Золадекс 10.8 mg

General characteristics. Structure:

Active agent: a gozerelina acetate of 10,8 mg (in terms of the gozerelin-basis)
Excipients: milk and glycolic acids copolymer (50:50) to the lump of 18,0 mg (the mg drug Золадекс® 3,6), low-molecular copolymer (95:5) of milk and glycolic acids and high-molecular copolymer (95:5) of milk and glycolic acids to the lump of 36,0 mg (a ratio between low-molecular and high-molecular copolymer – 3:1, on weight) (the mg drug Золадекс® 10,8).
DESCRIPTION
White or cream cylindrical pieces of solid polymeric material, free or almost free from visible inclusions.

Pharmacological properties:

Pharmacodynamics. Золадекс® the gonadotrophin-rileasing of hormone (GNRG) is a synthetic analog natural. At constant use the drug Zoladeks® inhibits allocation by a hypophysis of the luteinizing hormone (LH) that leads to decrease in concentration of testosterone in blood serum at men and concentration of oestradiol in blood serum at women. This effect is reversible after therapy cancellation. At an initial stage the drug Zoladeks®, like other agonists of GNRG, can cause temporary increase in concentration of testosterone in blood serum in men and concentration of oestradiol in blood serum in women. At early stages of therapy by the drug Zoladeks® at some women vaginal bleedings of various duration and intensity can be noted.
At men approximately by 21 days after introduction of the first capsule concentration of testosterone decreases to kastratsionny levels and continues to remain reduced at the continuous treatment which is carried out each 28 days in case of the drug Золадекс® 3,6 of mg or each 3 months in case of the mg drug Золадекс® 10,8. Such decrease in concentration of testosterone against the background of use of the drug Золадекс® 3,6 of mg for most of patients leads to regression of a tumor of a prostate and to symptomatic improvement.
At women concentration of oestradiol in serum decreases also approximately by 21 days after introduction of the first capsule of the drug Золадекс® 3,6 of mg and, at regular administration of drug each 28 days, remains lowered to level comparable with what is observed at women in a menopause. This decrease results in positive effect at hormonal and dependent forms of a breast cancer, endometriosis, fibromas of a uterus and suppression of development of follicles in ovaries. It also causes thinning of an endometria and is an amenorrhea origin at most of patients.
After administration of the drug Золадекс® 10,8 of mg concentration of oestradiol in serum at women decreases within 4 weeks after introduction of the first capsule and remains lowered to level comparable with what is observed at women in a menopause. At initial use of other analogs of GNRG and transition to the mg drug Золадекс® 10,8, suppression of level of oestradiol remains. Suppression of level of oestradiol results in medical effect at endometriosis and fibromas of a uterus.
It is shown that the mg drug Золадекс® 3,6 in a combination with iron preparations causes an amenorrhea and increase in level of hemoglobin and the corresponding hematologic parameters in women with fibromas of a uterus and the accompanying anemia.
Against the background of reception of agonists of GNRG at women approach of a menopause can take place. Seldom, some women have no recovery of periods after the end of therapy.
Administration of the drug Золадекс® 3,6 of mg each four weeks or the mg drug Золадекс® 10,8 each 12 weeks provides maintenance of effective concentration. Cumulation in fabrics at the same time does not happen. The drug Zoladeks® badly contacts protein, and the elimination half-life it makes 2 - 4 hours at patients with normal function of kidneys of blood serum. The elimination half-life increases at patients with disturbances of renal function. At monthly administration of the drug Золадекс® 3,6 of mg or the drug Золадекс® 10,8 of mg this change will not have considerable effects therefore it is not required to change a dose for these patients. At patients with a liver failure of considerable changes in pharmacokinetics it is not observed.

