Buserelin-long FS

General characteristics. Structure:

Active ingredient: 3,93 mg of a buserelin of acetate (3,75 mg in terms of бусерелин).

Excipients: dl-milk and glycolic acids copolymer, d-Mannitolum, karmelloza of sodium, polysorbate-80.

Solvent: mannitol, solution of 0,8%.

Solvent: transparent colourless liquid. The recovered suspension: at addition of solvent and agitation homogeneous suspension of color, white or white with a weak yellowish shade, is formed; when standing suspension is besieged, but easily resuspended when stirring; suspension has to pass freely in the syringe through a needle No. 0840.

Pharmacological properties:

Pharmacodynamics. Synthetic analog of endogenous GNRG. Buserelin competitively contacts receptors of cells of a front share of a hypophysis, causing short-term increase in level of sex hormones in a blood plasma, further leads to total reversible block of gonadotropic function of a hypophysis, inhibiting, thus, allocation of LG and FSG.

Suppression of synthesis of sex hormones in gonads is as a result observed that is shown by decrease in concentration of oestradiol in a blood plasma to postclimacteric values at women and decrease in content of testosterone to postkastratsionny level at men. After the first introduction of a buserelin by 21st day at men concentration of testosterone decreases to postkastratsionny level (characteristic of a condition of an orchidectomy), i.e. pharmacological castration is caused. And at women concentration of oestradiol decreases to the level corresponding to an ovariectomy or a postmenopause.

Concentration of testosterone and oestradiol remains lowered during the entire period of the treatment which is carried out each 28 days that leads to growth inhibition and involution of hormonedependent tumors. After the termination of treatment physiological secretion of hormones is recovered.

Pharmacokinetics: Bioavailability is high. Cmax in plasma is reached approximately in 2–3 h after introduction in oil and remains at the level sufficient for inhibition of synthesis of gonadotrophins a hypophysis not less than 4 weeks.

Indications to use:

- Hormonedependent prostate cancer.

- Breast cancer.

- Endometriosis (before - and postoperative the periods).

- Hysteromyoma.

- Hyperplastic processes of an endometria.

- Treatment of infertility (when carrying out the program of extracorporal fertilization (EKO)).

Route of administration and doses:

At a hormonedependent prostate cancer of Buserelin-long of FS enter in a dose 3,75 mg (1 injection) intramusculary each 4 weeks (in oil). At treatment of endometriosis, hyperplastic processes of an endometria the drug is administered in a dose of 3,75 mg in oil once by each 4 weeks. Treatment should be begun in the first five days of a menstrual cycle. Treatment duration – 4 - 6 months.

At treatment of a hysteromyoma of Buserelin-long of FS enter in a dose 3,75 mg in oil once each 4 weeks. Treatment should be begun in the first five days of a menstrual cycle. Treatment duration – before operation 3 months, in other cases - 6 months.

At treatment of infertility by method of extracorporal fertilization (EKO) Buserelin-long of FS enter in a dose 3,75 mg (1 injection) in oil once at the beginning of follikulinovy (for the 2nd day of a menstrual cycle) or in the middle of a lyuteinovy phase (21 - 24 days) of the menstrual cycle preceding stimulation. After blockade of the pituitary function confirmed with decrease in concentration of estrogen in blood serum not less than for 50% of initial level (usually is defined in 12 - 15 days after an injection of Buserelin-long of FS), in the absence of oothecomas (according to ultrasonography), endometria thickness no more than 5 mm, stimulation of a superovulation under ultrasonic monitoring and control of level of oestradiol in blood serum begins gonadotropic hormones.

Rules of preparation of suspension and administration of drug:
1. The drug is administered only intramusculary
2. Suspension for an injection in oil is prepared just before introduction by means of the enclosed solvent.
3. Drug has to prepare and be entered by only specially trained medical personnel.
4. FS you discipline a bottle with Buserelin-long vertically. Easily tapping on a bottle, achieve that all lyophilisate was at the bottom of a bottle.

 

Figure 1. The correct provision of a bottle with preparatom.5. Open the syringe, attach to it a needle of 1,2 mm x 50 mm in size for a solvent intake.
6. Open an ampoule with solvent and gather all contents of an ampoule in the syringe, install the syringe on a dose of 2 ml.

 

 

 Figure 2. Opening of an ampoule with solvent.

   

Figure 3. An ampoule contents fence order in the syringe.

 

Figure 4. Rules of installation of required amount of liquid in the syringe.

7. Remove a plastic lid from the bottle containing lyophilisate. Disinfect a rubber bung of a bottle a spirit tampon. Insert a needle into a bottle with lyophilisate through the center of a rubber bung and carefully enter solvent on an internal wall of a bottle, without concerning a bottle contents needle. Take out the syringe from a bottle.

