Goserelin
When ATH:
L02AE03
Characteristic.
Antitumor hormonal, synthetic decapeptide - analogue of gonadotropin releasing hormone (GnRG). Goserelin Acetate - almost white powder. Free soluble in acetic acid, soluble in water; 0,1M hydrochloric acid; 0,1M sodium chloride solution, dimethylformamide, dimethyl sulfoxide. Insoluble in acetone, xloroforme, ether. Molecular weight 1269,43 (goserelin), 1328 (goserelin acetate).
Pharmacological action.
Antitumor, anti-androgenic.
Application.
Goserelin 3,6 mg: hormonedependent prostate cancer, hormone-dependent breast cancer in women of reproductive age or perimenopausal, endometriosis, the need for a preliminary endometrial thinning prior to surgery, uterine fibroids (in combination with surgery), to suppress the pituitary gland in the preparation of superovulation in the framework of ECO (in vitro fertilization).
Goserelin 10,8 mg: hormonedependent prostate cancer, endometriosis, uterine fibroids.
Contraindications.
Hypersensitivity, incl. to other GnRH analogues; childhood and adolescence (to 14 years).
Restrictions apply.
Urinary tract obstruction (a history of men), metastases in the spine (the risk of spinal cord compression resulting from acute illness at the beginning of treatment).
Pregnancy and breast-feeding.
Contraindicated in pregnancy (adequate and well-controlled studies in humans have not held). Goserelin can cause adverse fetal effects when administered to pregnant women. Effects on reproduction as a result of the properties of matter antigonadotropnym observed in chronic administration. In women of childbearing age before treatment should be deleted pregnancy. Women should use a non-hormonal methods of contraception during treatment and during the goserelin 12 weeks after its cancellation. If goserelin used during pregnancy or if pregnancy occurred during therapy goserelin, The patient must be advised of the potential harm to the fetus and the risk of spontaneous abortion.
At the time of treatment should stop breastfeeding (unknown, Do goserelin penetrates into the breast milk of women, but it is known, that goserelin is excreted into the milk of lactating rats).
Side effects.
From the nervous system and sensory organs: dizziness, headache, sleep disturbance, excessive fatigue or weakness, anxiety, depression, paraesthesia, cerebrovascular accident.
Cardio-vascular system and blood (hematopoiesis, hemostasis): labile blood pressure, increased blood pressure, arrhythmia, myocardial infarction, occlusive peripheral circulatory disorders (soreness or cooling the hands and feet), exacerbation of chronic heart failure (swelling of feet, ankles), anemia.
From the respiratory system: exacerbation of COPD, upper respiratory tract infection.
From the digestive tract: decreased appetite, nausea, vomiting, constipation or diarrhea.
Allergic reactions: skin rash, anaphylactoid reactions.
Other: exacerbation of the symptoms of breast cancer, weight gain, hypercalcemia (in patients with bone metastases), gout (joint pain), increased sweating, tides; men - obstruction of the urinary tract, syndrome, spinal cord compression, reduced potency, gynecomastia; women - dry vaginal mucosa, tides, mood lability, decreased libido, menopause, amenorrhea (After discontinuation resumption of menstruation may not occur), bloody issues (at the beginning of treatment), the formation of ovarian cysts, reduction in bone density and bone mass.
Dosing and Administration.
P / (if necessary under local anesthesia), adult, into the anterior abdominal wall, depot 3,6 mg - every 28 days, depot 10,8 mg - every 12 days. Malignancy - long; in benign gynecological diseases - not more than 6 Months; for thinning the endometrium 2 Depot is administered at intervals of 4 Sun, wherein the operation is recommended during the first two weeks after the second depot.
Elderly patients, patients with renal or hepatic impairment dose adjustment carried out is not necessary.
When IVF goserelin 3,6 mg used for pituitary desensitization, which is determined by the concentration of estradiol in the serum.
Precautions.
Sick, receiving goserelin, should be under the supervision of a physician. In connection with the increase in the frequency of exacerbations of the disease due to increased testosterone levels in the blood, occurrence of urinary tract obstruction and spinal cord compression in the presence of metastases is necessary to carry out systematic monitoring of the state within the first month of therapy, including determination of serum concentration of testosterone, prostatic antigen, acid phosphatase activity.
Pain in the bones during temporary flare-ups can be treated symptomatically. Spinal cord compression or renal failure, caused by obstruction of the ureter, It should be treated in a conventional manner. In an extreme case, you should resort to orchiectomy.
Repeated courses of benign gynecological disorders are not recommended due to the high probability of osteoporosis. After the abolition of progressive therapy may restore bone density.
The treatment increases the tone of the cervix, may have difficulty dilatation.
With careful use of goserelin 3,6 IVF mg in patients with polycystic ovary syndrome, tk. can stimulate a large number of follicles.
