Lyukrin Depot - Instructions For Use, Drug Price, Reviews, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Lukrin depot

Lyukrin depot: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. Use in the elderly
12. 12. Drug interactions
13. 13. Analogs
14. 14. Terms and conditions of storage
15. 15. Terms of dispensing from pharmacies
16. 16. Reviews
17. 17. Price in pharmacies

Latin name: Lucrin depot

ATX code: L02AE02

Active ingredient: leuprorelin (Leuprorelin)

Manufacturer: Takeda Pharmaceutical Company, Limited (Japan)

Description and photo update: 2019-08-10

Prices in pharmacies: from 6799 rubles.

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Lukrin depot is an antineoplastic drug, analogue of gonadotropin-releasing hormone (GnRH).

Release form and composition

Lukrin depot dosage form:

• lyophilisate for the preparation of a suspension for intramuscular (i / m) and subcutaneous (s / c) administration of prolonged action: white powder with a colorless transparent solvent included. In the finished white suspension, when settling, a white precipitate is formed, which, when shaken, is easily resuspended [in a blister pack 1 set for single-dose administration, including the components that are necessary for one IV or SC injection: 1 clear glass bottle with a volume of 9 ml, containing 44.1 mg of lyophilisate, 1 ampoule of transparent glass containing 2 ml of solvent, 2 blisters containing 1 sterile needle, 1 empty sterile disposable propylene syringe, 1 napkin soaked in 70% isopropyl alcohol in paper laminated with polyethylene. In a plastic case with a first opening control system, 1 set for single-dose administration,including the components that are necessary for one i / v or s / c injection: 1 double-chamber syringe (consists of a finger rest, a glass cartridge with rubber stoppers and a front complex on which a needle closed with a plastic cap is attached), the first chamber of which is filled with 44, 1 or 130 mg of lyophilisate, and the second 1 ml of solvent, 1 plastic piston, 1 or 2 wipes soaked in 70% isopropyl alcohol in paper laminated with polyethylene];1 or 2 wipes impregnated with 70% isopropyl alcohol in polyethylene laminated paper];1 or 2 wipes impregnated with 70% isopropyl alcohol in polyethylene laminated paper];
• lyophilisate for preparation of a suspension for subcutaneous administration of prolonged action: white powder with colorless transparent solvent included. The finished suspension is white; when it stands, a white precipitate is formed in it, which, when shaken, is easily resuspended [in a plastic case with a first opening control system 1 set for single-dose administration, including the components that are necessary for one SC injection: 1 double-chamber syringe (consists of a finger rest, a glass cartridge with rubber stoppers and a front complex on which a needle closed with a plastic cap is attached), the first chamber of which is filled with 352.9 mg of lyophilisate, and the second with 1 ml of solvent, 1 plastic piston, 1 or 2 soaked 70 % isopropyl alcohol wipes in polyethylene laminated paper].

Each pack also contains instructions for the use of Lucrin Depot.

Composition of 44.1 mg of lyophilisate for the preparation of a suspension for intramuscular (i / m) and subcutaneous (s / c) administration of prolonged action:

• active substance: leuprorelin acetate - 3.75 mg;
• auxiliary components: mannitol - 6.6 mg; lactic and glycolic acid copolymer - 33.1 mg; gelatin - 0.65 mg.

Composition of 1 ml of solvent: polysorbate 80 - 1 mg; mannitol - 50 mg; carmellose sodium - 5 mg; water for injection - up to 1 ml.

Composition of 130 mg of lyophilisate for preparation of suspension for intramuscular (i / m) and subcutaneous (s / c) administration of prolonged action:

• active substance: leuprorelin acetate - 11.25 mg;
• auxiliary components: mannitol - 19.45 mg; lactic acid polymer - 99.3 mg.

Composition of 1 ml of solvent: polysorbate 80 - 1 mg; mannitol - 50 mg; carmellose sodium - 5 mg; water for injection - up to 1 ml; acetic acid - up to pH 5 to 7.

Composition of 352.9 mg of lyophilisate for preparation of suspension for s / c administration of prolonged action:

• active substance: leuprorelin acetate - 30 mg;
• auxiliary components: mannitol - 52.9 mg; lactic acid polymer - 270 mg.