 

Figure 5. Preparation and disinfection of a cover of a bottle with drug.

Figure 6. Administration of solvent in a bottle with drug.

8. The bottle has to remain solvent of lyophilisate and formation of suspension, motionless before full treatment (approximately for 3 – 5 minutes). Then, without overturning a bottle, check availability of dry lyophilisate at walls and a bottom of a bottle. At detection of the dry remains of lyophilisate, leave a bottle before full treatment.

 

Figure 7. Verification of presence of the dry rest in a bottle.

9. After you were convinced of lack of the remains of dry lyophilisate, carefully mix bottle contents roundabouts within 30-60 seconds before formation of homogeneous suspension. Do not overturn and do not stir up a bottle. 

 

Figure 8. Preparation of homogeneous suspension (slow rotation of a bottle).

10. Quickly insert a needle through a rubber bung into a bottle. Then lower a cut of a needle down and, having inclined a bottle at an angle of 45 degrees, slowly gather in the syringe suspension completely. Do not overturn a bottle at set. A small amount of drug can remain on walls and day of a bottle. The expense on the rest on walls and day of a bottle is considered. Right after a set of solution remove a needle. Replace with a needle of 0,8 mm x 40 mm in size, accurately turn the syringe and remove air from the syringe.

 

Figure 9. A drug intake order in the syringe.

Figure 10. The correct provision of a bottle at a drug intake in the syringe.

Figure 11. A technique of removal of air from the syringe.

11. You enter FS Buserelin-long suspension immediately after preparation.

12. By means of a spirit tampon disinfect the place of an injection. Enter a needle deeply into a gluteus, then slightly delay the syringe piston back to be convinced that there are no damages of a vessel. Enter suspension slowly with constant pressing the syringe piston. At a needle blockage, replace it with other needle of the same diameter.

13. At repeated injections the left and right parties should be alternated.

Features of use:

At women. Patients with any form of a depression during treatment by drug have to be under careful observation of the doctor.

Induction of an ovulation should be carried out under strict medical observation. In an initial stage of treatment by drug development of an oothecoma is possible.

Prior to treatment it is recommended to exclude pregnancy and to stop reception of hormonal contraceptives, however within the first two months of use of drug it is necessary to apply other (non-hormonal) methods of contraception.

After the treatment termination function of ovaries is recovered. The first periods renew in 3 months.

At men. For the purpose of effective prevention of possible side effects in the first phase of effect of drug use of anti-androgens in two weeks prior to the first injection of Buserelin-long of FS and for two weeks after the first injection is necessary.

Influence on ability to drive the car and other mechanisms. It is necessary to be careful at purpose of drug to the patients who are engaged in potentially dangerous types of activity, requiring special attention and speed of mental and motor reactions.

Side effects:

Allergic reactions: a small tortoiseshell, a dermahemia, it is rare - a Quincke's disease.

From TsNS: frequent change of mood, sleep disorder, depression, headache.

From a musculoskeletal system: at prolonged use - demineralization of bones that is risk of development of osteoporosis.

Women have a headache, a depression, perspiration and change of a libido, dryness of a mucous membrane of a vagina, pain in the bottom of a stomach, is rare - menstrualnopodobny bleeding (within the first weeks of treatment).

At men, at cancer therapy of a prostate - within the first 2 - 3 weeks after the first injection бусерелин can cause an aggravation and progressing of a basic disease (it is connected with stimulation of synthesis of gonadotrophins and, respectively, testosterone), a gynecomastia, "inflows", the strengthened sweating and decrease in a potentiality (seldom demands therapy cancellation), passing increase in concentration of androgens in blood, an urination delay, "renal hypostases" - face edemas, a century, legs are possible; muscular weakness in the lower extremities. In an initiation of treatment of patients with a prostate cancer there can be temporary strengthening of an ostealgia; in this case it is necessary to carry out symptomatic therapy. Noted separate cases of development of impassability of ureters and a prelum of a spinal cord.

Others: in isolated cases (relationship of cause and effect is accurately not established) -
thromboembolism of a pulmonary artery, dispepsichesky disturbances.

Interaction with other medicines:

Simultaneous use of the drug "Buserelin-long FS" with the drugs containing sex hormones (for example, in the mode of induction of an ovulation), can promote emergence of a syndrome of hyper stimulation of ovaries.

At simultaneous use of Buserelin-long of FS can reduce efficiency of hypoglycemic means.

Contraindications:

- pregnancy;
- lactation period;
- hypersensitivity to drug components.

Overdose:

Now about overdoses it was not reported.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

The lyophilisate for preparation of suspension for intramuscular introduction of the prolonged action containing 3,75 mg of a buserelin in bottles of dark glass and cardboard packs.