Pharmacological properties Zoladex Injection:
goserelin is a synthetic analogue of natural LH WG. With constant use of Zoladex Injection reversibly inhibits the secretion of LH in the anterior pituitary, which leads to lower testosterone levels in the blood serum in men and estradiol concentrations in serum of women. This effect is reversible after discontinuation of therapy. Early treatment Zoladex, like other agonists of LH WP can cause a temporary increase in the concentration of testosterone in the blood serum in men and estradiol – in women, some women at this time may experience vaginal bleeding of varying duration and intensity, which then pass on their own and are due to is likely to decrease estrogen levels.
In men, approximately 21 days after the first injection of the drug concentration of testosterone is reduced to a level comparable to that at castration, and continues to remain low, with regular administration of the drug with an interval of 28 days (when taking capsules containing 3.6 mg of goserelin) or 3 months ( when taking capsules containing 10.8 mg of goserelin).
The majority of patients with tumor regression mark of the prostate and clinical improvement.
If in exceptional circumstances, the reintroduction of the dose at 3 months (while taking capsules containing 10.8 mg of goserelin) does not occur, the data suggest that testosterone levels, which corresponds to that in the castration was maintained in most patients up to 16 weeks.
In women, estradiol concentrations in serum also reduced by about 21 days after the first injection and at regular intervals with repeated administration 28 days remains at a level comparable to that observed in postmenopausal women. This provides a therapeutic effect in hormone-dependent forms of breast cancer, endometriosis and uterine fibroids. This also causes thinning of the endometrium and is the cause of amenorrhea in most patients.
Zoladex in combination with iron supplementation causes amenorrhea and improvement in hemoglobin and red blood cell count in women with uterine fibroids and associated anemia. This combination provides an additional increase in hemoglobin levels by an average of 10 g / l compared with therapy with only iron supplementation.
Very rarely, some women during treatment with analogs of LH may WG menopause without restoration of the menstrual cycle after therapy.
The bioavailability of Zoladex is almost complete, its application in accordance with the recommendations for dosing provides effective action goserelin without clinically significant accumulation. The drug is weakly bound to plasma proteins. The half-life of 2-4 h. The maximum concentration in serum (mean maximum concentration – 8-10 mg / ml) was reached after approximately 2 h after a single dose of Zoladex of 10.8 mg. After that, the average concentration of goserelin remained relatively stable in the range 0.3-1 ng / ml until the end of treatment. In patients with impaired renal function the half-life of active substances from the body increases, but the introduction of monthly goserelin acetate depot in the form it is not significant and does not require changing the dosage for these patients. In patients with liver failure of significant changes in the pharmacokinetics of the drug is not marked.
INDICATIONS Zoladex Injection:
Prostate cancer: treatment of prostate cancer is sensitive to hormonal effects;
- Breast cancer that is sensitive to hormonal effects in women of reproductive age and during perimenopause;
- Endometriosis: Endometriosis therapy – reduces the size and number of endometrial lesions, alleviating symptoms, including pain;
- For thinning the endometrium: is indicated for endometrial thinning prior to ablation or surgical yogo resection;
- Uterine fibroids: Zoladex therapy reduces tumor volume, improves hematologic status of patients, reducing symptoms, including pain;
as an adjuvant in combination with surgery to reduce blood loss during surgery and to reduce interference;
- When using reproductive techniques – pituitary regulation in preparation for superovulation.
Application: Application of Zoladex 3.6 mg.
1) Prostate cancer is sensitive to hormonal influences.
2) Breast cancer, which is sensitive to hormonal effects in women of reproductive age and perimenopausal.
3) Endometriosis: to alleviate symptoms, including pain, and reduce the size and number of endometrial lesions.
4) The thinning of the endometrium prior to ablation or surgical resection.
5) uterine fibroids: Zoladex reduces tumor nodes, and improves hematologic status of patients and reduces symptoms, including pain. It is used as an adjuvant during surgery to facilitate the operative technique and to reduce blood loss during surgery.
6) In vitro fertilization for pituitary desensitization in preparation for the stimulation of superovulation.
The use of Zoladex 10.8 mg.
1) Prostate cancer is sensitive to hormonal influences.
2) Endometriosis: treatment of endometriosis, including the relief of symptoms such as pain, and reducing the size and number of endometrial lesions.
3) uterine fibroids: treatment fibroids, including the reduction of injuries, improved hematologic status and relief of symptoms such as pain. It is used as an adjuvant during surgery to facilitate the operative technique and to reduce blood loss during surgery.
The use of Zoladex 3.6 mg.
Adults.
One capsule (3.6 mg) of the drug Zoladex is injected subcutaneously into the anterior abdominal wall every 28 days. Duration of drug administration Zoladex for cancer determined by a physician for each patient individually.
In Vitro Fertilization: Zoladex 3.6 mg is indicated for the desensitization of the pituitary gland, which is determined by the concentration of estradiol in the blood and must meet for what exists in the early follicular phase (approximately 150 pmol / l). This usually occurs between 7 and 21 day menstrual cycle. Superovulation (controlled ovarian stimulation) with gonadotrophin start, when it reached desensitization. Desensitization caused by the introduction of LHRH agonist (Zoladex) is more stable, so in some cases, you may need to increase the dose of gonadotropins. At the appropriate stage of development of the follicles of gonadotropin administration is terminated and subsequently injected human chorionic gonadotropin for ovulation induction. Control treatments, and procedures for oocyte fertilization carried out in accordance with normal practice, each medical institution.
For patients with renal or hepatic insufficiency, as well as for elderly patients there is no need to adjust the dose.
