Index of drugs

Treatment of hormone-dependent, advanced prostate cancer. In combination with radiotherapy - treatment of hormone-dependent high-risk cancer limited to the prostate and hormone-dependent locally advanced prostate cancer.

1 amp-syringe. with powder for solution for injection contains 7.5 mg, 22.5 mg or 45 mg of leuprolide acetate.

Leuprorelin is a synthetic nonapeptide, an agonist of naturally occurring gonadotrophin releasing hormone (GnRH). Administered continuously inhibits gonadotropin secretion by the pituitary gland and inhibits steroidogenesis in the testes in men. It works more strongly than a naturally occurring hormone, and the time it takes to get an initial testosterone concentration can vary in individual patients. Administration of the drug results in a decrease in testosterone below the castration threshold (≤ 50 ng / dl). This reduction in concentration is observed within 3-5 weeks after the start of treatment. The testosterone concentration after 6 months of treatment is on average 6.1 (± 0.4) ng / dl and is comparable to the concentration after bilateral orchidectomy. C_max after the first administration occurs after 4-8 hours after injection. After initial elevation of leuprorelin after each injection (the plateau phase is reached 2 to 28 days after injection), blood levels remain relatively unchanged. The drug in 43-49% is bound to plasma proteins. The final elimination half-life is about 3 hours.

Hypersensitivity to leuprorelin acetate or other GnRH agonists or to any of the excipients. Patients undergoing an orchiectomy (similar to other GnRH agonists, the drug does not cause further reduction in blood testosterone levels in patients undergoing surgical castration). Monotherapy in patients with prostate cancer who have pressure on the spinal cord or spinal metastases. Women. Youth and children.

An additional antiandrogen treatment should be considered from the 3rd day prior to initiating leuprorelin treatment and for up to 2-3 weeks of treatment, in order to alleviate the effects of the initial increase in testosterone in the blood. If any symptoms of compression of the spinal cord or renal failure occur during therapy, standard treatment of these complications should be implemented. During the first weeks of treatment, patients with spinal and / or brain metastases as well as patients with urinary tract stenosis should be closely monitored. In the case of a pituitary haemorrhage (symptoms: sudden headache, vomiting, visual disturbances, eye muscle pains, mental state changes, sometimes circulatory collapse), immediate medical attention is required. In patients who do not show clinical improvement despite adequate reduction in testosterone levels, the possibility of tumors that do not respond to hormonal treatment should be considered - further treatment with leuprorelin in these patients will not be beneficial. During treatment, periodic blood Glucose and / or glycosylated hemoglobin (HbA1c) should be checked and the currently prescribed treatment for hyperglycaemia or diabetes mellitus should be used. Patients using GnRH agonists should be monitored for signs and symptoms suggestive of cardiovascular disease development and follow current clinical practice. Clinical trials have not been conducted in patients with impaired liver or kidney function.

Not applicable - the drug is contraindicated for use in women.

Very common: hot flushes, ecchymosis, erythema, fatigue, burning at the injection site, disturbances of sensation at the injection site. Common: nasopharynxitis, nausea, diarrhea, pruritus, night sweats, joint pain, limb pain, muscle pain, urinary incontinence, difficulty urinating, painful urination, nocturia, oliguria, breast tenderness, testicular atrophy, pain testicular, infertility, hypertrophy of the breast glands, malaise, pain at the injection site, bruising at the injection site, pricking at the site of administration, muscle stiffness, weakness, haematological abnormalities, increased CK activity, prolonged coagulation time.Uncommon: urinary tract infection, local infection of the skin, increased diabetes, unusual dreams, depression, decreased libido, dizziness, headache, sensation loss, insomnia, taste disorder, impaired odor, hypertension, hypotension, runny nose, shortness of breath , constipation, dry mouth, indigestion, vomiting, sweating, increased sweating, back pain, muscle spasms, bladder contraction, haematuria, increased frequency of urination, urinary retention, gynecomastia, impotence, testicular diseases, pruritus at the injection site, drowsiness, pain, fever, increase in ALT, increase in serum triglycerides, prolonged prothrombin time, weight gain. Rare: involuntary movements, fainting, collapse, bloating, belching, alopecia, skin eruptions, breast pain, ulceration at the injection site. Very rare: necrosis at the injection site. Frequency unknown: QT interval prolongation. In addition, peripheral edema, pulmonary embolism, palpitations, muscle pain, muscle weakness, abnormal skin sensation, chills, dizziness, rash, amnesia, visual disturbances, impaired glucose tolerance, decreased bone density may occur (long-term Leuprorelin therapy may increase the symptoms of osteoporosis). There have been reports of an increased risk of myocardial infarction, sudden cardiac death and stroke due to the use of GnRH agonists. After administration of both short and long-acting GnRH agonists, pituitary infarction following pituitary haemorrhage and thrombocytopenia and leukopenia have been reported rarely. During the first weeks of treatment with leuprorelin, there may be exacerbation of subjective and objective symptoms of the disease. If you have severe changes such as spinal metastases and / or narrowing of the urinary tract or haematuria, neurological symptoms may appear such as weakness and / or paresthesia in the lower limbs or a further worsening of urological symptoms.

Subcutaneously. Adult men: 7.5 mg every month or 22.5 mg every 3 months or 45 mg every 6 months. Therapy for advanced prostate cancer is long-lasting and should not be interrupted when remission or improvement occurs. The drug can be used in the treatment of neoadjuvant or adjuvant in combination with radiotherapy for high-risk cancer limited to the prostate and locally advanced prostate cancer. Response to treatment should be monitored by assessing the clinical condition and measuring the concentration of prostate antigen (PSA) in the blood. If the patient's response to treatment is less than expected, it is recommended to confirm that blood levels of testosterone have decreased to the level of castration or whether they remain at this level.Way of giving. Contents of 2 amp-syringe. (powder + starter) should be mixed immediately before injection. As a result of incorrect reconstitution, the lack of clinical efficacy may occur. Proper preparation of a ready-to-administer drug is a key stage of administration, ensuring safe and effective treatment. Please read the instructions on the appropriate methods for preparing the finished drug and its administration and follow these instructions - see SPC and leaflet. Do not administer intra-arterially or intravenously. Periodically change the injection sites.