The antineoplastic drug, a synthetic analogue of GnRH. Buserelin competitively binds to the cell receptors of the anterior pituitary, causing a short-term increase in the level of sex hormones in the blood plasma.
On average 12-14 days after application of the drug at therapeutic doses, results in complete blockade gonadotropic pituitary function, inhibiting, thus selection of LH and FSH. As a result of the suppression of the synthesis of sex hormones in the gonads, which is manifested decrease of estradiol concentration in blood plasma values to post-menopausal women and a reduction of testosterone to postcastration levels in men.
testosterone concentration during continuous treatment for 2-3 weeks is reduced to a content characteristic of the state of orchiectomy, i.e. drug causes pharmacological castration.
Bioavailability is high. C max in plasma is about 2-3 hours after the / m and kept at a level sufficient to inhibit the synthesis of gonadotrophins by the pituitary gland of at least 4 weeks.
For adults on prescription
buserelin acetate, 3.93 mg, or 3.75 mg buserelin content
copolymer of DL-lactic and glycolic acids – 200 mg,
mannitol – 85 mg,
carmellose sodium – 30 mg,
Polysorbate 80 – 2 mg.
rr mannitol 0.8% d / and – 2 ml.
Cancer, Breast Cancer
- hormone-dependent prostate cancer;
- breast cancer;
- endometriosis (pre- and postoperative periods);
- uterine fibroids;
- endometrial hyperplasia;
- infertility treatment (in case of in vitro fertilization program).
- increased sensitivity to the drug.
Allergic reactions: urticaria, flushing of the skin; rarely – angioedema.
CNS: frequent changes of mood, sleep disturbances, depression, headache.
On the part of the musculoskeletal system: bone demineralization, which is the risk of developing osteoporosis.
Women – headache, depression, sweating and changes in libido, dryness of the vagina, pain in the abdomen; rarely – menstrualnopodobnoe bleeding (usually in the first few weeks of treatment).
In men with prostate cancer treatment – during the first 2-3 weeks after the first injection may exacerbation and progression of the underlying disease (due to the stimulation of synthesis of gonadotrophins and consequently testosterone), gynecomastia, possible “hot flushes”, sweating and decreased potency ( rarely requires changing therapy), transient increase in androgen concentrations in the blood, urinary retention, “kidney” edema (swelling of the face, eyelids, feet), muscle weakness in the lower extremities. At the beginning of the treatment of patients with prostate cancer may occur temporary increase in pain in the bones; in this case should be symptomatic therapy. We noted some cases of obstruction of the ureters and spinal cord compression.
Other: in single cases (causal relationship has not been clearly established) – pulmonary embolism, dyspepsia.
How to accept, acceptance rate and dosage
When hormone-prostate cancer – 3.75 mg / m every 4 weeks. In the treatment of endometriosis, endometrial hyperplasia – 3.75 mg / m once every 4 weeks. Treatment should begin during the first five days of the menstrual cycle. Duration of treatment – 4-6 months.
In the treatment of uterine fibroids – 3.75 mg / m once every 4 weeks. Treatment should begin during the first five days of the menstrual cycle. Duration of treatment – 3 months prior to surgery, in other cases – 6 months.
In the treatment of infertility by in vitro fertilization – 3.75 mg / m once early follicular (on the 2nd day of the menstrual cycle) or in mid-luteal phase (days 21-24) of the menstrual cycle prior to stimulation. After blocking pituitary function, confirmed by a decrease in serum estrogen concentration of not less than 50% of baseline (usually determined 12-15 days after injection buserelin-depot), in the absence of cysts in the ovaries (by ultrasound), endometrial thickness no more than 5 mm, begins superovulation gonadotropin hormones under ultrasound monitoring and control of serum estradiol.
Terms slurry preparation and administration
The drug is administered only / m. A suspension for a / th injection is prepared with the supplied solvent just prior to administration. The drug should be prepared and administered only by specially trained medical personnel.
Bottle of buserelin-depot should be held vertically. Easily tapping the bottle, it is necessary to ensure that all of the lyophilisate was at the bottom of the vial.
Open the syringe needle attached thereto with pink pavilion (1,2 × 50 mm), to collect the solvent.
Open the vial into the syringe and collect all contents of the vial with the solvent, to establish a syringe 2 ml per dose.
It should remove the plastic cap with the vial containing the lyophilisate. Disinfect the rubber stopper of the vial with an alcohol swab. Insert the needle into the vial with lyophilisate through the center of the rubber stopper and gently introduce the solvent on the inner wall of the vial without touching the contents of the bottle needle. Remove the syringe from the vial.
The bottle must remain stationary until complete impregnation solvent lyophilizate and form a suspension (approximately 3-5 minutes). Then, without turning the bottle, check the presence of dry lyophilisate in the walls and bottom of the vial. Upon detection of dry residues left lyophilisate vial until complete impregnation.
Once residues dry lyophilizate is left, the contents of the vial should be mixed gently in a circular motion for 30-60 seconds to form a uniform suspension. Do not turn and shake the bottle, it can lead to flocculation and the unsuitability of the suspension.
Need to quickly insert the needle through the rubber stopper into the vial. Then cut and fold down the needle, the vial tilting angle of 45 °, to dial into the syringe slowly slurry completely. Do not turn the bottle when typing. A small amount of the drug can remain on the walls and bottom of the vial. Consumption for the rest of the walls and bottom of the vial is taken into account.
Immediately replace the needle with the needle pink pavilion with green pavilion (0,8 × 40 mm), gently invert the syringe and remove air from the syringe.
The suspension buserelin-depot should be administered immediately after preparation.
With the help of alcohol swabs need to disinfect the injection site. , Then gently pull the syringe plunger back to insert the needle deep into the gluteal muscle to make sure that there is no damage to the vessel. Enter suspension intramuscularly slowly with constant pressure on the syringe plunger. By plugging the needle, it is substituted by another needle of the same diameter.
In a dry place, protected from light, at a temperature of 8-20 ° C
The simultaneous use of buserelin-depot preparations containing hormones (e.g., in an ovulation induction regime) can contribute to ovarian hyperstimulation syndrome.
With simultaneous use of buserelin may reduce the effectiveness of hypoglycemic agents.
Patients with any form of depression during treatment with Buserelin depot should be under close medical supervision. Ovulation induction should be under strict medical supervision. In the initial stage of treatment may develop ovarian cysts.
Prior to the beginning of treatment is recommended to exclude pregnancy and to stop taking hormonal contraceptives, but during the first two months of the drug is necessary to use other (non-hormonal) method of contraception.
In order to effectively prevent possible side effects in the first phase of action of the drug is necessary to use anti-androgens for 2 weeks before the first injection, buserelin-depot and during 2 weeks after the first injection.
Effects on ability to drive vehicles and other machines that require high concentration of attention
Caution should be exercised when administering the drug to patients involved in potentially hazardous activities that require increased attention and psychomotor speed reactions.
Pregnancy and lactation
Application of pregnancy and lactation is contraindicated.
Currently, the cases of drug overdose Buserelin depot were reported.