Endometriosis can be treated with no more than 6 months, since there are no clinical data regarding longer periods of use. Repeated courses of therapy should not carry the danger of the loss of minerals and reduced bone density. It has been demonstrated that patients who received Zoladex in connection with endometriosis, additional hormone replacement therapy (daily doses of estrogens and progestagens drugs) reduced loss of bone mineral density and severity of vasomotor symptoms.
For the thinning of the endometrium are 2 capsules at intervals of 4 weeks, while the operation plan between the 0th and the 2nd week after the second capsule.
The use of Zoladex 10.8 mg.
Adult men.
One capsule (10.8 mg) of the drug Zoladex is injected subcutaneously into the anterior abdominal wall every 3 months.
Adult women.
Endometriosis and uterine fibroids: treatment should not exceed six months, since there are no clinical data regarding longer periods of use.
Repeated treatments should not be at the risk of loss of mineral components and to reduce bone density.
Patients who received 3.6 mg of Zoladex for endometriosis, an additional gormonozamenyayuschaya therapy (estrogen daily decision and progestrogennyh drugs) reduced the loss of bone mineral density and severity of vasomotor symptoms.
Experience of using gormonozamenyayuschey therapy in women who received Zoladex 10.8 mg, no.
For patients with renal or hepatic insufficiency, as well as for elderly patients there is no need to adjust the dose.
Contraindications: pregnancy and lactation, hypersensitivity to the drug or other analogs of LH WG. Zoladex is not used in pediatric practice.
SIDE EFFECTS Zoladex Injection:
Hypersensitivity reactions, including anaphylaxis, arthralgia, paresthesia nonspecific, skin rash (usually disappears without the drug), changes in blood pressure (transient arterial hypo-or hypertension, in some cases requiring drug discontinuation), rarely – Local reaction in the form of subcutaneous bleeding at the injection site.
As in the case of other drugs of this class in the early treatment of rare bleeding may occur in the pituitary gland, symptoms of which are headache, fever, poor coordination of movements.
In men, there may be “hot flashes”, sweating and lower potency, they rarely require discontinuation. Rarely observed swelling and breast tenderness. At the beginning of the treatment of patients with prostate cancer may occur a temporary increase of pain in the bones, in this case should be symptomatically. Noted isolated cases of ureteral obstruction and the development of spinal cord compression.
Women may be “hot flashes”, sweating and violation of sexual desire, often requiring discontinuation of the drug, and sometimes – headache, frequent mood swings, depression, dryness of the vaginal mucosa, is rare – the change in the mammary glands. At the beginning of treatment in patients with breast cancer can temporarily increase the severity of symptoms, in this case, symptomatic treatment (aromatase inactivators and progestins). In rare cases after initiation of therapy in patients with bone metastases occur hypercalcemia. In women with uterine fibroids can celebrate degeneration fibromatous nodes. In a few cases during therapy for breast cancer with bone metastases developed hypercalcaemia. Using the drug in the reproductive program in combination with gonadotropin were cases of ovarian hyperstimulation syndrome. It is believed that the pituitary desensitization using the drug in some cases, the need to increase the dose of gonadotropins. If necessary, the introduction of human chorionic gonadotropin should be stopped. There have been reports on the formation of follicular cysts and corpus luteum cysts during treatment with LH WG. Most cysts are asymptomatic, non-functional, different size and disappeared on their own.
SPECIAL INSTRUCTIONS Zoladex Injection:
Zoladex is not indicated for the treatment of children, since safety and efficacy in this patient group have not been established.
Zoladex should be used with caution in men who have a risk of urinary tract obstruction or compression of the spinal cord. Necessary to carry out systematic monitoring these patients during the first month of therapy. In the case of spinal cord compression or obstruction of the ureters are usually prescribed for treatment of these complications.
The use of analogs of LH RG women can cause osteoporosis. Available at this time, data on the drug Zoladex evidence of decline on average by 4.6% the density of vertebral bone loss in parts of mineral components after 6-month course of treatment and the progressive restoration of the mean value decreasing by 2.6% (in compared with baseline) at 6 months after stopping treatment. Zoladex should be prescribed with care for women with bone metabolic disorders. Zoladex can also cause an increase in resistance of the cervix and in connection with the difficulty of dilation.
Zoladex (3.6 mg) should be used only as part of reproductive techniques under the supervision of specialists. As with other agonists of LH WG, there were cases of ovarian hyperstimulation syndrome (NWFS) associated with the use of Zoladex (3.6 mg) in combination with HCG. It is believed that the pituitary regulation with depot dosage form, in some cases increases the need for gonadotropins. Cycle of stimulation should be performed with caution in patients at risk for NWFS. In the case of human chorionic gonadotropin careful clinical monitoring.
It should be used with caution Zoladex (3.6 mg) in reproductive techniques in patients with polycystic ovary syndrome.
Although experimental studies have teratogenic drugs have been identified, Zoladex should not be used during pregnancy, since theoretically the application of agonists, N WG there is a risk of fetal abnormalities and miscarriage. Patients of childbearing age should avoid possible pregnancy before starting treatment Zoladex. During therapy, you should use non-hormonal methods of contraception and endometriosis – to restore the menstrual cycle.
Not recommended for Zoladex in breast-feeding.
If you plan to use Zoladex during in vitro fertilization, early treatment to exclude pregnancy. Clinical data on the use of Zoladex for this indication is limited. But in the available data do not suggest for a single case of oocyte developmental abnormalities or pregnancy.
The effect on driving ability and other mechanisms. No effect.
