Firmagon, lyophilizate 80 mg

Progressive hormone-dependent prostate cancer.

Active ingredient

Composition

1 vial contains:

Active ingredients:

Degarelix 80 mg.

In a vial of 80 mg of lyophilizate.

There is 1 vial in the carton pack.

How to take, the dosage

Introduce by injection by injection, into the abdominal area with periodic change of injection site. The initial dose is 240 mg divided into 2 injections of 120 mg each. A maintenance dose of 80 mg is administered 1 month after the initial dose.

Degarelix is not intended for IV or IM administration.

Interaction

Because Degarelix may cause QT interval prolongation, the concomitant use of degarelix with drugs that cause QT interval prolongation or ventricular tachycardia (e.g., quinidine, disopyramide), neuroleptics, antiarrhythmic drugs (e.g., amiodarone, sotalol, dofetilide, ibutilide), and methadone, cisapride and moxifloxacin should be evaluated.

A clinically significant pharmacokinetic interaction between degarelix and agents that affect the CYP450 enzyme system is unlikely.

Special Instructions

The use of Degarelix has not been studied in patients with a history of QTc interval greater than 450 msec, in patients with risk factors for ventricular pirouette arrhythmias, in combination with drugs that can prolong the QT interval. If it is necessary to use Degarelix in such cases, the expected benefits and risks of therapy should be carefully evaluated.

The therapeutic efficacy of degarelix should be evaluated according to clinical parameters and serum PSA levels. Testosterone suppression occurs immediately after administration of the initial dose, with plasma testosterone levels falling to medical castration testosterone levels (< 0.5 ng/mL) in 96% of patients after three days and in 100% of patients after one month. Prolonged, up to 1 year, maintenance therapy provides testosterone suppression (< 0.5 ng/mL) in 97% of patients. If the therapeutic effect is not clearly expressed in the patient, it should be made sure that the serum testosterone levels remain sufficiently reduced. Degarelix does not cause fluctuations in testosterone levels, so there is no need to use antiandrogenic medications at the beginning of treatment.

There is no need to change the dose for elderly patients or for patients with mild to moderate impairment of hepatic or renal function. Caution should be exercised when using degarelix in patients with severe hepatic or renal impairment, as it has not been studied in this patient population.

Changes in bone density with degarelix have not been studied, but patients who have had orchiectomies or have taken GnRH agonists show decreased bone density. Therefore, there may be decreased bone density due to testosterone suppression induced by the use of Degarelix.

The effect of degarelix on insulin and blood glucose levels has not been studied. However, in patients who have had an orchiectomy or have taken GnRH agonists, there is a decrease in insulin sensitivity to glucose and possible development or exacerbation of diabetes mellitus. Therefore, regular monitoring of blood glucose levels is recommended during treatment with Degarelix.

Pediatric use

There are no substantiated indications for the use of Degarelix in children or adolescents.

Impact on ability to drive or operate vehicles and other mechanisms requiring increased concentration

Degarelix use may cause fatigue and dizziness, which may affect the patient’s ability to drive or engage in other potentially hazardous activities.

Contraindications

A hypersensitivity to degarelix.

Side effects

Nervous system disorders: frequent (≥ 1%, < 10%) – insomnia, dizziness, headaches; rare (≥ 0.01%, < 0.1%) – decreased libido, depression, irritability, tinnitus.

Cardiovascular system: very common (≥10%) – hot flashes; rare (≥0.01%, < 0.1%) – 1st degree AV blockade, QT interval prolongation, increased BP, vasovagal syncope, varicose veins.

Gastrointestinal system disorders: very frequently (≥10%) – nausea; frequently (≥1%, < 10%) – diarrhea, vomiting, flatulence, dry mouth, constipation, increased liver transaminase activity; rarely (≥0.01%, < 0.1%) – decreased appetite.

Respiratory system: rare (≥ 0.01%, < 0.1%) – cough.

Hematopoietic system: rare (≥ 0.01%, < 0.1%) – anemia.

Dermatological reactions: frequently (≥ 1%, < 10%) – increased sweating (including night sweating); rarely (≥ 0.01%, < 0.1%) – urticaria, hyperpigmentation of skin, hair loss, softened nails, rash, erythema.

Muscular system disorders: rare (≥0.01%, < 0.1%) – muscle pain, muscle weakness.

Gender system disorders: rare (≥0.01%, < 0.1%) – erectile dysfunction, testicular atrophy, gynecomastia, lower abdominal pain, prostatic soreness, retrograde ejaculation, testicular soreness.

Urinary system disorders: rare (≥0.01%, < 0.1%) – frequent urination, urgent urge to urinate, renal failure.

Metabolism: 6% – marked hypokalemia (≥5.8 mmol/L); 2% – decreased creatinine levels (≥177 μmol/L); 15% – increased blood urea nitrogen (≥10.7 mmol/L).

Others: very common (≥10%) – irritation at the injection site; common (≥1%, < 10%) – chills, fever, weakness, fatigue, colds; rare (≥0.01%, < 0.1%) – hypersensitivity reactions, swelling at the injection site.

Overdose

Symptoms: There are no data on the symptoms of acute overdose of Degarelix.

Treatment: In case of overdose, the patient should be monitored and supportive therapy used if necessary.