Firmagon 120mg Each Inj (2 Vials)
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
Pharmacologic Class
Gonadotropin-releasing hormone (GnRH) receptor antagonist
Pregnancy Category
Not applicable (for male use)
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
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Administer the medication as a subcutaneous injection into the fatty tissue in your abdominal area. After injection, avoid applying pressure to the injection site, such as wearing a tight waistband or belt.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage.
Missing a Dose
If you miss a dose, contact your doctor to determine the best course of action.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Administer the medication as a subcutaneous injection into the fatty tissue in your abdominal area. After injection, avoid applying pressure to the injection site, such as wearing a tight waistband or belt.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage.
Missing a Dose
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Maintain a healthy diet and regular exercise to help manage potential side effects like weight gain and fatigue.
- Discuss any new or worsening symptoms with your doctor promptly.
- Report any signs of injection site reactions (pain, redness, swelling) to your healthcare provider.
- Be aware of symptoms of heart problems (e.g., chest pain, shortness of breath, dizziness, fainting) and seek immediate medical attention if they occur.
- Avoid driving or operating machinery if you experience dizziness or fatigue.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Loading 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:
advanced_prostate_cancer:
Loading dose: 240 mg (two 120 mg injections). Maintenance dose: 80 mg 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:
No dose adjustment necessary, but caution is advised due to limited data.
Dialysis:
Not available; caution advised.
Hepatic Impairment:
Mild:
No dose adjustment necessary.
Moderate:
No dose adjustment necessary, but caution is advised due to limited data.
Severe:
Not recommended due to lack of data and potential for increased exposure.
Confidence:
Medium
Pharmacology
Mechanism of Action
Degarelix is a synthetic decapeptide gonadotropin-releasing hormone (GnRH) receptor antagonist. It competitively binds to and blocks the GnRH receptors in the anterior pituitary gland, thereby rapidly reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to a rapid and profound suppression of testicular testosterone production, which is crucial for the growth of prostate cancer cells.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90% (relative to IV administration)
Tmax:
2 days (loading dose), 1 day (maintenance dose)
FoodEffect:
Not applicable (subcutaneous injection)
Distribution:
Vd:
Approximately 1000 L (suggests extensive tissue distribution)
ProteinBinding:
Approximately 90%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 28-43 days (loading dose), 28-43 days (maintenance dose)
Clearance:
Approximately 9 L/hour
ExcretionRoute:
Primarily fecal (70-80%), with a smaller portion excreted renally (20-30%) as metabolites.
Unchanged:
Less than 1% (renal)
Pharmacodynamics
OnsetOfAction:
Rapid; testosterone suppression within 3 days.
PeakEffect:
Testosterone suppression to castration levels (<50 ng/dL) typically achieved within 3 days.
DurationOfAction:
Approximately 28 days (maintenance dose)
Confidence:
High
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
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
+ Fainting
+ 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 fainting
This medication may also cause weak bones, particularly with long-term use, which can increase the risk of fractures. If you experience bone pain, contact your doctor right away.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Pain, redness, or swelling at the injection site
Hot flashes
Weight gain
Erectile dysfunction
Decreased libido
Fatigue or weakness
Back pain
Joint pain
Chills
* Constipation
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
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
+ Fainting
+ 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 fainting
This medication may also cause weak bones, particularly with long-term use, which can increase the risk of fractures. If you experience bone pain, contact your doctor right away.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Pain, redness, or swelling at the injection site
Hot flashes
Weight gain
Erectile dysfunction
Decreased libido
Fatigue or weakness
Back pain
Joint pain
Chills
* Constipation
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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 or persistent injection site reactions (e.g., large swelling, severe pain, infection signs)
- Signs of liver problems (yellowing of skin or eyes, dark urine, severe stomach pain, unusual tiredness)
- Symptoms of heart problems (chest pain, shortness of breath, irregular heartbeat, dizziness, fainting)
- Severe dizziness or lightheadedness
- Unusual bleeding or bruising
- Sudden, severe headache or vision changes
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, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have any electrolyte imbalances, such as abnormal levels of sodium, potassium, or phosphate.
* 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 an 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 list is not exhaustive, and it is crucial to disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues to your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have any electrolyte imbalances, such as abnormal levels of sodium, potassium, or phosphate.
* 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 an 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 list is not exhaustive, and it is crucial to disclose all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues to your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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, it is crucial 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.
You should 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 your doctor before initiating treatment with this medication to discuss the potential effects on fertility.
As this medication may interfere with certain laboratory tests, it is crucial 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.
You should 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 your doctor before initiating treatment with this medication to discuss the potential effects on fertility.
Overdose Information
Overdose Symptoms:
- Exaggerated pharmacological effects (e.g., severe testosterone suppression)
- Injection site reactions
What to Do:
There is no specific antidote. In case of overdose, discontinue degarelix and manage symptoms supportively. Call 1-800-222-1222 (Poison Control) for further guidance.
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.
- Androgen deprivation therapy (ADT) may prolong the QT interval. Caution with other drugs that prolong QT.
Moderate Interactions
- Drugs that affect electrolyte balance (e.g., diuretics) may increase the risk of QT prolongation if hypokalemia or hypomagnesemia occurs.
- Warfarin (or other anticoagulants): Monitor INR/PT more frequently as ADT may affect coagulation parameters, though direct interaction with degarelix is not well-established.
