The article will present instructions for the use of Buserelin. What is this drug?
Spray "Buserelin" is a medication for intranasal use, an analogue of gonadotropin-releasing hormone produced by the hypothalamus. It is used in the treatment of hormone-dependent pathologies of the reproductive system, for example, uterine fibroids, endometrial hyperplasia, since these diseases develop due to an excess of estrogen in the blood. Buserelin nasal spray suppresses ovarian function, as a result of which the spread of pathological processes stops. Treatment begins on the first day of menstruation by injecting 150 µg of the drug solution three times a day into each nostril. In addition, a nasal spray is prescribed for IVF - 150 micrograms four times a day.
Instructions for "Buserelin" for injection suggests that the medication is an antitumor drug. It is available in bottles containing a lyophilisate for the preparation of a special suspension. The injection is given once a month intramuscularly. This use is due to the fact that this drug has a prolonged effect and completely inhibits the production of sex hormones that stimulate the growth of tumors.
Forms of drug release
In accordance with the instructions for use, the spray “Buserelin” is available in plastic bottles equipped with a special dispenser, in the form of a colorless, odorless liquid complete with a cork-pump.
Buserelin-Depot lyophilisate for prolonged-release intramuscular injection is available in the form of a white powder, sometimes having a slight yellowish tint. A special solvent is included in the package - a clear, colorless liquid. The resulting suspension is homogeneous, white with a slight yellowish tint, contained in bottles of darkened glass. The kit also includes: solvent, syringe, needles (2 pcs.) And alcohol swabs (2 pcs.).
The composition of the medical product
According to the instructions for Buserelin, one spray bottle contains:
- the main substance is buserelin acetate - 2.1 mg;
- additional substances - benzalkonium chloride - 0.1 mg, purified water - 1 ml.
One bottle contains 3.75 mg of buserelin - the active substance.
As additional ingredients are:
- 2 mg - polysorbate 80;
- 85 mg - mannitol;
- 30 mg - sodium carmellose;
- 200 mg is a copolymer of DL-lactic and glycolic acids.
0.8% mannitol solution and water for injection - solvent.
Pharmacokinetics
Buserelin is a synthetic analogue of natural GnRH that binds to cell receptors in the anterior pituitary gland, causing a temporary increase in levels of all sex hormones.
The use of a drug in therapeutic doses entails a complete blockade of the pituitary gonadotropic function, inhibits the release of FSH and LH, as a result of which there is a suppression of the production of sex hormones in the ovaries, as well as a decrease in the concentration of the hormone estradiol in the blood up to postmenopausal indicators.
When using this medication intranasally, its substances are completely absorbed through the nasal mucosa.
In a small amount, this substance can be excreted in breast milk.
Indications for use
As indicated by the instruction to Buserelin, the drug is used for hormone-dependent diseases of the reproductive system, which are caused by relative or absolute hyperestrogenia. These include:
- Endometriosis, including in the postoperative period.
- Uterine fibroids.
- Hyperplastic processes in the endometrium.
- Infertility therapy, including in vitro fertilization.
This is stated in the instructions for use. Reviews and analogues to Buserelin will be presented below.
Dosage and administration
When treating the symptoms of endometriosis, endometrial hyperplastic phenomena and uterine fibroids, the drug is introduced into the nasal passages after the procedure for their purification in a dosage of 900 mcg / day.
A single dose of the drug when the pump is pressed is approximately 150 mcg.
The daily dosage of the drug is administered in equal portions several times a day, one injection in each nasal passage at equal time intervals.
Treatment with Buserelin should begin on the first or second day of the menstrual cycle and continue continuously for six months.
In the treatment of infertility with in vitro fertilization techniques, the drug is administered intranasally, one click in each nostril at regular intervals. The daily dosage should not exceed 1200 mcg.
What else does the application instruction for Buserelin tell us?
The medication in this case is prescribed at the beginning of the follicular or in the middle of the luteal phase of the menstrual cycle that precedes the stimulation of egg production.
After about two weeks, with a decrease in estradiol in the blood of patients not less than half of the initial level, as well as in the absence of an ovarian cyst and an endometrial layer thickness of not more than 5 mm, they begin to stimulate superovulation with gonadotropic hormones under ultrasound monitoring and control of estradiol levels in the blood.