Pharmacokinetics. Administration of the drug Золадекс® 3,6 of mg each four weeks or the mg drug Золадекс® 10,8 each 12 weeks provides maintenance of effective concentration. Cumulation in fabrics at the same time does not happen. The drug Zoladeks® badly contacts protein, and the elimination half-life it makes 2 - 4 hours at patients with normal function of kidneys of blood serum. The elimination half-life increases at patients with disturbances of renal function. At monthly administration of the drug Золадекс® 3,6 of mg or the drug Золадекс® 10,8 of mg this change will not have considerable effects therefore it is not required to change a dose for these patients. At patients with a liver failure of considerable changes in pharmacokinetics it is not observed.

Indications to use:

For the mg drug Золадекс® 10,8
• Prostate cancer
• Endometriosis
• Uterus fibromas

Route of administration and doses:

Adult men
Mg drug Золадекс® 10,8
The drug Золадекс® 10,8 of mg is administered subcutaneously in a front abdominal wall by each 3 months.
Adult women
The drug Золадекс® 10,8 of mg is administered subcutaneously in a front abdominal wall by each 12 weeks.
Patients of advanced age, patients with a renal or liver failure: dose adjustment is not required.

Features of use:

• It is necessary to appoint with care the drug Zoladeks® to the males subject to extra risk of emergence of impassability of ureters or prelums of a spinal cord. At these patients it is necessary to carry out careful monitoring within the first month of therapy. If the prelum of a spinal cord or the renal failure caused by ureteric impassability take place or develop, it is necessary to appoint treatment, standard for these complications.
• At women the drug Золадекс® 10,8 of mg is shown only for treatment of endometriosis and fibromas of a uterus. For the women needing treatment gozereliny according to other indications use the mg drug Золадекс® 3,6.
• When using the drug Zoladeks® at women before recovery of periods non-hormonal methods of contraception have to be applied.
• As well as when using other analogs of GNRG, at use of the drug Золадекс® 3,6 of mg in a combination with a gonadotrophin, it was reported about exceptional cases of development of a syndrome of hyper stimulation of ovaries (SGSYa). It is supposed that the desensitization caused by use of the drug Золадекс® 3,6 of mg can lead in some cases to increase in a necessary dose of a gonadotrophin. It is necessary to monitorirovat carefully stimulation of a cycle to reveal patients with risk of development of SGSYa as expressiveness and frequency of manifestations of a syndrome can depend on the dose mode of a gonadotrophin. Introduction of a chorionic gonadotrophin of the person needs to be stopped if it is required.
• Use of agonists of GNRG for women can cause decrease in mineral density of a bone tissue. After the end of treatment most of women has a recovery of mineral density of a bone tissue. At the patients receiving the mg drug Золадекс® 3,6 for treatment of endometriosis, addition of gormono-replacement therapy (oestrogenic and progestagenny drugs daily) reduced loss of mineral density of bones and vasculomotor symptoms. There is no experience of use of gormono-replacement therapy at treatment by the mg drug Золадекс® 10,8 now.
• Resuming of periods after the end of treatment by the drug Zoladeks® at some patients can happen to a delay. In rare instances at some women during treatment by analogs of GNRG approach of a menopause without recovery of periods after the end of therapy can take place.
• Use of the drug Zoladeks® can lead to increase in cervical resistance, it is necessary to be careful at dilatation of a neck of uterus.
• There are no data on efficiency and safety of therapy by the drug Zoladeks® of benign gynecologic diseases lasting more than 6 months.
• The drug Золадекс® 3,6 of mg has to be used at extracorporal fertilization only under observation of the specialist having experience in this area.
• It is recommended to use with care the mg drug Золадекс® 3,6 at extracorporal fertilization at patients with a syndrome of polycystic ovaries as stimulation of a large number of follicles is possible.
• According to preliminary data use of a bisfosfonat in a combination with GNRG agonists at men promotes reduction of loss of mineral density of a bone tissue. Due to a possibility of development of decrease in tolerance to glucose against the background of reception of agonists of GNRG at men, it is recommended to control periodically the content of glucose in blood.
INFLUENCE ON ABILITY TO DRIVE THE CAR AND OTHER MECHANISMS
There are no data that the drug Zoladeks® leads to deterioration in these types of activity.

