ELIGARD

Active material: Leuprorelin
When ATH: L02AE02
CCF: An analogue of gonadotropin-releasing hormone – depot
ICD-10 codes (testimony): C61
When CSF: 15.07.04.01
Manufacturer: ASTELLAS PHARMA EUROPE B.V. (Netherlands)

Pharmaceutical form, composition and packaging

Valium for drug of a solution for s / c administration (Syringe B) from white to almost white, without any visible foreign matter. Attached is the solvent (A syringe) – viscous liquid from light yellow to light yellow with brownish shade, transparent, without any visible foreign matter; It allowed the presence of air bubbles. The prepared solution – viscous liquid from light yellow to light yellow with brownish shade, without any visible foreign matter; It allowed the presence of air bubbles.

Solvent: poly-D,L-lactide-coglycolide, N-метил-2-пирролидон.

Syringes [A complete syringe with a piston syringe B and a desiccant (again. 1 PC.); Used syringe complete with needle d / u and desiccant (again. 1 PC.) v penalties plastic] (2) – packings Valium (2) – packs cardboard.

Valium for drug of a solution for s / c administration (Syringe B) from white to almost white, without any visible foreign matter. Attached is the solvent (A syringe) – viscous liquid from colorless to pale yellow, transparent, without any visible foreign matter; It allowed the presence of air bubbles. The prepared solution – viscous liquid from colorless to pale yellow, without any visible foreign matter; It allowed the presence of air bubbles.

Solvent: poly-D,L-lactide-co-glycolide, N-метил-2-пирролидон.

Syringes [A complete syringe with a piston syringe B and a desiccant (again. 1 PC.); Used syringe complete with needle d / u and desiccant (again. 1 PC.) v penalties plastic] (2) – packings Valium (2) – packs cardboard.

Valium for drug of a solution for s / c administration (Syringe B) from white to almost white, without any visible foreign matter. Attached is the solvent (A syringe) – viscous liquid from colorless to pale yellow, transparent, without any visible foreign matter; It allowed the presence of air bubbles. The prepared solution – viscous liquid from colorless to pale yellow, without any visible foreign matter; It allowed the presence of air bubbles.

Solvent: poly-D,L-lactide-co-glycolide, N-метил-2-пирролидон.

Syringes [A complete syringe with a piston syringe B and a desiccant (again. 1 PC.); Used syringe complete with needle d / u and desiccant (again. 1 PC.) v penalties plastic] (2) – packings Valium (2) – packs cardboard.

* – excess laid in the preparation of the active substance to compensate for losses in the syringe and the needle.

Pharmacological action

An analogue of gonadotropin-releasing hormone – depot. Leuprorelin is a synthetic non-peptide analogue of the natural gonadotropin-releasing hormone (GnRG), which inhibits long-term use of hypophyseal gonadotropin secretion and suppresses testicular steroidogenesis in men. Analogs possess greater efficacy, than the natural hormone and its effect is reversible when you stop treatment. Appointment of leuprolide first leads to increased circulating levels of luteinizing hormone (LG) and FSH (FSH), as a result of, which temporarily increased levels of gonadal steroids, testosterone and dihydrotestosterone in males. Prolonged use of leuprolide levels of LH and FSH decreased. In men, testosterone is reduced to castrate levels (≤ 50 ng / dl) for 3-5nedel after treatment. The average level of testosterone through 6 months of treatment 6.1 (±0.4) ng / dL for dosing 7.5 mg; 10.1 (±0.7) ng / dL for dosing 22.5 mg 10.4 (±0.53) ng / dL for dosing 45 mg. These values ​​are comparable with the level of testosterone after bilateral orchiectomy.

Pharmacokinetics

Absorption Distribution

After the first injection via 4-8 h average concentrations of leuprolide (C_max), determined in serum, increases to 25.3 ng / dl, 127 ng / dl 82 ng / dL when used at a dose of leuprorelin 7.5 mg, 22.5 mg 45 mg respectively. After an initial increase (plateau phase is from 2 to 28 day dosing 7.5 mg; from 3 to 84 days – dosing 22.5 mg, from 3 to 168 days – dosing 45 mg) serum levels of leuprolide remained relatively stable (0.2-2 ng / ml). Data on the accumulation of substances with repeated injections are missing.

Plasma protein binding – 43-49%.

Deduction

When administered 1 mg leuprolide acetate / in healthy male volunteers revealed, that the application of a two-compartment model, the average clearance was 8.34 l / h with a final T_1/2 about 3 no. Studies on the removal of the drug Eligard was conducted.

Testimony

- Hormone-dependent prostate cancer.

Dosage regimen

Eligard appointed n / a 1 once a month at a dose 7.5 mg, 1 once every 3 months at a dosage of 22.5 mg 1 once every 6 months at a dosage of 45 mg. Introduced solution forms a depot preparation, providing sustained release of leuprolide for a specified period. Treatment long. At higher levels of prostate-specific antigen (PSA) against the backdrop of castration levels of testosterone treatment should be discontinued Eligardom.

The injection site should be changed periodically. Avoid the drug into the artery or vein.

Clinical data on the use of at Eligarda Patients with hepatic or renal insufficiency no.

