage

Spray

Buserelin spray is injected into the previously cleaned nasal passages.

In the treatment of uterine fibroids, endometriosis, endometrial hyperplastic processes:

It is recommended to start therapy on the 1st or 2nd day of the menstrual cycle, the drug should be injected continuously throughout the course of treatment;
The daily dose of Buserelin is 900 mcg. Full pressing of the pump provides a single dose of the drug, which is 150 μg;
The daily dose is administered in equal portions (1 injection into each nasal passage) 3 times a day, at regular intervals (6-8 hours);
The duration of treatment is 4-6 months.

In the treatment of infertility using the in vitro fertilization method:

It is recommended to start therapy on the 2nd day (the beginning of the folliculin phase), or on days 21-24 (the middle of the luteal phase) of the menstrual cycle preceding stimulation;
The daily dose of the drug is 900-1200 mcg. The drug is injected 3-4 times in knocks at regular intervals, 1 injection (150 μg) into each nasal passage;
After 14-17 days of therapy, with an endometrial thickness of no more than 5 mm, a decrease in the level of estradiol in the blood serum by at least 50% from the initial, and also in the absence of cysts in the ovaries, stimulation of superovulation with gonadotropic hormones begins under ultrasound monitoring and control of estradiol concentration in blood serum;
The dose of Buserelin spray can be adjusted if necessary.

Solution

The drug is injected subcutaneously.

In the treatment of female infertility using the in vitro fertilization method:

Therapy begins on the 21st day of the menstrual cycle prior to stimulation. Buserelin 0.1 mg (1 ml) is administered daily until the administration of chorionic gonadotropin. Starting from the 3rd day of the therapeutic menstrual cycle, the preparation of menopausal gonadotropin is administered. Chorionic gonadotropin is administered 34-36 hours before the planned follicle puncture;
The use of the drug begins from the 21st day of the menstrual cycle, preceding stimulation - Buserelin is injected daily at 0.5 mg (1 ml) until the 3rd day of the treatment cycle. Next, a daily administration of Buserelin of 0.1 mg (1 ml) is prescribed, which must also be used before the introduction of chorionic gonadotropin. From the 3rd day of the stimulating menstrual cycle, the preparation of menopausal gonadotropin is administered. Chorionic gonadotropin is administered 34-36 hours before the planned follicle puncture;
From the 1st day of the stimulating cycle, Buserelin is injected at 0.1 mg (1 ml) until the introduction of chorionic gonadotropin. From the 2nd day of the treatment cycle, a drug of menopausal gonadotropin is prescribed. Chorionic gonadotropin is administered 34-36 hours before the planned follicle puncture;

In the treatment of endometriosis, uterine fibroids:

In the first 7 days of therapy, 0.5 mg (1 ml) of Buserelin is administered once a day;
Then, daily, 0.1 mg (1 ml) to maintain the therapeutic effect.

The injection sites should be changed.

Side effects

The use of Buserelin can cause the following side effects:

From the endocrine system: increased sweating, decreased libido, demineralization of bones, "hot flashes" of blood to the upper chest and facial skin, vaginal dryness, pain in the lower abdomen; rarely - menstrual bleeding (observed in the first weeks of therapy);
From the side of the central nervous system: dizziness and headaches, fatigue, drowsiness, sleep disturbances, emotional lability, nervousness, decreased ability to concentrate and memory, development of depression or aggravation of its course;
From the digestive system: thirst, constipation, diarrhea, nausea and vomiting, weight loss or increase, impaired appetite;
From the senses: a feeling of pressure on the eyeball, tinnitus, visual impairment (blurred vision) and hearing;
From the side of the cardiovascular system: increased blood pressure (in patients with arterial hypertension), palpitations;
On the part of laboratory parameters: hyperglycemia, decreased glucose tolerance, increased serum transaminase activity, thrombocytopenia or leukopenia, changes in the lipid spectrum, hyperbilirubinemia;
Allergic reactions: pruritus, urticaria, skin flushing, very rarely - anaphylactic or anaphylactoid shock, bronchospasm, angioedema;
Others: in isolated cases - pulmonary embolism, acceleration or slowdown of hair growth on the head and body, nosebleeds, swelling in the feet and ankles, pain in the joints, back;
Local reactions (when using a spray): pain and dryness in the nose, irritation of the nasal mucosa.

Overdose

At the moment, cases of overdose of Buserelin are unknown.

special instructions

In the initial stages of treatment, there is a risk of developing an ovarian cyst.

When carrying out the induction of ovulation, strict medical supervision is necessary.

A repeated course of therapy is possible only with a careful assessment of the ratio of the potential risk of osteoporosis and the expected benefit.

Intranasal use of Buserelin for rhinitis is allowed, but in this case, the nasal passages must be cleared before injecting the drug.

Treatment of patients with depression requires close medical supervision.

During the treatment of endometriosis, the use of Buserelin in combination with surgical treatment reduces the blood supply to pathological foci and their size, inflammatory manifestations and, as a result, reduces the operation time. Postoperative therapy reduces the incidence of postoperative relapse and reduces adhesion formation, thereby improving treatment outcomes.

Patients using contact lenses may show signs of eye irritation during therapy.

Before starting therapy, you should exclude pregnancy and stop taking hormonal contraceptives. During the first 2 months of treatment, it is recommended to use non-hormonal methods of contraception.

In the course of therapy, it is recommended to be careful when carrying out potentially hazardous activities that require the speed of psychomotor reactions and increased concentration of attention, including when driving a car.

Drug interactions

When Buserelin is combined with drugs that include sex hormones (for example, in the ovulation stimulation mode), ovarian hyperstimulation syndrome may develop. When the drug is administered simultaneously with hypoglycemic agents, the effectiveness of the latter is often reduced.

Analogs

Buserelin's analogue is Buserelin FSintez.

Terms and conditions of storage

The shelf life of the spray is 3 years, the solution is 2 years. Store in a place protected from the sun, out of reach of children, spray at a temperature of 8-25 ° C, solution - 8-20 ° C.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Buserelin

According to reviews, Buserelin is most often used in the form of a spray. Evaluations of the effectiveness of the drug are very diverse. For some patients, this drug has actually worked, but many patients report certain adverse reactions, including cysts. Doctors say that Buserelin can be used only under the condition of qualified medical supervision of the patient's condition.

The price of Buserelin in pharmacies

The approximate price of Buserelin in the form of a nasal metered-dose spray is about 635-690 rubles (for a 17.5 ml bottle). The solution for subcutaneous administration is not currently on sale.

Buserelin: prices in online pharmacies

Drug name

Price

Pharmacy

Buserelin 150 mcg / dose nasal spray dosed 17.5 ml 1 pc.

482 r

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Buserelin 0.15 mg / dose nasal spray dosed 17.5 ml 1 pc.

639 RUB

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Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!