Degarelix

Name: Degarelix

Degarelix Interactions

On the day of your injection, avoid wearing a belt, tight waistband, or tight clothing around your stomach where the injection will be given.

This medicine can pass into body fluids (urine, feces, vomit). For at least 48 hours after you receive a dose, avoid allowing your body fluids to come into contact with your hands or other surfaces. Caregivers should wear rubber gloves while cleaning up a patient's body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.

Tell your doctor about all your current medicines and any you start or stop using, especially:

  • heart rhythm medicine--amiodarone, disopyramide, dofetilide, dronedarone, flecainide, procainamide, quinidine, sotalol, and others.

This list is not complete. Other drugs may interact with degarelix, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Degarelix and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if degarelix is excreted in human breast milk or if it will harm your nursing baby.

Degarelix Dosage

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully. The dose your doctor recommends may be based on the following:

  • the condition being treated
  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • your weight
  • your height
  • your age
  • your gender

The starting dose of degarelix is two 120 mg injections (240 mg) on the first day of treatment. The mainanence dose of one 80 mg injection is given 28 days after the first dose. The 80 mg maintenance dose will be given every 28 days until treatment ends.

 

What is the most important information I should know about degarelix?

Although degarelix is not for use by women, this medication should not be used by a woman who is pregnant or breast-feeding, or who may become pregnant.

Degarelix dosing information

Usual Adult Dose for Prostate Cancer:

-Initial Dose: 240 mg administered as 2 subcutaneous injections of 120 mg each at a concentration of 40 mg/mL.

-Maintenance Dose: 80 mg administered as 1 subcutaneous injection at a concentration of 20 mg/mL every 28 days.

Comments: Administer the first maintenance dose 28 days after the initial dose.

Use: Treatment of advanced prostate cancer

How do I store and/or throw out Degarelix?

  • If you need to store this medicine at home, talk with your doctor, nurse, or pharmacist about how to store it.

Pharmacology

Gonadotropin-releasing hormone (GnRH) antagonist which reversibly binds to GnRH receptors in the anterior pituitary gland, blocking the receptor and decreasing secretion of luteinizing hormone (LH) and follicle stimulation hormone (FSH), resulting in rapid androgen deprivation by decreasing testosterone production, thereby decreasing testosterone levels. Testosterone levels do not exhibit an initial surge, or flare, as is typical with GnRH agonists (Crawford 2011).

Distribution

Vd: >1000 L

Metabolism

Hepatobiliary, via peptide hydrolysis

Excretion

Feces (~70% to 80%, primarily as peptide fragments); urine (~20% to 30%)

Use Labeled Indications

Prostate cancer, advanced: Treatment of advanced prostate cancer

Dosing Adult

Prostate cancer, advanced: SubQ:

Loading dose: 240 mg administered as two 120 mg (3 mL) injections

Maintenance dose: 80 mg administered as one 4 mL injection every 28 days (beginning 28 days after initial loading dose)

Reconstitution

Wear gloves for preparation and administration. Reconstitute with provided prefilled syringe containing preservative free sterile water for injection (reconstitute each 120 mg vial with 3 mL; reconstitute the 80 mg vial with 4.2 mL). Swirl gently; do NOT shake (to prevent foaming). Dissolution usually takes a few minutes, although may take up to 15 minutes. May tilt the vial slightly if the powder adheres to the side of the vial. To withdraw for administration, turn the vial completely upside down and pull down on the plunger to withdraw all of the reconstituted solution from the vial to the syringe; expel all air bubbles. Administer within 1 hour (US labeling) or 2 hours (Canadian labeling, although immediate administration is preferred) of reconstitution. Use of concentrations other than those described in the manufacturer’s labeling is not recommended.

Test Interactions

Suppression of pituitary-gonadal function may affect diagnostic tests of pituitary gonadotropic and gonadal functions.

Warnings/Precautions

Concerns related to adverse effects:

• Anemia: Testosterone suppression is associated with the development of anemia.

• Decreased bone mineral density: Androgen deprivation therapy is associated with decreased bone mineral density.

• Hypersensitivity: Hypersensitivity reactions (including anaphylaxis, urticaria, and angioedema) have been reported. Discontinue for serious hypersensitivity reaction (immediately if dose not fully injected); manage hypersensitivity as clinically indicated. Do not rechallenge after serious hypersensitivity reaction.

