Active substanceGoserelinGoserelin
Similar drugsTo uncover
  • Zoladex®
    capsules PC 
    AstraZeneca UK Ltd     United Kingdom
  • Dosage form: & nbspcapsule for subcutaneous administration of prolonged action
    Composition:

    One capsule contains:

    active substance: goserelin acetate 3.6 mg or 10.8 mg (in terms of goserelin base);

    Excipients: lactic and glycolic acid copolymer (50:50) to a total weight of 18.0 mg (preparation Zoladex® 3.6 mg), a low molecular weight lactic and glycolic acid copolymer (95: 5) and a high molecular weight lactic and glycolic acid copolymer (95: 5) up to a total weight of 36.0 mg (ratio of low molecular weight to high molecular weight copolymer of 3: 1, by weight) (preparation Zoladex® 10.8 mg).

    Description:

    White or creamy cylindrical pieces of solid polymeric material, free or practically free of visible inclusions.

    Pharmacotherapeutic group:antitumor agent - gonadotropin-releasing hormone analogue
    ATX: & nbsp

    L.02.A.E.03   Goserelin

    Pharmacodynamics:

    Zoladex® is a synthetic analogue of natural gonadotropin-releasing hormone (GnRH). With constant use, Zoladex® inhibits pituitary luteinizing hormone (LH) release, which leads to a decrease in testosterone serum levels in men and a serum estradiol concentration in women. This effect is reversible after the abolition of therapy.At the initial stage, Zoladex®, like other GnRH agonists, can cause a temporary increase in serum testosterone concentration in men and a serum estradiol concentration in women. In the early stages of therapy with Zoladex®, some women may experience vaginal bleeding of varying duration and intensity.

    In men, approximately 21 days after the administration of the first capsule, the concentration of testosterone is reduced to castration levels and continues to be reduced with constant treatment every 28 days for Zoladex® 3.6 mg or every 3 months for Zoladex® 10.8 mg . Such a decrease in the concentration of testosterone against the background of the use of Zoladex® 3.6 mg in most patients leads to regression of the tumor of the prostate and to symptomatic improvement.

    In women, the serum estradiol concentration also decreases by about 21 days after the first capsule of Zoladex® 3.6 mg and, with regular administration of the drug every 28 days, remains reduced to a level comparable to that seen in women in menopause.This decrease leads to a positive effect with hormone-dependent forms of breast cancer, endometriosis, uterine fibroids and suppression of ovarian follicular development. This also causes thinning of the endometrium and is the cause of amenorrhea in most patients.

    After the administration of Zoladex® 10.8 mg, the serum estradiol concentration in women decreases within 4 weeks after the administration of the first capsule and remains reduced to a level comparable to that observed in women in menopause. With the initial use of other GnRH analogues and the transition to Zoladex® 10.8 mg, suppression of estradiol levels persists. Suppression of the level of estradiol leads to a curative effect in endometriosis and uterine fibroids.

    It was shown that Zoladex® 3,6 mg in combination with iron preparations causes amenorrhea and an increase in hemoglobin level and corresponding hematological parameters in women with uterine fibroids and concomitant anemia.

    Against the background of taking GnRH agonists, menopause may occur in women. Rarely, some women do not recover menstruation after the end of therapy.

    Pharmacokinetics:

    The introduction of Zoladex® 3.6 mg every four weeks or Zoladex® 10.8 mg every 12 weeks ensures maintenance of effective concentrations. Cumulation in the tissues does not occur. The drug Zoladex® binds poorly to the protein, and its half-life from serum is 2-4 hours in patients with normal renal function. The half-life is increased in patients with impaired renal function. With a monthly dose of Zoladex® 3.6 mg or Zoladex® 10.8 mg, this change will not have significant effects, so you do not need to change the dose for these patients. In patients with hepatic insufficiency, no significant changes in pharmacokinetics are observed.

    Indications:

    For the preparation Zoladex® 3.6 mg

    - Prostate cancer;

    - Ra breast cancer;

    - endometriosis;

    - fibroma of the uterus;

    - dFor thinning of the endometrium with planned operations on the endometrium;

    - Pin in vitro fertilization.

    For the preparation Zoladex® 10.8 mg

    - Prostate cancer;

    - endometriosis;

    - fibroma of the uterus.

    Contraindications:

    - Hypersensitivity to goserelin or other analogues of GnRH;

    - pregnancy and lactation;

    - childhood.

    Carefully:

    Men who are at special risk of obstruction of the ureters or compression of the spinal cord.

