Clinical and pharmacological group: & nbsp

Antineoplastic hormonal agents and hormone antagonists

Included in the formulation
  • Firmagon
    lyophilizate PC 
  • АТХ:

    L.02.B.X   Other hormone antagonists and similar drugs

    L.02.B.X.02   Degarelix

    Pharmacodynamics:

    Degarelix is ​​a selective antagonist of the pituitary GnRG-receptors, dramatically reduces the release of gonadotropins, luteinizing hormone and follicle-stimulating hormone, due to which the secretion of testosterone in the testes decreases. Prostate cancer is considered a hormone-dependent tumor and is treatable, aimed at reducing the production of male sex hormones. Unlike agonists GnRG, antagonists of this hormone do not induce ejection luteinizing hormone followed by activation of testosterone release, tumor development and possible symptomatic exacerbation after initiation of treatment.

    Pharmacokinetics:

    The half-life for the first dose is 43 days, and for the maintenance dose, 28 days. Pharmacokinetics depends on the dose of the drug - the greater the concentration of the solution, the lower the bioavailability and the longer half-life. The connection with plasma proteins is 90%. Biotransformation takes place in the liver, and is eliminated through the gastrointestinal tract and partly through the urinary system.

    Indications:

    Progressing hormone-dependent prostate cancer.

    II.C60-C63.C61   Malignant neoplasm of prostate

    Contraindications:

    Hypersensitivity. Female patients, children and adolescents (due to the lack of indications for use in this population).

    Carefully:

    Chronic kidney disease; liver failure; patients with an elongated interval QT or simultaneous reception of drugs that extend the interval QT; polymorphic ventricular tachycardia of the "pirouette" type; diabetes.

    Pregnancy and lactation:

    Category FDA - X. Not applicable in pregnancy and lactation, due to lack of indications for use in this category.

    Dosing and Administration:

    Subcutaneous injection into the abdominal region (periodic change of injection site is necessary). The first dose is 240 mg, divided into two injections. The maintenance dose is 80 mg, it is used 1 month after the initial dose. The drug is not intended for intramuscular or intravenous administration.

    Side effects:

    From the nervous system: depression, dizziness, decreased libido, insomnia, headaches, ringing in the ears, irritability.

    From the gastrointestinal tract: nausea, vomiting, diarrhea, flatulence, dry mouth, increased activity of transaminases, decreased appetite.

    From the cardiovascular system: interval increase QT, arrhythmias, atrioventricular blockade of 1 degree, hot flashes, increased blood pressure, varicose veins, vasovagal syncope.

    From the respiratory system: cough.

    From the musculoskeletal system: muscle weakness, muscle pain.

    From the side of the circulatory system: anemia, febrile neutropenia.

    From the skin: urticaria, increased sweating, softening of nails, erythema, rash, hyperpigmentation of the skin, hair loss.

    From the genitourinary system: frequent urination, kidney failure, urgency to urinate, gynecomastia, tenderness of the prostate, soreness of the testicles, testicular atrophy, erectile dysfunction, retrograde ejaculation.

    From the side of metabolism: increased urea nitrogen, decreased creatinine, hypokalemia.

    Other: irritation at the injection site, edema, hypersensitivity, cold, fatigue, fever.

    Overdose:

    No data, symptomatic treatment.

    Interaction:

    It is not recommended to take joint medication with drugs that extend the interval QT and causing ventricular tachycardia (eg, quinidine, disopyramide), neuroleptics, antiarrhythmic drugs (for example, amiodarone, sotalol, dofetilide, ibutilide), as well as methadone, cisapride and moxifloxacin.

    Special instructions:

    Do not enter intravenously!

    Impact on the ability to drive vehicles and manage mechanisms

    When taking the drug is not recommended to drive or other mechanisms that require concentration.

    Instructions
    Up