Zoladex is an anticancer drug, which is an analogue of gonadotropin-releasing hormone.
Release form and composition
Zoladex is produced in the form of capsules for subcutaneous administration of prolonged action (white or cream cylindrical pieces of solid polymer material), in syringes-applicators with a protective mechanism (Safety Glide safe injection system), 1 syringe each in laminated aluminum envelopes.
1 capsule contains:
- 3.6 mg goserelin (in the form of acetate) and auxiliary components: a copolymer of glycolic and lactic acids (50:50), glacial acetic acid;
- 10.8 mg goserelin (in the form of acetate) and auxiliary components: glacial acetic acid, low molecular weight copolymer of glycolic and lactic acids (95: 5) and high molecular weight copolymer of glycolic and lactic acids (95: 5) in a ratio of 3: 1.
Indications for use
Zoladex 3.6 mg is prescribed:
- With prostate cancer;
- In breast cancer;
- To thin the endometrium during the planned operations on the endometrium;
- With endometriosis;
- When conducting in vitro fertilization;
- With uterine fibroids.
Zoladex 10.8 mg is prescribed for the treatment of:
- Prostate cancer;
- Fibromas of the uterus.
The use of Zoladex is contraindicated:
- Nursing and pregnant women;
- Children under 18;
- In case of hypersensitivity to goserelin or other GnRH analogues.
With caution, the drug is prescribed to men who are at particular risk of spinal cord compression or obstruction of the ureters, as well as in vitro fertilization in women with polycystic ovary syndrome.
Dosing and Administration
Adults inject the drug into the anterior abdominal wall subcutaneously.
Zoladex 3.6 mg is administered to men and women every 28 days.
In case of benign gynecological diseases, the drug is used for not more than 6 months, in case of malignant neoplasms - for a long time.
For the thinning of the endometrium, 2 injections are usually given at intervals of 28 days, while ablation of the uterus is recommended during the first 14 days after the second dose.
During in vitro fertilization, Zoladex 3.6 mg is used for desensitization of the pituitary gland. Usually the required estradiol level is reached between 7 and 21 days. Monitoring therapy is carried out in accordance with the established practice of the medical institution.
Zoladex 10.8 mg is usually prescribed:
- Men - every 3 months;
- Women - every 12 weeks.
Elderly patients, as well as patients with hepatic or renal insufficiency, dosage adjustment is not required.
In the application of Zoladex may develop side effects, manifested with different frequency.
During the use of the drug may cause tumors:
- Very rare: pituitary tumors;
- Unspecified frequency: degeneration of fibromatous nodes in uterine fibroids.
Disorders of the cardiovascular system usually manifest as:
- Very often: hot flashes (sometimes it is possible to cancel the drug);
- Often: changes in blood pressure (hypotension or hypertension), in men - heart failure and myocardial infarction.
Metabolic changes in the form of impaired glucose tolerance often develop in men and manifest as diabetes mellitus or impaired control of blood glucose levels in patients with diabetes mellitus in history. Women may develop hypercalcemia.
Violations of the genitourinary system are manifested in the form of:
- 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);
- Infrequently: pains of the mammary glands, obstruction of the ureters (in men);
- Rarely: ovarian cysts (in women), ovarian hyperstimulation syndrome (in women, with simultaneous use with gonadotropins);
- Unspecified frequency: vaginal bleeding (in women).
On the part of the psychic sphere and the nervous system, disorders are manifested as:
- Very often: decrease in libido (withdrawal of the drug is sometimes possible);
- Often: depression, headache, decrease in mood (in women), paresthesia, compression of the spinal cord (in men);
- Very rare: psychotic disorders.
On the part of the skin and subcutaneous tissue during the application of Zoladex may occur:
- Very often: increased sweating (withdrawal of the drug is sometimes possible);
- Often: alopecia (in women), rash;
- Unspecified frequency: alopecia (in men).
Disorders of the musculoskeletal system may manifest as:
- Often: arthralgia (in women), bone pain (in men). At the beginning of therapy in patients with prostate cancer, a temporary increase in bone pain is possible, in which case symptomatic treatment is indicated;
- Infrequently: arthralgia (in men).
On the part of the immune system, hypersensitivity reactions (infrequently) and anaphylactic reactions (rarely) can occur.
Disorders of the endocrine system occur very rarely in the form of hemorrhage in the pituitary gland.
On the part of laboratory studies, a decrease in bone mineral density and an increase in body weight are often observed.
Among other side effects may develop:
- Very often: reactions at the injection site (in women);
- Often: reactions at the injection site (in men), temporary increase in symptoms of the disease in women with breast cancer at the beginning of treatment.
When prescribing Zoladex to men who have a particular risk of developing obstruction of the ureters or squeezing the spinal cord, during the first month of therapy, careful monitoring of the condition is necessary. If necessary, prescribe a standard therapy for these complications.
In women, Zoladex 10.8 mg should be used only for the treatment of uterine fibroids and endometriosis, according to other indications Zoladex 3.6 mg is prescribed. During therapy before the restoration of menstruation, non-hormonal methods of contraception should be used. The resumption of menstruation after the end of treatment in some cases may occur with a delay, sometimes after the end of the use of the drug, menopause occurs without restoring menstruation.
Therapy in women can cause a decrease in bone mineral density, which is restored after the end of the course. In the treatment of endometriosis using Zoladex 3.6 mg, the addition of hormone replacement therapy (daily progestogen and estrogen preparations) reduces the loss of bone mineral density and vasomotor symptoms. Experience with the use of hormone replacement therapy using Zoladex 10.8 mg no.
During treatment, an increase in cervical resistance is possible, so care should be taken when dilating the cervix.
There are no data on the safety and efficacy of treatment of benign gynecological diseases lasting more than 6 months.
According to preliminary data, the use of a bisphosphonate simultaneously with GnRH agonists in men contributes to reducing the loss of bone mineral density. Because of the possibility of developing a decrease in glucose tolerance while taking GnRH agonists, men are recommended to periodically monitor their blood glucose levels.
There is no evidence that Zoladex reduces the ability to drive motor vehicles and work with machinery.
Analogues of Zoladex on the mechanism of action are: Anabrez, Aromeston, Bicalutera, Hormplex, Dermestril, Letrozole, Nolvadex, Oreta, Sandostatin, Suprefact, Flutaplex and other antitumor hormones and hormone antagonists.
Terms and conditions of storage
Keep out of reach of children at temperature up to 25 ° C.
The shelf life of the drug - 3 years.