Side effects:

Frequency of emergence of undesirable effects is presented as follows:
Often (> 1/100, <1/10); Infrequently (> 1/1000, <1/100); Seldom (> 1/10 000, <1/1 000); Very seldom (<1/10 000), including separate messages.
New growths
Very seldom: hypophysis tumor.
Not specified frequency: a degeneration of fibromatous nodes at women with uterus fibroma.
From immune system
Infrequently: hypersensitivity reactions.
Seldom: anaphylactic reactions.
From endocrine system:
Very seldom: hemorrhage in a hypophysis.
Metabolic disturbances:
Often: disturbance of tolerance to glucose. At the men receiving GNRG agonists decrease in tolerance to glucose was observed. Decrease in tolerance to glucose was shown by development of a diabetes mellitus or deterioration in control over glucose level in blood at patients with a diabetes mellitus in the anamnesis.
Infrequently: a hypercalcemia (at women).
From a nervous system and the mental sphere:
Very often: the decrease in a libido connected with pharmacological effect of drug and, in rare instances, leading to its cancellation.
Often: decrease in mood, a depression (at women), paresthesia, a prelum of a spinal cord (at men), a headache (at women).
Very seldom: psychotic frustration.
From cardiovascular system:
Very often: the inflows connected with pharmacological effect of drug and, in rare instances, leading to its cancellation.
Often: a myocardial infarction (at men); heart failure (at men) which risk increases at co-administration of anti-androgenic drugs. Change of level of arterial pressure, shown as hypotension or hypertensia. These changes usually tranzitorny, are also allowed or in the course of therapy by the drug Zoladeks®, or after its termination. In rare instances these changes demanded medical intervention, including drug withdrawal of Zoladeks®.
From skin and hypodermic cellulose:
Very often: the increased perspiration connected with pharmacological effect of drug and, in rare instances, leading to its cancellation.
Often: an alopecia (at women), as a rule, slightly expressed, including, at young patients with high-quality new growths; the rash which generally is slightly expressed which was often resolved against the background of therapy continuation.
Not specified frequency: an alopecia (at men) which was shown as a hair loss on all body owing to decrease in level of androgens.
From a musculoskeletal system:
Often: an arthralgia (at women), an ostealgia (at men). In an initiation of treatment patients with cancer of a prostate can often experience temporary strengthening of an ostealgia which is treated symptomatic.
Infrequently: an arthralgia (at men).
From urinogenital system:
Very often: erectile dysfunction (at men), dryness of a mucous membrane of a vagina and increase in the size of mammary glands (at women).
Often: a gynecomastia (at men).
Infrequently: morbidity of chest glands (at men), obstruction of ureters (at men)
Seldom: an oothecoma (at women), a syndrome of hyper stimulation of ovaries (at women, at combined use with gonadotrophins).
Not specified frequency: vaginal bleeding (at women)
Others:
Very often: reaction in a drug injection site (at women)
Often: reaction in a drug injection site (at men); temporary strengthening of symptoms of a disease at patients with a breast cancer at the beginning of therapy.
Laboratory researches:
Often: decrease in mineral density of a bone tissue, increase in body weight.

Interaction with other medicines:

It is not known.

Contraindications:

- Hypersensitivity to a gozerelin or other analogs of GNRG
- Pregnancy and lactation
- Children's age
WITH CARE
Males subject to extra risk of emergence of impassability of ureters or prelums of a spinal cord. At extracorporal fertilization at patients with a syndrome of polycystic ovaries.

Overdose:

Experience of overdose of drug at people is limited. In case of inadvertent administration of the drug Zoladeks® before of term or in higher dose clinically significant undesirable phenomena were not noted. Data on overdose are not available for people. In case of overdose the patient should appoint a symptomatic treatment.

Storage conditions:

To store at a temperature below 25 °C. To store in the places unavailable to children. Period of validity 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

The capsule for hypodermic introduction of the prolonged action 10, 8 mg in the syringe applicator with the protective mechanism (System of safe introduction Safety Glide).
One syringe applicator is located in the laminated aluminum envelope. The envelope with movably attached tag summary is located in a cardboard pack with the application instruction.