This effect is reversible after discontinuation. At the initial stage of preparation , like other GnRH agonists, can cause a temporary increase in the concentration of testosterone primobolan steroid in serum in men and estradiol concentrations in the serum of women. In the early stages of therapy with , some women may experience vaginal bleeding of varying duration and intensity.
In men by around 21 days after the first capsule concentration of testosterone is reduced to castrate levels and continues to be reduced at a constant treatment, conducted every 28 days in the case of the drug mg every 3 months, or when the drug . This reduction in the concentration of testosterone during treatment with the drug mg in most patients results in a regression of prostate tumors and symptomatic improvement.
In women, serum estradiol concentration is reduced also to about 21 days after the first capsule formulation , with regular administration of the drug every 28 days, is reduced to a level comparable to that seen in postmenopausal women. This reduction leads to a positive effect on hormone-dependent forms of breast cancer, endometriosis, uterine fibroids and suppressing the development of follicles in the ovaries. It also causes a thinning of the endometrium and cause amenorrhea in most patients.
After administration mg estradiol primobolan steroid concentration in serum decreases in women within 4 weeks after the first capsule and is reduced to a level comparable to that observed in menopausal women. When initial application of other GnRH analogues, and the transition to the drug 10.8 mg estradiol suppression is maintained. Estradiol suppression leads to a therapeutic effect in endometriosis and uterine fibroids.
It is shown that the drug 3.6 mg in combination with iron supplementation causes amenorrhea and increased hemoglobin and related haematological parameters in women with fibroids and associated anemia.
On receiving background GnRH agonists in women may occur menopause. Rarely, some women there is no recovery of menstruation after the end of therapy.
Introduction formulation 3.6 mg every four weeks or formulation Zoladex ® 10.8 mg every 12 weeks maintains effective concentrations. Accumulation in the tissues at the same time does not occur. Preparation binds poorly to protein and its half-life from the blood serum is 2 – 4 hour front patients with normal renal function. The half-life is increased in patients with impaired renal function. When the monthly administration of the drug 3.6 mg or drug 10.8 mg of this change will have significant effects, so change the dose for these patients is not required. Patients with liver failure significant changes in the pharmacokinetics was observed.
For the drug Zoladex ® 3.6 mg
- Prostate cancer
- Mammary cancer
- uterine fibroids
- For thinning the endometrium during planned operations on the endometrium
- In vitro fertilizationFor the drug Zoladex ® 10.8 mg
- Prostate cancer
- uterine fibroidsCONTRAINDICATIONS
– Hypersensitivity to goserelin or other analogues of GnRH
– Pregnancy and lactation
– Children’s ageWITH CARE
Persons male at special risk of ureteral obstruction or spinal cord compression. In extra-corporeal fertilization in patients with polycystic ovary syndrome.
DOSAGE AND ADMINISTRATION The drug Zoladex ® 3.6 mg Adults drug Zoladex ® 3.6 mg injected subcutaneously into the anterior abdominal wall every 28 days. – In malignancies is long – in benign gynecological disorders are not more than 6 months – for thinning the endometrium do two injections at intervals of 4 weeks, with the uterus ablation recommended during the first two weeks after the second dose.
In vitro fertilization
drug Zoladex ® 3.6 mg used for pituitary desensitization. Desensitization is defined by the concentration of estradiol in the serum. As a rule, the required level of estradiol, which corresponds to that in the early follicular phase of the cycle (about 150 pmol / L), reached between 7 and 21 days. When the desensitization start superovulation (controlled ovarian stimulation) using gonadotropin. Pituitary desensitization caused when applying the depot GnRH agonist may be more stable, which may lead to an increased need for gonadotropins. At the appropriate stage of follicular gonadotropin administration stops further human chorionic gonadotrophin is administered to induce ovulation. Control of the performed treatment, the procedure primobolan steroid of oocyte retrieval and fertilization are carried out in accordance with the established practice of the medical establishment.
The drug Zoladex ® 10.8 mg Adult men drug Zoladex ® 10.8 mg is administered subcutaneously in the abdominal wall every 3 months.
drug Zoladex ® 10.8 mg is administered subcutaneously in the anterior abdominal wall every 12 weeks.
Elderly patients, patients with renal or hepatic impairment: Dosage adjustment is not required.
The frequency of adverse effects were as follows:
often (> 1/100, <1/10); Uncommon (> 1/1000, <1/100); Rare (> 1/10 000, <1/1 000); Very rare (<1/10 000), including isolated reports.
Very rare: pituitary tumor.
Unspecified frequency: Degeneration fibromatous nodes in women with uterine fibroids.
Uncommon:. Hypersensitivity reactions
Rare: anaphylactic reactions.
From endocrine system:
Very rare: bleeding in the pituitary gland.
Common: impaired glucose tolerance. In men receiving GnRH agonists, there was a decrease in glucose tolerance. Impaired glucose tolerance was manifested the development or worsening of diabetes control blood glucose levels in patients with diabetes mellitus in anamnesis.
Uncommon: hypercalcaemia (in women).
From the nervous system and psychiatric:
Very common: decreased libido associated with the pharmacological action of the drug and, in rare cases, lead primobolan steroid to its cancellation.
