Composition, form of production and packaging
Capsules for the c / o administration of prolonged action in the form of white or creamy cylindrical pieces of solid polymeric material, free or practically free of visible inclusions.
goserelin (in the form of acetate) 10.8 mg
Auxiliary substances: a low molecular weight lactic and glycolic acid copolymer (95: 5) and a high molecular weight lactic and glycolic acid copolymer (95: 5) in a ratio of 3: 1 to 36 mg, glacial acetic acid (low content of acetic anhydride) qs
Syringe applicator (1) with protective mechanism (Safety Glide safety system) - aluminum laminated envelopes (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2012.
Synthetic analogue of natural GnRH (gonadotropin releasing hormone). With continued use, Zoladex В® inhibits the pituitary glandularization of luteinizing hormone (LH), which leads to a decrease in serum testosterone concentration in men and a concentration of estradiol in the blood serum in women. This effect is reversible after the abolition of therapy. In the initial stage, Zoladex В® , like other GnRH agonists, can cause a temporary increase in serum testosterone in men and a serum estradiol concentration in women. In the early stages of Zoladex therapy, 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, conducted every 3 months.
In women, the serum estradiol concentration 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 analogues of GnRH and the transition to Zoladex В® 10.8 mg, suppression of the level of estradiol persists.
Suppression of the level of estradiol leads to a therapeutic effect in endometriosis and uterine fibroids.
Against the background of taking GnRH analogues in women, menopause may occur.
Rarely, some women do not recover menstruation after the end of therapy.
The administration of the capsule every 12 weeks ensures the maintenance of effective concentrations. Cumulation in the tissues does not occur.
Binding to plasma proteins is low. In patients with normal renal function, T 1/2 of blood serum is 2-4 hours. In patients with impaired renal function, T 1/2 increases.With the introduction of Zoladex 10.8 mg every 12 weeks, this change will not have significant consequences, so you do not need to change the dose for this category of patients.
In patients with hepatic insufficiency no significant changes in pharmacokinetics are observed.
- prostate cancer;
- uterine fibroid.
Adult male capsule preparation Zoladex В® 10.8 mg is injected into the anterior abdominal wall every 3 months.
For adult women, a capsule of Zoladex В® 10.8 mg is injected into the anterior abdominal wall every 12 weeks.
Patients with renal or hepatic insufficiency , as well as patients of advanced age , do not need dose adjustment.
The frequency of undesirable effects is as follows: often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1 000); very rarely (<1/10 000, including individual messages).
Neoplasms: very rarely - pituitary tumor; Unspecified frequency - degeneration of fibromatous nodes in women with uterine fibroids.
From the immune system: infrequently - hypersensitivity reactions; rarely anaphylactic reactions.
From the endocrine system: very rarely - hemorrhage in the pituitary gland.
Metabolic disorders: often - a violation of 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 impaired control of blood glucose levels in patients with diabetes mellitus in history;infrequently, hypercalcemia (in women).
From the nervous system and the 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 - depression of mood, depression (in women), paresthesia, compression of the spinal cord (in men), headache (in women); very rarely - a psychotic disorder.
From the side of the cardiovascular system: very often - tides associated with the 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 appointment of antiandrogenic drugs. A change in the level of blood pressure, manifested as hypotension or hypertension. These changes are usually transient, and are resolved either during the treatment with ZoladexВ®, or after its discontinuation. In rare cases, these changes required medical intervention, including the abolition of Zoladex В® .
From the skin and subcutaneous tissue: very often - increased sweating, associated with the pharmacological effect of the drug and, in rare cases, leading to its cancellation; often, alopecia (in women), as a rule, slightly expressed (including in young patients with benign tumors), a rash, mostly slight, which was often resolved while continuing therapy; Unspecified frequency - alopecia (in men), which manifested itself as hair loss throughout the body due to decreased levels 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), ureteral obstruction (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 - a reaction at the injection site (in women); often a 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.
From the side of laboratory studies: often - decrease in bone mineral density, increase in body weight.
- Hypersensitivity to goserelin or other analogues of GnRH.
Caution should be applied to the drug in men who are at particular risk of obstruction of the ureters or compression of the spinal cord, as well as in extracorporeal fertilization in patients with polycystic ovary syndrome.
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with renal insufficiency do not need dose adjustment.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Patients with hepatic insufficiency do not need dose adjustment.
APPLICATION FOR CHILDREN
Contraindicated in childhood.
APPLICATION IN ELDERLY PATIENTS
Older patients are not required to adjust the dose.
Caution should be given to ZoladexВ® in men who are at particular risk for developing ureteral obstruction or for squeezing the spinal cord. This category of patients should be closely monitored during the first month of therapy. In the event that compression or development of spinal cord compression or renal failure due to obstruction of the ureters, a standard treatment for these complications should be prescribed.
In women Zoladex В® 10.8 mg is indicated only for the treatment of endometriosis and uterine fibroids. For women requiring treatment with goserelin for other indications, use the drug Zoladex В® 3.6 mg.
When using the drug Zoladex В® in women before the recovery of menstruation should be used non-hormonal methods of contraception.
The use of GnRH analogues in women can cause a decrease in bone mineral density. After the end of treatment, bone mineral density is restored. In patients who received Zoladex В® 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 В®10.8 mg.
The resumption of menstruation after the end of treatment with Zoladex В® in some patients may occur with a delay. 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 В® 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 В® treatment of benign gynecological diseases lasting more than 6 months.
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 developing a decrease in glucose tolerance against the acceptance of GnRH agonists in men, it is recommended to periodically monitor the glucose level in the blood.
Impact on the ability to drive vehicles and manage mechanisms
There is no evidence that Zoladex В® worsens the ability to drive vehicles and work with machinery.
The experience of drug overdose in humans is limited. In the case of unintentional administration of Zoladex В® before the term or at a higher dose, there were no clinically significant adverse events.
Treatment: symptomatic therapy.
Drug interaction of Zoladex В® is not described.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature below 25 В° C. Shelf life - 3 years.