Zoladex (gozerelin) capsules for subcutaneous use 10.8 mg.

$674.00

Prostate cancer: therapy for prostate cancer, which may have a hormonal effect; endometriosis; uterine fibroma; with in vitro fertilization; the need for thinning of the endometrium before planned operations; breast cancer (hormone-dependent) in reproductive age and perimenopause.

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Description

ZOLADEX

Prostate cancer: therapy for prostate cancer, which may have a hormonal effect; endometriosis; uterine fibroma; with in vitro fertilization; the need for thinning of the endometrium before planned operations; breast cancer (hormone-dependent) in reproductive age and perimenopause.

Storage:
active substance: 1 capsule for subcutaneous administration of prolonged action contains goserelin acetate equivalent to 3.6 mg of goserelin-based;

excipients: copolymer of lactide and glycolide.

Dosage form
Capsule for subcutaneous injection of prolonged action.

Basic physical and chemical properties:
pieces of solid polymer of cylindrical shape from white to cream color.

Pharmacotherapeutic group
Gonadotropin-releasing hormone analogues.
ATC code L02A E03.

Mechanism of action

Zoladex (D-Ser (But) 6Azgly10 LG-RG) is a synthetic analogue of the natural luteinizing hormone – hormone releasing hormone (LG-RG). With constant use Zoladex inhibits the secretion of LH by the pituitary gland, which leads to a decrease in the concentration of testosterone in the serum of men and the concentration of estradiol in the serum of women. This effect is reversible after discontinuation of therapy. In the initial stage, Zoladex, like other LH-RG agonists, may cause a temporary increase in serum testosterone levels in men and serum estradiol levels in women. In the early stages of Zoladex therapy, some women may experience vaginal bleeding of varying duration and intensity. This bleeding is probably a reaction to estrogen withdrawal and should stop on its own. In men, until about the 21st day after the first capsule, the concentration of testosterone is reduced to castration levels and remains reduced with continuous treatment, ie with the introduction of the drug every 28 days. This decrease in testosterone levels in most patients leads to regression of prostate tumor and symptomatic improvement. In women, the concentration of estradiol in the serum also decreases until about the 21st day after the first capsule and with continuous treatment, ie with the drug every 28 days, remains reduced to a level comparable to that observed in women in the postmenopausal period. This reduction leads to a positive effect in hormone-dependent forms of breast cancer, endometriosis and uterine fibroids. It also causes thinning of the endometrium and amenorrhea in most patients.

Zoladex in combination with iron supplements has been shown to cause amenorrhea, leading to increased hemoglobin levels and improved hematological parameters in women with uterine fibroids and concomitant anemia. This combination will give an additional 10 g / l increase in hemoglobin concentration compared to therapy with iron supplements alone. Some women may experience menopause during treatment with Zoladex. In a small number of patients, menstruation does not resume after treatment.

Pharmacokinetics

Zoladex is almost completely bioavailable. Administration of the capsule every four weeks provides maintenance of effective concentrations. Accumulation in tissues does not occur. Zoladex is poorly bound to the protein and has a half-life of 2-4 hours in patients with normal renal function. The half-life increases in patients with impaired renal function. With monthly administration of the drug in the form of a capsule, this change will not have significant consequences. Therefore, there is no need to change the dose for patients with impaired renal function. No significant changes in pharmacokinetic parameters were observed in patients with hepatic insufficiency.

Indication

Prostate cancer.

Treatment of prostate cancer in the following cases:

  •  treatment of metastatic prostate cancer – the use of Zoladex had a beneficial effect on survival, similar to the effect of surgical castration;
  •  treatment of locally advanced prostate cancer as an alternative to surgical castration – the use of Zoladex had a beneficial effect on survival, similar to the effect of antiandrogen use;
  •  as adjuvant therapy to radiation therapy in patients with localized high-risk prostate cancer or locally advanced prostate cancer – Zoladex improved disease-free survival and overall survival;
  •  as neoadjuvant therapy prior to radiation therapy in patients with high-risk localized prostate cancer or locally advanced prostate cancer – Zoladex improved no-disease survival;
  •  as adjuvant therapy for radical prostatectomy in patients with locally advanced prostate cancer and a high risk of disease progression – Zoladex improved survival without signs of disease.
  • Breast cancer. Treatment of common hormone-sensitive breast cancer in pre- and perimenopausal women.

As an alternative to chemotherapy as part of standard treatment of pre / perimenopausal women with estrogen receptor (ER) positive early breast cancer.

Endometriosis. Relieves symptoms, including pain, decreased size and number of endometrial injuries.

Thinning of the endometrium. For pre-thinning of the endometrium before its ablation or resection.

Uterine fibroids. In combination with iron therapy to improve the hematological status of patients with anemia with fibroids before surgery.

At in vitro fertilization. Desensitization of a pituitary gland in preparation for stimulation of superovulation.

Contraindication

Hypersensitivity to goserelin acetate or to other analogues of LH-RG (luteinizing hormone – hormone release) is known.

Pregnancy or breastfeeding

Children’s age.

