Buserelin 0.15% 17.5ml nasal spray

The composition and form of issue:

Spray nasal. 1 dose contains:

buserelina acetate to 157.5 µg

in terms of buserelin — 150 µg 

excipients: benzalkonium chloride 7,5 mg water for injection — up to 75 al 

in dark glass bottles 17.5 ml (nominal number of doses — not less than 187), complete with a plastic tube with pump in cardboard pack 1 set.

Description pharmaceutical form:

Transparent colorless liquid without foreign inclusions.

Pharmacokinetics:

In intra application buserelin completely absorbed through the mucous membrane of the nose. T1/2 is about 3 h.

Small amounts of the drug is excreted in breast milk.

Description pharmacological action:

Buserelin is a synthetic analog of endogenous GnRH. Competitive binds to receptors on cells of the anterior lobe of the pituitary gland and causes a short-term increase in the level of sex hormones in the blood plasma. Further, the use of therapeutic doses of the drug (average 12-14 days) results in complete blockade of the gonadotropic function of the pituitary gland and reduces the secretion of LH and FSH. The result is a suppression of the synthesis of sex hormones in the ovaries and a decrease in the concentration of estradiol (E2) in blood plasma to post-menopausal values.

Indications:

Hormone-dependent pathology of the reproductive system caused by an absolute or relative giperestrogenia:

• endometriosis (pre – and postoperative periods)
• uterine fibroids
• hyperplastic processes of the endometrium
• infertility treatment (during the in vitro fertilization (IVF).

Contraindications:

• hypersensitivity to the drug
• pregnancy
• lactation.

With caution in diseases such as:

• hypertension
• diabetes
• depression.

Application of pregnancy and breast-feeding:

Contraindicated.

Side effects:

Allergic reactions: urticaria, hyperemia of skin, itching, rarely — anaphylactic shock, angioedema.

CNS: dizziness, headache, frequent mood swings, sleep disturbances, nervousness, fatigue, loss of memory and ability to concentrate, depression.

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

Gastrointestinal: nausea, vomiting, diarrhea, constipation, loss of appetite, thirst.

Other: abdominal pain, vaginal dryness, decreased libido rarely menstrualnopodobnoe bleeding (usually within the first weeks of treatment) in rare cases, epistaxis pulmonary embolism swelling of the ankles and feet, pain in back, joints.

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

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

Drug interactions:

The simultaneous use of the drug Buserelin Fences with preparations containing sex hormones (for example, the mode of induction of ovulation), may facilitate the occurrence of ovarian hyperstimulation syndrome.

Diabetes type 1 and 2 the Buserelin Fences can reduce the effectiveness of gipoglikemicakih funds.

Method of application and dose:

Intranasally, after cleansing the nasal passages. Single dose it pump is 150 mcg.

The glass vial is remove the plastic screw cover (should be a click control the first opening) and the metering screw plastic tube-pump. Holding your fingers wide rim of tube-pumps, remove the protective cap. To send a vial with the solution straight up and 3-5 times sharply tap the rim for a trial edition of the solution into the air (it is necessary to fill the spray head drug mixture). The product is ready for use.

In the treatment of endometriosis, uterine fibroids, endometrial hyperplasia the recommended daily dose of the drug Buserelin Fences — 900 mg/day.

The daily dose is administered in equal portions one injection (150 mcg) in each nostril 3 times a day at equal intervals of time (8 hours) in the morning, afternoon and evening. Treatment buserelina should start in the 1st or 2nd days of the menstrual cycle, the drug should be continuous for the duration of your course of treatment. The course of treatment is 4-6 months.

In the treatment of infertility with IVF, the recommended daily dose of the drug Buserelin Fences — 600 mcg. The drug is administered one injection (150 mg) in one nostril 4 times a day at equal intervals of time, from mid-luteal phase of the menstrual cycle (21-24 th day of the cycle) until the day of the introduction of ovulatory dose of HCG. On this background in the achievement of the blockade of the synthesis of estradiol from 2-5-day menstrualnopodobnoe bleeding on the standard scheme is the stimulation of preparations of gonadotropins.

In severe blockade of the reproductive system and low ovarian response to ovulation stimulation drugs gonadotropin daily dose of the drug Buserelin Fences should be reduced to 2 injection per day or increase the dose of gonadotropins.

Repeated treatment is carried out only on prescription and after a medical examination under the dynamic control of the hormonal profile and ultrasound monitoring.

Overdose:

Currently, the cases of drug overdose were reported.

Special instructions:

Before starting treatment with Buserelin Fences it is recommended to exclude pregnancy and to stop taking a hormonal contraceptive, but during the first two months of the application it is necessary to use other (non-hormonal) methods of contraception.

During the period of drug treatment patients with any form of depression should be under a doctor’s supervision.

The use of the drug Buserelin Fences before surgical treatment of endometriosis reduces the size of lesions, their vascularization, inflammatory manifestations and, therefore, reduces operation time and postoperative therapy improves the results, reducing the frequency of postoperative recurrence and reducing the formation of adhesions.

A second course of treatment should be started only after careful evaluation of the ratio of expected benefits and potential risks.

Ovulation induction should be done under strict medical supervision.

In the initial stage of treatment may develop ovarian cyst.

Patients using contact lenses, there may be signs of eye irritation.

Given the intranasal method of administration, may result in irritation of the mucous membrane of the nose, and sometimes nasal bleeding. The drug can be used with rhinitis, however before use it is necessary to clear the nasal passages.

Effects on ability to drive and other mechanisms. Care should be taken when administering the drug to patients when driving vehicles and occupation potentially hazardous activities that require greater attention and speed of mental and motor reactions.