Composition of 1 ml of solvent: acetic acid - from 0 to 0.05 mg; polysorbate-80 - 1 mg; mannitol - 50 mg; carmellose sodium - 5 mg; water for injection - up to 1 ml.

Pharmacological properties

Pharmacodynamics

Leiprorelin is a GnRH agonist, which, when used for a long time in therapeutic doses, effectively inhibits the secretion of gonadotropins. The use of the substance in humans serves as an initial increase in the concentration of follicle-stimulating and luteinizing hormone, which leads to a transient increase in the concentrations of sex hormones - estradiol and estrone in women, dihydrotestosterone and testosterone in men.

However, long-term use of leuprorelin leads to a decrease in the concentration of sex, luteinizing and follicle-stimulating hormones. Testosterone levels in men drop to prepubertal or castration levels. In women who are in a state before menopause, the concentration of estrogen decreases to the postmenopausal level. Such hormonal changes appear within a month from the start of using Lucrin Depot in recommended doses.

Suppression of steroidogenesis in the testes and ovaries is a reversible process that stops after completion of therapy.

Pharmacokinetics

The bioavailability of leuprorelin with subcutaneous and intramuscular administration is comparable. When the drug is administered at a dose of 7.5 mg, the absolute bioavailability is approximately 90%.

In patients with prostate cancer after a single intramuscular and subcutaneous injection of Lucrin Depot in doses of 3.75 / 7.5 mg, its plasma concentration by the end of the first month averaged 0.7 / 1 ng per ml, respectively.

Eleven premenopausal breast cancer patients had a serum leuprorelin concentration of 3.75 mg for 12 months. On average, the concentration of the substance exceeded 0.1 ng per 1 ml after 4 weeks and after repeated administration (at 8 and 12 weeks) remained stable.

There was no accumulation of the drug. The average equilibrium volume of distribution of the substance is 27 liters. Plasma protein binding varies from 43 to 49%. Systemic clearance is 7.6 liters per hour. The half-life is approximately 3 hours.

Since leuprorelin is a peptide, it is mainly subject to metabolic degradation by peptidase to shorter inactive peptides: metabolite I - pentapeptide; metabolites II and III - tripeptides; metabolite IV is a dipeptide.

The maximum concentration of the main metabolite M1 is reached within a period of 2 to 6 hours and corresponds to 6% of the maximum concentration of leuprorelin. After 7 days after injection, the average concentration of M1 in plasma is 20% of the average concentration of the substance.

After the administration of Lukrin Depot at a dose of 3.75 mg, its content in urine, like the content of M1, was less than 5% of the dose used 27 days after the drug was administered.

The pharmacokinetics of Lucrin Depot in patients with impaired liver / kidney function has not been studied.

Indications for use

Lukrin depot in the form of a lyophilisate for preparing a suspension for intramuscular and subcutaneous administration of prolonged action is used in such cases as:

• progressive prostate cancer, including cases where orchiectomy or the use of estrogens are not indicated or are not applicable in this patient (for palliative therapy);
• endometriosis (as the main therapy or in addition to surgical treatment for a period not exceeding six months). In combination with hormone replacement therapy for the treatment of the disease and its relapses;
• fibroids of the uterus (within a period of up to six months as a preoperative preparation for the removal of fibroids / hysterectomy or for symptomatic therapy and improvement of the condition of patients during menopause who refuse surgery);
• premature puberty of central origin in children (Lukrin depot at a dose of 3.75 mg);
• breast cancer in the perimenopausal period (in combination with hormone therapy).

Lyophilisate for the preparation of a suspension for s / c administration of prolonged action is prescribed to patients with prostate cancer who require a decrease in testosterone levels to castration levels.

Contraindications

Absolute:

• surgical castration;
• hormone-independent prostate cancer;
• pregnancy and lactation;
• age under 18 years (for the drug at a dosage of 3.75 mg, the exception is children with a diagnosis of premature puberty of central origin);
• individual intolerance to the components of the drug Lukrin Depot and similar drugs of protein origin.

In addition, for a lyophilisate for preparing a suspension for intramuscular and subcutaneous administration of prolonged action, contraindications are vaginal bleeding of unknown origin and age over 65 years in women.