• QT prolongation: Androgen deprivation therapy may prolong the QT interval. Use with caution in patients with congenital long QT syndrome, known history of QT prolongation, or other risk factors for QT prolongation (eg, concomitant use of medications known to prolong QT interval, heart failure, and/or electrolyte abnormalities). Consider periodic electrolyte and ECG monitoring.

Disease-related concerns:

• Cardiovascular disease: Androgen-deprivation therapy may increase the risk for cardiovascular disease (Levine 2010).

• Diabetes: Androgen deprivation therapy may be associated with an increased risk for insulin resistance and diabetes (Keating 2006).

• Hepatic impairment: Degarelix exposure is decreased in patients with hepatic impairment, dosage adjustment is not recommended in patients with mild to moderate hepatic impairment, although testosterone levels should be monitored. Has not been studied in patients with severe hepatic impairment; use with caution. Mild transient increases in transaminases have been observed; monitor liver function in patients with known or suspected hepatic disorder.

• Renal impairment: Data for use in patients with moderate to severe renal impairment (CrCl <50 mL/minute) is limited; use with caution.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

For the Consumer

Applies to degarelix: subcutaneous powder for solution

Along with its needed effects, degarelix may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur while taking degarelix:

More common
  • Back pain
  • blurred vision
  • dizziness
  • fever
  • flushing or redness of the skin
  • hard lump
  • headache
  • nervousness
  • pain
  • pounding in the ears
  • slow or fast heartbeat
  • small lumps under the skin
  • swelling
  • unusually warm skin
Less common
  • Bladder pain
  • bloody or cloudy urine
  • chills
  • decrease in testicle size
  • decreased interest in sexual intercourse
  • difficult, burning, or painful urination
  • difficulty in moving
  • frequent urge to urinate
  • inability to have or keep an erection
  • increased sweating
  • loss in sexual ability, desire, drive, or performance
  • lower back or side pain
  • muscle pain or stiffness
  • pain in the joints
Rare
  • Chest pain or discomfort
  • fainting
  • irregular heartbeat
  • pounding heartbeat
  • shortness of breath

Some side effects of degarelix may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Difficulty having a bowel movement (stool)
  • feeling of warmth
  • increased weight
  • redness of the face, neck, arms, and occasionally, upper chest
  • sudden sweating
  • unusual tiredness or weakness
Less common
  • Diarrhea
  • lack or loss of strength
  • nausea
  • night sweats
  • sleeplessness
  • swelling of the breasts or breast soreness
  • trouble sleeping
  • unable to sleep

Liver Dose Adjustments

-Mild to Moderate Hepatic Impairment (Child-Pugh A and B): No adjustment recommended.
-Severe Hepatic Impairment (Child-Pugh C): Data not available; use with caution.

Degarelix Breastfeeding Warnings

There is no relevant use of this drug in women; use during breastfeeding is not recommended. Excreted into human milk: Unknown Excreted into animal milk: Data not available. Comments: The effects in the nursing infant are unknown.

Highlights for degarelix

Degarelix is used to treat advanced prostate cancer.

This drug comes as a solution that’s injected into your abdomen subcutaneously (under your skin). A healthcare provider will give you this drug. You won’t give yourself this drug at home.

Degarelix is only available as the brand-named drug Firmagon. It isn’t available as a generic drug.

The more common side effects of this drug can include pain, redness, and swelling at the injection site. They can also include hot flashes, weight gain, and liver problems.

In some cases, degarelix can cause serious side effects. These can include allergic reactions and heart problems. This drug can also harm a pregnancy if a woman takes it during pregnancy.

IMPORTANT INFORMATION
  • Allergic reactions See Details

  • Injection location See Details

  • QT prolongation See Details

  • Pregnancy See Details

What is Degarelix?

This drug is a prescription drug. It comes as a solution that’s injected into your abdomen subcutaneously (under your skin). A healthcare provider will give you this drug. You won’t give yourself this drug at home.

This drug is only available as the brand-named drug Firmagon. It isn’t available as a generic drug.

This drug may be used as part of a combination therapy. This means you may need to take it with other medications.

Why it's used

This drug is used to treat advanced prostate cancer.

How it works

This drug belongs to a class of drugs called GnRH receptor blockers.

See Details

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