Firmagon 80mg Inj, 1 Vial
It is used to treat prostate cancer. If you have been given this drug for some other reason, talk with your doctor for more information.
Drug Class
Antineoplastic agent, Gonadotropin-releasing hormone (GnRH) receptor antagonist
Pharmacologic Class
GnRH receptor antagonist
Pregnancy Category
Not applicable (indicated for males)
FDA Approved
Dec 2008
DEA Schedule
Not Controlled
Overview
What is this medicine?
Firmagon is a medicine used to treat advanced prostate cancer in men. It works by lowering the amount of testosterone in your body, which helps to slow down the growth of cancer cells. It is given as an injection under the skin, usually in the stomach area.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Administer the medication as a subcutaneous injection into the fatty tissue of the abdominal area. After injection, avoid applying pressure to the injection site, such as wearing a tight waistband or belt.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep the medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the next steps to take.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep the medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the next steps to take.
Lifestyle & Tips
- Maintain a healthy diet and exercise regularly to help manage potential side effects like weight gain and fatigue.
- Discuss bone health with your doctor, as long-term use of hormone therapy can lead to bone thinning (osteoporosis). Calcium and Vitamin D supplements may be recommended.
- Report any new or worsening symptoms, especially chest pain, shortness of breath, or dizziness, as hormone therapy can affect heart health.
- Avoid alcohol or other sedatives if experiencing dizziness or fatigue.
- Stay hydrated.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose: 240 mg administered as two subcutaneous injections of 120 mg each. Maintenance dose: 80 mg administered as one subcutaneous injection every 28 days.
Dose Range:
80 - 240 mg
Condition-Specific Dosing:
advancedProstateCancer:
Initial: 240 mg SC (two 120 mg injections); Maintenance: 80 mg SC every 28 days.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment necessary.
Moderate:
No dose adjustment necessary.
Severe:
Use with caution; no specific dose adjustment recommendations available, but close monitoring is advised.
Dialysis:
Not available (primarily eliminated via biliary-fecal route, renal excretion is minor).
Hepatic Impairment:
Mild:
No dose adjustment necessary.
Moderate:
No dose adjustment necessary.
Severe:
Use with caution; no specific dose adjustment recommendations available, but close monitoring is advised.
Pharmacology
Mechanism of Action
Degarelix is a selective gonadotropin-releasing hormone (GnRH) receptor antagonist. It reversibly binds to GnRH receptors in the pituitary gland, immediately suppressing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to a rapid and profound decrease in testicular testosterone production, which is crucial for the growth of prostate cancer cells.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80-90% (relative to IV)
Tmax:
2-3 days (after initial dose)
FoodEffect:
Not applicable (subcutaneous injection)
Distribution:
Vd:
Approximately 1000 L (large volume of distribution)
ProteinBinding:
Approximately 90%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 28-43 days (terminal half-life)
Clearance:
Approximately 9 L/hour
ExcretionRoute:
Primarily biliary-fecal excretion (approximately 70-80%), with minor renal excretion (approximately 20-30%)
Unchanged:
Not available (undergoes peptide hydrolysis)
Pharmacodynamics
OnsetOfAction:
Rapid (testosterone suppression within 3 days)
PeakEffect:
Testosterone suppression maintained throughout treatment
DurationOfAction:
Approximately 28 days (for maintenance dose)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Signs of a urinary tract infection (UTI), such as:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Fast or abnormal heartbeat
Dizziness or passing out
Bone pain (this medication may cause weak bones, especially with long-term use, which can increase the risk of broken bones)
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Pain, redness, or swelling at the injection site
Hot flashes
Weight gain
Erectile dysfunction
Decreased interest in sex
Fatigue or weakness
Back pain
Joint pain
Chills
Constipation
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Signs of a urinary tract infection (UTI), such as:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Fast or abnormal heartbeat
Dizziness or passing out
Bone pain (this medication may cause weak bones, especially with long-term use, which can increase the risk of broken bones)
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Pain, redness, or swelling at the injection site
Hot flashes
Weight gain
Erectile dysfunction
Decreased interest in sex
Fatigue or weakness
Back pain
Joint pain
Chills
Constipation
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe injection site reactions (e.g., persistent pain, redness, swelling, skin breakdown)
- Chest pain, shortness of breath, or other signs of heart problems
- Sudden weakness or numbness on one side of the body, sudden severe headache, or vision changes (signs of stroke)
- Increased thirst, frequent urination, or unexplained weight loss (signs of new-onset or worsening diabetes)
- Severe dizziness or fainting spells
- Irregular heartbeats or palpitations
- Signs of allergic reaction (rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you have any electrolyte imbalances, such as abnormal sodium, potassium, or phosphate levels.
If you are pregnant, plan to become pregnant, or are breastfeeding. This medication is not approved for use in these situations, as it may harm the unborn baby or increase the risk of pregnancy loss. If you are pregnant, plan to become pregnant, or are breastfeeding, discuss this with your doctor.
This is not an exhaustive list of all potential interactions with this medication. Therefore, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor and pharmacist to ensure it is safe to take this medication.
Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you have any electrolyte imbalances, such as abnormal sodium, potassium, or phosphate levels.
If you are pregnant, plan to become pregnant, or are breastfeeding. This medication is not approved for use in these situations, as it may harm the unborn baby or increase the risk of pregnancy loss. If you are pregnant, plan to become pregnant, or are breastfeeding, discuss this with your doctor.
This is not an exhaustive list of all potential interactions with this medication. Therefore, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor and pharmacist to ensure it is safe to take this medication.
Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor will instruct you to undergo regular blood tests, bone density assessments, and electrocardiograms (ECGs) to monitor your heart rhythm.
As this medication may interfere with certain laboratory tests, be sure to notify all your healthcare providers and laboratory personnel that you are taking this drug. To minimize potential skin irritation, avoid scratching or rubbing the area where the medication is administered.
Be aware that reducing male hormone levels in the body may increase the risk of developing a type of abnormal heartbeat known as prolonged QT interval. Discuss this potential risk with your doctor. Additionally, this medication may impact fertility, potentially leading to difficulties in becoming pregnant or fathering a child. If you are planning to conceive, consult with your doctor before initiating treatment with this medication.
As this medication may interfere with certain laboratory tests, be sure to notify all your healthcare providers and laboratory personnel that you are taking this drug. To minimize potential skin irritation, avoid scratching or rubbing the area where the medication is administered.
Be aware that reducing male hormone levels in the body may increase the risk of developing a type of abnormal heartbeat known as prolonged QT interval. Discuss this potential risk with your doctor. Additionally, this medication may impact fertility, potentially leading to difficulties in becoming pregnant or fathering a child. If you are planning to conceive, consult with your doctor before initiating treatment with this medication.
Overdose Information
Overdose Symptoms:
- No specific symptoms of overdose have been reported in clinical trials. Exaggerated pharmacological effects (e.g., profound testosterone suppression) are possible.
What to Do:
There is no specific antidote. In case of overdose, treatment should be symptomatic and supportive. Monitor vital signs and ECG. Call 1-800-222-1222 (Poison Control) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Drugs known to prolong the QT interval (e.g., Class IA antiarrhythmics like quinidine, procainamide; Class III antiarrhythmics like amiodarone, sotalol; antipsychotics; macrolide antibiotics; fluoroquinolones). Concomitant use should be avoided if possible, or used with extreme caution and ECG monitoring.
Moderate Interactions
- Androgen deprivation therapy (ADT) may prolong the QT interval. Caution with other drugs that prolong the QT interval or cause Torsade de Pointes.
Monitoring
Baseline Monitoring
Serum Testosterone
Rationale: To confirm baseline levels and monitor treatment efficacy (goal is castration levels < 50 ng/dL).
Timing: Prior to first dose.
Prostate-Specific Antigen (PSA)
Rationale: To establish baseline and monitor disease response.
Timing: Prior to first dose.
Electrocardiogram (ECG)
Rationale: To assess baseline QT interval, especially in patients with risk factors for QT prolongation (e.g., history of cardiac disease, electrolyte abnormalities, concomitant QT-prolonging drugs).
Timing: Prior to first dose, if risk factors present.
Serum Electrolytes (Potassium, Magnesium, Calcium)
Rationale: To identify and correct any imbalances that could predispose to QT prolongation.
Timing: Prior to first dose, if risk factors present.
Liver Function Tests (LFTs)
Rationale: To assess baseline hepatic function, especially given its primary elimination route.