Relative (Lukrin depot is prescribed under medical supervision): metastases in the spine, obstruction of the urinary tract, hematuria.

Lyukrin depot, instructions for use: method and dosage

Lyophilisate for preparation of suspension for i / m and s / c administration of prolonged action 3.75 mg

The suspension prepared from the lyophilizate Lukrin Depot is injected i / m or s / c.

Injections are carried out once a month. It is important to periodically change the injection site. Immediately before use, the lyophilisate (3.75 mg) is mixed with the supplied solvent (1 ml).

A single dose for patients with prostate or breast cancer is 3.75 mg. The duration of therapy is determined by the doctor on an individual basis.

The dose of Lukrin Depot for uterine fibroids and endometriosis is 3.75 mg. The first injection for patients of reproductive age is administered on the 3rd day of menstruation. The duration of treatment should not exceed six months.

The initial dose for children with premature puberty is 0.3 mg per 1 kg of body weight (minimum dose is 7.5 mg). The drug is administered once every 28 days.

The total dose of the drug / number of syringes or vials for injecting Lucrin Depot at a dosage of 3.75 mg, depending on the weight of the child, are respectively:

• less than 25 kg: 7.5 mg / 2 pcs.;
• from 25 to 37.5 kg: 11.25 mg / 3 pcs.;
• 37.5 kg: 15 mg / 4 pcs.

In cases where the required total dose involves the introduction of two or more injections, they are carried out simultaneously.

In the absence of complete suppression of the progression of premature puberty, the dose of the drug is increased by 3.75 mg every 28 days.

Withdrawal of therapy should be considered at age 11 years in girls and 12 years in boys.

Lyophilisate for preparation of suspension for intramuscular and subcutaneous administration of prolonged action 11 mg

The suspension prepared from the lyophilizate Lukrin depot is administered immediately after dilution i / m or s / c at a dose of 11 mg once every 3 months.

The medicinal product is used only under medical supervision.

Lyophilisate for preparation of suspension for subcutaneous administration of prolonged action 30 mg

The suspension prepared from the lyophilizate Lukrin depot is injected s / c at a dose of 30 mg once every six months immediately after dilution.

The medicinal product is used only under medical supervision. It is important to change the injection site periodically.

Suspension preparation instructions

When using Lukrin Depot at a dose of 3.75 mg in vials, first, the solvent from the ampoule is drawn into the syringe with the needle, and then it is added to the drug (the remaining solvent is disposed of). The bottle is shaken well until a homogeneous milky suspension is formed. Immediately after dilution, the entire contents of the vial are drawn into a syringe (maximum - 2 ml) and a s / c or i / m injection is performed.

Despite the fact that the Lukrin Depo suspension remains stable for 24 hours after preparation, it should be used immediately after dilution. Residues of the drug must be disposed of.

When using the drug in a dose of 3.75, 11 or 30 mg in two-chamber syringes, first the white plunger is screwed into the end tube until the plug starts to rotate. The syringe is held upright. Slowly, pressing the plunger, begin to inject the solvent until the first plug is in the middle of the syringe on the blue line. The syringe is kept upright.

Then, by gentle rocking, the preparation is thoroughly mixed with the solvent until a homogeneous suspension (suspension) of milky color is formed. Continuing to hold the syringe in an upright position, the cap is removed from the needle upward with the other hand, without unscrewing it, and the piston is pushed forward (due to this, air is removed from the syringe). Since the suspension settles very quickly, immediately after its formation, the entire content of the drug in a dose of 3.75 or 11 mg is injected i / m or s / c, at a dose of 30 mg - s / c.

