Degarelix – Uses, Dosage, Side Effects, Interaction

Degarelix Acetate is the acetate form of a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing the secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes.

Use in Cancer

Degarelix is approved to treat:

• Prostate cancer is advanced.

Contraindications

• low amount of magnesium in the blood
• low amount of potassium in the blood
• prolonged QT interval on EKG
• chronic? heart failure
• abnormal EKG with QT changes from birth
• liver problems
• decreased calcification or density of bone
• pregnancy

Dosage?

Strengths: 80 mg; 120 mg

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.
• Administer the first maintenance dose 28 days after the initial dose.

Renal? Dose Adjustments

• Mild Renal? Impairment (CrCl 50 to 80 mL/min): No adjustment recommended.
• Moderate to Severe Renal? Impairment (CrCl less than 50 mL/min): Use with caution.

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.

Administration Advice:

• Administer this drug in the abdominal region only.
• Vary the injection site periodically to minimize patient discomfort, and administer in abdomen areas not exposed to pressure (e.g., not close to the waistband or belt, not close to the ribs).
• Perform a slow, deep subcutaneous injection over 30 seconds.
• This drug is for subcutaneous injection only; do not administer intravenously or intramuscularly.
• Use this drug only as a first-line androgen deprivation therapy; there is no data available on the use of this drug in patients who have failed treatment with GnRH agonists (e.g., leuprorelin, goserelin).
• Confirm serum testosterone levels are remaining sufficiently suppressed if a patient’s clinical response appears to be sub-optimal.

Side Effects

The Most Common

• pain?, redness, swelling?, hardness, or itching in the place where the medication was injected
• hot flashes
• excessive sweating or night sweats
• nausea?
• constipation?
• diarrhea?
• weight gain or loss
• weakness?
• dizziness
• pain? in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache?
• tiredness
• difficulty falling asleep or staying asleep
• enlargement of the breasts
• decreased sexual desire or ability
• back or joint pain?
• hives
• rash?
• difficulty breathing or swallowing
• rapid, irregular, or pounding heartbeat
• swelling? of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• hoarseness
• fluttering feeling in the chest
• fainting
• painful, frequent, or difficult urination
• fever? or chills

More common

• pain?: Back pain means pain in the spine, muscles, discs, joints, or nerves of the back. সহজ বাংলা: পিঠ/কোমরের ব্যথা।" data-rx-term="back pain" data-rx-definition="Back pain means pain in the spine, muscles, discs, joints, or nerves of the back. সহজ বাংলা: পিঠ/কোমরের ব্যথা।">Back pain?
• blurred vision
• dizziness
• fever?
• flushing or redness of the skin
• hard lump
• pain? in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache?
• nervousness
• pain?
• pounding in the ears
• slow or fast heartbeat
• small lumps under the skin
• swelling?
• unusually warm skin
• fast or pounding heartbeats, fluttering in your chest;
• shortness of breath;
• sudden dizziness (like you might pass out); or
• severe pain? in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache?, blurred vision, and pounding in your neck or ears.
• hot flashes;
• abnormal liver function tests; or
• pain?, swelling?, redness, itching, or a hard lump where the medicine was injected.
• weight gain;

Rare

• 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
• Chest pain or discomfort
• fainting
• irregular heartbeat
• pounding heartbeat
• Cough
• difficulty swallowing
• hives, itching, or skin rash
• puffiness or swelling of the eyelids or around the eyes, face, lips or tongue
• tightness in the chest
• trouble breathing
• unusual tiredness or weakness

Drug Interaction

Pregnancy and Lactation

FDA Pregnancy Risk Category: X 

AU TGA pregnancy category D

Pregnancy

There are no controlled data on human pregnancy. Drugs that have caused, are suspected to have caused, or may be expected to cause, an increased incidence of human fetal malformations or irreversible damage. These drugs may also have adverse pharmacological effects. Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in the use of the drug in pregnant women clearly outweigh the potential benefits.

Lactation

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

References