Degarelix - Uses, Dosage, Side Effects, Interaction

Degarelix is a parenterally administered, gonadotropin-releasing hormone (GnRH) antagonist that effectively blocks androgen production and is used to treat advanced prostate cancer. Degarelix therapy is associated with serum enzyme elevations during therapy but has yet to be linked to instances of clinically apparent acute liver injury. Testosterone is a male hormone that promotes the growth of many prostate tumors and therefore reducing circulating testosterone to very low (castration) levels is often the treatment goal in the management of advanced prostate cancer. Degarelix has an immediate onset of action, binding to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocking their interaction with GnRH. This induces a fast and profound reduction in luteinizing hormone (LH), follicle-stimulating hormone (FSH), and in turn, testosterone suppression.^[rx]

Degarelix is 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.

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.

Mechanism of Action

Degarelix competitively inhibits GnRH receptors in the pituitary gland, preventing the release of luteinizing hormone (LH) and follicle-stimulating hormone. Reduced LH suppresses testosterone release, which slows growth and reduces the size of prostate cancers.

Degarelix is a selective gonadotrophin-releasing-hormone (GnRH) antagonist that competitively and reversibly binds to the pituitary GnRH receptors, thereby rapidly reducing the release of the gonadotrophins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), and thereby reducing the secretion of testosterone (T) by the testes. Prostatic carcinoma is known to be androgen-sensitive and responds to treatment that removes the source of androgen. Unlike GnRH agonists, GnRH antagonists do not induce an LH surge with subsequent testosterone surge/tumor stimulation and potential symptomatic flare after the initiation of treatment

Degarelix, a synthetic decapeptide, is a gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin) antagonist. The drug immediately, competitively, and reversibly binds to and blocks GnRH receptors in the pituitary, thereby reducing the release of gonadotropins (i.e., luteinizing hormone [LH], follicle-stimulating hormone [FSH]) and, consequently, testosterone without initial stimulation of the hypothalamic-pituitary-gonadal axis and the associated testosterone surge. Degarelix appears to have low histamine-releasing potential compared with other GnRH antagonists; there have been no signs of immediate- or late-onset systemic allergic reactions with degarelix. Degarelix is a synthetic derivative of GnRH decapeptide, the ligand of the GnRH receptor. Gonadotropin and androgen production result from the binding of endogenous GnRH to the GnRH receptor. Degarelix antagonizes the GnRH receptor which in turn blocks the release of LH and FSH from the pituitary. LF and FSH decrease in a concentration-dependent manner. The reduction in LH leads to a decrease in testosterone release from the testes.

Gonadotrophin-releasing hormone receptors, GnRH₁ and GnRH₂ receptors (provisional nomenclature, also called Type I and Type II GnRH receptor, respectively ) have been cloned from numerous species, most of which express two or three types of GnRH receptor. GnRH I (p-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2) is a hypothalamic decapeptide also known as luteinizing hormone-releasing hormone, gonadoliberin, luliberin, gonadorelin or simply as GnRH. It is a member of a family of similar peptides found in many species including GnRH II (pGlu-His-Trp-Ser-His-Gly-Trp-Tyr-Pro-Gly-NH₂ (which is also known as chicken GnRH-II). Receptors for three forms of GnRH exist in some species but only GnRH I and GnRH II and their cognate receptors have been found in mammals. GnRH₁ receptors are expressed by pituitary gonadotrophs, where they mediate the effects of GnRH on gonadotropin hormone synthesis and secretion that underpin central control of mammalian reproduction. GnRH analogs are used in assisted reproduction and to treat steroid hormone-dependent conditions. Notably, agonists cause desensitization of GnRH-stimulated gonadotropin secretion, and the consequent reduction in circulating sex steroids is exploited to treat hormone-dependent cancers of the breast, ovary, and prostate. GnRH₁ receptors are selectively activated by GnRH I and all lack the COOH-terminal tails found in other GPCRs. GnRH₂ receptors do have COOH-terminal tails and (where tested) are selective for GnRH II over GnRH I. GnRH₂ receptors are expressed by some primates but not by humans. Phylogenetic classifications divide GnRH receptors into three or five groups and highlight examples of gene loss through evolution, with humans retaining only one ancient gene. The structure of the GnRH₁ receptor in complex with elagolix has been elucidated.

