Buserelin-depo lyophilisate suspension prolonged 3.75 mg, vial 1 pc.

Composition

Active ingredients:

buserelin acetate 3.93 mg, which corresponds to the content of buserelin 3.75 mg

Auxiliary substances:

copolymer of DL-lactic and glycolic acids-200 mg,

mannitol-85 mg,

carmellose sodium-30 mg,

polysorbate 80-2 mg.

Solvent:

mannitol solution 0,8% d / i-2 ml

. Pharmacological action

Pharmacodynamics

Antitumor drug, a synthetic analogue of GnRH. Buserelin competitively binds to the receptors of anterior pituitary cells, causing a short-term increase in the level of sex hormones in blood plasma.

On average, after 12-14 days, the use of the drug in therapeutic doses leads to a complete blockade of the gonadotropic function of the pituitary gland, thus inhibiting the release of LH and FSH. As a result, there is a suppression of the synthesis of sex hormones in the gonads, which is manifested by a decrease in the concentration of estradiol in the blood plasma to post-menopausal values in women and a decrease in the content of testosterone to the post-castration level in men.

The concentration of testosterone during continuous treatment for 2-3 weeks decreases to the content characteristic of the state of orchiectomy, i. e. the drug causes pharmacological castration.

Pharmacokinetics

Bioavailability is high. _Cmax in plasma is reached approximately 2-3 hours after intravenous administration and remains at a level sufficient to inhibit the synthesis of gonadotropins by the pituitary gland for at least 4 weeks.

Indications

• Hormone-dependent prostate cancer;
• breast cancer;
• endometriosis (pre-and postoperative periods);
• uterine fibroids;
• endometrial hyperplastic processes;
• infertility treatment (during the in vitro fertilization program).

Use during pregnancy and lactation

Use during pregnancy and lactation is contraindicated.

Contraindications

• Pregnancy;
• lactation;
• hypersensitivity to the components of the drug.

Side effects

Allergic reactions: urticaria, hyperemia of the skin; rarely-angioedema.

From the central nervous system: frequent mood swings, sleep disorders, depression, headache.

Musculoskeletal disorders: bone demineralization, which is a risk of developing osteoporosis.

In women-headache, depression, sweating and changes in libido, dryness of the vaginal mucosa, pain in the lower abdomen; rarely-menstrual bleeding (usually during the first weeks of treatment).

In men, when treating prostate cancer – during the first 2-3 weeks after the first injection, the underlying disease may worsen and progress (which is associated with stimulating the synthesis of gonadotropins and, accordingly, testosterone), gynecomastia, hot flashes, increased sweating and decreased potency (rarely requires a change of therapy), a transient increase in the concentration of androgens in the blood, urinary retention, “renal” edema (swelling of the face, eyelids, legs), muscle weakness in the lower extremities. At the beginning of treatment, patients with prostate cancer may experience a temporary increase in bone pain; in this case, symptomatic therapy should be performed. There were isolated cases of ureteral obstruction and spinal cord compression.

Other: in isolated cases (cause-and-effect relationship is not clearly established) – pulmonary embolism, dyspeptic phenomena.

Interaction

Simultaneous use of Buserelin depot with drugs containing sex hormones (for example, in the ovulation induction mode) may contribute to the occurrence of ovarian hyperstimulation syndrome.

When used concomitantly, buserelin may reduce the effectiveness of hypoglycemic agents.

How to take, course of administration and dosage

For hormone-dependent prostate cancer – 3.75 mg iv every 4 weeks. In the treatment of endometriosis, endometrial hyperplastic processes – 3.75 mg / m once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. The duration of treatment is 4-6 months.

In the treatment of uterine fibroids – 3.75 mg iv once every 4 weeks. Treatment should begin in the first five days of the menstrual cycle. The duration of treatment is 3 months before the operation, in other cases-6 months.

