Lyukrin Depo

Люкрин Депо Drug photo

The description is actual on 16.12.2015

  • Latin name: Lucrin depot
  • ATH code: L02AE02
  • Active ingredient: Leyprorelin (Leuprorelin)
  • Producer: Takeda Pharmaceutical Company (Japan)

Structure

Lyophilisate in bottles

Rolled into one 3,75 mg of a leyprorelin of acetate contain.
Act as excipients: 0,65 mg of gelatin, 33,1 mg of milk and glycolic acids of copolymer, 6,6 mg of Mannitolum. As solvent the ampoule contains 10 mg of a karmelloza of sodium, 100 mg of Mannitolum, 2 mg of polysorbate 80, for bringing to 2 ml diart. water for injections.

Lyophilisate in two-chamber syringes

One of cameras of the two-chamber syringe contains 3,75 mg of a leyprorelin of acetate. Act as excipients: 0,65 mg of gelatin, 33,1 mg of milk and glycolic acids of copolymer, 6,6 mg of Mannitolum. As solvent the second camera contains 5 mg of a karmelloza of sodium, 50 mg of Mannitolum, 1 mg of polysorbate 80, for bringing to 1 ml diart. water for injections.

Release form

Drug is implemented in the form of lyophilisate of the prolonged action intended for preparation of suspensions for in oil and hypodermic introduction. It can be packed:

  • in the bottles of 9 ml made of glass, containing 44,1 mg of lyophilisate; are completed with solvent in ampoules on 2 ml, 2 blisters with sterile needles, the one-time syringe and the napkin impregnated 70% with isopropanol;
  • in the two-chamber syringes containing in the camera of 11,25 mg of lyophilisate, next to a needle, and to 1 ml of solvent in the second camera; are completed with the plastic piston, 1-2 napkins impregnated 70% with isopropanol.

Pharmacological action

Drug has the antineoplastic and inhibiting secretion of gonadotrophins effect.

Pharmacodynamics and pharmacokinetics

Leyprorelin is an agonist of a gonadorelin. Long reception of therapeutic doses provides effective inhibition of secretion of gonadotrophins.

Leyprorelin leads to initial increase of concentration of luteinizing (LG) and follicle-stimulating hormones (FSG), leading to tranzitorny increase in concentration of sex hormones: at men – testosterone, dihydrotestosterone, at women – estrone, oestradiol. Long therapy leyproreliny (approximately in a month) causes permanent decrease in concentration of LG, FSG, sex hormones: at men — to level postkastratsionny (or prepubertatny), at women — to level post-menopausal. The steroidogenesis in testicles and ovaries is recovered after drug withdrawal.

Data on pharmacokinetics

Introduction of a dose of 7,5 mg p / to and in oil gives high rates of bioavailability of-90% and plasma concentration in 2–6 h (at single introduction within a month) – 0,7-1 ng/ml, cumulation is not observed. Linkng with proteins happens for 43–49%. Level of system clearance — 7,6 l an hour, a semi-removal time indicator — about 3 h.

Leyprorelin as peptide is exposed to degradation under the influence of peptidase to inactive metablolit — pentapeptide, dipeptide and two tripeptides. To 5% (from a dose of a leyprorelin of 3,75 mg) it is observed in urine for the 28th day of therapy.

Indications to use

Treatment Lyukriny Depot is effective:

  • at the progressing prostate cancer (palliative therapy), at an orkhiektomiya or treatment by the estrogen which is not shown to this patient;
  • at endometriosis (main therapy first 6 months or addition to surgical intervention);
  • at a uterus fibromyoma (therapy for preoperative preparation the first 6 months, during removal of myoma or a hysterectomy a symptomatic treatment and improvement of a state at the patients in a menopause who refused operations);
  • at a breast cancer in a perimenopauza (treatment is carried out to a combination with hormonal therapy);
  • in case of the premature puberty (PP) of the central genesis at children.

Contraindications

  • gormononezavisimy malignancy of a prostate;
  • at vaginal bleedings of unspecified genesis;
  • to patients after surgical castration;
  • to pregnant women, nursing mothers and elderly patients (from 65);
  • to children 18 years, except for the diagnosis – PPS of the central origin are younger;
  • hypersensitivity to active agent – a leyprorelin and its analogs of a proteinaceous origin, and also to the excipients which are a part of a dosage form.

With care treatment at patients with metastasises - the secondary center of pathological process in a backbone, a hamaturia or obstruction of urinary tract has to be carried out.

