Index of drugs

Treatment of prostate cancer when it is required to lower the testosterone concentration to a concentration characteristic of the lack of function of the gonads (castration concentration). Treatment of endometriosis for a period of 6 months (the preparation can be used only in pharmacological treatment or in pharmacological treatment complementary to surgery). Treatment of uterine leiomyomas (leiomyoma uteri) for a period not longer than 6 months (treatment can be used before surgery to remove fibroids or uterus, it can also be used to reduce the severity of symptoms in perimenopausal women who do not want to undergo surgery). In addition, Lucrin Depot 3.75 mg: causative treatment of children with premature puberty of hypothalamo-pituitary origin; Lucrin Depot 11.25 mg: treatment of estrogen-dependent breast cancer in pre-menopausal women and in the perimenopausal period in which pharmacological suppression of ovarian function is required.

One vial contains 3.75 mg or 11.25 mg leuprolide acetate microspheres for suspension for injection.

Synthetic gonadorelin analogue (LH-RH), characterized by a much longer half-life in the body and greater affinity to the receptor in comparison with natural gonadorelin. This hormone controls the release of gonadotropin hormones LH and FSH, which stimulates the synthesis of steroid hormones in the ovaries and testes. Administration of leuprolide acetate causes a few-day increase in the release of LH and FSH, and then leads to almost complete inhibition of gonadotropin synthesis and release, and as a result, suppresses gonadal function and reduces the concentration of sex hormones to castration values. Decrease in estrogen or testosterone levels in the blood leads to inhibition of growth of hormone-sensitive tumors. The drug is inactive after oral administration. The bioavailability of the drug after subcutaneous and intramuscular administration is similar and amounts to approximately 90%. It binds to plasma proteins in 43-49%. After administration of the drug at a dose of 3.75 mg after the initial increase in the concentration of the drug in the blood, it decreases within 2-4 days. The maximum blood concentration of the drug at the end of the first month is 0.7 μg / ml. After intramuscular or subcutaneous administration of 11.25 mg of the drug as a suspension, leuprolide acetate is released continuously for 3 months. The maximum concentration of the drug in the blood occurs 3 h after administration, the stationary concentration - 7-14 days after administration. The drug does not accumulate in the body. T_0,5 is 3 hours.

Hypersensitivity to leuprorelin acetate, similar nonapeptides or any of the excipients. Bleeding from the vagina of undetermined etiology. Pregnancy or reasonable suspicion of pregnancy.

Carefully used in patients with spinal metastasis or urinary retention (the need for hospitalization), due to the possibility of neurological disorders or worsening urinary tract disorders.

Use during pregnancy is contraindicated. Do not use during breast-feeding.