In the treatment of infertility by in vitro fertilization – 3.75 mg / m once at the beginning of the follicular (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21-24 days) of the menstrual cycle preceding stimulation. After a block of pituitary function, confirmed by a decrease in the concentration of estrogens in the blood serum by at least 50% from the initial level (usually determined 12-15 days after the injection of Buserelin-depot), in the absence of cysts in the ovaries (according to ultrasound), the endometrial thickness is not more than 5 mm, stimulation of superovulation with gonadotropins begins under ultrasound monitoring and monitoring of the level of estradiol in the blood serum.

Rules for suspension preparation and drug administration

The drug is administered only intravenously. The suspension for intravenous injection is prepared using the supplied solvent immediately prior to administration. The drug should be prepared and administered only by specially trained medical personnel.

The bottle with Buserelin depot should be kept strictly vertical. By tapping the bottle lightly, you need to ensure that all the lyophilizate is at the bottom of the bottle.

Open the syringe and attach a needle with a pink pavilion (1.2 x 50 mm) for solvent extraction.

Open the ampoule and fill the syringe with all the contents of the ampoule with solvent, set the syringe to a dose of 2 ml.

Remove the plastic cap from the lyophilizate bottle. Disinfect the rubber stopper of the bottle with an alcohol swab. Insert the needle into the lyophilizate bottle through the center of the rubber stopper and carefully insert the solvent along the inner wall of the bottle, without touching the contents of the bottle with the needle. Remove the syringe from the bottle.

The vial should remain stationary until the lyophilizate is completely soaked in the solvent and a suspension is formed (approximately 3-5 minutes). After that, without turning the bottle over, you should check for the presence of dry lyophilizate at the walls and bottom of the bottle. If dry lyophilizate residues are found, leave the bottle until it is completely soaked.

After no dry lyophilizate remains, the contents of the vial should be carefully mixed in a circular motion for 30-60 seconds until a homogeneous suspension is formed. Do not turn or shake the bottle, as this may cause flakes to fall out and make the suspension unusable.

You need to quickly insert the needle through the rubber stopper into the bottle. Then lower the needle section down and, tilting the bottle at an angle of 45°, slowly fill the suspension completely into the syringe. Do not turn the bottle over when typing. A small amount of the drug may remain on the walls and bottom of the bottle. Consumption for the remainder on the walls and bottom of the bottle is taken into account.

Immediately replace the pink pavilion needle with the green pavilion needle (0.8×40 mm), carefully turn the syringe over and remove the air from the syringe.

Buserelin depot suspension should be administered immediately after preparation.

Use an alcohol swab to disinfect the injection site. Insert the needle deep into the gluteal muscle, then pull the plunger of the syringe back slightly to make sure that there is no damage to the vessel. Enter the suspension intramuscularly slowly with constant pressure on the plunger of the syringe. If the needle is clogged, it is replaced with another needle of the same diameter.

Overdose

Currently, no cases of Buserelin depot overdose have been reported.

Special instructions

for women

Patients with any form of depression during treatment with Buserelin depot should be under close medical supervision. Ovulation induction should be performed under strict medical supervision. In the initial stage of treatment with the drug, an ovarian cyst may develop.

Before starting treatment with the drug, it is recommended to exclude pregnancy and stop taking hormonal contraceptives, but during the first two months of using the drug, other (non-hormonal) methods of contraception should be used.

Men

In order to effectively prevent possible side effects in the first phase of the drug, it is necessary to use antiandrogens 2 weeks before the first injection of Buserelin depot and within 2 weeks after the first injection.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Caution should be exercised when prescribing the drug to patients engaged in potentially dangerous activities that require increased attention and speed of psychomotor reactions.

Form of production

Lyophilizate for preparation of solution for intravenous administration

Storage conditions

Store in a dry place, protected from light, at a temperature of 8-20 °C

Shelf life

2 years

Active ingredient

Buserelin

Conditions of release from pharmacies

By prescription

Dosage form

suspension for injection

Purpose

For adults as directed by your doctor

Indications

Endometriosis, Breast Cancer, Infertility Treatment, Cancer

Bar Code and weight

Weight: 48 gr.