Indications

Degarelix is used for the management of advanced prostate cancer.
FIRMAGON is a gonadotrophin-releasing hormone (GnRH) antagonist indicated for the treatment of adult male patients with advanced hormone-dependent prostate cancer for treatment of high-risk localized and locally advanced hormone-dependent prostate cancer in combination with radiotherapy as a neo-adjuvant treatment prior to radiotherapy in patients with high-risk localized or locally advanced hormone dependent prostate cancer.
Degarelix is a parenterally administered, gonadotropin-releasing hormone (GnRH) antagonist that effectively blocks androgen production and is used to treat advanced prostate cancer.
Intended to treat patients with advanced prostate cancer … slows the growth and progression of prostate cancer by suppressing testosterone

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
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

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
fast or pounding heartbeats, fluttering in your chest;
shortness of breath;
sudden dizziness (like you might pass out); or
severe 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

Acrivastine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Acrivastine.
Adenosine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Adenosine.
Ajmaline	The risk or severity of QTc prolongation can be increased when Ajmaline is combined with Degarelix.
Alfuzosin	The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Degarelix.
Alimemazine	The risk or severity of QTc prolongation can be increased when Alimemazine is combined with Degarelix.
Amantadine	The risk or severity of QTc prolongation can be increased when Amantadine is combined with Degarelix.
Amifampridine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Amifampridine.
Amiodarone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Amiodarone.
Amisulpride	The risk or severity of QTc prolongation can be increased when Amisulpride is combined with Degarelix.
Amitriptyline	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Amitriptyline.
Amodiaquine	The risk or severity of QTc prolongation can be increased when Amodiaquine is combined with Degarelix.
Amoxapine	The risk or severity of QTc prolongation can be increased when Amoxapine is combined with Degarelix.
Anagrelide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Anagrelide.
Antazoline	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Antazoline.
Apomorphine	The risk or severity of QTc prolongation can be increased when Apomorphine is combined with Degarelix.
Arformoterol	The risk or severity of QTc prolongation can be increased when Arformoterol is combined with Degarelix.
Aripiprazole	The risk or severity of QTc prolongation can be increased when Aripiprazole is combined with Degarelix.
Aripiprazole lauroxil	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Aripiprazole lauroxil.
Arsenic trioxide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Arsenic trioxide.
Artemether	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Artemether.
Articaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Articaine.
Asenapine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Asenapine.
Astemizole	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Astemizole.
Atazanavir	The risk or severity of QTc prolongation can be increased when Atazanavir is combined with Degarelix.
Atomoxetine	The risk or severity of QTc prolongation can be increased when Atomoxetine is combined with Degarelix.
Atropine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Atropine.
Azatadine	The risk or severity of QTc prolongation can be increased when Azatadine is combined with Degarelix.
Azithromycin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Azithromycin.
Bedaquiline	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Bedaquiline.
Benzatropine	The risk or severity of QTc prolongation can be increased when Benzatropine is combined with Degarelix.
Benzocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Benzocaine.
Benzyl alcohol	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Benzyl alcohol.
Bepridil	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Bepridil.
Berotralstat	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Berotralstat.
Bilastine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Bilastine.
Bortezomib	The risk or severity of QTc prolongation can be increased when Bortezomib is combined with Degarelix.
Bretylium	The risk or severity of QTc prolongation can be increased when Bretylium is combined with Degarelix.
Brompheniramine	The risk or severity of QTc prolongation can be increased when Brompheniramine is combined with Degarelix.
Buclizine	The risk or severity of QTc prolongation can be increased when Buclizine is combined with Degarelix.
Bupivacaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Bupivacaine.
Buserelin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Buserelin.
Butacaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Butacaine.
