Buserelin-depot
Buserelin-depot: 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. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Buserelin-depo
ATX code: L02AE01
Active ingredient: Buserelin (Buserelin)
Manufacturer: Pharmsintez CJSC, Russia
Description and photo update: 2018-22-10
Prices in pharmacies: from 3716 rubles.
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Buserelin-depot is an antineoplastic drug, analogue of gonadotropin-releasing hormone.
Release form and composition
Dosage form Buserelin-depot - lyophilisate for preparation of suspension for intramuscular (i / m) administration of prolonged action: powdery mass, white with a weak yellow tint or white; solvent - a clear, colorless liquid; reconstituted suspension - a homogeneous solution, white with a faint yellow tint or white [in a glass bottle of dark color, in a cardboard box 1 bottle complete with a solvent (2 ml in an ampoule), a syringe, needles (2 pcs.) and alcohol swabs (2 PC.)].
1 bottle contains:
- active substance: buserelin acetate - 3.93 mg (which is equivalent to the content of 3.75 mg buserelin);
- auxiliary components: polysorbate-80, copolymer of glycolic and DL-lactic acids, sodium carmellose, mannitol.
Solvent: 0.8% mannitol solution for injection.
Pharmacological properties
Pharmacodynamics
The mechanism of action of Buserelin-depot is based on the competitive binding of Buserelin with the receptors of the cells of the anterior pituitary gland, as a result of which a short-term increase in the level of sex hormones occurs in the blood plasma. The use of the drug in therapeutic doses causes (after 12-14 days) a complete blockade of the gonadotropic function of the pituitary gland, thus slowing down the release of luteinizing and follicle-stimulating hormones. As a result, there is a suppression of the synthesis of sex hormones in the gonads, manifested by a decrease in the concentration in blood plasma:
- in women - estradiol up to postmenopausal level;
- in men - testosterone to the post-castration level.
Buserelin-depot causes pharmacological castration, since continuous treatment for 14–21 days leads to a decrease in testosterone levels to a value characteristic of the state of orchiectomy.
Pharmacokinetics
Buserelin is highly bioavailable. Its concentration in plasma reaches its maximum value approximately 2–3 hours after administration. The prolonged effect of the drug allows maintaining a level sufficient to inhibit the synthesis of gonadotropins by the pituitary gland for 28 days.
Indications for use
- uterine fibroids;
- mammary cancer;
- hyperplastic processes of the endometrium;
- endometriosis (pre- and postoperative period);
- infertility treatment during artificial insemination;
- hormone-dependent prostate cancer.
Contraindications
- period of pregnancy;
- breast-feeding;
- individual intolerance to the components of Buserelin-depot.
Instructions for use of Buserelin-depot: method and dosage
The ready-made solution of the lyophilisate (suspension) is intended only for intramuscular administration.
The procedure must be carried out in a hospital setting by specially trained medical personnel.
To prepare the suspension, use the supplied solvent.
Holding the bottle with Buserelin-depot in a strictly vertical position, gently tapping on it, you should ensure that all the powder settles to the bottom of the bottle. Using a syringe with a needle for aspiration of the solvent with a pink pavilion (1.2 x 50 mm), it is required to draw the entire contents of the ampoule with the solvent and set the syringe to a dose of 2 ml. Then, after removing the plastic cap from the vial with the lyophilisate, it is necessary to disinfect the rubber stopper of the vial with an alcohol swab. A needle is inserted into the vial through the center of the rubber stopper, and the solvent is carefully introduced along the inner wall of the vial, without touching the lyophilisate with the needle. After removing the syringe from the vial, the vial is left in a stationary position for 3-5 minutes to completely saturate the lyophilisate with a solvent and form a suspension. Without turning the bottle over, visually check the degree of dissolution of the lyophilisate. If there are dry powder particles on the sides and bottom of the vial, wait a while until they are completely saturated. Then, to form a homogeneous structure, the suspension must be stirred with careful circular movements for 0.5–1 min. In this case, the bottle should not be turned over or shaken to prevent the loss of flakes and deterioration of the suspension.
Quickly inserting the needle through the rubber stopper into the vial and tilting it at an angle of 45 ° (the vial cannot be turned over), slowly withdraw the suspension completely from the vial. There is a slight residue of the drug on the walls and bottom of the bottle.
After preparing the suspension, it should be administered immediately.
After replacing the solvent needle with a green pavilion needle (0.8 x 40 mm), gently turn the syringe over and remove air from it.
After disinfecting the injection site with the included alcohol swab, the needle is inserted deep into the gluteus muscle. To check for damage to the vessel, the syringe plunger is slightly pulled back. Then, with constant pressure on the syringe plunger, the suspension is slowly injected into the / m. If the needle becomes clogged, replace it.