Men with prostate cancer. Very common: dilation of blood vessels, hot flushes, increase in LDH activity in the blood. Common: anorexia, decreased libido, dyspnoea, nausea, vomiting, diarrhea, hyperhidrosis, joint pain, erectile dysfunction, atrophic changes of the testicles, pain, peripheral edema, fatigue, pain at the injection site, induration at the injection site, increased ALP activity in the blood, increase in AST in the blood. Uncommon: rhinitis, fungal skin infection, cancer, hyperglycemia, weight gain, insomnia, sleep disturbances, mood changes, depression, dizziness, paresthesia, drowsiness, earache, tinnitus, amblyopia, arrhythmia, angina pectoris, additional ventricular contractions, angiopathy, hypertension, peripheral circulatory disorders, epistaxis, haemoptysis, emphysema, alopecia, rash,maculopapular rash, hair disorder, night sweats, bone pain, muscle pain, muscle weakness, limb pain, painful or difficult urination, pollakiuria, hematuria, urinary stasis, polyuria, gynecomastia, breast enlargement, chest pain, weakness, inflammation at the injection site, erythema at the injection site, irritation at the injection site, chills, decreased hemoglobin in the blood, increased urea in the blood, increased uric acid in the blood, increased Calcium in the blood, increased ALT in the blood, increased activity GGT in the blood, reducing the number of platelets, increasing the number of white blood cells, the presence of protein in the urine. Frequency unknown: QT interval prolongation.Women with endometriosis / uterine myomas. Very common: weight gain, emotional instability, decreased libido, insomnia, depression, nervousness, anxiety, dizziness, headache, vasodilation, nausea, acne, vaginitis. Common: weight loss, hypercholesterolemia, confusion, hostility, unipolar depression, anxiety, paresthesia, migraine, hypertension, visual impairment, amblyopic dizziness, palpitations, constipation, nausea, vomiting, diarrhea, dry mouth, abdominal pain , flatulence, alopecia, ecchymosis, seborrhea, rash, dry skin, hyperhidrosis, hirsutism, arthropathy, joint pain, stiff neck, back pain, neck pain, painful or difficult urination, atrophic breast changes, germinal secretions , chest pain, pelvic pain, weakness, pain, chest pain, swelling, pain at the injection site, chills, thirst, abnormal results of liver function tests. Uncommon: infection, pyelonephritis, boil, rhinitis, vulvovaginal candidiasis, influenza, anorexia, increased appetite, personality disorders, delusions, abnormal thinking, euphoric mood, moodiness, apathy, drowsiness, amnesia, fainting, taste disorders, ataxia, eye disorder, eye pain, tachycardia, nosebleeds, dysphonia, abdominal distension, vomiting, indigestion, gastritis, bleeding gums, liver tenderness, maculopapular rash, unpleasant body odor, nail disorder, skin discoloration, photosensitivity reaction, vesicular dermatitis, hair disorders, muscle pain, arthritis, urinary incontinence, pollakiuria, menstrual disorder, breast enlargement, congestion and swelling of the breasts, galactorrhoea, uterine haemorrhage, menorrhagia, injection site reaction , lump at the injection site a, swelling of the face, hypersensitivity at the injection site, exacerbation of symptoms, abnormal laboratory results.Women with breast cancer. Very common: increased appetite, weight gain, weight loss, sudden mood changes, nervousness, insomnia, depression, dizziness, headache, hot flushes, nausea, sweating, joint pain, back pain, weakness, pain at the injection site , induration at the injection site, general deterioration of health, feeling hot. Common: Decreased appetite, sleep disorder, paraesthesia, drowsiness, conjunctivitis, dehydration, tremor, conjunctivitis, deafness, motion sickness, swelling of the ear, palpitations, rhinitis, dyspnoea, increased sputum, cough, constipation, vomiting, abdominal enlargement, diarrhea, gingivitis, gastritis, epigastric pain, abdominal pain, stomatitis, retching, abnormal liver function, fatty liver, erythema, alopecia, acne, rash, eczema, bone pain, neck pain, osteoarthritis, muscle weakness, muscle and skeletal rigidity, muscle tremor, pollakiuria, vaginal discharge, breast pain, uterine hemorrhage, menopausal symptoms, vaginitis, chest pain, edema, fatigue, fever , injection site reaction, pruritus at the injection site, erythema at the injection site a, irritability, malaise, positive result of faecal excrement, pain associated with surgery. Uncommon: infection of the upper respiratory tract, leukopenia, anorexia, increased body temperature.Children with precocious puberty of hypothalamic-pituitary origin. Common: growth retardation, weight gain, emotional instability, headache, vasodilation, acne, rash, unpleasant body odor, gynecomastia, vaginitis, pain, reaction at the injection site. Uncommon: infection, rhinitis, influenza, pharyngitis, sinusitis, cervical cancer, hypersensitivity reactions, precocious puberty, goiter, increased appetite, nervousness, depression, mood swings, drowsiness, fainting, increased mobility, bradycardia, hypertension , peripheral vascular disorder, nosebleeds, asthma, constipation, nausea, vomiting, difficulty in swallowing, gingivitis, indigestion, alopecia, hirsutism, hair disorder, nail disorder, vitiligo, skin hypertrophy, purpura, myalgia, arthropathy, myopathy , joint pain, urinary incontinence, vaginal haemorrhage, cervical disorder, dysmenorrhea, menstrual disorders, breast enlargement, vaginal discharge, breast pain, feminization, peripheral edema, fever, hypertrophy, aggravation of symptoms, presence of antinuclear antibodies, elevated descent red blood cells.Observations after placing the medicine on the market: pharyngitis, pneumonia, urinary tract infection, infection, skin cancer, anemia, anaphylactic reaction, goiter, pituitary haemorrhage (from patients with pituitary adenoma), dehydration, diabetes, increased appetite, hypoglycaemia, hyperlipidemia (total cholesterol, LDL cholesterol) , triglycerides), hyperphosphatemia, hypoproteinemia, depression, sudden mood changes, nervousness, insomnia, sleep disorders, anxiety, delusions, increased libido, suicidal thoughts, suicide attempts, dizziness, hypoesthesia, lethargy, neurogenic muscular disease, paresthesia, peripheral neuropathy, impaired memory, transient ischemic attack, syncope, loss of consciousness, dysgeusia, stroke, paralysis, headache, convulsions, visual impairment, amblyopia, blurred vision, dry eyes, eye disorder, hearing disorders, tinnitus, angina pectoris, bradycardia, arrhythmia, congestive heart failure, myocardial infarction o, tachycardia, sudden cardiac death, phlebitis, thrombosis, varicose vein, lymphoedema, ischemia, hypertension, hypotension, hot flushes, cough, dyspnoea, epistaxis, haemoptysis, pleural fibrillation, pulmonary fibrosis, pleural effusion, infiltration lung tissue, respiratory distress, swelling of the sinus mucosa, pulmonary embolism, interstitial lung disease, constipation, diarrhea, dry mouth, difficulty in swallowing, gastrointestinal haemorrhage, gastrointestinal disorder, nausea, peptic ulcer, rectal polyps, vomiting, abdominal distension, abnormal liver function, jaundice, severe liver damage, dermatitis, dry skin, abnormal hair growth, alopecia, pigmentation disorders, pruritus, rash, skin lesion, urticaria, ecchymosis, hypersensitivity reaction to the light, ankylosing arthritis spine, arthropathy a, joint pain, muscle ache, tenosynovitis, temporal bone region swelling, bladder contraction, hematuria, urinary incontinence, pollakiuria, urinary tract obstruction, urgency urinary urgency, urinary tract disorder, penile edema, penile disorder, prostate pain , atrophic changes of the testicles, testicular pain, testicular impairment, breast pain, breast tenderness, gynecomastia, vaginal haemorrhage, menstrual disorder, uterine hemorrhage, weakness, chills, fever, pain, edema, thirst, inflammation at the injection site, reaction in at the injection site, injection site pain, injection site abscess, injection site hematoma, lump, inflammation, pelvic fibrosis, abnormal liver function tests, increased blood urea, increased blood calcium , increase in blood creatinine, with decrease in blood potassium, increase in uric acid in the blood, increase in triglycerides in the blood, increase in bilirubin in the blood, increase in low-density lipoprotein in the blood, changes in ECG, decreased platelet count,increase or decrease in the number of white blood cells, prolongation of the partial thromboplastin time after activation, prolonged prothrombin time, heart murmurs, vertebrae fracture. Changes in bone mineral density and cases of major venous and arterial thromboembolic events, including deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke and transient ischemic attack, have been observed.

Intramuscularly or subcutaneously.Prostate cancer, endometriosis and uterine fibroids: 3.75 mg once a month or 11.25 mg once every three monthsEstrogen-dependent breast cancer: 11.25 mg once every three monthsPremature puberty of hypothalamic-pituitary origin: the dose should be selected individually, younger children require higher doses determined in mg / kg.The starting dose. The recommended starting dose is 0.3 mg / kg. every 4 weeks (at least 7.5 mg), according to the scheme - mc. ≤25 kg: 3.75 mg x 2, 1 injection (total dose 7.5 mg); mc. > 25-37.5 kg: 3.75 mg x 3.2 injections (total dose 11.25 mg); mc. > 37.5 kg: 3.75 mg x 4, 2 injections (total dose 15 mg). If administration of the recommended total dose requires 2 injections, it should be done at the same time.Maintenance dose.For most children, it is possible to use the first dose over the entire treatment period, which has caused a sufficient reduction in the secretion of sex hormones. In patients whose body weight has significantly increased over the course of treatment, it should be monitored whether adequate hormone secretion has been achieved. If hormone release is not achieved, the dose should be gradually increased by 3.75 mg every 4 weeks until proper hormone secretion is achieved. This dose will be a maintenance dose.