If necessary, dosage adjustment of the medication can be made.
Instructions for injection "Buserelin" confirms that the drug is intended for intramuscular administration.
Therapy of hormone-dependent prostate cancer involves intramuscular injections at a dose of 3.75 mg, prescribed every month.
Treatment of hyperplastic changes in the endometrium and endometriosis - 3.75 mg once with intramuscular injections every month. The beginning of therapy is combined with the first 5 days of the menstruation cycle. The course is from 4 to 6 months.
Treatment of uterine fibroids is carried out with a dosage of 3.75 mg of the active component, which is administered once intramuscularly every month. Instructions for use with Buserelin 3, 75 mg recommends that therapy be carried out in the first 5 days of the menstrual cycle. The course before surgery is 3 months, sometimes 6 months.
In the treatment of infertility according to the IVF program, a single dose of the drug is determined - 3.75 mg. Injection is carried out at the beginning of the follicular phase (on the second day of the cycle) or at the end of the luteal phase (21-24 days of the cycle) before stimulation.
Only an experienced healthcare professional can prepare the suspension. Ready solution should be used immediately after preparation.
Adverse reactions
According to the instructions, “Buserelin” in the bulk of cases is tolerated positively by patients, however, some specific reactions of the body sometimes manifest, which include:
- Reactions of the nervous system: cephalgia, dizziness, increased nervousness, fatigue, sleep disturbances, severe drowsiness, impaired memory and visual acuity, emotional instability, the occurrence of depression or the complication of its course.
- Sensory reactions: hearing and vision impairment (blurred eyes), tinnitus, sensation of pressure on the eyeball.
- Endocrine system reactions: flushing of the face and upper chest, increased sweating, vaginal dryness, decreased sex drive, lower abdominal pain, decreased bone mineralization, menstrual bleeding (usually in the first weeks of treatment).
- Reactions of the cardiovascular system: increased heart rate, increased blood pressure (especially in patients with arterial hypertension).
- Allergic manifestations: skin itching, urticaria, redness of the skin, bronchospasm, angioedema, anaphylactic shock.
- Digestive reactions: dyspepsia, increased thirst, changes in stool, impaired appetite, decreased or increased fat mass.
- Laboratory indicators: decreased glucose tolerance, changes in the lipid spectrum, hyperglycemia, increased transaminase activity, thrombocytopenia, hyperbilirubinemia or leukopenia.
- Other reactions: nosebleeds, swelling of the lower extremities, pulmonary thromboembolism, increased or weakened hair growth on the body and head, pain in the back and joints.
- Local reactions: symptoms of irritation of the nasopharynx, pain and dryness in the nose. This is confirmed by the instructions for use for Buserelin injections, as well as for the nasal spray.
Contraindications
This medication is strictly contraindicated for pregnant women, women during lactation, as well as in cases of hypersensitivity to the substances that make up its composition.
The Buserelin medication should be used with some caution in case of diabetes mellitus, hypotension, arterial hypertension, depressive and neurological disorders.
Patients with any form of depression during treatment with this medication should be monitored by specialists.
Ovulation induction also needs to 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 begins, as a rule, after a careful assessment of the ratio of the intended benefits and the potential risk of osteoporosis.
In patients using contact lenses, signs of irritation of the eye mucosa may occur. The instruction for spray “Buserelin” reports that with intranasal methods of using this drug, irritation of the inner surface of the nose is possible, and in some cases minor nasal bleeding may occur.
The medication is approved for use in rhinitis, however, before injecting the solution into the nasal passages, they should be thoroughly cleaned.
The use of the Buserelin medical device in combination with surgical methods for the treatment of 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 non-hormonal contraceptive methods should be used at the beginning of the medication. Such information contains instructions for Buserelin injections.
Interaction with other medical devices
Concomitant therapy with Buserelin medication with other medications that contain some sex hormones (for example, by inducing ovulation) can contribute to the development of ovarian over-stimulation syndrome.
In addition, the drug "Buserelin" can significantly reduce the effectiveness of certain hypoglycemic agents.
special instructions
Women should exclude pregnancy, including an ectopic pregnancy, before using this medication, and for effective prevention of negative phenomena, men should be prescribed antiandrogens 14 days before the initial injection of Buserelin and within 14 days after it. In case of signs of a decrease in potency, you should consult a doctor to adjust therapeutic methods or cancel the Buserelin medicine. The instruction will give all the explanations.
