ZOLADEX CAPSULES 10.8MG IN THE SYRINGE

Active ingredient

for s / c introduction:
1 capsule contains goserelin (in the form of goserelin acetate) 3.6 or 10.8 mg;
Excipients: lactic and glycolic acid copolymer;
1 syringe applicator complete with a safe injection system in a bag of aluminum foil in a cardboard box.

depot caps. 3.6 mg - P No. 013307/02-2001, 03.09.01
depot caps. 10.8 mg - P No. 013307/01-2001, August 13, 2001

Mechanism of action

Synthetic analogue of natural luteinizing hormone-releasing hormone (LGRG).
With continued use, Zoladex inhibits the secretion of pituitary LH, which leads to a decrease in serum testosterone concentrations in men and serum estradiol concentrations in women. This effect is reversible after discontinuation of therapy.
In the initial stage of the course of treatment, Zoladex, like other LHRH agonists, can cause a temporary increase in the concentration of testosterone in the blood serum in men and estradiol in women.
In men, by about 21 days after the injection of the first depot capsule, the testosterone concentration decreases to castration levels and continues to be lowered with constant treatment every 28 days (for Zoladex containing 3.6 mg goserelin) or every 12 weeks (with goserelin content 10.8 mg).In most patients, there is regression of the prostate gland and symptomatic improvement.
In women, the serum estradiol concentration also decreases by about 21 days after injection of 3.6 mg or 10.8 mg of Zoladex Depot first capsule and with constant treatment every 28 days remains reduced to a level comparable to that in menopausal women. This reduction leads to a positive effect in hormone-dependent forms of breast cancer, endometriosis, uterine fibroids and suppression of follicular development in the ovaries, and also causes endometrial thinning and is the cause of amenorrhea in most patients.
In the early stages of Zoladex therapy, some women may experience vaginal bleeding of varying duration and intensity. These bleedings are likely to be a reaction to a decrease in estrogen concentration and should stop on their own.
In the treatment of endometriosis, Zoladex reduces the severity of symptoms, including pain, and reduces the size and number of endometriotic lesions. In the treatment of fibroids, Zoladex, used as an adjuvant in combination with surgery, reduces the size of the uterus and myomatous nodes, reduces blood loss during surgery, improves the hematological status of patients.

For zoladex containing 3.6 mg goserelin:
- treatment of prostate cancer sensitive to hormonal effects;
- treatment of hormone-sensitive breast cancer in women of reproductive age and perimenopause;
- endometriosis;
- uterus fibromas (as an adjuvant in combination with surgical treatment);
- for preliminary thinning of the endometrium before its surgical ablation or resection;
- desensitization of the pituitary gland in preparation for the stimulation of superovulation in the framework of the in vitro fertilization program.
For zoladex containing 10.8 mg of goserelin:
- treatment of prostate cancer sensitive to hormonal effects;
- endometriosis;
- uterus fibromas (as an adjuvant in combination with surgical treatment).

Contraindications

- pregnancy;
- lactation;
- childhood;
- Hypersensitivity to goserelin or other analogues of LGRH.

Dosage and administration

Zoladex Depot 3.6 mg is injected subcutaneously into the anterior abdominal wall every 28 days, Zoladex Depot 10.8 mg every 12 weeks.
With malignant neoplasms the drug is prescribed for a long time.
To thin the endometrium 2 depot Zoladeksa 3.6 mg administered at intervals of 4 weeks, while the operation is recommended for the first two weeks after the introduction of the second capsule depot.
For benign gynecological tumors the drug is prescribed for no more than 6 months, since at the moment there are no clinical data on longer courses of therapy. Repeat courses should not be prescribed due to the danger of a decrease in bone mineral density.
In vitro fertilization desensitization of the pituitary gland is determined 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 (approximately 150 pmol / l), is reached between 7 and 21 days. When the pituitary is desensitized, the stimulation of superovulation (controlled stimulation of the ovaries) with gonadotropin begins. The induced desensitization of the pituitary when using Zoladex may be more persistent, which may lead to an increased need for gonadotropin. At the appropriate stage of follicular development, the introduction of gonadotropin is stopped and then human chorionic gonadotropin is administered to induce ovulation. Monitoring of the treatment, the procedure of oocyte extraction and fertilization is carried out in accordance with the established practice of this medical institution.
Patients with renal or hepatic failure, and elderly patients dose adjustment is not required.