Terms of preparation of the solution

The contents of the two pre-filled sterile syringe to be mixed immediately before administration. Mixing is done as follows:

1. Before use, the packaging is taken from the refrigerator and kept at room temperature until, until the temperature reaches room packing.

2. Remove the syringe and the syringe A B of the package. Remove the syringe from the B short piston with a second limiter, to get a long plunger with the syringe from the package A and insert it into the syringe B.

3. Remove the cover from the syringe A (solvent for solution) and syringe B (liofilizirovannыy leyprorelina acetate) and carefully connect the syringes. Mix the solution, alternately pressing the plunger of the syringe A and B 60 times to obtain a homogeneous solution,. Ready-to-use mixture should be colorless or light yellow.

4. Introduce the resulting mixture into the syringe B. Remove the syringe A, continuing to press on to the end of its piston. There may be small bubbles. This is normal and it does not affect the formation of the depot after injection. Insert the syringe sterile needle B.

5. The mixture is ready for s / c administration.

6. The solution should be administered immediately after mixing.

The solution is intended for single use only. Unused solution should be discarded.

Side effect

Side effects, seen with Eligarda, mainly due to the pharmacological action of the drug.

Cardio-vascular system: hot flashes, increased or decreased blood pressure, fainting; in some cases – peripheral edema, embolism pulmonary artery branches, heartbeat, breathlessness.

From the central and peripheral nervous system: gipesteziya, dizziness, headache, insomnia, taste disorders, disorders of smell, involuntary movements; in some cases – sleep disorders, depression, peripheral vertigo, amnesia, visual disturbances, and increased sensitivity of the skin.

From the digestive system: nausea, vomiting, diarrhea, dyspepsia, constipation, dry mouth, belching, flatulence, ALT elevation.

The respiratory system: rhinorrhea, labored breathing.

With the genitourinary system: dizurija, nocturia, oligurija, urinary infection, strangury, bladder spasms, hematuria, acute urinary retention, testicular atrophy, pain in the testicles, infertility, impotence, decreased libido.

On the part of the endocrine system: pain in the breasts, gynecomastia.

On the part of the musculoskeletal system: arthralgia, backache, pain in the extremities, myalgia, muscle cramps, muscular weakness.

Patients with surgical or medical castration there is a decrease in bone density. It will be appreciated, Eligarda that long-term use can also lead to a decrease in bone density and progression of osteoporosis.

From the hematopoietic system: reduction in the number of red blood cells, levels of hemoglobin and hematocrit; rarely – thrombocytopenia, leukopenia.

From the blood coagulation system: increase in clotting time, increased prothrombin time.

From the laboratory parameters: elevated levels of creatine kinase in the blood, elevated blood triglyceride.

Local reactions: burning / tingling, pain, redness, bruising or itching at the injection site; rarely – seal and ulceration at the injection site.

Other: feeling of uneasiness, increased fatigue, weakness, skin rash, alopecia, increased sweating, chills, change in glucose tolerance, weight gain. In the first weeks after initiation of therapy Eligardom may experience worsening of symptoms.

Contraindications

- Hirurgicheskaya castration;

- Hypersensitivity to leuprorelin, other GnRH agonists or to any excipient, incorporated in a dosage form.

Is contraindicated in women and children.

Cautions

Eligard should be used under medical supervision, having experience of anticancer therapy.

Eligard, Like other GnRH agonists, during the first week of treatment causes a transient increase in the concentration of testosterone, dihydrotestosterone and acid phosphatase in serum, in this connection, patients may worsen symptoms or cause new, such as bone pain, neurological disorders, hematuria, mochetochnika obstruction or obstruction infravezikalynaya. These symptoms usually disappear with continued therapy. When using a GnRH agonist also reported cases of spinal cord compression. If necessary, should be the standard treatment of these complications.

For patients with metastases in the spine and / or brain, as well as patients with urinary tract obstruction should be closely monitored during the first few weeks of treatment.

Additional administration of an appropriate antiandrogen 3 days prior to initiation of therapy and continued Eligardom his admission during the first two or three weeks of treatment prevents the effects of the initial increase in testosterone levels. Antiandrogen therapy increases the risk of bone fractures due to osteoporosis. In addition to the prolonged deficiency of testosterone on osteoporosis can affect age, smoking, alcohol consumption, overweight and insufficient exercise.

Due to a possible decrease in glucose tolerance, Patients with diabetes mellitus, They require more careful observation in the treatment of drug Eligard.

After performing the surgical castration Eligarda use does not lead to a further reduction of testosterone in serum.

Effects on ability to drive vehicles and management mechanisms

Some adverse drug reactions, such as increased fatigue, dizziness, visual impairment, may adversely affect the ability to drive a car and perform potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Overdose

Information regarding the overdose in humans is not available. In case of overdose, the patient should be treated symptomatically.

Drug Interactions

Research for the study of the drug Eligard pharmacokinetic interactions with other drugs has not been. About Eligarda interaction with other drugs have been reported.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at a temperature of 2 ° to 8 ° C in its original packaging. Shelf life – 2 year.

The final solution is stable chemically and physically during 30 minutes at 25 ° C.