Buserelin is a synthetic antineoplastic drug substitute gonadotropin-releasing hormone.
Buserelin has antigonadotropnym (suppresses the production of pituitary gonadotropins), an anti-estrogen, anti-androgen (reduces blood levels of male sex hormones) and anti-tumor effect.
Buserelin is capable of binding to the cell receptors, located on the anterior pituitary gland, thereby stimulating an increase in the concentration of sex hormones in the blood. The two-week use of the drug in therapeutic doses results in blockage gonadotrophic pituitary function, reducing the synthesis of testosterone and education lyuteotropina foliotropina and participating in the reproductive system.
After buserelin women decreases the concentration of estrogen in the blood to postmenopausal levels in males and testosterone - to postcastration value. Reviews of buserelin indicate that the continuous use of the drug for 2-3 weeks leads to a "pharmacological castration" in men.
Maximum concentration in blood buserelin achieved 2-3 hours after administration (intramuscular administration), and drug level sufficient for effective therapy is maintained for 4 weeks.
The active ingredient of the drug is buserelin acetate. According to pharmacological action, and all other characteristics of the depot and Buserelin Buserelin Buserelin Long are analogues.
Clinical studies and reviews Buserelin confirm whether the use of the drug in:
- prostate cancer;
- breast cancer;
- uterine cancer;
- infertility (in vitro fertilization of the program);
- hyperplastic endometrium.
Mode of application
Buserelin is produced in the form of a lyophilisate for the preparation of a suspension, solution for injection, subcutaneous implants and nasal spray. Buserelin Buserelin Long depot and produced as a lyophilized (dried by gentle way) powder for suspension intended for intramuscular injection, and having an ability of sustained release.
Intranasally (in the nose)
When uterine fibroids, endometriosis, endometrial hyperplastic processes Buserelin applied 3 times daily to 150 mcg in each nostril. The interval between administration of the drug should be in the range of 6-8 hours.
The daily dose is 900 micrograms buserelin. Drug treatment should start within the first two days of menstruation.
In the treatment of infertility by IVF Buserelin assigned 150 mcg in each nostril four times during the day of application. The drug is administered to 21-24 days of the menstrual cycle until the time of administration of human chorionic gonadotropin in a dose sufficient to call ovulation.
Treatment of hormone dependent prostate cancer and uterine fibroids occurs by administration of 3, 75 mg buserelin, buserelin depot or buserelin Long once every 4 weeks. The course of treatment usually lasts 4-6 months, should start in one of the first days of the menstrual cycle. In the case of infertility treatment is administered once at the second day of the menstrual cycle in an amount of 3, 75 mg.
The method is practiced usually buserelin administration during 7 days of therapy, when applied 3 times a day at eight-hour intervals with 500 micrograms of the drug. On day 8, it is recommended to transfer the patient to the intranasal administration of buserelin 1, 2 mg partitioned 3-4 times daily.
Subcutaneous implants containing 6, 3 mg buserelin is administered 1 time per month to 2 side surface of the abdomen.
After buserelin many women have missed periods for six months or more in some patients (12-30%) are observed spotting, and at 1, 2% - uterine bleeding. Reviews of buserelin confirm that menstruation is usually renewed at 83-84 days after the last dose.
Side effects after buserelin, depots and buserelin Buserelin Long expressed to a small extent and, except in rare cases, do not require discontinuation of the drug:
- flushing of the skin (overflow blood vessels), urticaria, angioedema shock;
- nosebleeds, rash, impaired functions of the digestive tract, pulmonary embolism;
- "Pharmacological menopause";
- headache, depression, sleep disorders, frequent changes of mood;
- women - decreased libido, vaginal dryness, increased sweating, bone demineralization, abdominal pain, bleeding menstrualnopodobnoe;
- men - gynecomastia, impotence, urinary retention, lymphedema, muscle weakness in the legs, kidney swelling, pain in the bones.
After buserelin, the initial stage of its application may develop ovarian cysts.
Contraindications specified in the instructions to buserelin
Buserelin is not assigned in the following cases:
- hypersensitivity to buserelin acetate;
- pituitary tumor.
Buserelin, like his counterparts of the same name, produced in Russia, only Buserelin station - since 2003, and Buserelin Long - since 2010.
Store this medication at a temperature in the range of 8-20
Useful drug is considered to be within 2 years from the date of manufacture.