Timing: Prior to first dose.
Routine Monitoring
Serum Testosterone
Frequency: Monthly (prior to each maintenance dose)
Target: < 50 ng/dL (castration level)
Action Threshold: If testosterone levels are not suppressed, evaluate adherence or consider alternative therapies.
Prostate-Specific Antigen (PSA)
Frequency: Periodically (e.g., every 3-6 months or as clinically indicated)
Target: Decreasing or stable levels
Action Threshold: Rising PSA may indicate disease progression or treatment failure.
ECG
Frequency: Periodically, as clinically indicated, especially if new risk factors for QT prolongation develop or if concomitant QT-prolonging drugs are initiated.
Target: Normal QT interval for age/sex
Action Threshold: Significant QT prolongation (e.g., QTc > 500 ms or increase > 60 ms from baseline) may require dose adjustment or discontinuation of degarelix or other QT-prolonging agents.
Serum Electrolytes
Frequency: Periodically, as clinically indicated, especially if risk factors for QT prolongation are present or if symptoms of electrolyte imbalance occur.
Target: Normal ranges
Action Threshold: Correct hypokalemia or hypomagnesemia promptly.
Liver Function Tests (LFTs)
Frequency: Periodically, as clinically indicated.
Target: Normal ranges
Action Threshold: Significant elevations may warrant further investigation or dose adjustment.
Symptom Monitoring
- Injection site reactions (pain, erythema, swelling, induration)
- Hot flashes/flushes
- Fatigue
- Weight gain
- Decreased libido
- Erectile dysfunction
- Musculoskeletal pain
- Dizziness
- Headache
- Nausea
- Diarrhea
- Signs of cardiovascular events (chest pain, shortness of breath, palpitations)
- Symptoms of electrolyte imbalance (muscle weakness, cramps, irregular heartbeats)
Special Patient Groups
Pregnancy
Degarelix is not indicated for use in women and is contraindicated in pregnant women. Based on its mechanism of action, it would cause fetal harm.
Trimester-Specific Risks:
First Trimester:
Not applicable (contraindicated)
Second Trimester:
Not applicable (contraindicated)
Third Trimester:
Not applicable (contraindicated)
Lactation
Degarelix is not indicated for use in women and is not expected to be used by lactating women. It is unknown if degarelix is excreted in human milk.
Infant Risk:
Not applicable
Pediatric Use
The safety and effectiveness of degarelix in pediatric patients have not been established. It is not indicated for use in children.
Geriatric Use
No dose adjustment is necessary based on age. Clinical studies included a large proportion of patients aged 65 and over, and no overall differences in safety or effectiveness were observed between these patients and younger patients.
Clinical Information
Clinical Pearls
- Degarelix provides rapid testosterone suppression without an initial testosterone surge (flare), unlike GnRH agonists, making it beneficial for patients with symptomatic prostate cancer (e.g., spinal cord compression, urinary obstruction).
- Administer degarelix as a subcutaneous injection only. Do not administer intravenously or intramuscularly.
- Rotate injection sites within the abdominal region to minimize injection site reactions.
- Patients should be informed about potential cardiovascular risks associated with androgen deprivation therapy (ADT), including degarelix.
- Monitor for signs and symptoms of diabetes and cardiovascular disease, as these risks may increase with ADT.
- Long-term ADT can lead to decreased bone mineral density; consider bone health management strategies.
- Ensure patients understand the importance of monthly maintenance injections for continuous testosterone suppression.
Alternative Therapies
- GnRH agonists (e.g., leuprolide, goserelin, triptorelin, histrelin)
- Androgen receptor inhibitors (e.g., enzalutamide, apalutamide, darolutamide)
- Androgen synthesis inhibitors (e.g., abiraterone acetate)
- Bilateral orchiectomy (surgical castration)
- Estrogens (historically used, but less common due to side effects)
Cost & Coverage
Average Cost:
Varies widely, typically several thousand USD per vial
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high co-pays or co-insurance)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed otherwise, do not flush medications down the toilet or pour them down the drain. If you are unsure about the correct disposal method, consult your pharmacist for guidance. Many communities offer drug take-back programs, which your pharmacist can help you locate. Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken to ensure prompt and effective treatment.