Buserelin nasal spray dosed 150 mcg/dose, bottle 17.5 ml

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

• endometriosis (pre- and postoperative periods);
• uterine fibroids;
• hyperplastic processes of the endometrium;
• infertility treatment (when conducting an in vitro fertilization program).

Pharmacodynamics

Synthetic analogue of natural GnRH. Competitively binds to the receptors of the cells of the anterior pituitary gland, causing a short-term increase in the level of sex hormones in the blood plasma.

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 concentration of estradiol (E2) in the blood plasma to postmenopausal values.

Pharmacokinetics

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

In small amounts excreted in breast milk.

T _1/2 is about 3 hours.

Manufacturer

Pharm-Sintez, Russia

Composition

Active ingredients:

buserelin acetate 150 mcg (2.1 mg).

Excipients:

benzalkonium chloride – 0.1 mg,

water d / i – up to 1 ml.

Application during pregnancy and lactation

The use of the drug during pregnancy and lactation is contraindicated.

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

Contraindications

• Pregnancy;
• lactation period;
• hypersensitivity to drug components.

With caution: the drug should be used for arterial hypertension, diabetes mellitus, depression.

Side effects

From the side of the central nervous system: headache, dizziness, nervousness, fatigue, sleep disturbance, drowsiness, decreased memory and ability to concentrate, emotional lability, the development of depression or worsening of its course.

From the senses: tinnitus, impaired hearing and vision (blurred vision), a feeling of pressure on the eyeball.

From the endocrine system: “hot flushes” of blood to the skin of the face and upper chest, increased sweating, vaginal dryness, decreased libido, pain in the lower abdomen, bone demineralization; rarely – menstrual bleeding (usually during the first weeks of treatment).

From the side of the cardiovascular system: palpitations, increased blood pressure (in patients with arterial hypertension).

Allergic reactions: urticaria, pruritus, skin flushing, very rarely – bronchospasm, anaphylactic and / or anaphylactoid shock, angioedema.

From the digestive system: nausea, vomiting, thirst, diarrhea, constipation, impaired appetite, increase or decrease in body weight.

On the part of laboratory parameters: decreased glucose tolerance, hyperglycemia; changes in the lipid spectrum; increased activity of serum transaminases, hyperbilirubinemia; thrombocytopenia or leukopenia.

Others: in isolated cases – nosebleeds; pulmonary embolism; swelling in the ankles and feet; weakening or increased hair growth on the head and body; back pain, joints.

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

Interaction

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

With the simultaneous use of Buserelin may reduce the effectiveness of hypoglycemic agents.

How to take, course and dosage

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

In the treatment of infertility by in vitro fertilization, the drug is administered intranasally, one injection (150 μg) into each nostril 3-4 times / day at regular intervals. The daily dose is 900-1200 mcg. Buserelin is prescribed at the beginning of the folliculin (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 estradiol in the blood serum of patients by at least 50% of the initial level, the absence of cysts in the ovaries, the thickness of the endometrium is not more than 5 mm, stimulation of superovulation with gonadotropic hormones begins under ultrasound monitoring and control of the level of estradiol in the blood serum. If necessary, the dose of Buserelin can be adjusted.

Overdose

Special instructions

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

Ovulation induction should be performed under strict medical supervision.

In the initial stage of drug treatment, the development of an ovarian cyst is possible. A repeated course of treatment should be started only after a careful assessment of the ratio of the expected benefit and the potential risk of osteoporosis.

Contact lens wearers may experience signs of eye irritation.

Given the intranasal route of administration, irritation of the nasal mucosa is possible, sometimes nosebleeds. The drug can be used for rhinitis, but before using it, you should clean the nasal passages.

The use of the drug Buserelin in combination with surgical treatment for endometriosis reduces the size of pathological foci and their blood supply, inflammatory manifestations and, therefore, shortens the operation time, and postoperative therapy improves the results, reducing the frequency of postoperative relapses and reducing the formation of adhesions.

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

Impact on the ability to drive vehicles and other mechanisms that require increased concentration

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Shelf life