Eligarde

Eligard is an analog of gonadoliberin - acts as a depot-form.

Indications of the eligarde

It is used in the treatment of prostate cancer hormone-dependent type.

[1]

Release form

Release in the form of a lyophilizate for the preparation of a solution introduced by the s / c method. The volume of syringes with the drug is 7.5, 22.5, and also 45 mg. Inside the package contains one of these syringes, complete with a second syringe - with a special solvent inside it.

[2]

Pharmacodynamics

Leiprorelin is an artificial analogue of natural GnRH (nonpeptidic). With prolonged administration, it slows the release of the pituitary gonadotropin, and also inhibits the process of male testicular steroidogenesis. This analog has a more powerful effect than the natural hormone, and its effect is reversible in the case of drug cancellation. Due to the use of leuprorelin, firstly, an increase in the indices of LH, as well as of FSH, is due to which, for some time, the testosterone values along with gonadal steroids as well as dihydrotestosterone increase in men.

With further continuation of the course, the indices of FSH with LH decrease. The testosterone values in men are reduced to castration (≤50 ng / dl) for 3-5 weeks after the start of the course. The average testosterone after six months of therapy is:

• 6.1 ± 0.4 ng / dl with a serving size of 7.5 mg;
• 10.1 ± 0.7 ng / dL with a dosage amount of 22.5 mg;
• 10.4 ± 0.53 ng / dl with a dosage of 45 mg.

These figures can be compared with the testosterone values after the procedure of bilateral orchidectomy.

[3], [4], [5]

Pharmacokinetics

After the administration of the first dose of the drug after 4-8 hours, an increase in the mean serum leuprorelin levels to 25.3 ng / dl, as well as 127 ng / dL or 82 ng / dL after the drug administration, respectively, in 7.5, 22.5 , as well as 45 mg.

At the initial increase (the plateau stage is equal to 2-28th days at a dosage of 7.5 mg, 3-84 days at 22.5 mg, and 3-168 days at a dose of 45 mg), the serum values of the leuprorelin component remain in sufficient stable state (approximately 0.2-2 ng / ml). Information on cumulation of drugs after repeated administration is not.

The synthesis of the substance with the plasma protein is 43-49%.

After intravenous injection of 1 mg of leuprorelin acetate to male volunteers, it was noted that in the case of a 2-chamber model, the average clearance rate reached 8.34 l / h with a final half-life of about 3 hours.

The tests for Eligard's excretion were not performed.

[6], [7]

Dosing and administration

Eligard should be administered subcutaneously once a month at a rate of 7.5 mg. It is also administered once every 3 months at a rate of 22.5 mg, and in addition, once every six months at a rate of 45 mg. The skin-under solution forms the drug depot, which ensures regular release of the active ingredient during the entire period indicated. The treatment process is long.

If there is an increase in PSA with castration testosterone, it is necessary to stop the use of drugs.

It is necessary to periodically change the site of introduction of the solution. It is also necessary to avoid penetration of the medication into the vein or artery.

Drug information about the use of drugs in people with kidney failure or liver is not.

The process of making a solution.

Mix the contents of 2 syringes immediately before the injection procedure. Prepare the mixture in this way:

• get the medicine package out of the refrigerator and hold it in a room so that the package is equal to its temperature in terms of its temperature;
• get syringes A and B from blisters. Next, pull a small piston from the B-syringe, which has a second limiter, after which a long special piston is pulled out of the blister with an A-syringe, and inserted into the B-syringe;
• remove plugs from both syringes (inside the A-syringe contains a solvent, and inside the B-syringe - lyophilizate medication) and carefully connect them. The solution is then required to be mixed, taking turns using the syringe pistons (60 pressures) until a homogeneous mixture is obtained. A solution that is allowed to be used for administration acquires a light yellow or colorless hue;
• the finished mixture is injected into the B-syringe, and the empty A-syringe is removed, pushing the piston to the end. Small bubbles may appear during the procedure. This phenomenon is absolutely normal, and does not affect the formation of the depot after drug injection. Then a sterile needle is inserted into the B-syringe;
• after which the mixture can be administered subcutaneously. In this case, the finished solution must be introduced immediately after the mixing procedure. If it was not used immediately, after a while you can not enter it. The drug is intended for single use.

[11]

Contraindications

The main contraindications:

• castration by surgical method;
• intolerance to leuprorelin, and other hormone agonists GnRH, or additional components of the drug;
• application in childhood or women.

[8]

Side effects of the eligarde

As a result of taking drugs, the following side effects may develop:

• violations of the function of the CAS: an increase or decrease in blood pressure, the appearance of hot flashes, the development of syncope. Occasionally, peripheral puffiness, dyspnea, palpitations, and PE can occur;
• reactions from the PNS and CNS: the appearance of headaches, taste or olfactory disorders, dizziness, hypoesthesia, involuntary movements, and insomnia. Sometimes depression, amnesia, various sleep or vision disorders, peripheral-type dizziness, and, in addition, cutaneous hypersensitivity, may develop;
• disorders of the function of the gastrointestinal tract: diarrhea, vomiting or nausea, constipation, dyspeptic manifestations, belching, dryness of the oral mucosa, bloating and increased level of ALT;
• manifestations of the respiratory system: problems with breathing or rhinorrhea;
• reactions of the organs of the urogenital system: the development of nocturia, dysuria or oliguria, and the appearance of infection in the urinary ducts. In addition, pain in the testicles or their atrophy, problems with urination, hematuria, spasms in the bladder, acute retention of urination, as well as weakening of libido, impotence and infertility;
• disruption of the endocrine system: development of gynecomastia and pain in the area of the mammary glands;
• manifestations in the structure of muscles and bones: pain in the limbs or back, arthralgia, muscle cramps or weakness, and myalgia. In people with castration of medicamentous or surgical type, the weakening of bone tissue density may develop. It should be borne in mind that prolonged administration of the solution can also reduce bone density and contribute to the progression of osteoporosis;
• disorders in the hematopoietic system: a decrease in the values of hematocrit with hemoglobin, a decrease in the number of erythrocytes. Occasionally, there is thrombocyto- or leukopenia;
• violations krovozvytyvaemosti: lengthening the time interval required for blood clotting, as well as an increase in the parameters of PTV;
• changes in the values of laboratory tests: an increase in the level of CK within the blood, as well as an increased rate of triglycerides;
• local manifestations: the onset of pain, sensation of tingling or burning, as well as redness, itching and bruising at the injection site. Occasionally, small ulcers or densations appear in the area of administration;
• others: an increased sense of fatigue, a feeling of severe weakness or malaise, and in addition, the appearance of alopecia, chills, skin rashes, hyperhidrosis, weight gain and changes in tolerance for glucose.

At the first stages of treatment, there may be an exacerbation of signs of pathology.

[9], [10]

Storage conditions

Contain Eligard is necessary in conditions of temperature within 2-8 ° C.

[12]

Special instructions

Eligard, according to the testimony of patients, showed an increase in the manifestations of the disease at the initial stage of therapy. In addition, there were pains in the bones, blood in the urine, as well as neurological disorders. Similar signs develop due to a flash of excretion of gonadotropic hormones. In the process of subsequent treatment, their oppression occurs. During prolonged use, according to individual reviews, there were hot flashes of moderate or mild severity, as well as nausea, burning in the area of administration and gynecomastia.

However, the medicine is unique because it uses a special Atrigel system (a biodegradable polymer used as a solvent) that promotes the formation of a drug depot within the subcutaneous layer for a period of 1-3-6 months, and also provides a stable result. Such a system helps to reduce the level of testosterone in 95% of those treated.

Among Eligard's merits, it should also be noted that due to the use of the 6-month-old depot, the incidence of local manifestations decreases, and the need for frequent visits to the doctor disappears.

[13],

Shelf life

Eligard can be used in the period of 2 years from the date of release of the medicinal product.