Butamben	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Butamben.
Butriptyline	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Butriptyline.
Capsaicin	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Capsaicin.
Carbinoxamine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Carbinoxamine.
Celiprolol	The risk or severity of QTc prolongation can be increased when Celiprolol is combined with Degarelix.
Ceritinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ceritinib.
Cetirizine	The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Degarelix.
Chlorcyclizine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Chlorcyclizine.
Chloroprocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Chloroprocaine.
Chloroquine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Chloroquine.
Chlorpheniramine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Chlorpheniramine.
Chlorpromazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Chlorpromazine.
Chlorprothixene	The risk or severity of QTc prolongation can be increased when Chlorprothixene is combined with Degarelix.
Cilostazol	The risk or severity of QTc prolongation can be increased when Cilostazol is combined with Degarelix.
Cinchocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Cinchocaine.
Cinnarizine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Cinnarizine.
Cinoxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Cinoxacin.
Ciprofloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ciprofloxacin.
Cisapride	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Cisapride.
Citalopram	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Citalopram.
Clarithromycin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Clarithromycin.
Clemastine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Clemastine.
Clofazimine	The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Degarelix.
Clomipramine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Clomipramine.
Clozapine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Clozapine.
Cocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Cocaine.
Crizotinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Crizotinib.
Cyclizine	The risk or severity of QTc prolongation can be increased when Cyclizine is combined with Degarelix.
Cyproheptadine	The risk or severity of QTc prolongation can be increased when Cyproheptadine is combined with Degarelix.
Dabrafenib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dabrafenib.
Darbepoetin alfa	The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Degarelix.
Dasatinib	The risk or severity of QTc prolongation can be increased when Dasatinib is combined with Degarelix.
Delafloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Delafloxacin.
Delamanid	Degarelix may increase the QTc-prolonging activities of Delamanid.
Desflurane	The risk or severity of QTc prolongation can be increased when Desflurane is combined with Degarelix.
Desipramine	The risk or severity of QTc prolongation can be increased when Desipramine is combined with Degarelix.
Desloratadine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Desloratadine.
Deutetrabenazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Deutetrabenazine.
Dexbromphenirami	The risk or severity of QTc prolongation can be increased when Dexbrompheniramine is combined with Degarelix.
Dexchlorphenirami	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dexchlorpheniramine maleate.
Digitoxin	The risk or severity of QTc prolongation can be increased when Digitoxin is combined with Degarelix.
Digoxin	The risk or severity of QTc prolongation can be increased when Digoxin is combined with Degarelix.
Diltiazem	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Diltiazem.
Dimenhydrinate	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dimenhydrinate.
Diphenhydramine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Diphenhydramine.
Disopyramide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Disopyramide.
Disulfiram	The risk or severity of QTc prolongation can be increased when Disulfiram is combined with Degarelix.
Dofetilide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dofetilide.
Dolasetron	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dolasetron.
Domperidone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Domperidone.
Dosulepin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dosulepin.
Doxepin	The risk or severity of QTc prolongation can be increased when Doxepin is combined with Degarelix.
Doxylamine	The risk or severity of QTc prolongation can be increased when Doxylamine is combined with Degarelix.
Dronedarone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Dronedarone.
Droperidol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Droperidol.
Dyclonine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Dyclonine.
Ebastine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ebastine.
Efavirenz	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Efavirenz.