Interaction with other drugs and other types of interactions

Because androgen deprivation therapy may lead to QT prolongation, concomitant use of Zoladex with drugs capable of prolonging QT or drugs that may cause ventricular tachycardia such as pirouette, such as class I antiarrhythmics, should be carefully evaluated. disopyramide) or class III (eg, amiodarone, sotalol, dofetilide, ibutilide), methadone, moxifloxacin, antipsychotics (see section “Special warnings and precautions for use”).

Features of application

Injections at the injection site, including pain, bruising, bleeding and vascular damage, have been reported with Zoladex. Patients with such lesions should be monitored for signs or symptoms of abdominal bleeding. In very rare cases, application errors resulted in vascular damage and hemorrhagic shock requiring blood transfusions and surgery. Caution should be exercised when using Zoladex in patients with low body mass index (BMI) and / or those receiving drugs for complete anticoagulation (see section “Method and Dosage”).

There are no data on the removal or dissolution of the capsule.

There is a high risk of developing depression (which can be severe) in patients receiving gonadotropin-releasing hormone agonists such as goserelin. Patients should be informed of this risk and, if symptoms occur, given appropriate treatment.

Androgen deprivation therapy may prolong the QT interval.

Before prescribing Zoladex to patients with a history of QT prolongation or risk factors for QT prolongation, as well as to patients taking concomitant medications that may cause QT prolongation (see section “Interaction with other medicinal products and other forms of interaction”). it is necessary to assess the benefit-risk balance, including the possibility of ventricular tachycardia type “pirouette”.

Men

Zoladex should be used with caution in men at risk of developing urinary tract obstruction or spinal cord compression, and should be closely monitored during the first month of therapy. In the presence or occurrence of spinal cord compression or renal failure due to urinary tract obstruction, standard treatment of such complications should be resorted to.

Antiandrogens should be considered during the initial treatment period with LH-RG analogues (eg, cyproterone acetate 300 mg / day for 3 days before and 3 weeks after Zoladex administration), as this has been reported to prevent the possible consequences of an initial rise in serum testosterone levels.

Patients with non-hormone-dependent prostate cancer are unlikely to benefit from such treatment. This resistance to treatment may be the result of a lack of response to castration or hormonal treatment.

The recommended dosage of testosterone before the introduction of treatment to assess the therapeutic benefit.

The use of LH-RG agonists can reduce bone mineral density. Preliminary data suggest that the use of bisphosphonates in men in addition to LH-RG agonists may reduce bone mineral loss. Particular caution should be exercised in patients with additional risk factors for osteoporosis (chronic alcohol abuse, smoking, long-term anticonvulsant or corticosteroid therapy, family history of osteoporosis).

There have been cases of mood swings, including depression. Patients with established depression and patients with hypertension need close supervision.

There is a high risk of low blood pressure (which can be severe) in patients treated with LH-RG agonists such as goserelin. Patients should be informed and treated appropriately if symptoms occur.

Cases of myocardial infarction and heart failure have been reported in a pharmacoepidemiological study of LH-RG agonists used to treat prostate cancer. The risk appears to increase when LH-RG agonists are used in combination with antiandrogens.

Decreased glucose tolerance was observed in men who used LH-RG agonists. This can manifest as diabetes or loss of glycemic control in people with pre-existing diabetes. Blood glucose control should be considered.

Women

Benign conditions as indications

Loss of bone mineral density

LH-RG agonists can cause a decrease in bone mineral density by an average of 1% over 6 months of treatment. Decreased bone mineral density for every 10% increases the risk of fractures by about 2-3 times. According to currently available data, in most women after discontinuation of treatment, bone mass is restored.

In patients taking Zoladex for the treatment of endometriosis, adjunctive hormone replacement therapy reduced the decrease in bone mineral density and the severity of vasomotor symptoms.

There are no specific data on the use of the drug in patients with established osteoporosis or risk factors for its development (such as chronic alcohol abuse, smoking, long-term therapy with drugs that reduce bone mineral density, such as anticonvulsants or corticosteroids, the presence of osteoporosis, familial anaporosis for example, nervous anorexia). Because a decrease in bone mineral density may be more dangerous in such patients, Zoladex should be considered on a case-by-case basis and therapy should only be initiated if a careful evaluation has determined that the benefit outweighs the risk. Additional measures should be taken to counteract the loss of bone minerals.

Breast cancer as an indication

Decrease in bone mineral density

The use of LH-RG agonists can lead to a decrease in bone mineral density. After 2 years of treatment of early stages of breast cancer, the average decrease in the mineral density of the femoral neck and lumbar spine in women was 6.2% and 11.5%, respectively. These losses were shown to be partially reversible: one year after cessation of treatment, the loss of femoral neck and lumbar spine mineral density was 3.4% and 6.4% lower, respectively, than before the drug, although data on bone mass recovery very limited. According to available data, in most women bone mass is restored after stopping treatment.

Preliminary data suggest that the use of Zoladex in combination with tamoxifen in breast cancer patients may reduce bone mineral loss.