Buserelin - instructions for use and release form, composition, contraindications and analogues

Neoplasms of a malignant nature currently occupy one of the leading places in terms of mortality among the population almost throughout the world. The longer a person puts off visiting a doctor, the more difficult and longer the path to recovery will be. It is in this direction of medicine that the words that lost time are equivalent to life could not be more true.

In the arsenal of modern pharmacology there are currently a lot of medications designed to fight malignant tumors that affect a variety of organs of the human body. For the treatment of hormone-dependent malignant neoplasms, drugs that are analogues of hormones from the hypothalamus (the part of the brain responsible for the functioning of the neuroendocrine system) are widely used today. One of these medications is Buserelin-Long.

Instructions for use of Buserelin

This antitumor drug is a representative of hormone analogs of the hypothalamus, a part of the brain that is responsible for the functioning of the neuroendocrine system. These medications help fight tumors. The action is to increase the amount of sex hormones in the body. The result is that the gonadotropic function of the pituitary gland is completely blocked. This leads to suppression of the synthesis of sex hormones in the ovaries and a decrease in the amount of estradiol in plasma. The drug has several release forms, differing in auxiliary components.

Composition and release forms

The active component of all forms of release of this medication is buserelin acetate in different concentrations. The excipients are somewhat different. The table describes the composition in more detail:

Pharmacological properties

The mechanism of action of the drug is competitive binding to the receptors of the cells of the anterior pituitary gland. The result of this is a short-term increase in the content of sex hormones in the blood plasma. Treatment with therapeutic doses of the drug after 12-14 days causes a complete blocking of the gonadotropic function of the pituitary gland. This inhibits the replication of luteinizing and follicle-stimulating hormone. The result is that the concentration of estradiol decreases to post-menopausal values ​​in women and testosterone during the post-castration periods in men.

The bioavailability of Buserelin is at a very high level. The maximum concentration in the blood plasma is observed 2-3 hours after the intramuscular injection. The effect lasts for 4 weeks. The level remains sufficient for the pituitary gland to inhibit the synthesis of gonadotropins. When using an intranasal spray, the active substance is adsorbed through the nasal mucosa. Its half-life is 3 hours. The substance is excreted in small quantities during feeding in breast milk.

Indications for use

A general indication for use is hormone-dependent diseases of the reproductive system that were caused by absolute or relative hyperestrogenism. This condition is characterized by increased levels of estrogen, which causes hormonal imbalance and disruption of many organs. Such diseases include:

• uterine fibroids;
• endometriosis in the post- and preoperative period to reduce relapses;
• infertility during IVF, i.e. in vitro fertilization;
• mammary cancer;
• endometrial hyperplasia;
• hormone-dependent prostate cancer.

Buserelin for endometriosis

The more estrogen there is in endometriosis, the more severe the symptoms of the disease. Buserelin is a drug that suppresses hypothalamic releasing factors, which creates conditions for a decrease in estrogen synthesis. Doctors use the following types of this medicine:

• Goserelin;
• Long and Depot forms
• Buserelin acetate in the form of a nasal spray.

The use of each product provides a lasting therapeutic effect, but the original drug Buserelin-Depot has more positive reviews from doctors. It has several advantages:

• does not lead to dysfunction of the kidneys, liver and digestive organs;
• does not affect weight;
• easy to use - injections are given monthly;
• does not lead to an increase in hormones with androgenic effects, i.e. acne, hirsutism or seborrhea will not occur;
• does not negatively affect metabolism.

For infertility

The medication is one of the drugs for the treatment of infertility. It is administered before hyperstimulation on days 21-24 or 2 of the menstrual cycle. After suppression of pituitary function, as evidenced by a reduced level of estrogen (at least 50%), the patient is prescribed a certain dose of gonadotropins to stimulate ovulation. This treatment method increases the chances of getting pregnant. It is carried out under mandatory monitoring of estradiol levels. Periodically, the woman is prescribed ultrasound monitoring.

Treatment of fibroids

A benign tumor in the muscular layer of the uterus, i.e. myometrium is called myoma. This is one of the most common gynecological diseases. The action of Buserelin in this case is to slow down the growth of the tumor, which depends on hormonal levels. When treating fibroids, this medication has several advantages:

• quick healing effect;
• preservation of reproductive function and the main reproductive organ;
• To get a good result, only 1 injection is required.

For what diseases is the drug used?

Instructions for use of Buserelin Long indicate the following indications for treatment with the drug:

• diseases of the uterus caused by excess estrogen (uterine fibroids, endometriosis, endometrial hyperplasia);
• breast tumors (with intact menstrual function and intact estrogen and progesterone receptors);
• before and after surgery for endometriosis (the drug reduces endometriotic lesions and the formation of adhesions after surgery);
• hormone-dependent forms of prostate cancer;
• before in vitro fertilization (IVF) - the drug suppresses the natural synthesis of estrogen, which makes it possible to create an artificial hormonal status necessary for embryo transfer.

Directions for use and dosage

Buserelin-Long and Buserelin-Depot are analogues of gonadotropic hormone. They have the same indications for use and are considered generics. The price of the former is lower due to the use of cheaper raw materials or manufacturing in other factories. Both drugs are produced in the form of a lyophilisate. Buserelin spray has different instructions for use:

1. In the treatment of uterine fibroids, foci of endometriosis and hyperplastic processes in tissues. You need to spray the medicine into the nasal passages at 900 mcg per day. When you press the pump once, 150 mcg of the product is released. The required dose of Buserelin is sprayed once into the nasal passage three times a day with a break of 6+8 hours. Therapy begins on days 1-2 of the menstrual cycle. The usual course duration is 4-6 months.
2. In the treatment of infertility in the case of IVF. The drug is used intranasally every 6-8 hours in each nostril, 150 mcg. The daily dosage is 900-1200 mcg. Treatment begins on days 2 or 21-24 of the cycle before IVF.

Buserelin-Long

This medication is used exclusively intramuscularly. The injection suspension is prepared immediately before the procedure. For various hormone-dependent diseases, a certain dosage is used:

1. Prostate cancer. One intramuscular injection every month is indicated. Dosage 3.75 mg.
2. Endometriosis, hyperplastic changes in the endometrium. Therapy begins on days 1-5 of the menstrual cycle. The drug is administered once every 4 weeks at a dose of 3.75 mg. Therapy lasts 4-6 months.
3. Uterine fibroids. To treat this disease, it is necessary to administer 3.75 mg every 4 weeks. Therapy begins on days 1-5 of the cycle. Before surgery, treatment lasts 3 months, and in other cases – six months.
4. Infertility before IVF. On days 2 or 21-24 of the cycle, 1 injection is administered intramuscularly, i.e. 3.75 mg. When pituitary function is confirmed, gonadotropic hormones that stimulate ovulation are prescribed.

Buserelin-Depot

This medication is a complete analogue of the previous remedy, so the instructions for its use are the same. The dosage does not change in the treatment of the following hormone-dependent diseases of the reproductive system:

• prostate cancer;
• endometriosis, hyperplastic changes of the endometrium;
• uterine fibroids;
• infertility before IVF.

Pharmacological group

The drug has antiestrogenic, antiandrogenic, antitumor and antigonadotropic effects. Buserelin-long binds to skin receptors located in the anterior lobe of the pituitary gland. Within two weeks, the drug can block its gonadotropic functions. The drug undergoes a process of inhibition of follicle-stimulating and luteinizing hormone. After using the drug, a decrease in testosterone in the testicles may be observed, and sex hormones located in the ovaries are suppressed. The drug can provoke a decrease in the level of estradiol in the blood up to menopausal levels.

special instructions

The medication has a number of application features. In men, this applies to the preliminary prescription of androgen drugs. They are necessary to prevent potential adverse reactions during the first time of treatment. They are prescribed 2 weeks before the start of therapy and continue to be taken for another 2 weeks after its completion. Features of use in women:

• if there are signs of severe depression, the patient should be constantly monitored by a doctor;
• ovulation induction is carried out under strict control in a special clinic;
• nasal spray can be used for rhinitis, but the nose is washed before the procedure;
• at the beginning of treatment, some patients experienced the development of ovarian cysts;
• after discontinuation of the drug, ovarian function is restored in approximately 3 months;
• You must be careful when driving a car.

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Analogs

The drug Buserelin Long has an insufficient number of analogues for use. Only a doctor can select an adequate substitute for a medication.

Buserelin depot

The drug Buserelin-depot also belongs to the group of antitumor compounds. The drug is used to treat hormone-dependent cancer pathologies in men and women. Taking this medication is strictly prohibited during pregnancy and breastfeeding.

