Buy Firmagon® vials 120 mg, 2 pcs
  • Buy Firmagon® vials 120 mg, 2 pcs

Firmagon® [Degarelix]

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2019-09-19
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Clinical Pharmacology

Selective GnRH antagonist. Degarelix is ​​able to competitively and reversibly bind to the pituitary GnRH receptors, sharply reducing the release of gonadotropins, LH and FSH. Thus, the secretion of testosterone in the testes decreases. Prostate carcinoma is considered a hormone-dependent tumor and is amenable to treatment aimed at reducing the production of male sex hormones. Unlike GnRH agonists, antagonists of this hormone do not induce the release of LH with the subsequent activation of testosterone release, the development of a tumor and a possible symptomatic exacerbation after the start of treatment.

A single dose of 240 mg of degarelix and subsequent maintenance therapy at a dose of 80 mg, carried out during a month, quickly decreases the concentration of LH, FSH and, as a result, testosterone. The concentration of dihydrotestosterone in the blood plasma is reduced in a manner similar to testosterone.

With the introduction of degarelix, a decrease in testosterone content is observed and its concentration is maintained at a level lower than during castration (0.5 ng / ml). Supporting monthly therapy at a dose of 80 mg resulted in prolonged suppression of testosterone in 97% of patients for at least one year.

The average testosterone level after treatment with degarelix for 1 year was 0.087 ng / ml.

The production of antibodies against degarelix was observed in 10% of patients after a year of treatment. There is no evidence of the effect of antibodies produced on the efficacy or safety of treatment with degarelix.

Pharmacokinetics

After subcutaneous administration of degarelix at a dose of 240 mg at a concentration of 40 mg / ml in patients with prostate cancer AUC0-28 days makes 635 (602-668) ng / ml / days, Cmax makes 66 (61-71) ng / ml, Tmax reached within 40 (37-42) h. Degarelix is ​​displayed in two phases. Average t1/2 is about 43 days for the initial dose and 28 days for the maintenance dose. Long t1/2 after s / c injection is a consequence of the slow release of degarelix from the depot, formed at the injection sites. The pharmacokinetics of degarelix depends on the concentration of the solution upon administration. So, Cmax and bioavailability decrease with increasing concentration of degarelix, while T1/2 is increasing.

Plasma protein binding is approximately 90%. Vd - about 1 l / kg.

Degarelix undergoes normal peptide degradation when passing through the hepatobiliary system and is excreted mainly as peptide fragments with feces. No significant metabolites were detected. In vitro experiments have shown that degarelix is ​​not a substrate of the CYP450 enzyme system.

Approximately 20-30% of the single dose is excreted in the urine, 70-80% is excreted through the hepato-biliary system.

Indications

Progressive hormone-dependent prostate cancer.

Composition

1 bottle contains:

Active substances: degarelix 120 mg.

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Firmagon® [Degarelix]

Dosage and Administration

Subcutaneous, in the abdomen with a periodic change of the injection site. The initial dose is 240 mg divided into 2 doses of 120 mg each. A maintenance dose of 80 mg is used 1 month after the initial dose.

Degarelix is ​​not intended for intravenous and intramuscular injection.

Adverse reactions

From the nervous system: often (≥ 1%, <10%) - insomnia, dizziness, headaches; rarely (≥ 0.01%, <0.1%) - decreased libido, depression, irritability, tinnitus.

Since the cardiovascular system: very often (≥ 10%) - tides; rarely (≥ 0.01%, <0.1%) - AV-block I degree, an increase in the QT interval, increased blood pressure, vasovagal syncope, varicose veins.

From the digestive system: very often (≥ 10%) - nausea; often (≥ 1%, <10%) - diarrhea, vomiting, flatulence, dry mouth, constipation, increased activity of hepatic transaminases; rarely (≥ 0.01%, <0.1%) - loss of appetite.

On the part of the respiratory system: rarely (≥ 0.01%, <0.1%) - cough.

From the hemopoietic system: rarely (≥ 0.01%, <0.1%) - anemia.

Dermatological reactions: often (≥ 1%, <10%) - increased sweating (including night sweats); rarely (≥ 0.01%, <0.1%) - urticaria, skin hyperpigmentation, hair loss, nail softening, rash, erythema.

From the musculoskeletal system: rarely (≥ 0.01%, <0.1%) - muscle pain, muscle weakness.

From the reproductive system: rarely (≥ 0.01%, <0.1%) - erectile dysfunction, testicular atrophy, gynecomastia, abdominal pain, prostate pain, retrograde ejaculation, testicular pain.

From the urinary system: rarely (≥ 0.01%, <0.1%) - frequent urination, urgent urge to urinate, renal failure.

Metabolism: 6% - severe hypokalemia (≥ 5.8 mmol / l); 2% - decrease in creatinine level (≥177 mcmol / l); 15% increase in blood urea nitrogen (≥10.7 mmol / l).

Other: very often (≥ 10%) - irritation at the injection site; often (≥ 1%, <10%) - chills, fever, weakness, fatigue, colds; rarely (≥ 0.01%, <0.1%) - hypersensitivity reactions, swelling at the injection site.

Contraindications

Hypersensitivity to degarelix.

Drug interactions

Since the use of degarelix may increase the QT interval, the need to simultaneously use degarelix and drugs that cause an increase in the QT interval or ventricular tachycardia (eg, quinidine, disopyramide), neuroleptics, antiarrhythmic drugs (eg, amiodarone, sotalol, dofetilide, ibutilid), as well as methadone, cisapride and moxifloxacin.

Clinically significant pharmacokinetic interaction of degarelix and agents affecting the CYP450 enzyme system is unlikely.

Special instructions

The use of degarelix has not been studied in patients with a history of more than 450 ms QTc interval, in patients with risk factors for developing ventricular arrhythmias of the pirouette type, when combined with drugs that can prolong the QT interval. If necessary, the use of degarelix in such cases should carefully evaluate the expected benefit and risk of therapy.

The therapeutic efficacy of degarelix should be assessed by clinical parameters and serum PSA levels. Testosterone is suppressed immediately after the initial dose is administered, and the plasma plasma testosterone level drops to testosterone levels during medical castration (<0.5 ng="" ml="" in="" 96="" of="" patients="" after="" three="" days="" and="" 100="" a="" month="" prolonged="" up="" to="" 1="" year="" supportive="" therapy="" suppresses="" testosterone="" 0="" 5="" 97="" if="" the="" patient="" s="" therapeutic="" effect="" is="" not="" clearly="" expressed="" you="" should="" make="" sure="" that="" level="" blood="" serum="" remains="" sufficiently="" low="" degarelix="" does="" cause="" fluctuations="" levels="" so="" there="" no="" need="" use="" antiandrogenic="" drugs="" at="" beginning="" treatment="" p="">

There is no need to change the dose for elderly patients or for patients with mild or moderate hepatic or renal dysfunction. With caution should be used degarelix in patients with severe hepatic or renal failure, because his study in this category of patients was not conducted.

The change in bone density in the use of degarelix has not been studied, however, in patients undergoing orchiectomy or taking GnRH agonists, there is a decrease in bone density.Therefore, due to the suppression of testosterone caused by the use of degarelix, a decrease in bone density is possible.

The effect of degarelix on insulin and glucose in the blood has not been studied. However, in patients undergoing orchiectomy or taking GnRH agonists, there is a decrease in insulin sensitivity to glucose and possibly the development or worsening of diabetes mellitus. Therefore, in the treatment of degarelix recommended regular monitoring of blood glucose levels.

Use in Pediatrics

There is no reasonable evidence for the use of degarelix in children or adolescents.

Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention

When using degarelix, fatigue and dizziness are possible, which may affect the patient's ability to drive and other potentially dangerous activities.

Overdosage

Symptoms: data on the symptoms of acute overdose of degarelix are not available.

