Firmagon

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Firmagon

Classes

Cytostatic Gonadotropin-Releasing Hormone Antagonists
Gonadotropin Releasing Hormone Receptor Antagonist

Administration

For storage information, see the specific product information within How Supplied section.
Hazardous Drugs Classification
NIOSH 2016 List: Group 1
NIOSH (Draft) 2020 List: Table 2
Observe and exercise appropriate precautions for handling, preparation, administration, and disposal of hazardous drugs.
Use double chemotherapy gloves and a protective gown. Prepare in a biological safety cabinet or compounding aseptic containment isolator with a closed system drug transfer device. Eye/face and respiratory protection may be needed during preparation and administration.

Injectable Administration Subcutaneous Administration

For subcutaneous injection in the abdominal region only. Do NOT administer intravenously.
Degarelix should only be administered by a healthcare professional.
 
General reconstitution information:
Gloves should be worn during preparation and administration; aseptic technique should be followed.
Keep vials vertical at all times; do NOT shake the vials.
Administer reconstituted drug within 1 hour (60 minutes) after addition of sterile water for injection (SWI).
 
Reconstitution of 120 mg vial (240 mg dose ONLY):
 
NOTE: To achieve a 240 mg dose, two 120 mg vials of degarelix must be used. Therefore, the following instructions will need to be repeated for each 120 mg vial.
Peel off the seal from the vial adaptor cover; do not touch the vial adaptor.
Press the vial adapter to the vial until the spike punctures the rubber stopper and the adaptor snaps into place. Pull the vial adaptor cover off the vial.
Attach the plunger to the prefilled 3 mL syringe of Sterile Water for Injection (SWI). Do not pull the back stopper (flange) off the syringe. You will only feel light resistance screwing the plunger rod in position.
Unscrew the gray syringe plug attached to the Luer lock adaptor on the syringe; do not pull off the Luer lock adaptor.
Attach the prefilled syringe with SWI onto the vial adaptor; be careful not to over-twist the syringe.
Inject the entire volume of SWI from the prefilled syringe slowly into a vial containing 120 mg of degarelix. In order to maintain sterility, do not remove the syringe from the vial.
Keep the vial in an upright position and swirl gently until the liquid looks clear and without undissolved powder. Avoid shaking to prevent foam formation. The vial can be tilted slightly to dissolve powder. The reconstitution process may take up to 15 minutes, but usually takes a few minutes.
Turn the vial upside down and withdraw 3 ml (40 mg/mL); remove any air bubbles.
Remove the syringe from the vial adapter and attach the needle provided in the kit.
Repeat the constitution procedure with a new vial, needle, and syringe for the second 120 mg dose (total dose = 240 mg)
 
Reconstitution of 80 mg vial:
Peel off the seal from the vial adaptor cover; do not touch the vial adaptor.
Press the vial adapter to the vial until the spike punctures the rubber stopper and the adaptor snaps into place. Pull the vial adaptor cover off the vial.
Attach the plunger to the prefilled 4.2 mL syringe of Sterile Water for Injection (SWI). Do not pull the back stopper (flange) off the syringe. You will only feel light resistance screwing the plunger rod in position.
Unscrew the gray syringe plug attached to the Luer lock adaptor on the syringe; do not pull off the Luer lock adaptor.
Attach the prefilled syringe with SWI onto the vial adaptor; be careful not to over-twist the syringe.
Inject the entire volume of SWI from the prefilled syringe slowly into vial containing 80 mg of degarelix. In order to maintain sterility, do not remove the syringe from the vial.
Keep the vial in an upright position and swirl gently until the liquid looks clear and without undissolved powder. Avoid shaking to prevent foam formation. The vial can be tilted slightly to dissolve powder. The reconstitution process may take up to 15 minutes, but usually takes a few minutes.
Turn the vial upside down and withdraw 4 ml (20 mg/mL); remove any air bubbles
Remove the syringe from the vial adapter and attach the needle provided in the kit.
 
Subcutaneous injection:
Degarelix is administered in the abdominal region in an area not exposed to pressure (e.g. not close to belt area, waistband, close to ribs); injection site should vary.
Disinfect the area to be injected with an alcohol pad.
Move the needle shield away from the needle and carefully remove the needle cover.
Grasp the skin of abdomen, elevate the subcutaneous tissue, and insert the needle deeply at a 45 degree angle, all the way to the needle hub.
Aspirate prior to injection to ensure a blood vessel has not been penetrated. If blood appears in the syringe, discontinue the procedure and discard the syringe and the needle. The reconstituted product can no longer be used and a new dose must be prepared.
Slowly inject the dose subcutaneously over 30 seconds. When giving the loading dose, which consists of two 120 mg doses, the second dose should be injected subcutaneously at a different site in the abdomen.
Remove the needle, and then release the skin. Do not rub the injection site after removing the needle.
To lock the needle into the shield, position the needle shield about 45 degrees to a flat surface. Press down with a firm, quick motion until a click is heard, and confirm that the needle is fully engaged under the lock.