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Eliglustat	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Eliglustat.
Emedastine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Emedastine.
Encainide	The risk or severity of QTc prolongation can be increased when Encainide is combined with Degarelix.
Encorafenib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Encorafenib.
Enoxacin	The risk or severity of QTc prolongation can be increased when Enoxacin is combined with Degarelix.
Entrectinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Entrectinib.
Epinastine	The risk or severity of QTc prolongation can be increased when Epinastine is combined with Degarelix.
Eribulin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Eribulin.
Erlotinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Erlotinib.
Erythromycin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Erythromycin.
Erythropoietin	The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Degarelix.
Escitalopram	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Escitalopram.
Esmolol	The risk or severity of QTc prolongation can be increased when Esmolol is combined with Degarelix.
Ethosuximide	The risk or severity of QTc prolongation can be increased when Ethosuximide is combined with Degarelix.
Ethyl chloride	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Ethyl chloride.
Etidocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Etidocaine.
Ezogabine	The risk or severity of QTc prolongation can be increased when Ezogabine is combined with Degarelix.
Famotidine	The risk or severity of QTc prolongation can be increased when Famotidine is combined with Degarelix.
Felbamate	The risk or severity of QTc prolongation can be increased when Felbamate is combined with Degarelix.
Felodipine	The risk or severity of QTc prolongation can be increased when Felodipine is combined with Degarelix.
Fexinidazole	The risk or severity of adverse effects can be increased when Degarelix is combined with Fexinidazole.
Flecainide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Flecainide.
Fluconazole	The risk or severity of QTc prolongation can be increased when Fluconazole is combined with Degarelix.
Fluorouracil	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Fluorouracil.
Fluoxetine	The risk or severity of QTc prolongation can be increased when Fluoxetine is combined with Degarelix.
Flupentixol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Flupentixol.
Fluspirilene	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Fluspirilene.
Formoterol	The risk or severity of QTc prolongation can be increased when Formoterol is combined with Degarelix.
Foscarnet	The risk or severity of QTc prolongation can be increased when Foscarnet is combined with Degarelix.
Fostemsavir	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Fostemsavir.
Gadobenic acid	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Gadobenic acid.
Galantamine	The risk or severity of QTc prolongation can be increased when Galantamine is combined with Degarelix.
Gatifloxacin	The risk or severity of QTc prolongation can be increased when Gatifloxacin is combined with Degarelix.
Gemifloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Gemifloxacin.
Gilteritinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Gilteritinib.
Glasdegib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Glasdegib.
Goserelin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Goserelin.
Granisetron	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Granisetron.
Grepafloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Grepafloxacin.
Halofantrine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Halofantrine.
Haloperidol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Haloperidol.
Histrelin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Histrelin.
Hydrochlorothia	The risk or severity of QTc prolongation can be increased when Hydrochlorothiazide is combined with Degarelix.
Hydroxychloroq	The risk or severity of QTc prolongation can be increased when Hydroxychloroquine is combined with Degarelix.
Hydroxyzine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Hydroxyzine.
Hyoscyamine	The risk or severity of QTc prolongation can be increased when Hyoscyamine is combined with Degarelix.
Ibandronate	The risk or severity of QTc prolongation can be increased when Ibandronate is combined with Degarelix.
Ibutilide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ibutilide.
Iloperidone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Iloperidone.
Imatinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Imatinib.
Imipramine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Imipramine.
Indacaterol	The risk or severity of QTc prolongation can be increased when Indacaterol is combined with Degarelix.
Indapamide	The risk or severity of QTc prolongation can be increased when Indapamide is combined with Degarelix.
Inotersen	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Inotersen.
Isoflurane	The risk or severity of QTc prolongation can be increased when Isoflurane is combined with Degarelix.
Isradipine	The risk or severity of QTc prolongation can be increased when Isradipine is combined with Degarelix.
Itraconazole	The risk or severity of QTc prolongation can be increased when Itraconazole is combined with Degarelix.
Ivabradine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ivabradine.
Ivosidenib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ivosidenib.
Ketoconazole	The risk or severity of QTc prolongation can be increased when Ketoconazole is combined with Degarelix.
Lacidipine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lacidipine.
Lamotrigine	The risk or severity of QTc prolongation can be increased when Lamotrigine is combined with Degarelix.
Lapatinib	The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Degarelix.
Lefamulin	Lefamulin may increase the QTc-prolonging activities of Degarelix.
Lenvatinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lenvatinib.
Leuprolide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Leuprolide.
Levacetylmethadol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Levacetylmethadol.
Levobupivacaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Levobupivacaine.
Levocabastine	The risk or severity of QTc prolongation can be increased when Levocabastine is combined with Degarelix.
Levocetirizine	The risk or severity of QTc prolongation can be increased when Levocetirizine is combined with Degarelix.
Levofloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Levofloxacin.
Levomenthol	The risk or severity of QTc prolongation can be increased when Levomenthol is combined with Degarelix.
Levosimendan	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Levosimendan.
Lidocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Lidocaine.
Lidoflazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lidoflazine.
Lofexidine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lofexidine.
Lomefloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lomefloxacin.
Loperamide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Loperamide.
Lopinavir	The risk or severity of QTc prolongation can be increased when Lopinavir is combined with Degarelix.
Losartan	The risk or severity of QTc prolongation can be increased when Losartan is combined with Degarelix.
Lumefantrine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lumefantrine.
Lurasidone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Lurasidone.
Macimorelin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Macimorelin.
Maprotiline	The risk or severity of QTc prolongation can be increased when Maprotiline is combined with Degarelix.
Mefloquine	The risk or severity of QTc prolongation can be increased when Mefloquine is combined with Degarelix.
Meloxicam	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Meloxicam.
Mepivacaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Mepivacaine.
Mepyramine	The risk or severity of QTc prolongation can be increased when Mepyramine is combined with Degarelix.
Mesoridazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mesoridazine.
Methadone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Methadone.
Methotrimeprazine	The risk or severity of QTc prolongation can be increased when Methotrimeprazine is combined with Degarelix.
Methoxy	The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Degarelix.
Methsuximide	The risk or severity of QTc prolongation can be increased when Methsuximide is combined with Degarelix.
Metoclopramide	The risk or severity of QTc prolongation can be increased when Metoclopramide is combined with Degarelix.
Metronidazole	The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Degarelix.
Mifepristone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mifepristone.
Mirabegron	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mirabegron.
Mirtazapine	The risk or severity of QTc prolongation can be increased when Mirtazapine is combined with Degarelix.
Mizolastine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mizolastine.
Mobocertinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Mobocertinib.

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Moexipril	The risk or severity of QTc prolongation can be increased when Moexipril is combined with Degarelix.
Moricizine	The risk or severity of QTc prolongation can be increased when Moricizine is combined with Degarelix.
Moxifloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Moxifloxacin.
Nalidixic acid	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nalidixic acid.
Nelfinavir	The risk or severity of QTc prolongation can be increased when Nelfinavir is combined with Degarelix.
Nicardipine	The risk or severity of QTc prolongation can be increased when Nicardipine is combined with Degarelix.
Nifedipine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nifedipine.
Nilotinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nilotinib.
Nilvadipine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nilvadipine.
Nimodipine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Nimodipine.
Nitrendipine	The risk or severity of QTc prolongation can be increased when Nitrendipine is combined with Degarelix.
Norfloxacin	The risk or severity of QTc prolongation can be increased when Norfloxacin is combined with Degarelix.
Nortriptyline	The risk or severity of QTc prolongation can be increased when Nortriptyline is combined with Degarelix.
Octreotide	The risk or severity of QTc prolongation can be increased when Octreotide is combined with Degarelix.
Ofloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ofloxacin.
Olanzapine	The risk or severity of QTc prolongation can be increased when Olanzapine is combined with Degarelix.
Olodaterol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Olodaterol.
Ondansetron	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ondansetron.
Orphenadrine	The risk or severity of QTc prolongation can be increased when Orphenadrine is combined with Degarelix.
Oxaliplatin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Oxaliplatin.
Oxatomide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Oxatomide.
Oxetacaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Oxetacaine.
Oxybuprocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Oxybuprocaine.
Oxytocin	The risk or severity of QTc prolongation can be increased when Oxytocin is combined with Degarelix.
Pacritinib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pacritinib.
Paliperidone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Paliperidone.
Panobinostat	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Panobinostat.
Papaverine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Papaverine.
Pasireotide	The risk or severity of QTc prolongation can be increased when Pasireotide is combined with Degarelix.
Pazopanib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pazopanib.
Pefloxacin	The risk or severity of QTc prolongation can be increased when Pefloxacin is combined with Degarelix.
Peginesatide	The risk or severity of Thrombosis can be increased when Peginesatide is combined with Degarelix.
Pentamidine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pentamidine.
Perflutren	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Perflutren.
Perhexiline	The risk or severity of QTc prolongation can be increased when Perhexiline is combined with Degarelix.
Pheniramine	The risk or severity of QTc prolongation can be increased when Pheniramine is combined with Degarelix.
Phenol	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Phenol.
Pimozide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pimozide.
Pinaverium	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Pinaverium.
Pitolisant	Degarelix may increase the QTc-prolonging activities of Pitolisant.
Ponesimod	The risk or severity of bradycardia can be increased when Ponesimod is combined with Degarelix.
Posaconazole	The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Degarelix.
Pramocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Pramocaine.
Pregabalin	The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Degarelix.
Prenylamine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Prenylamine.
Prilocaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Prilocaine.
Primaquine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Primaquine.
Probucol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Probucol.
Procainamide	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Procainamide.
Procaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Procaine.
Prochlorperazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Prochlorperazine.
Promazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Promazine.
Promethazine	The risk or severity of QTc prolongation can be increased when Promethazine is combined with Degarelix.
Propafenone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Propafenone.
Proparacaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Proparacaine.
Propofol	The risk or severity of QTc prolongation can be increased when Propofol is combined with Degarelix.
Propoxycaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Propoxycaine.
Protriptyline	The risk or severity of QTc prolongation can be increased when Protriptyline is combined with Degarelix.
Quetiapine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Quetiapine.
Quinidine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Quinidine.
Quinine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Quinine.
Ranolazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ranolazine.
Relugolix	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Relugolix.
Ribociclib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ribociclib.
Rilpivirine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Rilpivirine.
Risperidone	The risk or severity of QTc prolongation can be increased when Risperidone is combined with Degarelix.
Ritonavir	The risk or severity of QTc prolongation can be increased when Ritonavir is combined with Degarelix.
Romidepsin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Romidepsin.
Ropivacaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Ropivacaine.
Rosoxacin	The risk or severity of QTc prolongation can be increased when Rosoxacin is combined with Degarelix.
Roxithromycin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Roxithromycin.
Rupatadine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Rupatadine.
Salbutamol	The risk or severity of QTc prolongation can be increased when Salbutamol is combined with Degarelix.
Salmeterol	The risk or severity of QTc prolongation can be increased when Salmeterol is combined with Degarelix.
Saquinavir	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Saquinavir.
Sevoflurane	The risk or severity of QTc prolongation can be increased when Sevoflurane is combined with Degarelix.
Solifenacin	The risk or severity of QTc prolongation can be increased when Solifenacin is combined with Degarelix.
Sorafenib	The risk or severity of QTc prolongation can be increased when Sorafenib is combined with Degarelix.
Sotalol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sotalol.
Sparfloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sparfloxacin.
Sulfamethoxazole	The risk or severity of QTc prolongation can be increased when Sulfamethoxazole is combined with Degarelix.
Sulfisoxazole	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sulfisoxazole.
Sulpiride	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sulpiride.
Sultopride	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Sultopride.
Sunitinib	The risk or severity of QTc prolongation can be increased when Sunitinib is combined with Degarelix.
Tacrolimus	The risk or severity of QTc prolongation can be increased when Tacrolimus is combined with Degarelix.
Tamoxifen	The risk or severity of QTc prolongation can be increased when Tamoxifen is combined with Degarelix.
Telavancin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Telavancin.
Telithromycin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Telithromycin.
Terbutaline	The risk or severity of QTc prolongation can be increased when Terbutaline is combined with Degarelix.
Terfenadine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Terfenadine.
Terlipressin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Terlipressin.
Tetrabenazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Tetrabenazine.
Tetracaine	The risk or severity of methemoglobinemia can be increased when Degarelix is combined with Tetracaine.
Thioridazine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Thioridazine.
Thiothixene	The risk or severity of QTc prolongation can be increased when Thiothixene is combined with Degarelix.
Timolol	The risk or severity of QTc prolongation can be increased when Timolol is combined with Degarelix.
Tizanidine	The risk or severity of QTc prolongation can be increased when Tizanidine is combined with Degarelix.
Tolterodine	The risk or severity of QTc prolongation can be increased when Tolterodine is combined with Degarelix.
Toremifene	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Toremifene.

