Universal reference book for medicines
Product name: LUCRIN DEPO ® (LUCRIN DEPOT)

Active substance: leuprorelin

Type: Gonadotropin-releasing hormone analogue - depot form

Manufacturer: ABBOTT LABORATORIES (Spain) manufactured by TAKEDA PHARMACEUTICAL COMPANY (Japan) packed with ABBOTT LABORATORIES (Spain)

Composition, form of production and packaging
Lyophilizate for the preparation of a suspension for w / m and n / to the introduction of prolonged action
in the form of a white powder;
solvent - colorless transparent solution; a prepared suspension of white color; When settling, a white precipitate forms, which is easily resuspended by shaking.
1 f.

leuprorelin acetate 3.75 mg

Excipients: gelatin, copolymer of lactic and glycolic acids, mannitol.

Solvent: carmellose sodium, mannitol, polysorbate-80, water d / u.

Set for single-dose administration:

44.1 mg - bottles of glass with a capacity of 9 ml (1) complete with a solvent (amp 2 ml 1 pc.), Needles and / or (2 pcs.), A disposable sterile propylene syringe (1 pcs.), A napkin soaked in 70% isopropanol (1 pc.) - blister packs (1) - cardboard packs.

Lyophilizate for the preparation of a suspension for w / m and n / to the introduction of prolonged action in the form of a white powder;
solvent - colorless transparent solution; a prepared suspension of white color; When settling, a white precipitate forms, which is easily resuspended by shaking.
1 syringe

leuprorelin acetate 3.75 mg

Excipients: gelatin, copolymer of lactic and glycolic acids, mannitol.

Solvent: carmellose sodium, mannitol, polysorbate-80, water d / u.

Set for single-dose administration:

44.1 mg - two-chamber syringes (1) containing lyophilizate in the chamber nearest to the needle d / and (1 pc.) And solvent (1 ml) in the chamber nearest to the piston;
plastic piston and napkins (1 or 2 pcs.) - plastic pens (1) - packs of cardboard.
Lyophilizate for the preparation of a suspension for the long-acting administration of s-injection 1 syringe

leuprorelin acetate 30 mg

30 mg - two-chamber syringes (1) complete with plastic piston - 1 pc.
and a napkin soaked in 70% isopropyl alcohol - 1 pc. - plastic pencil cases.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Leuprorelin, a gonadotropin-releasing hormone agonist (GnRH), is an effective inhibitor of gonadotropin secretion with long-term admission in therapeutic doses.
In humans, the appointment of leuprorelin leads to an initial increase in the concentrations of luteinizing (LH) and follicle-stimulating (FSH) hormones, which leads to a transient increase in the concentrations of sex hormones (testosterone and dihydrotestosterone in men, estrone and estradiol in women). However, the long-term administration of leuprorelin leads to a decrease in the concentrations of LH, FSH and sex hormones. In men, the concentration of testosterone is reduced to the castration or prepubertal level. In women who are in a condition before menopause, the concentration of estrogen falls to the postmenopausal level. These hormonal changes occur within a month from the beginning of therapy with the drug in the recommended doses.
Suppression of steroidogenesis in the ovaries and testes is reversible and stops after the end of therapy.

PHARMACOKINETICS

Suction and distribution

Bioavailability of the drug for p / k and / m introduction is comparable.
The approximate value of absolute bioavailability when the drug is administered at a dose of 7.5 mg is 90%.
After a single sc and iv injection of leuprorelin in patients with prostate cancer at doses of 3.75 mg and 7.5 mg, the average plasma concentrations of the drug by the end of the first month were 0.7 ng / ml and 1 ng / ml, respectively.

Serum leuprorelin concentration of 3.75 mg is determined for 12 months in 11 patients with premenopausal breast cancer.
The average concentration of leuprorelin exceeded 0.1 ng / ml after 4 weeks and remained stable after repeated administration (at 8 and 12 weeks). No cumulation of the drug was noted.
The average V d in the equilibrium state is 27 liters.
Binding to plasma proteins - 43-49%.
Metabolism and excretion

Leuprorelin, being a peptide, undergoes metabolic degradation, mainly with the participation of peptidase to shorter inactive peptides - pentapeptide (metabolite I), tripeptides (metabolites II and III) and dipeptide (metabolite IV).

The time to reach C max in the blood plasma of the main metabolite (M-I) is 2-6 h and corresponds to 6% of C max leuprorelin.
1 week after the injection, the average plasma concentration of M-I is 20% of the average concentration of leuprorelin.
After the administration of leuprorelin at a dose of 3.75 mg, the content of leuprorelin and MI in urine was less than 5% of the administered dose 27 days after drug administration.

