Eligard
Eligard: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Eligard
ATX code: L02AE02
Active ingredient: leuprorelin (leuprorelin)
Manufacturer: Kenjin BioPharma, Inc. (USA), Tolmar Inc. (USA), Astellas Pharma Europe BV (Netherlands)
Description and photo update: 15.06.2018
Prices in pharmacies: from 8390 rubles.
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Eligard is an antineoplastic agent.
Release form and composition
Eligard dosage form - lyophilisate for preparation of a solution for subcutaneous administration: from white to almost white, without visible foreign particles [1 syringe (B) with a lyophilisate, complete with an injection needle and a desiccant + 1 syringe (A) with a solvent included with piston and desiccant, in a cell package 1 + 1 set; in a cardboard box 1 package].
Solvent:
- 7.5 mg: viscous, transparent liquid from light yellow to light yellow with a brownish tinge, without visible foreign particles;
- 22.5 and 45 mg: viscous, transparent liquid from colorless to light yellow, without visible foreign particles.
Reconstituted solution:
- dosage 7.5 mg: a viscous liquid from light yellow to light yellow with a brownish tint, without visible foreign particles, possibly the presence of air bubbles;
- dosage of 22.5 and 45 mg: a viscous liquid from colorless to light yellow, without visible foreign particles, possibly the presence of air bubbles.
1 syringe B contains the active substance: leuprorelin acetate - 10.2 mg, 28.2 mg or 58.2 mg (the excess compensates for losses in the needle and syringe, in the administered dose the amount of active substance is 7.5 mg, 22.5 mg or 45 mg).
1 syringe A contains an auxiliary substance: a solvent consisting of a copolymer of poly-D, L-lactide-co-glycolide and N-methyl-2-pyrrolidone - 330 mg, 440 mg and 426 mg, respectively for the drug in doses of 7.5 mg, 22.5 mg and 45 mg.
Pharmacological properties
Pharmacodynamics
Leiprorelin is a synthetic non-peptide analogue of natural gonadotropin-releasing hormone (GnRH), which with prolonged use suppresses testicular steroidogenesis and inhibits the secretion of pituitary gonadotropin in men. Unlike the natural hormone, the analog is more effective. In addition, its effect is reversible after drug withdrawal.
At the beginning of the use, leuprorelin increases the level of circulating luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as a result of which there is a temporary increase in the level of testosterone, dihydrotestosterone and gonadal steroids in men, but with prolonged use the levels decrease. In this case, the concentration of testosterone decreases to the castration level (≤ 50 ng / dL) within 3-5 weeks after the start of taking Eligard. After 6 months of therapy, the average testosterone level, depending on the dosage in which the drug was used, is: 7.5 mg - (6.1 ± 0.4) ng / dL, 22.5 mg - (10.1 ± 0.7) ng / dl, 45 mg - (10.4 ± 0.53) ng / dl. These rates are comparable to testosterone levels in men after bilateral orchiectomy.
Pharmacokinetics
The maximum concentration of leuprorelin is determined in blood serum 4-8 hours after the first injection and is approximately 25.3 ng / dl, 127 ng / dl or 82 ng / dl (respectively, with the introduction of 7.5 mg, 22.5 mg or 45 mg Eligard).
The time to reach the plateau phase, depending on the dose of the drug used: 7.5 mg - from 2 to 28 days, 22.5 mg - from 3 to 84 days, 45 mg - from 3 to 168 mg. After the initial increase, serum leuprorelin remains relatively stable (0.2–2 ng / ml).
There is no information about the accumulation of Eligard with repeated injections.
The connection with plasma proteins is 43–49%.
With the intravenous administration of 1 mg of leuprorelin acetate to healthy volunteers (men), it was found that when using a two-chamber model, the average clearance was 8.34 l / h, the final half-life was about 3 hours.
Studies on the elimination of leuprorelin have not been conducted.