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Trazodone	The risk or severity of QTc prolongation can be increased when Trazodone is combined with Degarelix.
Treprostinil	The risk or severity of QTc prolongation can be increased when Treprostinil is combined with Degarelix.
Triclabendazole	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Triclabendazole.
Trimebutine	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Trimebutine.
Trimethadione	The risk or severity of QTc prolongation can be increased when Trimethadione is combined with Degarelix.
Trimipramine	The risk or severity of QTc prolongation can be increased when Trimipramine is combined with Degarelix.
Triprolidine	The risk or severity of QTc prolongation can be increased when Triprolidine is combined with Degarelix.
Triptorelin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Triptorelin.
Trovafloxacin	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Trovafloxacin.
Valproic acid	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Valproic acid.
Vandetanib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Vandetanib.
Vardenafil	The risk or severity of QTc prolongation can be increased when Vardenafil is combined with Degarelix.
Vemurafenib	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Vemurafenib.
Vernakalant	The risk or severity of QTc prolongation can be increased when Vernakalant is combined with Degarelix.
Vilanterol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Vilanterol.
Voriconazole	The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Degarelix.
Vorinostat	The risk or severity of QTc prolongation can be increased when Vorinostat is combined with Degarelix.
Ziprasidone	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Ziprasidone.
Zonisamide	The risk or severity of QTc prolongation can be increased when Zonisamide is combined with Degarelix.
Zuclopenthixol	The risk or severity of QTc prolongation can be increased when Degarelix is combined with Zuclopenthixol.