Often: depressed mood, depression (in women), paresthesia, and compression of the spinal cord (in men) , headache (in women).
Very rare: psychotic disorder.
Very common: hot flushes associated with the pharmacological action of the drug and, in rare cases, lead to its cancellation.
Common: myocardial infarction (men); heart failure (for men), the risk of which is increased with concomitant administration of anti-androgen drugs. Changes in blood pressure, manifest as hypotension or hypertension. These changes are usually transient, and resolved either in the course of therapy with Zoladex ® , or after its termination. In rare cases, these changes require medical intervention, including the abolition of the drug Zoladex ® .
Skin and subcutaneous tissue:
Very common: sweating, associated with the pharmacological action of the drug and, in rare cases, lead to its cancellation.
Common: alopecia (for women), as a rule, slightly expressed, including, in young patients with benign tumors; rash, mostly slightly pronounced, which is often resolved on the background of continued therapy.
unspecified frequency: alopecia (males) which manifested itself as hair loss throughout the body due to the decline in androgen levels.
From the musculoskeletal system:
Common: arthralgia (in women), bone pain (in males). At the beginning of the treatment of patients with prostate cancer can often experience a temporary increase in bone pain, which is treated symptomatically.
Uncommon: arthralgia (men).
With the genitourinary system:
Very common: erectile dysfunction (males), dryness of the vaginal mucosa and increasing the size of the breast (in women).
Often: gynecomastia (male).
Uncommon: painful breast (men), ureteral obstruction ( men)
rare: ovarian cysts (women), ovarian hyperstimulation syndrome (in women when combined with gonadotropin).
, unspecified frequency: vaginal bleeding (in women)
Very common: the reaction at the site of injection (in women)
often: a reaction at the site of injection (for men); temporary increase of symptoms in patients with breast cancer in early therapy.
Common: decrease in bone mineral density, increased body mass index
of drug overdose experience in humans is limited. In case of accidental administration of the drug Zoladex ® first period or at a higher dose were observed clinically significant adverse events. Data concerning overdose in humans are not available. In case of overdose, the patient should appoint symptomatic treatment.
INTERACTIONS WITH OTHER MEDICINES AND OTHER DRUG INTERACTIONS
- Caution should be prescribed the drug primobolan steroid to males at special risk of ureteral obstruction or spinal cord compression. These patients should be monitored closely during the first month of therapy. In that case, if the spinal cord compression or renal impairment due to ureteric obstruction are taking place or are developing, should be given the standard treatment for these complications.
- In women, the drug 10.8 mg is shown only for the treatment of endometriosis and uterine fibroids. For women who need goserelin treatment for other indications, use the drug Zoladex ® 3.6 mg.
- When using the drug women to restore menstruation should be used non-hormonal methods of contraception.
- As with other GnRH analogues, when using the drug 3.6 mg in combination with gonadotrophin, reported rare cases of ovarian hyperstimulation syndrome (OHSS). It is assumed that desensitization caused by the use of the drug mg may in some cases lead to an increase in the required dose of gonadotropin. It is necessary to carefully monitor the stimulation cycle to identify patients at risk for OHSS, since the frequency and severity of the manifestations of the syndrome may be dependent on the dose of gonadotropin mode. Introduction of human chorionic gonadotropin should be stopped, if necessary.
- The use of GnRH agonists in women may cause a reduction in bone mineral density. After treatment, most women occurs in bone mineral density recovery. Patients receiving the drug Zoladex ® 3.6 mg for the treatment of endometriosis, the addition of hormone replacement therapy (estrogen and progestogen drugs daily) reduced the loss of bone mineral density and vasomotor symptoms. There is currently no experience of the use of hormone-replacement therapy in the treatment of drug Zoladex ® 10.8 mg.
- Resumption of menstruation after the end of treatment with Zoladex ® some patients may be delayed. In rare cases, some women during treatment with GnRH analogues may occur menopause without the restoration of menstruation after the end of therapy.
- The use of the drug Zoladex ® may lead to an increase in cervical resistance, care must be taken when cervical dilatation.
- No data on the efficacy and safety of therapy with Zoladex ® benign gynecological disease lasting more than 6 months.
- The drug Zoladex ® 3.6 mg should be used only in vitro fertilization under the supervision of a specialist who has experience in this field.
- It is recommended to use the drug with caution Zoladex ® 3.6 mg at ekstra¬korporalnom fertilization in patients with polycystic ovary syndrome, as there may be stimulation of a large number of follicles.
- According to preliminary data of the primobolan steroid use of a bisphosphonate in combination with GnRH agonists in men reduces the loss of bone mineral density.In connection with the possibility of reducing the tolerance of glucose in patients receiving GnRH agonists in men, it is recommended to periodically monitor blood glucose.Effects on ability to drive and use other mechanisms
do not have information about how the drug Zoladex ® leads to deterioration of these activities.PACKAGING
capsule to subcutaneous depot 3.6 mg or 10 mg 8-syringe applicator with a protective mechanism (Safety Glide secure delivery system).
One syringe applicator is placed in an aluminum laminate envelope. Envelope with attached movable flag-annotation is placed in a cardboard box with instructions for use.
Store at a temperature below 25 o C. The Keep out of the reach of children.
3 years. Do not use beyond the expiration date printed on the package.