Side effects

• cardiovascular system: impaired peripheral circulation, increased / decreased blood pressure, palpitations, edema, thrombosis, arterial and venous thromboembolism (including pulmonary embolism), stroke, phlebitis, myocardial infarction, transient ischemic attacks, orthostatic hypotension, changes in vasodilatation on the electrocardiogram, chronic heart failure, arrhythmia, tachycardia, bradycardia, angina pectoris, sudden cardiac death;
• digestive system: taste disturbance, flatulence, nausea, diarrhea / constipation, vomiting, thirst, dry mouth or hyposalivation, decreased / lack of appetite, gastritis, dysphagia, increased activity of hepatic transaminases, gastrointestinal bleeding, severe liver damage;
• endocrine system: breast tenderness, diabetes mellitus, impaired glucose tolerance, pituitary apoplexy, enlarged thyroid gland, galactorrhea, gynecomastia, androgen-like effects (voice change, increased hair growth, seborrhea, acne, virilization);
• hematopoietic organs: increased prothrombin and activated partial thromboplastin time, neutropenia, leukopenia, increased leukocyte count, thrombocytopenia, anemia;
• musculoskeletal system: osteoporosis, changes in bone density against the background of bone densitometry in women due to a decrease in estrogen levels, increased muscle tone, myalgia, arthralgia, bone pain;
• central and peripheral nervous system: hallucinations, dizziness, sleep disturbance (increased drowsiness, insomnia), headache, memory impairment, depression, increased irritability, fainting, confusion, hyperesthesia, paresthesia, thoughts of suicide and suicidal attempts, muscle weakness, seizures, peripheral neuropathy, neuromuscular disorders, personality changes, emotional lability, lethargy;
• respiratory system: pharyngitis, nosebleeds, respiratory distress, shortness of breath, cough, interstitial lung disease, infiltrates or fibrous formations in the lungs, pleural effusion;
• skin and its appendages: photosensitivity reactions, nail changes, eczema, dry skin, dermatitis, discoloration of the skin, alopecia, urticaria, hyperpigmentation, ecchymosis, pruritus / rash (including maculopapular); in women - hirsutism, hypertrichosis, acne;
• sense organs: tinnitus, hearing and vision impairment, conjunctivitis;
• genitourinary system: erectile dysfunction, decreased libido, pain in the testicles or prostate gland, testicular atrophy, edema of the penis, vaginal discharge, vaginitis, dryness of the vaginal mucosa, vaginal bleeding, dysmenorrhea, irregularities in the menstrual cycle, polyuria, hematuria, dysuria;
• laboratory parameters: an increase in the concentration of prostate-specific antigen, uric acid, blood urea nitrogen, bilirubin in the blood, the number of reticulocytes, the appearance of protein in the urine, an increase in the activity of aspartate aminotransferase, lactate dehydrogenase, alkaline phosphatase, hyperuricemia, hypokalemia, hyperglycemia, hypoglycemia, hyperglyceridemia (increased, low density lipoprotein cholesterol and total cholesterol), hypoproteinemia, hypercreatininemia, hypercalcemia;
• local reactions: abscess, hyperemia, tissue induration, irritation, swelling and pain at the injection site;
• others: increased sweating, flushing of the skin of the face and upper chest, flu-like syndrome, changes in body odor, increase / decrease in body weight, peripheral edema, increased fatigue, asthenia, allergic reactions (including anaphylactic shock), growth retardation in children, accession of secondary infections, compression of the spinal cord and / or acute urinary retention in men in the first 14 days of therapy, enlargement of lymph nodes in the first 7 days of the use of Lucrin Depot, the appearance of secondary tumor diseases (breast cancer, cervical cancer, skin).

Adverse events associated with the pharmacological effect of leuprorelin on steroidogenesis:

• benign / malignant / unspecified neoplasms, including polyps and cysts: progression of prostate cancer;
• metabolism: increase / decrease in body weight;
• nervous system: increased emotional lability, muscle weakness, headache;
• vascular system: orthostatic hypotension, decreased blood pressure, hot flashes, vasodilation;
• skin and subcutaneous tissue: nail / hair disorders, eczema, hirsutism, cold sweat, pigmentation disorders, hypotrichosis, night sweats, abnormal hair growth, urticaria, rash, abnormal skin odor, hyperhidrosis, dry skin, seborrhea, acne;
• reproductive system and mammary gland: increase / loss / decrease in libido, testicular pain, erectile dysfunction, testicular atrophy, penile edema, prostate pain, menorrhagia, vaginitis, dyspareunia, menopausal symptoms, metrorrhagia, galactorrhea, pain / congestion in breasts, breast enlargement, vaginal discharge, breast tenderness / atrophy, menstrual irregularities, vaginal bleeding, gynecomastia;
• others: an increase in the concentration of prostate-specific antigen, a decrease in bone density, irritability, a feeling of heat, dryness of the mucous membranes.

