Buserelin depot, lyophilizate 3.75mg

Pharmacodynamics

Antitumor drug, a synthetic analog of GnRH. Buserelin competitively binds to receptors of cells in the anterior pituitary lobe, causing a transient increase in plasma levels of sex hormones.

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, suppression of sex hormone synthesis in gonads is observed, which is manifested by decrease of estradiol concentration in blood plasma to postmenopausal values in women and decrease of testosterone to post-castration level in men.

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

Pharmacokinetics

The bioavailability is high. C_max in plasma is reached approximately 2 to 3 h after i.v. administration and remains at a level sufficient to inhibit pituitary gonadotropin synthesis for at least 4 weeks.

Indications

Active ingredient

Composition

Active ingredients:

bucerelin acetate 3.93 mg, corresponding to 3.75 mg of bucerelin

Associates:

DL-lactic acid and glycolic acid copolymer – 200 mg,

Mannitol – 85 mg,

Sodium carmellose – 30 mg,

Polysorbate 80 – 2 mg.

Solvent:

Mannitol 0.8% d/i solution – 2 ml.

How to take, the dosage

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

In the treatment of uterine myoma – 3.75 mg in utero/m once every 4 weeks. Treatment should be started in the first five days of the menstrual cycle. The duration of treatment is 3 months before surgery and 6 months in other cases.

In infertility treatment by in vitro fertilization – 3.75 mg/m once at the beginning of the folliculin phase (on the 2nd day of the menstrual cycle) or in the middle of the luteal phase (21-24 days) of the menstrual cycle preceding the stimulation. After a blockade of pituitary function, confirmed by a decrease in the concentration of oestrogens in the blood serum by at least 50% of 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) and with endometrial thickness of no more than 5 mm, the stimulation of superovulation with gonadotropic hormones under ultrasound monitoring and control of serum levels of estradiol starts.

Regulations for suspension preparation and administration

The drug is administered only in m/m. Suspension for intravenous injection is prepared using the included solvent immediately prior to administration. The drug should only be prepared and administered by specially trained medical personnel.

The vial of Buserelin-depo should be held strictly vertically. Gently tap the vial to ensure that all the lyophilizate is at the bottom of the vial.

Open the syringe and attach a needle with a pink pavilion (1.2 × 50 mm) to draw out the solvent.

Open the ampoule and draw the entire contents of the solvent ampoule into the syringe, setting the syringe to a 2 ml dose.

The plastic cap should be removed from the vial containing the lyophilizate. Disinfect the rubber stopper of the vial with an alcohol swab. Insert the needle into the vial with the lyophilizate through the center of the rubber stopper and carefully inject the solvent along the inner wall of the vial, without touching the contents of the vial with the needle. Remove the syringe from the vial.

The vial should remain still until the lyophilizate is completely saturated with the solvent and a suspension is formed (approximately 3-5 minutes). After that, without turning the vial over, check for dry lyophilizate on the walls and bottom of the vial. If dry lyophilizate residue is found, leave the vial until it is completely saturated.

When no dry lyophilizate residue remains, the contents of the vial should be stirred gently in a circular motion for 30-60 seconds to form a homogeneous suspension. Do not invert or shake the vial; this may cause flakes to fall out and the suspension to become unusable.

Just quickly insert the needle through the rubber stopper into the bottle. Then, with the needle tip down, tilt the vial at a 45° angle and slowly draw the entire suspension into the syringe. Do not turn the vial upside down while filling. A small amount of the drug may remain on the walls and the bottom of the bottle. Consumption for residue on the sides and bottom of the bottle is indicated.

Please immediately replace the pink pavilion needle with a green pavilion needle (0.8×40 mm), carefully invert the syringe, and remove any air from the syringe.

The Buserelin Depot suspension should be administered immediately after preparation.

The injection site should be disinfected with an alcohol swab. Insert the needle deep into the gluteal muscle, then pull the syringe plunger back slightly to make sure there is no vessel damage. Inject the suspension intramuscularly slowly with constant pressure on the syringe piston. If the needle becomes blocked, replace it with another needle of the same diameter.

Interaction

The concomitant use of Buserelin depot with drugs containing sex hormones (e.g., in ovulation induction mode) may contribute to ovarian hyperstimulation syndrome.

Concomitant use of buserelin may decrease the effectiveness of hypoglycemic agents.

Special Instructions

Women

Patients with any form of depression should be under close medical supervision during treatment with Buserelin Depot. Ovulation induction should be performed under close medical supervision. At the initial stage of treatment with the drug it is possible to develop ovarian cysts.

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

Men

In order to effectively prevent possible side effects in the first phase of the drug, it is necessary to use anti-androgens 2 weeks before the first injection of Buserelin Depot and for 2 weeks after the first injection.

Influence on ability to drive vehicles and other mechanisms requiring increased concentration

Cautions should be taken when prescribing the drug to patients engaged in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Contraindications

Side effects

Allergic reactions: urticaria, skin hyperemia; rarely – angioedema.

CNS disorders: frequent mood swings, sleep disorders, depression, headache.

Skeletal and muscular system disorders: bone demineralization, which is a risk of osteoporosis.

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

. In men during treatment of prostate cancer – during the first 2-3 weeks after the first injection an aggravation and progression of the underlying disease (which is associated with stimulation of gonadotropin synthesis and, consequently, testosterone), gynecomastia are possible, possible “hot flashes”, increased sweating and decreased potency (rarely requires a change of therapy), transient increase in androgen blood concentration, urinary retention, “kidney” edema (swelling of the face, eyelids, legs), muscle weakness in the lower extremities. At the beginning of treatment of patients with prostate cancer, a temporary increase in bone pain may occur; in this case, symptomatic therapy should be given. Individual cases of ureteral obstruction and spinal cord compression have been reported.

Others: in single cases (cause-effect relationship is not clearly defined) – pulmonary embolism, dyspeptic complaints.

Overdose

There are currently no reported cases of overdose with Buserelin Depot.

Pregnancy use

The use during pregnancy and lactation is contraindicated.