Depot Provera

Depo-Provera is a medicinal product and is considered a hormonal contraceptive with antitumor activity. Medications are used for the purpose of contraception, as well as for the treatment of certain oncological pathologies in women.

Buserelin and alcohol

The manufacturer does not indicate the possible consequences of drinking alcohol during treatment with Buserelin, but doctors still recommend eliminating alcohol. It cannot be combined with taking any medication. The reaction to such a combination can be unpredictable. This is not only an increase in side effects, but also a sharp deterioration in memory, decreased concentration, hearing, and vision. Hormonal drugs already have a large list of negative reactions, and in combination with alcohol they have an even more harmful effect on the body.

Contraindications for use

This medication is strictly contraindicated for use by pregnant women, women during lactation, as well as in cases of hypersensitivity to the substances included in its composition.

The drug "Buserelin" should be used with some caution in case of diabetes mellitus, hypotension, arterial hypertension, depressive and neurological disorders. Patients with any form of depression should be supervised by specialists during therapy with this medication.

Patients with any form of depression should be under the supervision of specialists during therapy with this medication.

Ovulation induction must also be carried out under appropriate supervision. At the initial stage of treatment, the formation of cysts on the ovaries is possible.

An additional course of treatment is usually started after a thorough assessment of the balance between the expected benefit and the potential risk of osteoporosis.

Patients using contact lenses may experience signs of irritation of the eye mucosa. The instructions for the Buserelin spray indicate that with intranasal methods of using this drug, irritation of the inner surface of the nose is possible, and in some cases, minor nosebleeds may occur.

The medication is approved for use for rhinitis, but before injecting the solution into the nasal passages, they should be thoroughly cleaned.

The use of the medical product “Buserelin” in combination with surgical methods of treating endometriosis reduces pathological lesions in size and their blood supply, and relieves inflammation. As a result, the operation time is significantly reduced, and postoperative treatment is more successful. In addition, the incidence of postoperative relapses is significantly reduced and the formation of adhesions is reduced.

Before starting treatment with this drug, it is recommended to exclude pregnancy and stop using hormonal contraceptives, and at first, non-hormonal contraceptive methods should be used when taking the medication. This information is contained in the instructions for Buserelin injections.

Side effects of Buserelin

Like most hormonal drugs, this medication has a long list of side effects. It includes the following undesirable reactions from different organ systems:

• headache;
• hives;
• sleep phase disturbance;
• mood swings;
• nosebleeds;
• skin hyperemia;
• depression;
• osteoporosis;
• angioedema.

Women often experienced symptoms of vaginal dryness and bleeding similar to menstruation. These signs are observed in the first weeks of treatment. In rare cases, episodes have been observed:

• spinal cord compression;
• development of ureteral obstruction;
• dyspeptic disorders;
• pulmonary embolism.

An exacerbation of the disease can occur in men during treatment for prostate cancer. The reason is the stimulation of the synthesis of gonadotropins and testosterone. Some men experienced the development of gynecomastia, decreased potency, hot flashes and increased sweating. With such symptoms, a revision of the dosage is required, otherwise the following symptoms may develop:

• urinary retention;
• increase in androgens in the blood;
• weakness in the lower extremities;
• swelling of the face, eyelids, legs.

In childhood

There is no reliable information on the use of the drug in pediatrics. This is explained by the fact that the diseases for which it is used are most often diagnosed in adult patients. In addition, hormonal drugs are strong, and therefore less aggressive medications are used in pediatrics. Although childhood age is not listed as a contraindication for use, the drug cannot be used to treat children.

Reviews from doctors about Buserelin will also be presented.

Buserelin price

It is worth remembering that to purchase medication you need a prescription from a doctor. This also applies to purchases from an online pharmacy. The price of the medicine varies depending on the manufacturer and place of purchase. The approximate cost range is reflected in the table:

Myoma therapy

Myoma is a benign tumor in the uterine muscle layer, that is, in the myometrium. This is one of the most common gynecological diseases. The effect of the drug in this case is to reduce the growth of the tumor, depending on hormonal levels. During the treatment of fibroids, the medication has a number of advantages:

• preservation of the function of childbirth and the main reproductive organ;
• accelerated therapeutic effect;
• One injection is needed to get a positive result.

Reviews about Buserelin Depot confirm this.