With prolonged exposure to leuprorelin (from 6 to 12 months), the development of osteoporosis, diabetes mellitus, an increase in the concentration of triglycerides, low-density lipoproteins and total cholesterol, and impaired glucose tolerance were observed.

Side effects of Lucrin Depot, which were noted in clinical studies and post-marketing observations:

• invasions and infections: influenza, sepsis, candidiasis, viral infection, boils, pyelonephritis, bronchitis, infection of the bladder and urinary tract;
• benign / malignant / unspecified tumors (including polyps and cysts): pseudolymphoma;
• blood and lymphatic system: eosinophilia, anemia;
• immune system: hypersensitivity reactions;
• metabolism: excessive weight loss / increase, hypercholesterolemia, dehydration, hypoglycemia, hyperglycemia, increased appetite, anorexia;
• nervous system: peripheral neuropathy, simple partial seizures, tremor, ataxia, hypertonicity, migraine, fainting, drowsiness, paresthesia, headache, dizziness, apathy, hostility, euphoria, confusion, delirium, anxiety, depression, insomnia, decreased sex drive, nervousness, personality disorders, mood swings;
• sensory organs: vestibular dizziness, visual impairment (including amblyopia), eye pain, dry eyes, decreased visual acuity;
• cardiovascular system: hematoma, vascular collapse, aneurysm, thrombophlebitis, increased blood pressure, lymphedema, vasodilation, hot flashes, atrioventricular block, bradycardia, palpitations, heart failure, tachycardia, angina pectoris;
• respiratory system: chronic obstructive pulmonary disease, bronchospasm, asthma, cough, emphysema, hemoptysis, shortness of breath, nosebleeds;
• digestive system: abdominal pain, dry mouth, bleeding gums, nausea, constipation, vomiting, diarrhea, bloating, flatulence, gastrointestinal bleeding, dyspepsia, gastritis, hepatocellular damage, hepatic cholestasis, liver tenderness, dysfunction liver;
• skin and subcutaneous fat: itching, hair growth disorders, hirsutism, hyperhidrosis, photosensitivity reactions, seborrhea, acne, dry skin, maculopapular rash, ecchymosis, alopecia;
• musculoskeletal system: muscle spasms, pain in limbs and bones, muscle weakness, stiff neck, arthritis, back pain, arthralgia, myalgia;
• genitourinary system: pain in the prostate gland, edema of the penis, pelvic pain, discharge from the genitals, vaginitis, galactorrhea, engorgement / atrophy / enlargement of the mammary glands, pain in the mammary glands, erectile dysfunction, gynecomastia, urinary disorders, urinary retention / incontinence, nocturia, hematuria, pollakiuria, dysuria;
• others: gait disturbances, flu-like condition, malaise, thirst, chills, hypersensitivity / edema / pain / induration / reaction at the injection site, fatigue, asthenia, dry mucous membranes, edema of the lower extremities and face, gravitational and peripheral edema, chest pain;
• laboratory parameters: an increase in the concentration of bilirubin, testosterone and triglycerides in the blood, low density lipoproteins and prostate specific antigen, heart murmurs, an increase in the activated partial thromboplastin and prothrombin time, a decrease in the concentration of potassium in the blood, abnormalities on the electrocardiogram, an increase in the activity of gamma-glutamyl transpeptidase, lactase lactase, aspartate aminotransferase and alanine aminotransferase, alkaline phosphatase in the blood, decreased platelet count, abnormal liver function tests, increased erythrocyte sedimentation rate.

Since the drug has several indications for use, not all of the listed side effects can be attributed to every patient. For most adverse events, a causal relationship with the reception of Lukrin depot has not been established.

In post-marketing studies, the following side effects were noted (the frequency of their development is unknown):

• invasions and infections: pneumonia, pharyngitis;
• tumors, benign / malignant / unspecified (including cysts and polyps): skin cancer;
• immune system: anaphylactic reactions;
• endocrine system: pituitary apoplexy, goiter;
• metabolism: hypoproteinemia, hyperphosphatemia, hyperlipidemia, diabetes mellitus;
• nervous system: sleep disorders, increased libido, mood swings, neuromyopathy, paralysis, seizures, transient ischemic attack, loss of consciousness, including fainting, cerebrovascular disorders, peripheral hypesthesia, neuropathy, dysgeusia, memory impairments, including amnesia, lethargy, attempts at suicide;
• sense organs: hearing impairment, ringing in the ears, dry eyes, decreased visual acuity;
• cardiovascular system: varicose veins, decreased blood pressure, thrombosis, phlebitis, myocardial infarction, arrhythmia, congestive heart failure, sudden cardiac death;
• respiratory system: interstitial lung disease, pulmonary embolism, sinus congestion, pulmonary infiltration, pleural effusion, hemoptysis, pulmonary fibrosis, pleural friction noise;
• digestive system: jaundice, severe liver failure, liver dysfunction, rectal polyps, duodenal ulcer, peptic ulcer, dysphagia, gastrointestinal bleeding;
• skin and subcutaneous fat: hair growth disorders, skin rashes, pigmentation disorders, dermatitis, urticaria;
• musculoskeletal system: tenosynovitis, ankylosing spondylitis, arthropathy, bone swelling;
• genitourinary system: pain in the prostate gland, edema of the penis, pain in the testicles, testicular atrophy, metrorrhagia, menstrual irregularities, vaginal bleeding, breast tenderness, obstruction of the urinary tract, bladder spasm, persistent urge to urinate;
• others: inflammation, induration or reaction at the injection site; intrapelvic fibrosis, inflammation, nodule, hematoma, aseptic abscess, fever, spinal fracture;
• deviations in laboratory parameters: an increase in the concentration of calcium, triglycerides, bilirubin, urea nitrogen, creatinine, low density lipoproteins in the blood; murmur in the region of the heart, signs of myocardial ischemia on an electrocardiogram, a decrease or increase in the number of leukocytes, a decrease in the concentration of potassium in the blood, a deviation from the norm in liver function tests, an increase in the activated partial thromboplastin and prothrombin time, a decrease in the number of platelets.

Against the background of the use of Lucrin Depot in men, serious cases of arterial and venous thromboembolism were revealed, including transient ischemic attack, stroke, myocardial infarction, pulmonary embolism and deep vein thrombosis. Although a transient relationship was noted in some cases, most episodes were associated with concomitant medications or risk factors. It is not known whether there is a connection between these events and the use of GnRH agonists.

The use of leuprorelin in patients has been associated with changes in bone density. In a clinical study in women with endometriosis who received therapy with Lukrin Depot at a dose of 3.75 mg for 6 months, bone density was measured using the X-ray absorptiometry method. In the course of the study, a decrease in the level of density was found on average by 3.9% compared to the values before the start of therapy. The average bone density of the tissue after 6–12 months after discontinuation of treatment was restored to the initial (± 2%).

Injections of Lukrin Depot at a dose of 3.75 mg for 3 months with uterine fibroids were associated with a decrease in the mineral density of the cancellous bones of the spine by 2.7% compared with the initial values, as established by quantitative radiography. Six months after the cessation of therapy, there was a tendency to recovery.

Overdose

There are no data on an overdose of Lucrin Depot in humans.

The use of the drug at a dose of up to 20 mg per day for 2 years in patients with prostate cancer did not cause the development of undesirable effects different from those when using the drug at a dose of up to 1 mg per day.

It is recommended to apply symptomatic therapy in case of overdose.

special instructions

The use of Lukrin Depot should be carried out only under medical supervision.

In post-marketing studies of the drug, cases of seizures have been recorded. Their appearance was noted in children, women, patients with cerebrovascular disorders, epilepsy, seizures, developmental abnormalities or tumors of the central nervous system, against the background of the combined use of drugs that can cause seizures (for example, selective serotonin reuptake inhibitors or bupropion). Seizures have also occurred in patients without these conditions.

During 1 week of treatment, in most episodes, testosterone concentration increases compared to baseline. By the end of 2 weeks, the content of the hormone decreases to or below the initial value. Postcastration concentration is achieved within 2-4 weeks and is maintained throughout the period of regular use of leuprorelin.

Against the background of the first few weeks of Lucrin Depot injections, there may be transient signs of deterioration of the patient's condition or additional symptoms and manifestations of the underlying pathology may appear. In a small number of cases, bone pain increases, which is relieved with symptomatic therapy.

If the condition of patients with hematuria, urinary tract obstruction or metastases in the spine worsens during the first few weeks of using Lucrin Depot, neurological problems may appear - worsening of urological symptoms, paresthesia, temporary weakness of the lower extremities. The use of leuprorelin, as well as other GnRH analogs, has been associated with urinary tract obstruction and spinal cord compression, which could be complicated by paralysis with or without fatal outcome. In this regard, in the presence of metastases in the spine and severe obstruction of the urinary tract during the first few weeks of therapy, careful monitoring should be carried out.

The use of GnRH analogues in men led to the development of hyperglycemia and an increased likelihood of diabetes mellitus. Hyperkalemia may indicate both the development of diabetes mellitus and the deterioration of glycemic control in patients suffering from the disease. It is important to control blood glucose and / or glycosylated hemoglobin levels, as well as to treat hyperglycemia or diabetes mellitus.

There are reports of an increased risk of stroke, myocardial infarction, and sudden death in men who have used GnRH analogues, which indicate that this risk is low. When prescribing Lucrin Depot for the treatment of prostate cancer, it should be assessed taking into account the risk factors for the development of cardiovascular pathologies. It is important to monitor the signs and indicators that indicate the occurrence of cardiovascular pathologies in patients receiving GnRH analogues.

Prolonged QT interval has been observed with prolonged treatment for androgen deprivation. If the combined use of class IA antiarrhythmic drugs (for example, procainamide, quinidine) or class III (sotalol, amiodarone) is necessary, with chronic heart failure, abnormal electrolyte levels or congenital long QT syndrome, the decision to use Lukrin Depot should be made by a doctor after evaluating the potential benefits of androgen deprivation treatment with the perceived risks.

Usually at the very beginning of the use of Lukrin Depot, a transient increase in the concentration of sex hormones is noted, which is associated with the physiological manifestations of its action. Some aggravation of manifestations at the beginning of treatment quickly enough passes with the continuation of the course with adequately selected doses of the drug. There are reports of the development of severe vaginal bleeding, which requires surgical or conservative therapy.

During the period of use of leuprorelin and until menstruation is restored, non-hormonal methods of contraception should be used. Fertility suppressed due to treatment or the ability to fertilize is restored within a period of up to 2 years after its cancellation.

In women with bone densitometry, a decrease in bone density due to a decrease in estrogen content is reversible and is restored after discontinuation of the drug.

In women receiving Lukrin Depot, the functions of the pituitary-gonadotropic system are inhibited. The function is restored 3 months after the end of therapy. It should be borne in mind that the results of diagnostic tests that indicate the function of the gonads or pituitary gland, which are carried out during the treatment period and for 3 months after its completion, may be distorted.

The criteria by which it is determined whether a drug can be used to treat premature puberty include:

• clinical diagnosis of idiopathic or neurogenic precocious puberty with the onset of secondary sexual characteristics in girls under 8 years old and in boys under 9 years old;
• confirmation of the diagnosis with a GnRH stimulation test. It should be taken into account that bone age is 1 year ahead of biological age.

The initial examination includes measuring the child's body weight and height, determining the concentration of sex hormones, adrenal steroids (in order to exclude congenital adrenal hyperplasia), human chorionic gonadotropin (to exclude the presence of a hormone-secreting tumor). Also, ultrasound examination of the adrenal glands and pelvic organs (to exclude a steroid-producing tumor) and computed tomography of the head (to exclude the presence of an intracranial tumor) are performed.

The dose of leuprorelin for the preparation of depot suspensions for children should be individualized. Its calculation is based on the ratio of the amount of the drug (mg) to the body weight (kg). For young children, higher doses of the drug are required in terms of mg per 1 kg of body weight. After 1 or 2 months from the start of the use of Lucrin Depot or a change in its dose when using any form of dosage, to confirm suppression, a control examination of children is carried out with a test of stimulation of GnRH, sex hormones and staging according to Tammer.