Recommended dosage:
- endometriosis, endometrial hyperplastic processes: once, 3.75 mg with an interval of 4 weeks. The use of Buserelin-depot should be started within the first five days of the menstrual cycle. Treatment course - 4-6 injections;
- uterine fibroids: 3.75 mg once every 4 weeks. Treatment should be started within the first five days of the menstrual cycle. Treatment course - 3 injections before surgery, in other cases - 6 injections;
- infertility treatment by in vitro fertilization: 3.75 mg once on the 2nd day of the menstrual cycle (the beginning of the follicular phase) or from the 21st to the 24th day of the menstrual cycle (middle of the luteal phase) preceding stimulation. 12-15 days after the injection, the pituitary function is blocked. Its confirmation is the decrease in the level of estrogen in the blood serum from the initial level by at least 50%. If there are no cysts in the ovaries (according to ultrasound), stimulation of superovulation with gonadotropic hormones should be started with an endometrial thickness of no more than 5 mm, under the control of the level of estradiol in the blood serum and ultrasound monitoring;
- hormone-dependent prostate cancer: 3.75 mg with an interval of 4 weeks.
Side effects
- from the central nervous system: often - mood swings; sleep disorders, headache, depression;
- allergic reactions: skin flushing, urticaria; rarely - angioedema;
- on the part of the musculoskeletal system: bone demineralization (risk of developing osteoporosis);
- others: in some cases (a clear cause-and-effect relationship has not been established) - dyspeptic phenomena, pulmonary embolism.
In addition, the following side effects may occur:
- in women: lower abdominal pain, sweating, headache, changes in libido, depression, dryness of the vaginal mucosa; rarely - menstrual bleeding (more often during the first weeks of therapy);
- in men: it is possible - progression or exacerbation of the underlying disease (after the first injection within 2-3 weeks), temporary increase in bone pain, gynecomastia, hot flashes, decreased potency, increased sweating, urinary retention, transient increase in the level of androgens in the blood, renal edema (legs, face, eyelids), muscle weakness in the lower limbs; in some cases - the development of ureteral obstruction, compression of the spinal cord.
Overdose
Symptoms of an overdose with Buserelin have not been established.
special instructions
Before using Buserelin-depot, women are advised to exclude pregnancy and stop taking hormonal contraceptives. During the first two months of treatment, it is necessary to use non-hormonal contraception methods. For any form of depression, the patient needs close medical supervision. Ovulation induction must be carried out under the strict supervision of a physician. There is a risk of developing an ovarian cyst at the beginning of therapy.
For effective prevention of adverse events in men during the first phase of the drug action, it is necessary to prescribe the use of antiandrogens 2 weeks before the first injection of the drug and within 2 weeks after it. In rare cases, a decrease in potency requires a change in therapy.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment, care should be taken when performing potentially dangerous activities that require an increased speed of psychomotor reactions and special attention.
Application during pregnancy and lactation
According to the instructions, Buserelin-depot is contraindicated for use during gestation and lactation.
Drug interactions
With the simultaneous use of Buserelin-depot:
- with drugs containing sex hormones: the risk of ovarian hyperstimulation syndrome increases;
- with hypoglycemic agents: the effectiveness of the latter may decrease.
Analogs
The analogues of Buserelin-depot are Decapeptyl depot, Decapeptil, Differelin, Lyukrin depot, Zoladex, Eligard.
Terms and conditions of storage
Keep out of the reach of children.
Store at a temperature of 8-25 ° C in a dark place.
Shelf life: lyophilisate - 3 years, solvent - 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Buserelin-depot
Reviews about Buserelin-depot from patients are controversial. Most of them indicate the effectiveness of the drug in the treatment of ovarian endometriosis, uterine fibroids, infertility. In positive reviews, women share their impressions of the adverse events they have suffered, but the desire to recover or become pregnant, to achieve the desired result potentiates them to patience and optimism. There are many negative reviews in which it is recommended to abandon the use of the drug (indicating the terrible side effects).
Reviews of doctors who assess the quality of the drug by the end result are positive about the therapeutic effect of the drug.
Price for Buserelin-depot in pharmacies
The price for Buserelin-depot for a package containing 1 bottle of lyophilisate can range from 3922 to 4304 rubles.
Buserelin-depot: prices in online pharmacies
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Drug name Price Pharmacy |
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Buserelin-depot 3.75 mg lyophilisate for preparation of a suspension for intramuscular administration of prolonged action 1 pc. 3716 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