System clearance - 7.6 liters.
T 1/2 - about 3 hours.
Pharmacokinetics in special clinical cases

Pharmacokinetics of the drug in patients with impaired liver or kidney function has not been investigated.

INDICATIONS

- Progressive prostate cancer (palliative treatment), incl.
when an orchiectomy or treatment with estrogens is not shown or is not applicable in this patient;
- endometriosis (for up to 6 months as a basic therapy or addition to surgical treatment);

- uterine fibroids (for up to 6 months as a pre-operative preparation for the removal of fibroids or hysterectomy, as well as for symptomatic treatment and improvement in women during menopause who refuse surgery);

- breast cancer in perimenopause in combination with hormone therapy;

- Children with premature puberty of the central genesis.

DOSING MODE

Enter in / m or p / to 1 time / month.
The injection site should be changed every month.
In prostate or breast cancer, a single dose is 3.75 mg.
The duration of treatment is determined by the doctor.
With endometriosis, fibroids of the uterus - 3.75 mg.

Women of reproductive age are given the first injection on the third day of menstruation.
Duration of treatment is no more than 6 months.
With premature puberty, the initial dose is 0.3 mg / kg (minimum 7.5 mg) once every 4 weeks.

The initial dose can be determined from the calculation of the body weight of the child:

Body weight of the child Dose Number of syringes or flasks for injection Total dose

?
25 kg 3.75 mg 2 7.5 mg
> 25 to 37.5 kg 3.75 mg 3 11.25 mg

> 37.5 kg 3.75 mg 4 15 mg

If two or more injections are required to obtain the desired total dose, they must be administered simultaneously.

Supportive dose for premature puberty

If complete suppression of disease progression is not achieved, the dose should be increased every 4 weeks by 3.75 mg.

Cancellation of Lucrin Depot ® should be considered before the age of 11 years in girls and 12 years of age in boys.

Instructions for the preparation of suspension and injection of Lucrin Depot ® in vials

The injection suspension is prepared immediately prior to administration using the supplied solvent at a concentration of 3.75 mg / ml.

1. Draw into the syringe with the needle, available in the kit 1 ml of solvent from the ampoule and insert it into the vial with lyophilizate (residual solvent should be disposed of).

2. Shake the bottle well until a uniform suspension is obtained.
The suspension becomes milky.
3. Immediately after dilution, dial the entire contents of the vial (or 2 bottles) in a syringe (maximum 2 ml per syringe) and make a n / c or IM injection.

Although the prepared suspension of Lucrin Depot ® remains stable for 24 hours after reconstitution, it should be used immediately after preparation.
The rest of the drug must be disposed of.
Instructions for injection of Lucrin Depot ® in two-chamber syringes

1. Screw the white piston into the end plug until the plug starts to rotate.

2. Hold the syringe in the upright position.
Introduce the solvent, slowly (for 6-8 seconds), pressing the piston, until the first stopper is on the blue line in the middle of the syringe.
3. Hold the syringe upright.
With gentle rocking, carefully mix the lyophilizate with the solvent until a uniform slurry (suspension) forms. The suspension becomes milky.
4. Hold the syringe upright.
With the other hand, remove the needle cap from the top, without twisting it.
5. Hold the syringe upright.
Push the piston forward to remove air from the syringe.
6. Immediately after the formation of the suspension, immediately enter the entire contents of the syringe in / m or n / k, t.
the suspension settles very quickly.
SIDE EFFECT

Cardiovascular system: edema, angina, palpitations, bradycardia, tachycardia, arrhythmia, chronic heart failure, ECG changes, increased or decreased blood pressure, myocardial infarction, phlebitis, pulmonary embolism, stroke, thrombosis, transient ischemic attacks, varicose veins veins.

From the digestive system: change (increase, decrease or absence) of appetite, change in taste, dry mouth, thirst, dysphagia, nausea, vomiting, diarrhea or constipation, flatulence, increased or decreased body weight, abnormal liver function, abnormalities functional tests of the liver, jaundice.

On the part of the endocrine system: pain and sensitivity of the mammary glands, gynecomastia, lactation, an increase in the thyroid gland, impotence, decreased libido, diabetes, androgen-like effects - virilization, acne, seborrhea, voice change.

On the part of the hematopoiesis system: anemia, thrombocytopenia, leukopenia, leukocytosis, neutropenia, increased prothrombin time and APTT.

From the musculoskeletal system: bone pain, arthralgia, myalgia, increased muscle tone, decreased bone density, joint disorders, retroperitoneal fibrosis.