Indications for use
According to the instructions, Eligard is used to treat hormone-dependent prostate cancer in men.
Contraindications
- surgical castration;
- hypersensitivity to the drug or other GnRH agonists.
Eligard is not used in women and children.
Instructions for the use of Eligard: method and dosage
The solution prepared from the lyophilisate is injected subcutaneously, alternating the injection sites. Do not allow the drug to enter an artery or vein.
The frequency of administration, depending on the dose in which Eligard is prescribed: 7.5 mg - once a month, 22.5 mg - once every 3 months, 45 mg - once every 6 months. The injected drug forms a depot that provides a sustained release of leuprorelin for the indicated periods of time.
The duration of the drug use is determined individually. Long-term treatment.
In the case of an increase in the level of PSA (prostate-specific antigen) against the background of the castration level of testosterone, Eligard is canceled.
Recommendations for preparing an injection solution:
- Take the drug out of the refrigerator and keep it until the package temperature reaches room temperature.
- Remove syringes from packaging.
- Remove the short plunger from syringe B. Remove the long plunger from the package with syringe A and insert it into syringe B.
- Remove the caps from both syringes (A and B) and carefully connect the syringes. By alternately pressing the plungers of the syringes, mix the solution until it becomes homogeneous (about 60 strokes). The ready-to-use solution should be colorless or light yellow.
- Introduce the finished solution in full into the syringe B and remove the syringe A, continuing to press on its plunger until it stops. Insert a sterile needle into syringe B.
- It is necessary to mix the contents of the two syringes immediately before the introduction. Unused solution cannot be stored.
Air bubbles may form during mixing. This phenomenon is considered normal and does not affect the effectiveness of Eligard.
Side effects
- from the genitourinary system: urinary tract infection, acute urinary retention, bladder spasms, difficulty urinating, nocturia, hematuria, dysuria, oliguria, testicular pain, testicular atrophy, decreased libido, impotence, infertility;
- from the nervous system: a disorder of smell, taste disturbances, dizziness, headache, hypesthesia, insomnia, involuntary movements; in some cases - increased skin sensitivity, visual disturbances, sleep disturbances, peripheral dizziness, amnesia, depression;
- from the cardiovascular system: increase or decrease in blood pressure, hot flashes, fainting; in some cases - shortness of breath, palpitations, embolism of the branches of the pulmonary artery, peripheral edema;
- from the musculoskeletal system: muscle cramps, muscle weakness, pain in the limbs, back pain, arthralgia, myalgia; with prolonged use of Eligard - a decrease in bone density, the progression of osteoporosis;
- from the respiratory system: shortness of breath, watery discharge from the nasal cavity (rhinorrhea);
- from the digestive system: belching, dry mouth, flatulence, diarrhea or constipation, nausea, vomiting, dyspepsia;
- from the endocrine system: breast pain, gynecomastia;
- on the part of laboratory parameters: an increase in the content of triglycerides and creatine phosphokinase in the blood, a decrease in the number of erythrocytes, hematocrit and hemoglobin level, an increase in the level of alanine aminotransferase, an increase in prothrombin time and blood coagulation time, leukopenia, thrombocytopenia;
- local reactions: itching, pain, burning or tingling, redness and bruising at the injection site; in rare cases, induration and ulceration at the injection site;
- others: chills, increased sweating, weakness, increased fatigue, feeling unwell, weight gain, changes in glucose tolerance, alopecia, skin rash, exacerbation of symptoms of the underlying disease in the first weeks after starting treatment with the drug.
Overdose
Overdose cases have not been reported. If the recommended dose is significantly exceeded, symptomatic treatment must be carried out to eliminate the violations that have arisen.
special instructions
The use of Eligard is impractical after surgical castration, since the drug in this case does not cause a further decrease in serum testosterone.
Therapy should be carried out under the supervision of a physician experienced in the use of anticancer drugs.