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.

How should this medicine be used?

Degarelix injection comes as a powder to be mixed with liquid and injected under the skin in the stomach area, away from the ribs and waistline. It is usually injected once every 28 days by a doctor or nurse in a medical facility.

After you receive a dose of degarelix injection, be sure that your belt or waistband does not put pressure on the place where the medication was injected.

Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient.

Other uses for this medicine

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

What special precautions should I follow?

Before receiving degarelix injection,

tell your doctor and pharmacist if you are allergic to degarelix injection, any other medications, or any of the ingredients in degarelix injection. Ask your pharmacist or check the patient’s information for a list of the ingredients.
tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: amiodarone (Cordarone), disopyramide (Norpace), quinidine, procainamide, or sotalol (Betapace). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
tell your doctor if you have or have ever had long QT syndrome (a rare heart problem that may cause irregular heartbeat, fainting, or sudden death); high or low levels of calcium, potassium, magnesium, or sodium in your blood; or heart, liver, or kidney disease.
women who are or who may become pregnant should not receive degarelix injections. Degarelix injection may harm the fetus. If you receive degarelix injection while you are pregnant, call your doctor immediately. If you are breastfeeding, talk to your doctor before you receive degarelix injection.

References

Degarelix – Uses, Dosage, Side Effects, Interaction

Mechanism of Action