    With in vitro fertilization in patients with polycystic ovary syndrome.

    Dosing and Administration:

    Preparation Zoladex® 3.6 mg

    Adults

    The drug Zoladex® 3.6 mg is administered subcutaneously in the anterior abdominal wall every 28 days

    - with malignant neoplasms for a long time;

    - with benign gynecological diseases no more than 6 months;

    - for thinning the endometrium, two injections are done at 4-week intervals, with ablation of the uterus being recommended in the first two weeks after the second dose.

    In Vitro Fertilization

    The preparation Zoladex® 3,6 mg is used for desensitization of the pituitary gland. Desensitization is determined by the concentration of estradiol in the blood serum. Typically, the required level of estradiol, which corresponds to that in the early follicular phase of the cycle (approximately 150 pmol / L), is reached between 7 and 21 in the afternoon. At the onset of desensitization, stimulation of superovulation (controlled stimulation of the ovaries) with the help of gonadotropin begins.The resulting desensitization of the pituitary gland with the depot of the GnRH agonist may be more resistant, which may lead to an increased need for gonadotropin. At the appropriate stage of the development of the follicle, the administration of gonadotropin ceases and further human chorionic gonadotropin is introduced to induce ovulation. Control over the treatment, oocyte extraction and fertilization procedures are carried out in accordance with the established practice of this medical institution.

    Preparation Zoladex® 10.8 mg

    Adult Men

    Zoladex® preparation 10.8 mg is injected subcutaneously into the anterior abdominal wall every 3 months.

    Adult women

    Zoladex® 10.8 mg is injected subcutaneously into the anterior abdominal wall every 12 weeks.

    Elderly patients, patients with renal or hepatic impairment: dose adjustment is not required.

    Side effects:

    The frequency of undesirable effects is as follows:

    Often (> 1/100, <1/10); Infrequently (> 1/1000, <1/100); Rarely (> 1/10000, <1/1000); Very rarely (<1/10000), including individual messages.

    Neoplasms:

    Very rarely: a pituitary tumor.

    Unspecified frequency: degeneration of fibromatous nodes in women with uterine fibroids.

    From the immune system:

    Infrequent: hypersensitivity reactions.

    Rarely: anaphylactic reactions.

    From the endocrine system:

    Very rarely: hemorrhage in the pituitary gland.

    Metabolic disorders:

    Often: impaired glucose tolerance. Men who received GnRH agonists experienced a decrease in glucose tolerance. Decreased glucose tolerance was manifested by the development of diabetes mellitus or a worsening of control over the concentration of glucose in the blood in patients with diabetes mellitus in the anamnesis.

    Infrequent: hypercalcemia (in women).

    From the nervous system and mental sphere:

    Very often: a decrease in libido, associated with the pharmacological effect of the drug and, in rare cases, leading to its abolition.

    Often: mood changes (in women), depression (in women), mood swings (in men), paresthesia, spinal cord compression (in men), headache (in women).

    Very rarely: a psychotic disorder.

    From the cardiovascular system:

    Very often: "tides" associated with pharmacological action of the drug and, in rare cases, leading to its cancellation.

    Often: myocardial infarction (in men); heart failure (in men), the risk of which increases with the simultaneous use of antiandrogenic drugs.Changes in blood pressure, manifested by a decrease in blood pressure or increased blood pressure. These changes are usually transient, and are resolved either during the treatment with Zoladex®, or after its discontinuation. In rare cases, these changes required medical intervention, including the abolition of Zoladex®.

    From the skin and subcutaneous tissue:

    Very often: increased sweating, associated with the pharmacological action of the drug and, in rare cases, leading to its cancellation; acne (in women), in most cases occurs within 1 month after the start of therapy with Zoladex®.

    Often: alopecia (in women), as a rule, is slightly expressed, including in young patients with benign neoplasms; The rash, mostly, slightly pronounced, which was often resolved on the background of continuation of therapy.

    Unspecified frequency: alopecia (in men), which manifested itself as hair loss throughout the body due to decreased concentrations of androgens.

    From the musculoskeletal system:

    Often: arthralgia (in women), bone pain (in men).At the beginning of treatment, prostate cancer patients can often experience a temporary increase in pain in the bones, which is treated symptomatically.

    Infrequently: arthralgia (in men).

    From the genitourinary system:

    Very often: erectile dysfunction (in men), dryness of the vaginal mucosa and increase in the size of the mammary glands (in women).

    Often: gynecomastia (in men).