Effect on concentration
The drug significantly reduces the speed of mental and motor reactions, so you should be especially careful when driving motor vehicles and complex mechanisms. In addition, caution should be exercised during therapy during work requiring increased attention and speed of nerve reactions. This describes the instructions for the Buserelin nasal spray.
Application against the background of endometriosis
The tool very effectively treats this disease. Endometriosis is currently diagnosed in approximately 10% of women after thirty years. This pathology is estrogen-dependent, and clinical manifestations directly depend on the degree of inclusion of nearby organs in the disease process. To treat the disease, it is necessary to suppress estrogen secretion, therefore it is advisable to use gonadotropin-releasing hormone analogues, one of which is Buserelin spray. The instruction indicates that the drug significantly reduces or leads to the complete disappearance of signs of endometriosis, prevents the occurrence of relapses of the disease for a long period after stopping this medication. However, the medicine does not completely cure endometriosis; after some time, some patients may relapse. The most radical solution to this problem is surgical intervention with concomitant drug therapy.
Men are prescribed a drug for cancer of the prostate, and women with the development of endometriosis, breast cancer, uterine fibroids and hyperplasia in the endometrium. Treatment should begin in the first few days of menstruation. At the beginning of therapy, an exacerbation of the underlying disease is possible, but subsequently, ovarian function is suppressed, and the hormone-dependent disease is suspended.
Are there any analogues to Buserelin Depot injections? The instruction does not contain such information.
Analogue drugs
In the modern pharmaceutical market there is a wide selection of drugs similar in effect to the Buserelin drug, but their use in each individual case requires the appointment of a qualified specialist, since such drugs are serious hormonal treatments for specific diseases, the treatment of which is exclusively the prerogative of the doctor.
Thus, the analogues of this medication are:
- "Velbin";
- "Dzhevtana";
- "Androfarm";
- Casodex
- Honwan;
- Novantron;
- "Diferelin";
- "Estradurin";
- "Biculid";
- Tsiproteron-Teva;
- Arecloc;
- "Adriblastin";
- “Depo-Provera”;
- "Flucin";
- "Kalumid";
- Leiprorelin;
- Bicalutamide-Teva;
- Indigal
- Sinestrol;
- Vantas
- "Endoxan";
- Zoladex;
- "Syndroxocin";
- Decapeptil;
- "Navelbin";
- "Eligard";
- Flutazin
- Zytiga
- "Goserelin";
- Chlorrtrianisen.
Analogues of the drug "Buserelin-depot" are presented by the following drugs:
- Decapeptil.
- "Eligard."
- Zoladex.
- Decapeptil Depot.
- "Lucrin Depot."
- "Diferelin".
Reviews
This drug is, in a sense, specific, therefore it is rarely prescribed. This fact determines the small number of reviews about this medication. Basically, patients of gynecological clinics, for whom the drug “Buserelin” was prescribed for the treatment of endometriosis, some cases of infertility and menstrual irregularities, left their opinions on it. For men, this medication is rarely prescribed, only if certain oncological diseases occur, for example, malignant tumors of the prostate gland.
Patients were satisfied with the effectiveness of this medication, since the therapeutic effect was observed already in the first months of treatment. Despite the fact that the drug does not completely cure endometriosis, patients note that the manifestations of such a disease have significantly decreased, which was also proved by some diagnostic observations (ultrasound of the pelvic organs), when after the examination the results showed the suspension of the uterus and neighboring organs.
In the reviews there are observations of women with endometrial hyperplasia syndrome, which indicate that the excessive growth of the endometrium during treatment with Buserelin has stopped.
Negative reviews about this medication also take place, since there are a lot of side effects. Patients experienced severe headaches, felt a violation of the digestive processes, which was expressed by dyspepsia and dyspepsia. In addition, patients complained of severe drowsiness, distraction, and decreased attention.
A special place in the reviews about the drug is given to depressive disorders. The instructions indicate that during treatment with this medication, many patients could not control their psychological state, so they had to stop taking the drug.
We reviewed the instructions for use and reviews for the spray "Buserelin" and injections.