Zoladex capsules for subcutaneous administration of 10.8 mg 1 pc
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Goserelin
Release form
Capsules
Composition
1 caps: goserelin (in the form of acetate) 10.8 mg Auxiliary substances: low molecular weight copolymer of lactic and glycolic acids (95: 5) and high molecular weight copolymer of lactic and glycolic acids (95: 5) - to a total weight of 36 mg (ratio between low and high molecular weight copolymer - 3: 1, by weight).
Pharmacological effect
Synthetic analogue of natural GnRH (gonadotropin releasing hormone). With constant use, Zoladex inhibits the secretion of pituitary luteinizing hormone (LH), which leads to a decrease in the concentration of testosterone in the blood serum in men and the concentration of estradiol in the blood serum in women. This effect is reversible after discontinuation of therapy. At the initial stage, Zoladex, like other GnRH agonists, can cause a temporary increase in the concentration of testosterone in the blood serum in men and the concentration of estradiol in the blood serum in women. In the early stages of Zoladex therapy, some women may experience vaginal bleeding of varying duration and intensity. In men, by about 21 days after the first capsule is injected, testosterone concentration decreases to castration levels and continues to be reduced with constant treatment every 3 months. In women, estradiol concentration in serum it decreases within 4 weeks after the first capsule is injected and remains reduced to a level comparable to that observed in menopausal women. With the initial use of other GnRH analogues and switching to Zoladex 10.8 mg, the suppression of estradiol levels persists. The suppression of estradiol levels leads to a therapeutic effect in endometriosis and uterine fibromas. Against the background of GnRH analogues in women, menopause is possible. menstruation after the end of therapy.
Pharmacokinetics
The administration of the capsule every 12 weeks ensures the maintenance of effective concentrations. There is no cumulation in the tissues. The binding to plasma proteins is low. In patients with normal renal function, T1 / 2 from serum is 2-4 hours. In patients with impaired renal function, T1 / 2 increases.With the introduction of Zoladex 10.8 mg every 12 weeks, this change will not have significant consequences, therefore, changing the dose for this category of patients is not required. In patients with liver failure, there are no significant changes in pharmacokinetics.
Indications
- prostate cancer; - endometriosis; - uterine fibroma.
Contraindications
- pregnancy; - lactation; - childhood; polycystic ovaries.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Dosage and administration
For adult men, the capsule of Zoladex 10.8 mg is injected sc into the anterior abdominal wall every 3 months. For adults, the capsule of the drug Zoladex 10.8 mg is injected sc into the anterior abdominal wall every 12 weeks. dose not required.
Side effects
The frequency of adverse 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). New formations: very rarely - pituitary tumor; unspecified frequency - degeneration of fibromatous nodes in women with uterine fibroma. On the immune system: infrequently - hypersensitivity reactions; rarely - anaphylactic reactions. From the endocrine system: very rarely - hemorrhage in the pituitary gland. Metabolic disorders: often - impaired glucose tolerance. In men who received GnRH agonists, there was a decrease in glucose tolerance. A decrease in glucose tolerance was manifested by the development of diabetes mellitus or a deterioration in the control of blood glucose levels in patients with diabetes mellitus in history; infrequently - hypercalcemia (in women). From the nervous system and mental sphere: very often - a decrease in libido associated with the pharmacological action of the drug and, in rare cases,led to its cancellation; often - decrease in mood, depression (in women), paresthesia, compression of the spinal cord (in men), headache (in women); very rarely - psychotic disorder. From the cardiovascular system: very often - hot flashes 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. Changes in blood pressure, manifested as hypotension or hypertension. These changes are usually transient, and are resolved either during the treatment with Zoladex or after its termination. In rare cases, these changes required medical intervention, including the abolition of Zoladex. On the side of the skin and subcutaneous tissue: very often, excessive sweating associated with the pharmacological action of the drug and, in rare cases, leading to its cancellation; often - alopecia (in women), as a rule, slightly pronounced (including in young patients with benign tumors), rash, mostly slightly pronounced, which was often resolved during the continuation of therapy; unspecified frequency - alopecia (in men), which manifested itself as hair loss throughout the body due to a decrease in the level 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 bone pain, which is treated symptomatically; infrequently - arthralgia (in men). From the urogenital system: very often - erectile dysfunction (in men), dry vaginal mucosa and an increase in the size of the mammary glands (in women); often - gynecomastia (in men); infrequently - tenderness of the mammary glands (in men), obstruction of the ureters (in men); rarely - an ovarian cyst (in women), ovarian hyperstimulation syndrome (in women, when used together with gonadotropins); unspecified frequency - vaginal bleeding (in women). Other: very often - the 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 laboratory studies: often - a decrease in bone mineral density, an increase in body weight.
Overdose
Experience overdose in humans is limited.In the event of the unintentional administration of Zoladex before the time limit or at a higher dose, no clinically significant adverse events were noted. Treatment: symptomatic therapy.
Interaction with other drugs
Drug interaction of the drug Zoladex is not described.
special instructions
Zoladex should be carefully prescribed to men who are at particular risk of developing obstruction of the ureters or squeezing of the spinal cord. In this category of patients should be carefully monitored during the first month of therapy. If spinal cord compression or renal failure caused by obstruction of the ureters is observed or developed, 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, Zoladex 3.6 mg is used. When using Zoladex in women before menstruation is restored, non-hormonal methods of contraception should be used. 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 receiving Zoladex 3.6 mg for the treatment of endometriosis, the addition of hormone replacement therapy (estrogen and progestogen preparations daily) reduced the loss of bone mineral density and vasomotor symptoms. Currently, there is no experience with the use of hormone replacement therapy in the treatment with Zoladex 10.8 mg. Resumption of menstruation after the end of treatment with Zoladex may be delayed in some patients. In rare cases, some women during treatment with GnRH analogues may have menopause without restoring menstruation after the end of therapy. Using the drug Zoladex may 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 drug therapy benign gynecological diseases lasting more than 6 months. According to preliminary data, the use of bisphosphonate in combination with Ago nistami GnRH in men helps to reduce the loss of bone mineral density.In connection with the possibility of developing a decrease in glucose tolerance while taking GnRH agonists in men, it is recommended to periodically monitor blood glucose levels. Effect on ability to drive vehicles and control mechanisms There is no evidence that Zoladex impairs ability to drive vehicles and work with mechanisms.