Adverse Reactions
Severe

injection site reaction / Rapid / 0-2.0
elevated hepatic enzymes / Delayed / 0-1.0
anaphylactoid reactions / Rapid / Incidence not known
angioedema / Rapid / Incidence not known

Moderate

hot flashes / Early / 26.0-26.0
erythema / Early / 17.0-17.0
hypertension / Early / 6.0-6.0
constipation / Delayed / 5.0-5.0
QT prolongation / Rapid / 0-1.0
testicular atrophy / Delayed / 1.0
impotence (erectile dysfunction) / Delayed / 1.0
osteopenia / Delayed / Incidence not known
osteoporosis / Delayed / Incidence not known

Mild

weight gain / Delayed / 9.0-9.0
back pain / Delayed / 6.0-6.0
chills / Rapid / 5.0-5.0
fever / Early / 1.0-5.0
infection / Delayed / 5.0-5.0
arthralgia / Delayed / 5.0-5.0
fatigue / Early / 1.0-5.0
asthenia / Delayed / 1.0-5.0
dizziness / Early / 1.0-5.0
headache / Early / 1.0-5.0
night sweats / Early / 1.0-5.0
nausea / Early / 1.0-5.0
insomnia / Early / 1.0-5.0
gynecomastia / Delayed / 1.0
diarrhea / Early / 1.0
hyperhidrosis / Delayed / 1.0
urticaria / Rapid / Incidence not known

Common Brand Names

Firmagon

Dea Class

Rx

Description

Gonadotropin-releasing hormone (GnRH) receptor antagonist
Used for the treatment of advanced prostate cancer
Coadministration of certain drugs may need to be avoided due to the risk of QT prolongation; review drug interactions

Dosage And Indications
For the treatment of advanced prostate cancer. Subcutaneous dosage Adults

240 mg subcutaneously (given as 2 separate subcutaneous injections of 120 mg); 28 days later, begin maintenance therapy with degarelix 80 mg subcutaneously every 28 days. Coadministration of certain drugs may need to be avoided; review drug interactions. Treatment with degarelix resulted in testosterone suppression to castration levels (less than 50 ng/dL) in 97.2% of patients with advanced prostate cancer compared with 96.4% of those who received leuprolide in a randomized, open-label clinical trial; castration levels were reached more quickly in the degarelix arm as well, with 99% achieving testosterone levels of 50 ng/dL or less by day 7 compared to 1% in the leuprolide arm.

Dosing Considerations
Hepatic Impairment

Specific guidelines for dosage adjustment in patients with hepatic impairment are not available; it appears that dosage adjustments are not necessary.

Renal Impairment

Specific guidelines for dosage adjustment in patients with renal impairment are not available; it appears that dosage adjustments are not necessary.

