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FIRMAGON is a brand name for Degarelix, supplied as a powder for solution. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE ..............................................................................3 CONTRAINDICATIONS ...................................................................................................4 WARNINGS AND PRECAUTIONS…
Verbatim from this product's HC label. Tap a section to expand.
Adverse Drug Reaction Overview In total, 1839 patients with prostate cancer have been exposed to degarelix, including 1567 exposed for at least 6 months and 1178 exposed for more than one year. Degarelix was studied primarily in an active-controlled trial (N = 610) and in uncontrolled trials, including long-term extension studies evaluating safety and tolerability.
The population was male patients with prostate cancer; the median age was 74 years and the age range was 47 to 98 years of age. Patients were given degarelix at monthly (N = 1259) or 3-monthly (N = 580) intervals. Most patients have received mean monthly doses of 60-120 mg, given as subcutaneous injections at 28-days intervals (N = 875).
g. pain, erythema, swelling, nodule or induration), hot flashes, increased weight, fatigue, dizziness, anemia and increases in serum levels of transaminases and gamma-glutamyltransferase (GGT). The majority of the adverse reactions were Grade 1 or 2, with Grade 3/4 adverse reaction incidences of 1% or less.
Adverse reactions reported as uncommon were cardiac arrhythmia (incl. atrial fibrillation, QT-prolongation), hypertension, hyperglycemia/diabetes mellitus, hypersensitivity (including urticaria, rash and pruritus), osteoporosis/osteopenia and renal impairment.
The most commonly observed adverse reactions during degarelix therapy in the confirmatory Phase III trial (N= 409) were due to the expected physiological effects of testosterone suppression, including hot flashes and weight increase (reported in 25% and 7%, of patients receiving treatment for one year) and injection site reactions.
Transient chills, fever or influenza like illness were reported to occur hours after dosing (in 3%, 2% and 1% of patients, respectively). Clinical Trial Adverse Drug Reactions Degarelix was studied in an active-controlled trial (N = 610) in which patients with prostate cancer were randomized to receive degarelix (subcutaneous) or leuprolide (intramuscular) monthly for 12 months.
Adverse events reported in 5% of patients or more regardless of causality are shown in Table 1 below. 5 mg (intramuscular) N=202 N=207 N=201 % % % Percentage of subjects with adverse events 83 79 78 Body as a whole Injection site adverse events 44 35 <1 Weight increase 11 9 12 Fatigue 6 3 6 Chills 3 5 0 Cardiovascular system Hot flash 26 26 21 Hypertension 7 6 4 Musculoskeletal system Back pain 6 6 8 Arthralgia 3 5 9 Urogenital system Urinary tract infection 1 5 9 Digestive system Increases in Transaminases and GOT 10 10 5 Constipation 3 5 5 Nausea 5 4 4 Hypercholesterolemia 6 3 2 The most frequently reported adverse reactions at the injection sites were pain (28%), erythema (17%), swelling (6%), induration (4%) and nodule (3%) with the FIRMAGON 240/80 mg dosing regimen.
Hypersensitivity to degarelix or to any of the excipients. FIRMAGON is not indicated for use in women and is contraindicated in women who are or who may become pregnant. WARNINGS AND PRECAUTIONS General Route of administration FIRMAGON is for subcutaneous administration only and is not to be administered intravenously.
Gently pull back the plunger to check if blood is aspirated. If blood appears in the syringe, the reconstituted product can no longer be used. Discontinue the procedure and discard the syringe and the needle (reconstitute a new dose for the patient) (See Dosage and Administration Section).
FIRMAGON is administered as a subcutaneous injection in the abdominal region. As with other drugs administered by subcutaneous injection, the injection site should vary periodically. g. not close to waistband or belt nor close to the ribs.
Serious Warnings and Precautions:
FIRMAGON® (degarelix) should be prescribed by a qualified health professional that is experienced in the use of hormonal therapy in prostate cancer. FIRMAGON should be administered under the supervision of a physician (see Dosage and Administration section).
FIRMAGON has not been studied in patients with severe hepatic or severe renal impairment (see Hepatic/Biliary/Pancreatic and Renal sections below). The following are clinically significant adverse events: QT prolongation (see Cardiovascular section below and Drug-Drug Interactions section).
Osteoporosis (see Musculoskeletal section below and Other Clinical Trial Adverse Drug Reactions section). PrFIRMAGON® Page 5 of 46 Cardiovascular An increased risk of heart disease has been observed in men who have had orchiectomy or who have been treated with a GnRH agonist or antiandrogen monotherapy.
5 mg group. Screening for and intervention to prevent/treat cardiovascular disease is warranted.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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These adverse reactions were mostly transient, of mild to moderate intensity, occurred primarily with the starting dose and led to few discontinuations (<1%). Grade 3 injection site reactions occurred in 2% or less of patients receiving degarelix.
