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Active ingredient: 3,75 mg of a buserelin.
- 200 mg — dl-milk and glycolic acids;
- 30 mg — a karmelloza of sodium;
- 85 mg — d-Mannitolum;
- 2 mg — polysorbate-80.
As solvent apply 0,8% mannitol solution in 1 ml of water to injections.
Lyophilisate for suspension production (the prolonged action) for carrying out intramuscular injections. One packaging contains one bottle of drug + solvent.
Pharmacodynamics and pharmacokinetics
Buserelin Long – the antineoplastic medicine which is analog of GRF.
The mechanism of action of Buserelin consists in his ability to cause short-term increase in a blood plasma of sex hormones, thanks to competitive linkng with the cellular receptors which are on a front share of a hypophysis.
Administration of drug in medical doses leads to full blocking of gonadotropic pituitary function (on average in 12-14 days). Buserelin lowers production of LG, FSG, and also testosterone and leads to oppression in gonads of synthesis of sex hormones. At women concentration of oestradiol reaches postclimacteric values, at men the content of testosterone falls to values of the postkastratsionny period.
At the continuous therapy lasting for 2-3 weeks concentration of testosterone considerably goes down, reaching a condition of an orkhiektomiya, that is there is a pharmacological castration.
After carrying out an intramuscular injection bioavailability high.
TCmax, is reached for 2-3 hours after introduction of one dose of 3,75 mg and remains at the level sufficient for further oppression by a hypophysis (not less than 4 weeks) of synthesis of gonadotrophins.
Indications to use
- hormonedependent prostate cancer (prostate);
- endometriosis (before an operative measure and after it);
- breast cancer;
- hyperplastic pathologies of an endometria;
- within carrying out the EKO program (extracorporal fertilization), for treatment of infertility.
- hypersensitivity to drug components;
- period of pregnancy and lactation.
- progressing or aggravation of a basic disease, and also the strengthening of pain in bones demanding a symptomatic treatment — at therapy of a prostate cancer (the first weeks of treatment);
- rushes of blood to the person;
- the strengthened sweating;
- passing increase in concentration in blood of androgens;
- hypostases (legs, century, persons);
- muscular weakness in legs;
- urination delay;
- decrease in a potentiality (can sometimes demand cancellation or replacement of therapy);
- exceptional cases of pressure upon a spinal cord and impassability of ureters are recorded.
- menstrualnopodobny bleedings;
- sleep disorders;
- frequent change of mood;
- the increased sweating;
- dryness of a vagina;
- pains in a stomach bottom;
- decrease in a libido.
- small tortoiseshell;
- demineralization of bones (there is a risk of development of osteoporosis);
- extremely seldom (several cases are described) — dispeptic manifestations and a thromboembolism of a pulmonary artery of an unspecified origin.
Application instruction (Way and dosage)
At purpose of drug Buserelin-Long the application instruction indicates his introduction exclusively intramusculary.
Preparation of suspension for intramuscular injections is carried out just before introduction procedure, using the solvent entering packaging.
Production of ready suspension, as well as medicine input process, only specially prepared medical personnel have to be engaged.
The recommended doses, duration of therapy and the recommendation to drug use Buserelin-Long are given at various pathologies below.
Hormonedependent prostate cancer — one intramuscular injection in a dose of 3,75 mg every 4 week.
Hyperplastic changes of an endometria and endometriosis — therapy begin in the first 5 days of a menstrual cycle in the single dose 3,75 mg entered every 4 week with a course of treatment of 4-6 months.
The hysteromyoma – a single dose of an intramuscular injection makes 3,75 mg of Buserelin-Long, every 4 week. Treatment is begun in the first 5 days of a menstrual cycle, with a therapy course, before an operative measure – 3 months, and 6 months in other cases.
Therapy of infertility (EKO program) – the application instruction recommends purpose of 1 injection of drug Buserelin-Long in the dose of 3,75 mg entered intramusculary for the 2nd days of a menstrual cycle (carrying out an injection for 21-24 days of a menstrual cycle is possible) before hyper stimulation. After confirmation of oppression of pituitary function about which tells lowering in blood serum of concentration of estrogen (not less than 50%) appoint use of gonadotropic hormones. Treatment is carried out in the absence of cysts of ovaries, under control of concentration of oestradiol and with use of ultrasonic monitoring.
There are no confirmed data on overdose cases drug Buserelin-Long.
Simultaneous therapy by drug Buserelin Long and medicines which part sex hormones are (for example, in the course of carrying out induction of an ovulation) can promote emergence of a syndrome of hyper stimulation of ovaries.
Buserelin-Long can lower effect of hypoglycemic drugs, at their simultaneous use.
Terms of sale
According to the recipe.
Drug Buserelin-Long belongs to the list B. It is necessary to store in the dark, unavailable place for children, at a temperature not above 25 °C.
Period of validity
For the purpose of effective prevention of potential side effects, mainly observable in the first phase of action of Buserelin-Long, recommend purpose of the anti-androgenic drugs used in 2 weeks prior to the first introduction and within 2 weeks after an injection.
At symptoms of a depression, in time carrying out therapy by drug Buserelin-Long, the patient has to be under continuous supervision of the attending physician.
The induction of an ovulation is carried out under strict control, in special clinic, the doctor having experience of carrying out similar therapy. The patient has to undergo all appointed procedures and follow all recommendations of medical personnel.
At the beginning of therapy with medicine use Buserelin-Long, in certain cases observed development of cysts of ovaries.
After drug withdrawal Buserelin-Long function of ovaries is recovered, as a rule, in 3 months.
It is necessary to be careful when driving the car and during the work which demands high concentration of attention.
Coincidence on the ATH code of the 4th level:
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