From the central nervous system and peripheral nervous system: headache, dizziness, fainting, sleep disturbances (insomnia), increased irritability, anxiety, apoplexy of the pituitary gland (in patients with pituitary adenoma), depression, fatigue, paresthesia, memory impairment, hallucinations, hyperesthesia, emotional lability, personality disorders, violation of neuromuscular transmission, peripheral neuropathy, drowsiness;
very rarely - thoughts of suicide and suicide attempts.
On the part of the respiratory system: cough, shortness of breath, epistaxis, hemoptysis, pharyngitis, pleural effusion, fibrotic lesions in the lungs, lung infiltrates, respiratory distress.

Dermatological reactions: dermatitis, dry skin, photosensitization, itching, rash, erythema, urticaria, ecchymosis, alopecia, hyperpigmentation, striae;
in women - acne, a change in the formation of the hairline (growth / loss of hair).
From the senses: dry eyes, amblyopia, visual and hearing impairment, ringing in the ears.

From the urinary system: dysuria.

On the part of the reproductive system: dysmenorrhea, breakthrough and prolonged vaginal bleeding, dry vaginal mucosa, vaginitis, vaginal odor, leucorrhoea, prostate gland, testicular atrophy, testicular pain, hematuria, swelling of the penis.

On the part of laboratory indicators: an increase in blood urea nitrogen, elevated levels of calcium, creatinine, bilirubin, uric acid;
hyperlipidemia (increase in the concentration of total cholesterol, LDL cholesterol, triglycerides), hyperphosphatemia, hypoglycemia, hyponatremia, hypoproteinemia, hypokalemia.
Local reactions: tissue tightening, hyperemia and pain at the injection site.

Other: allergic reactions (including anaphylactic shock), flu-like syndrome, flushing of the blood to the skin of the face and upper chest, increased sweating, swollen lymph nodes, chills, fever, lump in the throat, asthenia, dehydration.

CONTRAINDICATIONS

- surgical castration;

- Pregnancy;

- lactation period;

- vaginal bleeding of unclear etiology;

- prostate cancer (hormone-independent);

- Children under 18 years of age, except for children with premature puberty of the central genesis;

- women over 65;

- hypersensitivity to leuprorelin and other components of the drug;

- hypersensitivity to similar drugs of protein origin.

Caution should be used in patients with metastases in the spine, with obstruction of the urinary tract or hematuria.

PREGNANCY AND LACTATION

The drug is contraindicated in pregnancy and lactation, so before starting the drug is recommended to exclude the presence of pregnancy.

APPLICATION FOR CHILDREN

Contraindication: children under 18 years of age, except for children with premature puberty (PPP) of the central genesis.

APPLICATION IN ELDERLY PATIENTS

Contraindication: women over 65 years.

SPECIAL INSTRUCTIONS

Lucrin Depot ® should only be used under medical supervision.

Prostate Cancer

In most patients, the testosterone concentration rises from baseline during the first week, and then decreases to or below the baseline concentration at the end of the second week of treatment.
Postastratsionnaya concentration is achieved within 2-4 weeks and maintained throughout the period of regular use of the drug.
During the first few weeks of treatment with Lucrin Depot ® , transient symptoms of impairment may develop or additional signs and symptoms of the underlying disease may appear.
In a small number of patients, pains in the bones that can stop with symptomatic treatment may increase. The increase in symptoms of worsening during the first few weeks of treatment with Lucrin Depot ® in patients with spinal metastases, with obstruction of the urinary tract or with hematuria, may lead to neurological problems such as temporary weakness of the lower limbs, paresthesia and weighting of urologic symptoms. As with other gonadotropin-releasing hormone analogues, individual cases of urinary tract obstruction and spinal cord compression have been observed with the use of Lucrin Depot ® , which can be complicated by paralysis with or without a fatal outcome. Therefore, during the first few weeks of treatment, patients with metastases in the spine and severe obstruction of the urinary tract require careful monitoring
Endometriosis / fibroids of the uterus

At the very beginning of the course of treatment, a transient increase in the concentration of sex hormones is usually noted, which determines the physiological manifestations of the action of the drug.
Some aggravation of the symptoms at the beginning of therapy of the drug Lyukrin Depot ® passes quickly enough with the continuation of treatment with adequately selected doses of the drug. Reported cases of severe vaginal bleeding, requiring conservative or surgical treatment.
During treatment and before the restoration of menstruation, non-hormonal methods of contraception should be used.

Ability to fertilize or fertility, suppressed as a result of therapy, is restored in the period up to 24 weeks after the end of treatment.