Serious injection site reactions were reported such as injection site infection, injection site abscess or injection site necrosis that could require surgical treatment/drainage. Hepatic laboratory abnormalities were primarily Grade 1 or 2 and were generally reversible.
Grade 3 hepatic laboratory abnormalities occurred in less than 1% of patients. Changes in hepatic laboratory values were similar for degarelix and the comparator. In 1-5% of patients in the active controlled trial the following adverse reactions, not already listed, were considered related to degarelix by the investigator: Body as a whole: Asthenia, fever, night sweats; Digestive system: Nausea; Nervous system: Dizziness, headache, insomnia.
PrFIRMAGON® Page 10 of 46 In uncontrolled trials the following adverse reactions, not already listed, were reported to be drug-related by the investigator in ≥1% of patients: erectile dysfunction, gynecomastia, hyperhidrosis, testicular atrophy, and diarrhea.
Abnormal Hematologic and Clinical Chemistry Findings Changes in laboratory parameters: Changes in laboratory values seen during one year of treatment were in the same range for degarelix and a GnRH-agonist (leuprolide) used as comparator.
Markedly abnormal (>3*ULN) liver transaminase values (ALT, AST and GGT) were seen in 2-6% of patients with normal values prior to treatment, following treatment with both medicinal products. 37) and hemoglobin (<115 g/L) were seen in 40% and 13- 15%, respectively, of patients with normal values prior to treatment, following treatment with both medicinal products.
It is unknown to what extent this decrease in hematological values was caused by the underlying prostate cancer and to what extent it was a consequence of androgen deprivation therapy. 7 mmol/L) in patients with normal values prior to treatment, were seen in 6%, 2% and 15% of degarelix treated patients and 3%, 2% and 14% of leuprolide treated patients, respectively.
Other Clinical Trial Adverse Drug Reactions The following less common adverse reactions were reported in the active-controlled trial. Cardiovascular: atrio-ventricular first degree block, hypertension, vaso-vagal reaction Haematologic: anemia Immune: hypersensitivity, urticaria Musculoskeletal: musculoskeletal pain, muscular weakness Renal: renal impairment, pollakiuria, micturition urgency Anti-Degarelix Antibody development: Anti-degarelix antibody development has been observed in 12% of […]
Effect on QT/QTc interval:
Long-term androgen deprivation therapy prolongs the QT interval. g. g. g. flecainide, propafenone) antiarrhythmic medications. In the randomized, active-controlled trial comparing degarelix to leuprolide, periodic electrocardiograms were performed.
Both therapies showed QT/QTc intervals exceeding 450 msec in approximately 20% of the patients. 5 mg group, had a QTcF ≥500 msec. 7 msec. v. infusion of degarelix over 60 min. The mean Cmax reached 222 ng/mL, approx. 7-fold the Cmax obtained during prostate cancer treatment.
Endocrine and Metabolism Changes in glucose tolerance:
A reduction in glucose tolerance has been observed in men who have had orchiectomy or who have been treated with a GnRH agonist. Development or aggravation of diabetes may occur; therefore diabetic patients may require more freq uent monitoring of blood glucose when receiving androgen deprivation therapy.
The effect of degarelix on insulin and glucose levels has not been studied. Hematologic Anemia is a known physiological consequence of testosterone suppression. 5 mg group. Hepatic/Biliary/Pancreatic Patients with known or suspected hepatic disorder have not been included in long-term clinical trials with degarelix.
Mild, transient increases in ALT and AST have been seen, these were not PrFIRMAGON® Page 6 of 46 accompanied by a rise in bilirubin or clinical symptoms. Monitoring of liver function in patients with known or suspected hepatic disorder is advised during treatment.
A single dose of 1 mg degarelix administered as an intravenous infusion over 1 hour has been studied in a pharmacokinetic study in 16 non-prostate cancer patients with mild to moderate hepatic impairment. Compared to non-prostate cancer patients with normal liver function, the exposure of degarelix decreased by 10% and 18% in patients with mild and moderate hepatic impairment, respectively.
Therefore, dose adjustment is not necessary in patients with mild or moderate hepatic impairment. However, since hepatic impairment can lower degarelix exposure, it is recommended that in patients with hepatic impairment testosterone concentrations should be monitored on a monthly basis until medical castration is achieved.
Once medical castration is achieved, an every-other-month testosterone monitoring approach could be considered. Patients with severe hepatic dysfunction have not been studied and caution is therefore warranted in this group.
Immune Hypersensitivity:
Degarelix has not been studied in patients with a history of severe untreated asthma, anaphylactic reactions, severe urticaria or angioedema. No immediate onset of generalized hypersensitivity was seen in the development program. Hypersensitiviy reactions including anaphylaxis, urticaria and angioedema have been […]