Side effects

Side undesirable effects can arise from such systems:

  • Alimentary system: change or absence at patients of appetite, the changed flavoring perception, dryness of an oral cavity, feeling of thirst, nausea, emergence of emetic desires, dysphagies, diarrhea or a lock, a meteorism, fluctuations of body weight, functional disturbances of a liver, jaundice.
  • CCC: puffiness, stenocardia, bradycardia, tachycardia, arrhythmia, heartbeat, congestive type heart failure, various changes on an ECG increased or reduced by the ABP phlebitis, a pulmonary embolism, fibrinferments, passing ischemic attacks, a myocardial infarction, a stroke, a varicosity.
  • TsNS: headaches and dizziness, faints, a sleep disorder, for example, sleeplessness, uneasiness, irritability, a hypophysis apoplexy (at hypophysis adenoma), a depression, frustration of the personality, suicide attempts, paresthesia, disturbances of memory, a hallucination, emotional lability, hyper - or a hypesthesia, peripheral neuropathy.
  • Endocrine system: increase in the sizes of a thyroid gland, a diabetes mellitus, sensitivity and mammary gland pains, a gynecomastia, a lactation, impotence, a reduced libido, androgenopodobny manifestations — a masculinization, a hirsutism, seborrhea, an acne, change of a voice.
  • Hemopoiesis: anemia, leukopenia, leukocytosis, thrombocytopenia, neutropenia, increase in prothrombin and partially tromboplastinovy time.
  • Musculoskeletal system: ostealgias, disturbances of joints, Ormond's illness, arthralgia, mialgiya, increase of a muscle tone, reduction of density of a bone tissue.
  • System of breath: cough, short wind, pneumorrhagia, nasal bleedings, pleural exudate, pneumosclerosis, infiltrates, pharyngitis.
  • Epidermis: dryness, itch, rash, hemorrhages and inflammation of integuments, erythema, pigmentation, small tortoiseshell, photosensitization, alopecia, extensions, acne.
  • Sense bodys: vision disorders, hearing, for example, a xerophthalmus, an amblyopia, a ring in ears.
  • Urinogenital system: a dysmenorrhea, a dysuria, vaginal bleedings, dryness of mucous also began to smell vaginas, vaginita, bleach, prostate gland pains, a hamaturia, an atrophy and pain in testicles, penis hypostases.
  • Changes of laboratory indicators: increase of level of an urea nitrogen in blood, contents of calcium, bilirubin, creatinine; lipidemia hyperphosphatemia, hyponatremia, hypoproteinemia, hypoglycemia, hypopotassemia.
  • Reactions are local: consolidation, a hyperemia, inflammatory process and painful feelings in an injection site.
  • Others: allergic reactions (up to development of an acute anaphylaxis), an angiomegaly, grippopodobny manifestations, inflow, the increased perspiration, a fever, fever, an adynamy, dehydration.

Lyukrin Depo, application instruction (way and dosage)

Pricks Lyukriny Depot do in oil or p / to once a month, periodically changing an injection site. The suspension prepared way of administration of solvent to lyophilisate (to shake up) should be prepared in concentration 3,75 mg for 1 ml just before introduction.

Algorithm of preparation of suspension in the two-chamber syringe

1. To twist white color the piston that the trailer stopper began to rotate.

2. To enter solvent by slow pressing on the piston that the first stopper appeared on the blue line, then – to mix (to constantly hold the syringe vertically).

3. To remove a needle cap, to remove air, having advanced the piston. To start immediate introduction of contents of the syringe in oil or p / to in order to avoid formation of a deposit.

Dosage depending on the established diagnosis

  • the cancer of a prostatic or mammary gland – is appointed a one-time dose in the amount of 3,75 mg (duration of therapy is established individually);
  • endometriosis, uterus fibromyoma — a one-time dose makes 3,75 mg; to patients of reproductive age the injection is done for the 3rd day of a menstrual cycle (therapy duration – till 6 months);
  • PPS at children – begin with a dose 0,3 mg on 1 kg (not less than 7,5 mg) once in 4 weeks; the maintenance dose when progressing a disease or incomplete suppression – has to increase each 4 weeks by 3,75 mg (drug withdrawal in at girls in 11 years, boys – 12).

Overdose

Overdose cases leyproreliny at people were not registered. The symptomatic treatment is recommended.

Interaction

It is improbable in connection with the peptide nature of the leyprorelin which is exposed to disintegration under the influence of enzyme — peptidases, but not Tsitokhroma P450.

Terms of sale

It is necessary to show the recipe.

Storage conditions

Temperature has to be within +15+25 ° Celsius, without subjecting drug to a freezing.

Storage in the unavailable place for children is recommended.

Period of validity

Is subject to storage during 3 flyings.

Special instructions

At use in pediatrics parents and trustees have to be notified on need of continuous treatment Lyukriny Depot.

Analogs

  • Eligard (lyophilisate);
  • Leyprorelin Sandoz;
  • Lyuprayd Depo.

Zdravzona

  • Lyukrin of depot lyophilisate for No. 1 suspension 3,75mg shpritsabbott GMBH
  • Lyukrin of depot lyophilisate for No. 1 suspension 3,75mg flakonabbott GMBH

Drugstore of IFC

  • Lyukrin Depo liof. for susp. in oil 3.75mg fl No. 1, Abbott Gmbhyaponiya
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Section: Antineoplastic
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Education: Graduated from the Nikolaev national university of V. A. Sukhomlinsky, gained the diploma of the specialist with honors as "An embryologist, a cytologist, a histologist". Also, the human physiology and animals, the teacher of biology" graduated from a magistracy majoring in ". The course on discipline "Pharmacology" is with honors passable.

Experience: Worked as the senior laboratory assistant of department of Physiology and biochemistry of the Nikolaev national university of V. A. Sukhomlinsky in 2010 - 2011.

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