Measurements of the advance of bone age should be taken every six months / year. The physician should titrate the dose until there is no progression of the pathology, according to laboratory and / or clinical studies. In most children, the first dose that is sufficient to maintain adequate suppression can be maintained throughout the course of treatment. However, there is insufficient data on the establishment of an adjusted dose when patients move to higher weight categories after starting the use of Lucrin Depot at a very young age and using low doses. For patients whose body weight has increased significantly during therapy, confirmation of adequate suppression should be carried out.

In girls / boys who have reached the age of 11/12 respectively, the need for drug withdrawal should be considered. An incorrectly selected dose, as well as a violation of the lyophilisate regimen, can lead to inadequate control of the puberty process. The consequences of insufficient control include the resumption of pubertal manifestations (growth of testicles, development of mammary glands, menstruation). The long-term consequences of inadequate control of gonadal steroid secretion are unknown. Presumably, this could include subsequent growth impairment in adulthood.

After 1–2 months from the start of injections with Lucrin Depot, the response to the treatment should be monitored. For this, a GnRH stimulation test and determination of the content of sex hormones are used. The fact that the patient was prescribed an inadequate dose of leuprorelin will be indicated by the concentration of sex hormones exceeding the limits of puberty. After the establishment of a therapeutic dose, the concentration of sex hormones and gonadotropins will decrease to prepubertal levels.

The parents or guardians of the child should be advised of the need for continuous treatment before starting the child. In girls, bloody discharge or menstruation may appear during the first two months of drug administration. In cases where bleeding lasts more than 2 months, you should seek medical attention. It is important to tell your doctor immediately if irritation occurs at the injection site and if there are any unusual symptoms or manifestations.

Influence on the ability to drive vehicles and complex mechanisms

Since dizziness, drowsiness and other undesirable phenomena may appear against the background of the use of Lucrin Depot, patients during the period of treatment are advised to refrain from driving vehicles and engaging in potentially hazardous activities, the implementation of which requires the speed of psychomotor reactions and increased concentration of attention.

Application during pregnancy and lactation

Lucrin depot is not prescribed during pregnancy / lactation. It is important to exclude pregnancy before using the drug.

Pediatric use

In patients under 18 years of age, Lucrin Depot is not used. The exception is children with premature puberty, for the treatment of which a lyophilisate is used at a dosage of 3.75 mg.

Use in the elderly

Patients over the age of 65 are contraindicated in the appointment of a lyophilisate for the preparation of a suspension for intramuscular and subcutaneous administration of prolonged action (3.75 and 11 mg).

Drug interactions

There are no data on the interaction of Lucrin Depot with other drugs, since pharmacokinetic studies have not been conducted.

Since leuprorelin is of a peptide nature and, under the influence of peptidase, rather than cytochrome P450 enzymes, it undergoes primary degradation, and approximately 46% of its dose binds to blood plasma proteins, drug interactions are unlikely.

Analogs

Analogues of Lukrin depot are Eligard, Leiprorelin Sandoz, Buserin depot, Buserin, Suprefakt depot.

Terms and conditions of storage

Store in a place protected from light and moisture at a temperature of 15 to 25 ° C. Do not freeze, keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Lukrin depot

According to reviews, Lukrin Depot is a safe and effective drug used in the treatment of oncology, endometriosis, uterine fibroids and premature puberty in children.

Among the shortcomings most often indicate the presence of a wide list of possible side effects arising from injections, the high cost of the drug and a long period of therapy.

Price for Lukrin depot in pharmacies

The approximate price for Lukrin depot, a lyophilisate for preparing a suspension for intramuscular and subcutaneous administration with prolonged release (in a cardboard box, 1 bottle of 3.75 mg) is from 7050 to 8735 rubles.

Lukrin depot: prices in online pharmacies

Drug name Price Pharmacy

Lukrin depot 3.75 mg lyophilisate for the preparation of a suspension for intramuscular and subcutaneous administration of prolonged action 1 pc. RUB 6799 Buy

Lukrin depot lyof. d / suspension. for i / m and p / c int. prolong. 3.75mg n1 (vial 9ml) RUB 7039 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!