Monitoring
Baseline Monitoring
Serum Testosterone
Rationale: To confirm baseline levels and monitor response to therapy (aim for castration levels).
Timing: Prior to initiation of therapy.
Prostate-Specific Antigen (PSA)
Rationale: To monitor disease progression and response to therapy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function, as degarelix is metabolized in the liver and liver enzyme elevations have been reported.
Timing: Prior to initiation of therapy.
Serum Electrolytes (Potassium, Magnesium, Calcium)
Rationale: To assess baseline electrolyte status, especially if patient is at risk for QT prolongation or on concomitant medications affecting electrolytes.
Timing: Prior to initiation of therapy.
Electrocardiogram (ECG)
Rationale: To assess baseline QT interval, especially in patients with pre-existing cardiac conditions or on concomitant medications known to prolong QT.
Timing: Prior to initiation of therapy, if clinically indicated.
Routine Monitoring
Serum Testosterone
Frequency: Monthly for the first 3 months, then every 3-6 months or as clinically indicated.
Target: < 50 ng/dL (castration level)
Action Threshold: If testosterone levels are not suppressed to castration levels, evaluate adherence or consider alternative therapies.
Prostate-Specific Antigen (PSA)
Frequency: Every 3-6 months or as clinically indicated.
Target: Decreasing or stable levels
Action Threshold: Rising PSA may indicate disease progression or treatment failure.
Liver Function Tests (ALT, AST, bilirubin)
Frequency: Periodically, or if symptoms of liver dysfunction develop.
Target: Within normal limits
Action Threshold: Significant elevations may require dose adjustment or discontinuation.
Serum Electrolytes (Potassium, Magnesium, Calcium)
Frequency: Periodically, especially if patient is at risk for QT prolongation or on concomitant medications affecting electrolytes.
Target: Within normal limits
Action Threshold: Correct electrolyte imbalances promptly.
ECG
Frequency: Periodically, if patient has risk factors for QT prolongation or develops symptoms suggestive of arrhythmia.
Target: Normal QT interval
Action Threshold: Significant QT prolongation (e.g., QTc > 500 ms) or Torsade de Pointes requires immediate medical attention and re-evaluation of therapy.
Symptom Monitoring
- Injection site reactions (pain, erythema, swelling, induration, nodule)
- Hot flashes/flushes
- Fatigue
- Weight gain
- Edema (peripheral)
- Dizziness
- Headache
- Nausea
- Diarrhea
- Constipation
- Elevated liver enzymes (jaundice, dark urine, abdominal pain)
- Symptoms of cardiovascular events (chest pain, shortness of breath, palpitations)
- Symptoms of QT prolongation (dizziness, syncope, palpitations)
Special Patient Groups
Pregnancy
Degarelix is not indicated for use in women and is contraindicated in women who are or may become pregnant. It is expected to cause fetal harm based on its mechanism of action.
Trimester-Specific Risks:
First Trimester:
Expected to cause fetal harm due to hormonal effects.
Second Trimester:
Expected to cause fetal harm due to hormonal effects.
Third Trimester:
Expected to cause fetal harm due to hormonal effects.
Lactation
Degarelix is not indicated for use in women. It is unknown if degarelix is excreted in human milk. Due to the potential for serious adverse reactions in a breastfed infant, it should not be used by lactating women.
Infant Risk:
High (potential for serious adverse reactions due to hormonal effects)
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 overall differences in safety or effectiveness were observed between elderly (âĨ65 years) and younger patients. No dose adjustment is necessary based on age alone.
Clinical Information
Clinical Pearls
- Degarelix provides rapid testosterone suppression without the initial testosterone surge (flare) seen with GnRH agonists, making it a preferred option for patients with symptomatic metastatic prostate cancer or those at risk of clinical flare (e.g., spinal cord compression, ureteral obstruction).
- Administer degarelix as a subcutaneous injection only, typically in the abdominal area. Rotate injection sites.
- Ensure proper mixing and administration technique as per manufacturer's instructions to avoid injection site reactions and ensure proper drug delivery.
- Patients should be monitored for signs and symptoms of QT prolongation, especially those with pre-existing cardiac conditions or on concomitant medications that prolong the QT interval.
- Injection site reactions (pain, erythema, swelling, induration) are common but usually mild to moderate and transient. Proper injection technique can help minimize these.
- Regular monitoring of PSA and testosterone levels is crucial to assess treatment response.
Alternative Therapies
- GnRH agonists (e.g., leuprolide, goserelin, triptorelin): Cause an initial testosterone surge, often requiring co-administration with an antiandrogen.
- Androgen receptor inhibitors (e.g., enzalutamide, apalutamide, darolutamide): Used in various stages of prostate cancer.
- Androgen synthesis inhibitors (e.g., abiraterone acetate): Used in metastatic castration-resistant prostate cancer.
- Bilateral orchiectomy (surgical castration): Permanent testosterone suppression.
Cost & Coverage
Average Cost:
Varies widely, typically several thousand USD per 120mg/80mg injection kit
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 do not improve or worsen over time, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others or take someone else's medication. 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 drain. Instead, consult your pharmacist for advice on the best disposal method or inquire about potential drug take-back programs in your area. Some medications may include an additional patient information leaflet, which can be obtained from your pharmacist. If you have any questions or concerns about this 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 medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred.