Buserelin Long powder 3.75mg #1

Buserelin Long instruction

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Composition

Active ingredient: 3.75 mg buserelin.
Additional Ingredients:
    200 mg - dl-lactic and glycolic acids;
    30 mg - carmellose sodium;
    85 mg of d-mannitol;
    2 mg - polysorbate-80.
As a solvent, 0.8% mannitol in 1 ml of water for injection is used.

Form of issue

Lyophilizate for the manufacture of a suspension (prolonged action) for intramuscular injection. One package contains one bottle of the drug + a solvent.

pharmachologic effect

Antiandrogenic, antitumor.

Pharmacodynamics and pharmacokinetics

Buserelin Long is an antitumor drug that is analogous to GFR.
The mechanism of action of Buserelin Long in its ability to cause a short-term increase in the blood plasma sex hormones, due to competitive binding to cellular receptors located on the anterior lobe of the pituitary gland.
Administration of the drug in therapeutic doses leads to complete blockage of gonadotropic pituitary function (on average 12-14 days). Buserelin lowers the production of LH, FSH, and testosterone and leads to inhibition of gonads in the synthesis of sex hormones. In women, the concentration of estradiol reaches post-menopausal values, in men the content of testosterone drops to the post-stress period.
With continuous therapy lasting for 2-3 weeks the concentration of testosterone decreases significantly, reaching the state of orchiectomy, that is, pharmacological castration occurs.
After carrying out intramuscular injection, bioavailability is high.
TCmax, is achieved within 2-3 hours after the administration of a single dose of 3.75 mg and remains at a level sufficient for further inhibition of gonadotropin synthesis by at least 4 weeks by the pituitary (at least 4 weeks).

Indications for use

    hormone-dependent prostate cancer (prostate);
    endometriosis (before surgery and after it);
    uterine myoma;
    mammary cancer;
    hyperplastic pathology of the endometrium;
    in the framework of the IVF program (in vitro fertilization), for the treatment of infertility.

Contraindications

    hypersensitivity to the components of the drug;
    period of pregnancy and lactation.

Side effects

In men:

    progression or exacerbation of the underlying disease, as well as increased pain in the bones, requiring symptomatic treatment - in the treatment of prostate cancer (the first weeks of treatment);
    flushes of blood to the face;
    gynecomastia;
    increased sweating;
    a transient increase in the concentration of androgens in the blood;
    edema (legs, eyelids, faces);
    muscle weakness in the legs;
    retention of urination;
    decreased potency (sometimes may require cancellation or replacement therapy);
    recorded rare cases of pressure on the spinal cord and ureter obstruction.

Among women:

    menstrual like bleeding;
    depression;
    sleep disorders;
    frequent changes of mood;
    headache;
    increased sweating;
    tides;
    dryness of the vagina;
    pain in the lower abdomen;
    decreased libido.

Are common:

    hyperemia of the skin;
    hives;
    demineralization of bones (there is a risk of osteoporosis);
    extremely rare (several cases have been described) - dyspeptic manifestations and thromboembolism of the pulmonary artery of unknown origin.

Instructions for use (Method and dosage)

With the appointment of Buserelin-Long, the instructions for use indicate its administration exclusively by intramuscular injection.
Preparation of suspension for intramuscular injection is carried out immediately before the procedure of administration, using the solvent entering into the package.
The preparation of the finished suspension, as well as the process of drug administration, should be handled only by specially trained medical personnel.
Below are the recommended doses, duration of therapy and recommendations for the use of the drug Buserelin-Long in various pathologies.
Hormone-dependent prostate cancer is one intramuscular injection at a dose of 3.75 mg every 4 weeks.
Hyperplastic changes in the endometrium and endometriosis - therapy begin in the first 5 days of the menstrual cycle in a single dose of 3.75 mg, administered every 4 weeks, with a course of treatment of 4-6 months.
Myoma of the uterus - a single dose of intramuscular injection is 3.75 mg Buserelina-Long, every 4 weeks. Treatment begins in the first 5 days of the menstrual cycle, with the course of therapy, before the surgery - 3 months, and 6 months in other cases.
Infertility therapy (IVF program) - Instruction for use recommends the appointment of 1 injection of the drug Buserelin-Long at a dose of 3.75 mg, administered intramuscularly on the 2nd day of the menstrual cycle (it is possible to inject on the 21-24th day of the menstrual cycle) before hyperstimulation. After confirming the oppression of the pituitary gland, indicated by a decrease in serum levels of estrogen (not less than 50%), the administration of gonadotropic hormones is prescribed. The treatment is performed in the absence of ovarian cysts, under the control of the concentration of estradiol and using ultrasound monitoring.

Overdose

There is no confirmed data on cases of overdose with Buserelin-Long.

Interaction

Simultaneous therapy with Buserelin Long and drugs, which include sex hormones (for example, during induction of ovulation), can contribute to the emergence of the syndrome of ovarian hyperstimulation.
Buserelin-Long can reduce the effect of hypoglycemic drugs, with their simultaneous application.

Storage conditions

The drug Buserelin-Long refers to the list B. It should be stored in a dark, inaccessible place for children, at a temperature of no higher than 25 ° C.
Shelf life - 24 months.

special instructions

For men

In order to effectively prevent potential side effects, mainly observed in the first phase of the Buserelin-Long action, the use of antiandrogenic drugs, applied 2 weeks before the first administration and within 2 weeks after the injection, is recommended.

Among women

When signs of depression, during the treatment with Buserelin-Long, the patient should be under constant supervision of the attending physician.
Induction of ovulation is carried out under strict control, in a special clinic, by a doctor who has experience of such therapy. The patient must undergo all prescribed procedures and follow all the recommendations of medical personnel.
At the beginning of therapy with the use of the drug Buserelin-Long, in some cases, the development of ovarian cysts was observed.
Before the appointment of therapy, pregnancy should be excluded and the use of hormonal contraceptives should be suspended, with the transition to other contraceptives during the first 2 months of treatment.
After the cancellation of the drug Buserelin-Long, the function of the ovaries is restored, usually after 3 months.
Care must be taken when driving a car and when working, which requires a high concentration of attention.

Children

There is no reliable information about the use of the drug Buserelin-Long in childhood.

With alcohol

It is necessary to refrain from drinking alcohol during the treatment.

In pregnancy and lactation

Contraindicated.

Reviews about Buserelin Long

The doctors' comments on the effectiveness of Buserelin-Long, for the treatment of the above-described diseases are mostly positive, Buserelin has especially proved itself in the infertility treatment as part of the IVF program.
However, all the doctors who conduct therapy with this group of drugs note frequent negative manifestations observed during the treatment, which is confirmed by reviews of side effects of Buserelin-Long in user forums.
Among the side effects of the drug most often called: hot flashes, bleeding, depression, decreased libido and mood swings.