Reduction of bone density with bone densitometry in women as a result of a decrease in the concentration of estrogens is reversible, and after the cessation of leuprorelin treatment, bone tissue density is restored.

The use of Lucrin Depot ® in women causes oppression of the function of the pituitary-gonadotropic system.
After the end of treatment, the function is restored after 3 months. However, diagnostic tests that testify to the function of the pituitary gland or gonads, carried out during treatment and up to 3 months after its termination, may be distorted.
Premature puberty

The drug is prescribed for the treatment of premature puberty, based on the following criteria:

1. Clinical diagnosis of premature puberty (idiopathic or neurogenic) with the appearance of secondary sexual characteristics up to 8 years in girls and up to 9 years in boys.

2. The diagnosis should be confirmed by the GnRH stimulation test, and it must also be taken into account that the bone age is one year ahead of the biological one.

3. Initial examination includes:

- measurement of height and body weight;

- determination of the concentration of sex hormones;

- determination of the concentration of adrenal steroids to exclude congenital hyperplasia of the adrenal glands;

- determination of the concentration of human chorionic gonadotropin to exclude the presence of a tumor secreting chorionic gonadotropin;

- ultrasound examination of small pelvis and adrenal glands to exclude steroid-producing tumors;

- Computed tomography of the head to exclude intracranial tumor.

The dose of Lucrin Depot ® for the preparation of depot suspension should be individualized for each child.
The dose is based on the ratio of the amount of the drug to body weight (mg / kg). Young children require higher doses in terms of mg / kg.
If any form of dosing is used after 1 or 2 months after the start of therapy or a dose change, a follow-up examination of the child should be carried out with a GnRH stimulation test, sex hormones and Tammer staging to confirm suppression.
Measure the advance of bone age should be carried out every 6-12 months. The dose should be titrated until the absence of disease progression, according to clinical and / or laboratory data.
The first dose, which was sufficient to maintain adequate suppression, can be maintained throughout the therapy in most children.
However, sufficient data to establish the dose-corrected at the transition patients in higher weight categories after beginning therapy at a very young age and with lower dosages exist.
It is recommended to confirm adequate suppression in patients whose body weight increased significantly during treatment.
Abolition of the drug Lyukrin Depot ® should be considered before reaching the age of 11 in girls and age 12 in boys.
An abnormality ingestion or incorrectly picked dose may lead to an inadequate control of puberty process. Among the consequences of a lack of control include the resumption of pubertal symptoms such as menstruation, breast development and growth of the testes. The long-term consequences of inadequate control of the secretion of gonadal steroids are not known, but perhaps they include violation of subsequent growth into adulthood.
Laboratory tests
monitoring response to therapy with Lyukrin Depot ® should be carried out after 1 or 2 months after the beginning of therapy with the GnRH stimulation test and determining the concentration of sex hormones. Measurement of advancing bone age should be performed every 6-12 months.
The concentration of sex hormones can be increased above the limits in the case of prepubertal levels inadequate dose. After establishing a concentration of a therapeutic dose of gonadotropins and sex hormones would be reduced to prepubertal levels.
Information for Parents
Before starting therapy with Lyukrin Depot ® , parents or guardians should be aware of the importance of continuous therapy.
During the first 2 months of therapy in girls may be menstruation or spotting. If the bleeding continues for more than two months, you should inform your doctor. The doctor should immediately report the occurrence of irritation at the injection site and any unusual symptoms or signs.
Impact on the ability to drive vehicles and manage mechanisms

Data on the effect of medication on driving ability and work with no mechanisms. However, since you may experience side effects such as drowsiness, dizziness, it is recommended to refrain from driving and busy with other activities require high concentration and psychomotor speed reactions.
OVERDOSE

Information regarding overdose of leuprorelin no people. In patients with prostate cancer at a dose of leuprolide appointment of up to 20 mg / day for 2 years did not cause the development of adverse events other than those that occur when using the drug at a dose of 1 mg / day. In case of overdose, the patient should be given symptomatic treatment.
DRUG INTERACTION

Pharmacokinetic studies of drug interactions Lyukrina Depot ® with other drugs was conducted.
Leuprorelin acetate is a substance of peptide nature and is subjected to a primary disintegration under the action of peptidases, but not cytochrome P450 enzyme system. Furthermore, about 46% of the drug is bound to plasma proteins, therefore drug interactions Lyukrina Depot ® unlikely.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be kept out of reach of children at a temperature of from 15 ° to 25 ° C.
Do not freeze. Shelf life - 3 years.
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