Adverse reactions

There have been rare cases of hypersensitivity reactions, including manifestations of anaphylaxis.
In patients treated with Zoladex, changes in blood pressure were sometimes noted (both hypertension and hypotension). These changes are transient in nature, very rarely require medical correction and are either in the process of therapy or after discontinuation of the drug.
When using Zoladex (containing 3.6 mg goserelin), there were cases of skin rash (usually minor, and its regression, as a rule, occurred without discontinuation of therapy) and arthralgia. With the use of Zoladex (containing 10.8 mg goserelin), these side effects are not observed.
The use of the drug in men and women can cause bone demineralization.
Have the men marked hot flashes and reduced potency, which rarely requires discontinuation of therapy. Swelling and tenderness of the mammary glands were rarely observed. At the initial stage, patients with prostate cancer may experience a temporary increase in bone pain, in which case symptomatic therapy may be indicated. Individual cases of ureteral obstruction and compression of the spinal cord were noted.
Have of women hot flashes, increased sweating, and a change in libido are noted, which rarely requires discontinuation of therapy. Sometimes there were headaches, mood changes, including depression, vaginal mucosa dryness, change in the size of the mammary glands. At the initial stage, patients with breast cancer may experience a temporary increase in the signs and symptoms of the disease, in which case symptomatic treatment can be carried out.In women with uterine fibromas, fibromatous nodes can be degenerated. In rare cases, after initiation of therapy in patients with bone metastases, hypercalcemia has occurred.
When using Zoladex in combination with gonadotropin, as in the case of using this combination with other LHRH analogues, cases of the development of ovarian hyperstimulation syndrome were reported.

Pregnancy and breastfeeding

The drug is contraindicated for use during pregnancy and lactation.
Zoladex should not be prescribed during pregnancy, since theoretically there is a risk of abortion or fetal abnormalities when using LHRH agonists.
Have women of childbearing age possible pregnancy should be excluded before treatment with zoladex.
During therapy, non-hormonal methods of contraception should be used until menstruation resumes.

Special notes

Zoladex should be administered with caution to male patients who are known to be at risk for ureteral obstruction or compression of the spinal cord. In this category of patients should be systematically monitored during the first month of therapy. In the event of symptoms of compression of the spinal cord or renal failure caused by ureteral obstruction, the standard treatment for these complications should be prescribed.
During treatment and before menstruation is restored, non-hormonal methods of contraception should be used.
The use of the drug in men and women can cause bone demineralization.Currently available data indicate an average decrease of 4.6% in bone mineral density of the vertebrae during a 6-month course of treatment. Bone density is gradually restored after cessation of treatment, remaining below the initial level by an average of 2.6% (there is no separate information about this when using Zoladex containing 10.8 mg of goserelin). It was shown that in patients receiving Zoladex for endometriosis, additional hormone replacement therapy (daily estrogen and progestogen preparations) reduced the loss of bone mineral density and the severity of vasomotor symptoms. Currently, there is no experience with the use of hormone replacement therapy in the treatment with Zoladex containing 10.8 mg of goserelin.
Zoladex should be used with caution in women with impaired bone metabolism.
Currently, there are no clinical data on the safety and efficacy of Zoladex treatment of benign gynecological diseases for periods of time longer than 6 months.
The resumption of menstruation after the end of treatment with Zoladex may be delayed. In some women, in rare cases, during treatment with Zoladex (as with the treatment of other LHRH analogues), menopause may occur, i.e. after the abolition of therapy, menstruation may not occur.
Zoladex can also cause an increase in the resistance of the cervix, and in this connection - difficulties in dilating the cervix.
For in vitro fertilization, Zoladex should be used only under the supervision of a specialist with experience in this field.
When using Zoladex in combination with gonadotropin, as in the case of using this combination with other LHRH analogues, cases of ovarian hyperstimulation syndrome were reported, therefore, during the stimulation of superovulation, careful monitoring is necessary to identify patients at risk of ovarian hyperstimulation syndrome. If necessary, the introduction of human chorionic gonadotropin should be discontinued.
It is recommended to use Zoladex with caution during in vitro fertilization in patients with polycystic ovary syndrome, since possible stimulation of a large number of follicles.

Data regarding overdose in humans is not available.
Treatment: conduct symptomatic therapy.

Drug interaction of the drug Zoladex is not described.

The drug should be stored at temperatures below 25 ° C. 

- 3 years.
Pharmacy sales terms
The drug is available on prescription.

Zoladex