    Infrequent: tenderness of the mammary glands (in men), obstruction of the ureters (in men).

    Rarely: ovarian cyst (in women), ovarian hyperstimulation syndrome (in women, when combined with gonadotropins).

    Unspecified frequency: vaginal bleeding (in women).

    Other:

    Very often: reaction at the injection site (in women).

    Often: reaction at the injection site (in men); a temporary increase in the symptoms of the disease in patients with breast cancer at the beginning of therapy.

    Laboratory research:

    Often: decrease in mineral density of bone tissue, increase in body weight.

    Postmarketing application

    Against the background of the use of Zoladex®, isolated cases of changes in blood test parameters, violations of liver function, pulmonary embolism and interstitial pneumonia have been noted.

    Overdose:

    The experience of drug overdose in humans is limited.In the event of unintentional administration of Zoladex® before the term or at a higher dose, there were no clinically significant adverse events. Data on overdose in humans is not available.

    In case of an overdose, the patient should be prescribed symptomatic treatment.

    Interaction:

    It is not known.

    Special instructions:

    - Caution is advisable to prescribe Zoladex® to men who are at particular risk for obstruction of the ureters or compression of the spinal cord. These patients should be closely monitored during the first month of therapy. In the event that compression of the spinal cord or renal failure due to ureteric obstruction, occur or develop, a standard treatment for these complications should be prescribed.

    - In women, Zoladex® 10.8 mg is indicated only for the treatment of endometriosis and uterine fibroids. For women who need goserelin for other indications, use Zoladex® 3.6 mg.

    - When using the drug Zoladex® in women before the recovery of menstruation should be used non-hormonal methods of contraception.

    - As with other GnRH analogues, when Zoladex® 3,6 mg was used in combination with gonadotropin, there were reports of rare cases of ovarian hyperstimulation syndrome (GSSA). It is assumed that desensitization caused by the use of Zoladex® 3.6 mg may, in some cases, lead to an increase in the required dose of gonadotropin. It is necessary to carefully monitor cycle stimulation to identify patients at risk of developing CHD because the severity and frequency of the syndrome may depend on the dose regimen of the gonadotropin. The introduction of human chorionic gonadotropin should be discontinued if required.

    - The use of GnRH agonists in women can cause a decrease in bone mineral density. After the termination of treatment in the majority of women there is a restoration of mineral density of an osteal tissue. In patients treated with 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.At present, there is no experience with the use of hormone replacement therapy in the treatment with Zoladex® 10.8 mg.

    - The resumption of menstruation after the end of treatment with Zoladex® in some patients may be delayed. In rare cases, some women during the treatment of GnRH analogs may have the onset of menopause without restoring menstruation after the end of therapy.

    - The use of Zoladex® can lead to an increase in cervical resistance, care must be taken when dilating the cervix.

    - There is no data on the efficacy and safety of Zoladex® treatment of benign gynecological diseases lasting more than 6 months.

    - The drug Zoladex® 3.6 mg should be used for in vitro fertilization only under the supervision of a specialist with experience in this field.

    - It is recommended to use with caution the drug Zoladex® 3.6 mg for in vitro fertilization in patients with polycystic ovary syndrome, since it is possible to stimulate a large number of follicles.

    - According to preliminary data, the use of bisphosphonate in combination with GnRH agonists in men helps to reduce the loss of bone mineral density. In connection with the possibility of reducing tolerance to glucose on the background of admission of agonists GnRH in men, it is recommended to periodically monitor the glucose level in the blood.

    Effect on the ability to drive transp. cf. and fur:

    There is no evidence that the preparation Zoladex® leads to a deterioration in these activities.

    Form release / dosage:Capsule for subcutaneous administration of prolonged action, 3.6 mg, 10.8 mg.
    Packaging:

    By 3.6 mg or 10.8 mg in a syringe applicator with a protective mechanism (Safe injection system Safety Glide).

    One syringe applicator is placed in a laminated aluminum envelope.

    Envelope with a movably attached flag-annotation is placed in a cardboard box with instructions for use.

    Storage conditions:

    Store below 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013307 / 01
    Date of registration:27.08.2011
    The owner of the registration certificate:AstraZeneca UK LtdAstraZeneca UK Ltd United Kingdom
    Manufacturer: & nbsp
    ASTRAZENECA UK, Ltd. United Kingdom
    Representation: & nbspAstraZeneca Pharmaceuticals Ltd.AstraZeneca Pharmaceuticals Ltd.
    Information update date: & nbsp23.12.2015
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