Buserelin Spray 150 mcg/dose, 17.5 ml

Pharmacodynamics

A synthetic analogue of natural GnRH. Competitively binds to receptors of cells of the anterior pituitary lobe, causing a transient increase in plasma levels of sex hormones.

The use of the drug in therapeutic doses leads (on average after 12-14 days) 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 ovaries and a decrease in the plasma concentration of estradiol (E2) to postmenopausal values.

Pharmacokinetics

In intranasal administration, the drug is completely absorbed through the nasal mucosa.

In small amounts it is excreted with the breast milk.

The T_1/2 is about 3 hours.

Indications

Hormone-dependent pathology of the reproductive system due to absolute or relative hyperestrogenism:

• endometriosis (pre- and postoperative periods);
• uterine myoma;
• endometrial hyperplastic processes;
• infertility treatment (under the program of in vitro fertilization).

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Active ingredient

Buserelin

Composition

Active ingredients:

Buserelin acetate 150 µg (2.1 mg).

Excipients:

benzalkonium chloride – 0.1 mg,

d/i water – up to 1 ml.

How to take, the dosage

In the treatment of endometriosis, uterine myoma, endometrial hyperplastic processes, the drug is administered into the nasal passages after clearing them in a dose of 900 mcg/day. A single dose of the drug when the pump is fully pressed is 150 mcg. The daily dose of the drug is administered in equal portions, one injection into each nostril 3 times/day at equal time intervals (6-8 hours) in the morning, afternoon and evening. Treatment with Buserelin should begin on the first or second day of the menstrual cycle, administered continuously throughout the course of treatment. The course of treatment is 4-6 months.

In infertility treatment by in vitro fertilization the drug is administered intranasally by one injection (150 mcg) into each nostril 3-4 times/day at regular intervals. The daily dose is 900-1200 mcg. Buserelin is administered at the beginning of 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 stimulation. After 14-17 days, with a decrease in the patient’s serum estradiol by at least 50% of the initial level, absence of ovarian cysts, and endometrial thickness of no more than 5 mm, the stimulation of superovulation with gonadotropic hormones begins with ultrasound monitoring and control of serum estradiol levels. If necessary, the dose of Buserelin may be adjusted.

Interaction

Concomitant use of Buserelin with other 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

Patients with any form of depression should be under close medical supervision during treatment with Buserelin.

Ovulation induction should be performed under close medical supervision.

In the initial phase of treatment with the drug, ovarian cysts may develop. A repeated course of treatment should be started only after careful evaluation of the ratio of expected benefit to potential risk of osteoporosis.

Patients who wear contact lenses may have signs of eye irritation.

In view of the intranasal route of administration, nasal mucosa irritation and sometimes nasal bleeding are possible. The drug can be used for rhinitis, but the nasal passages should be cleared before using it.

The use of Buserelin in combination with surgical treatment in endometriosis reduces the size of lesions and their blood supply and inflammatory manifestations and, therefore, shortens the time of surgery, and postoperative therapy improves results by reducing the rate of postoperative recurrences and reducing the formation of adhesions.

Before starting treatment with the drug, it is recommended that pregnancy be avoided and hormonal contraceptives discontinued, but other (non-hormonal) contraceptive methods should be used for the first two months of treatment.

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

When using the drug, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

• Pregnancy
• lactation period
• high sensitivity to the drug components.

With caution: the drug should be used in patients with arterial hypertension, diabetes, depression.

Side effects

CNS disorders: headache, dizziness, nervousness, fatigue, sleep disturbance, drowsiness, decreased memory and ability to concentrate, emotional lability, development of depression or worsening of its course.

Sensory organs: tinnitus, impaired hearing and vision (blurred vision), feeling of pressure on the eyeball.

Endocrine system disorders: blood “rushes” to the skin of the face and upper chest, increased sweating, vaginal dryness, decreased libido, lower abdominal pain, bone demineralization; rarely – menstrual-like bleeding (usually during the first weeks of treatment).

Cardiovascular system: palpitations, increased BP (in patients with arterial hypertension).

Allergic reactions: urticaria, skin itching, skin hyperemia, very rare – bronchospasm, anaphylactic and/or anaphylactoid shock, angioedema.

Digestive system disorders: nausea, vomiting, thirst, diarrhea, constipation, poor appetite, weight gain or loss.

Laboratory findings: decreased glucose tolerance, hyperglycemia; changes in lipid spectrum; increased activity of serum transaminases, hyperbilirubinemia; thrombocytopenia or leukopenia.

Others: in single cases – nasal bleeding; pulmonary embolism; edema of ankles and feet; weakening or enhancement of hair growth on the head and body; back and joint pain.

Local reactions: irritation of the nasal mucosa, dryness and pain in the nose.

Overdose

There are currently no reported cases of Buserelin overdose.

Pregnancy use

The drug is contraindicated in pregnancy and lactation.

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 using the drug.