Treatment: in case of overdose, observe the patient and, if necessary, use supportive therapy.

  • Brand name: Firmagon®
  • Active ingredient: Degarelix
  • Dosage form: Lyophilisate for preparation of solution for subcutaneous injection.
  • Manufacturer: Teva

Studies and clinical trials of Degarelix (Click to expand)

  1. Population PK/PD Modeling of Testosterone (T), LH and Dihydrotestosterone (DHT) Response to Single SC Degarelix in Male Volunteers
  2. Pharmacokinetic/Pharmacodynamic Modellingof GnRH Antagonist Degarelix: A Comparisonof the Non-linear Mixed-Effects Programs NONMEM and NLME
  3. Semi-Mechanistic Pharmacodynamic Modeling for Degarelix, a Novel Gonadotropin Releasing Hormone (GnRH) Blocker
  4. Dégarélix, nouvelle étape dans le cancer de la prostate
  5. Degarelix, a novel GnRH antagonist, causes minimal histamine release compared with cetrorelix, abarelix and ganirelix in an ex vivo model of human skin samples
  6. The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer
  7. Changes in alkaline phosphatase levels in patients with prostate cancer receiving degarelix or leuprolide: results from a 12-month, comparative, phase III study
  8. Efficacy and safety of androgen deprivation therapy after switching from monthly leuprolide to monthly degarelix in patients with prostate cancer
  9. Population Pharmacokinetic Modeling of a Subcutaneous Depot for GnRH Antagonist Degarelix
  10. Degarelix: a new hormonal treatment for prostate cancer
  11. Degarelix: A gonadotropin-releasing hormone antagonist for the management of prostate cancer
  12. The dosing solution influence on the pharmacokinetics of degarelix, a new GnRH antagonist, after s.c. administration to beagle dogs
  13. Degarelix: A Novel Gonadotropin-Releasing Hormone (GnRH) Receptor Blocker—Results from a 1-yr, Multicentre, Randomised, Phase 2 Dosage-Finding Study in the Treatment of Prostate Cancer
  14. Editorial Comment on: Degarelix: a Novel Gonadotropin-Releasing Hormone (GnRH) Receptor Blocker—Results from a 1-yr, Multicentre, Randomised, Phase 2 Dose-Finding Study in the Treatment of Prostate Cancer
  15. Editorial Comment on: Degarelix: A Novel Gonadotropin-Releasing Hormone (GnRH) Receptor Blocker—Results from a 1-yr, Multicentre, Randomised, Phase 2 Dose-Finding Study in the Treatment of Prostate Cancer
  16. Re: The Efficacy and Safety of Degarelix: A 12-Month, Comparative, Randomized, Open-Label, Parallel-Group Phase III Study in Patients with Prostate Cancer
  17. Corrigendum to: “Re: The Efficacy and Safety of Degarelix: A 12-Month, Comparative, Randomized, Open-Label, Parallel-Group Phase III Study in Patients with Prostate Cancer” by Dieter Jocham and Christian Doehn [Eur Urol 2009;55:1488–9]
  18. Additional Analysis of the Secondary End Point of Biochemical Recurrence Rate in a Phase 3 Trial (CS21) Comparing Degarelix 80 mg Versus Leuprolide in Prostate Cancer Patients Segmented by Baseline Characteristics
  19. Is there a need for Degarelix as LH/RH Antagonist in treatment of advanced PCa: Comparative Review of Literartue
  20. Degarelix: An Antagonist to GnRH—Theoretical and Treatment Considerations in Paraphilia
  21. Androgen deprivation therapy for volume reduction, lower urinary tract symptom relief and quality of life improvement in patients with prostate cancer: degarelix vs goserelin plus bicalutamide
  22. Morphological and genomic endometrial development with long-acting degarelix starting in the mid-luteal or early follicular phase compared to daily ganirelix starting in the mid-follicular phase
  23. Synchronisation of the follicle cohort with the GnRH antagonist degarelix: a randomised, assessor-blind, placebo-controlled trial

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