During the first week, against the background of treatment with Eligard, there is a short-term increase in the concentration of dihydrotestosterone, acid phosphatase and testosterone, which may cause an increase in existing symptoms of the disease and the development of new ones, for example, bone pain, hematuria, neurological disorders, ureteral obstruction, bladder outlet obstruction. Usually, with continued therapy, these disorders go away on their own. There are also known cases of spinal cord compression when using GnRH agonists. Standard treatment for these complications is carried out if necessary.
The consequences of an initial increase in testosterone levels can be prevented by additional administration of an antiandrogen: 3 days before the first administration of Eligard and during the first 2-3 weeks of its use.
In the first few weeks of therapy, close monitoring is required in patients with urinary tract obstruction, metastases to the brain and / or spine.
Eligard increases the risk of bone fractures due to the development of osteoporosis. In addition to prolonged testosterone deficiency, the following factors can affect the formation of osteoporosis: old age, insufficient physical activity, excess weight, alcohol consumption, smoking.
The drug can reduce glucose tolerance, in connection with which patients with diabetes mellitus should be under more careful medical supervision during treatment.
Influence on the ability to drive vehicles and complex mechanisms
Eligard can cause some side effects that can negatively affect the speed of reactions and the ability to concentrate, such as dizziness, fatigue, visual impairment. In this regard, it is recommended to be careful when driving and performing potentially hazardous work.
Application during pregnancy and lactation
Eligard is not intended for use in women.
Pediatric use
Eligard is contraindicated for use in childhood.
With impaired renal function
There is no clinical data on the use of Eligard in the treatment of patients with renal insufficiency.
For violations of liver function
There are no clinical data on the use of Eligard in the treatment of patients with hepatic impairment.
Drug interactions
Special studies on the possible pharmacokinetic interactions of Eligard with other drugs have not been conducted. There were no reports of adverse reactions with the simultaneous use of other drugs.
Analogs
The analogues of Eligard are the drugs Lukrin Depot and Prostap.
Terms and conditions of storage
Shelf life is 2 years.
Store in original packaging at 2–8 ° C. Keep out of the reach of children.
The reconstituted solution retains its physical and chemical properties for 30 minutes after preparation (at 25 ° C).
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Eligard
Given the indication of the drug for which it is used, patients rarely share their impressions of the therapy. According to reviews, Eligard causes an increase in the symptoms of the disease in the first week of treatment, in some cases provokes the development of new symptoms, such as bone pain, blood in the urine, and neurological disorders. With continued therapy, these complications disappear. During long-term treatment, some patients report mild to moderate hot flashes, nausea, gynecomastia, and burning at the injection site.
Doctors speak positively about Eligard. The dosage form of this drug is designed in such a way that allows you to create a depot of leuprorelin in the subcutaneous tissue for 1, 3 or 6 months (depending on the dose administered) and thus provides a long-term stable effect. This system effectively reduces testosterone levels in 95% of patients. Due to the introduction of the solution once every 6 months (Eligard 45 mg), the incidence of side effects, especially local reactions, is significantly reduced, and frequent visits to the doctor are not required.
Price for Eligard in pharmacies
Approximate prices for Eligard, depending on the dosage: 7.5 mg - 7,700 rubles, 22.5 mg - 22,650 rubles, 45 mg - 33,300 rubles.
Eligard: prices in online pharmacies
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Drug name Price Pharmacy |
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Eligard 7.5 mg lyophilisate for preparation of solution for subcutaneous administration 1 pc. RUB 8390 Buy |
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Eligard 22.5 mg lyophilisate for the preparation of a solution for subcutaneous administration 1 pc. RUB 14800 Buy |
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Eligard 22.5 mg lyophilisate for preparation of solution for subcutaneous administration 2 pcs. 19800 RUB Buy |
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Eligard 45 mg lyophilisate for preparation of a solution for subcutaneous administration 1 pc. RUB 31,000 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!