Drug Interactions

Adagrasib: (Major) Concomitant use of adagrasib and androgen deprivation therapy (i.e., degarelix) increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Alfuzosin: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving alfuzosin as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Alfuzosin may prolong the QT interval in a dose-dependent manner.
Amiodarone: (Major) If possible, avoid coadministration of amiodarone with degarelix due to the risk of QT prolongation. Amiodarone, a Class III antiarrhythmic agent, is associated with a well-established risk of QT prolongation and torsades de pointes (TdP). Although the frequency of TdP is less with amiodarone than with other Class III agents, amiodarone is still associated with a risk of TdP. Due to the extremely long half-life of amiodarone, a drug interaction is possible for days to weeks after discontinuation of amiodarone. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Amisulpride: (Major) Monitor ECGs for QT prolongation when amisulpride is administered with degarelix. Amisulpride causes dose- and concentration- dependent QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Amoxicillin; Clarithromycin; Omeprazole: (Major) Avoid coadministration of clarithromycin with degarelix. Clarithromycin is associated with an established risk for QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Anagrelide: (Major) Do not use anagrelide with degarelix due to the risk of QT prolongation. Torsade de pointes (TdP) and ventricular tachycardia have been reported with anagrelide. In addition, dose-related increases in mean QTc and heart rate were observed in healthy subjects. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Androgens: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Apomorphine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving apomorphine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Dose-related QTc prolongation is associated with therapeutic apomorphine exposure.
Aripiprazole: (Moderate) Concomitant use of aripiprazole and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Arsenic Trioxide: (Major) Avoid concomitant use of arsenic trioxide and degarelix due to the potential for additive QT prolongation; discontinue or select an alternative drug that does not prolong the QT interval prior to starting arsenic trioxide therapy. If concomitant drug use is unavoidable, frequently monitor electrocardiograms. Torsade de pointes (TdP), QT interval prolongation, and complete atrioventricular block have been reported with arsenic trioxide use. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Artemether; Lumefantrine: (Major) Avoid coadministration of artemether; lumefantrine with degarelix due to the potential for additive QT prolongation. Consider ECG monitoring if degarelix must be used with or after artemether; lumefantrine treatment. Artemether; lumefantrine is associated with prolongation of the QT interval. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Asenapine: (Major) Avoid using asenapine in combination with degarelix due to the potential for QT prolongation; coadministration may also reduce the efficacy of degarelix. Asenapine has been associated with QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval. Asenapine can also cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Atomoxetine: (Moderate) Concomitant use of atomoxetine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Azithromycin: (Major) Avoid coadministration of azithromycin with degarelix due to the increased risk of QT prolongation. If use together is necessary, obtain an ECG at baseline to assess initial QT interval and determine frequency of subsequent ECG monitoring, avoid any non-essential QT prolonging drugs, and correct electrolyte imbalances. QT prolongation and torsade de pointes (TdP) have been spontaneously reported during azithromycin postmarketing surveillance. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Bedaquiline: (Major) Monitor ECGs if bedaquiline is coadministered with degarelix. Discontinue bedaquiline if evidence of serious ventricular arrhythmia or QTcF interval greater than 500 ms. Bedaquiline prolongs the QT interval and androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Bismuth Subcitrate Potassium; Metronidazole; Tetracycline: (Moderate) Concomitant use of metronidazole and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Bismuth Subsalicylate; Metronidazole; Tetracycline: (Moderate) Concomitant use of metronidazole and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Brexpiprazole: (Major) Avoid coadministration of degarelix with brexpiprazole due to the risk of reduced efficacy of degarelix. Brexpiprazole can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Buprenorphine: (Major) Concomitant use of buprenorphine and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Buprenorphine; Naloxone: (Major) Concomitant use of buprenorphine and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Cabotegravir; Rilpivirine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving rilpivirine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Supratherapeutic doses of rilpivirine (75 to 300 mg/day) have caused QT prolongation.
Cariprazine: (Major) Avoid coadministration of degarelix with cariprazine due to the risk of reduced efficacy of degarelix. Cariprazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Ceritinib: (Major) Avoid coadministration of ceritinib with degarelix if possible due to the risk of QT prolongation. If concomitant use is unavoidable, periodically monitor ECGs and electrolytes; an interruption of ceritinib therapy, dose reduction, or discontinuation of therapy may be necessary if QT prolongation occurs. Ceritinib causes concentration-dependent prolongation of the QT interval. Androgen deprivation therapy (i.e., degarelix) is also associated with QT prolongation.
Chloroquine: (Major) Avoid coadministration of chloroquine with degarelix due to the increased risk of QT prolongation. If use together is necessary, obtain an ECG at baseline to assess initial QT interval and determine frequency of subsequent ECG monitoring, avoid any non-essential QT prolonging drugs, and correct electrolyte imbalances. Chloroquine is associated with an increased risk of QT prolongation and torsade de pointes (TdP); the risk of QT prolongation is increased with higher chloroquine doses. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Chlorpromazine: (Major) Avoid coadministration of degarelix with chlorpromazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Chlorpromazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, chlorpromazine, a phenothiazine, is associated with an established risk of QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Cimetidine: (Minor) In the absence of relevant data and as a precaution, drugs that cause hyperprolactinemia, such as cimetidine, should not be administered concomitantly with degarelix, as hyperprolactinemia downregulates the number of pituitary gonadotropin-releasing hormone receptors.
Ciprofloxacin: (Moderate) Concomitant use of ciprofloxacin and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Cisapride: (Contraindicated) Because of the potential for torsade de pointes (TdP), use of degarelix with cisapride is contraindicated. QT prolongation and ventricular arrhythmias, including TdP and death, have been reported with cisapride. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Citalopram: (Major) Concomitant use of degarelix and citalopram increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Clarithromycin: (Major) Avoid coadministration of clarithromycin with degarelix. Clarithromycin is associated with an established risk for QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Class IA Antiarrhythmics: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents such as class IA antiarrhythmics. Class IA antiarrhythmics (disopyramide, procainamide, and quinidine) are associated with QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Clofazimine: (Moderate) Concomitant use of clofazimine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Clomipramine: (Major) Avoid coadministration of degarelix with clomipramine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Clomipramine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may also prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations).
Clozapine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving clozapine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Treatment with clozapine has been associated with QT prolongation, torsade de pointes (TdP), cardiac arrest, and sudden death.
Codeine; Phenylephrine; Promethazine: (Major) Avoid coadministration of degarelix with promethazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Promethazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Promethazine, a phenothiazine, is associated with a possible risk for QT prolongation.
Codeine; Promethazine: (Major) Avoid coadministration of degarelix with promethazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Promethazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Promethazine, a phenothiazine, is associated with a possible risk for QT prolongation.
Crizotinib: (Major) Avoid coadministration of crizotinib with degarelix due to the risk of QT prolongation. If concomitant use is unavoidable, monitor ECGs for QT prolongation and monitor electrolytes. An interruption of therapy, dose reduction, or discontinuation of therapy may be necessary for crizotinib patients if QT prolongation occurs. Crizotinib has been associated with concentration-dependent QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Danazol: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Dasatinib: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents such as dasatinib as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Desflurane: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like halogenated anesthetics. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Halogenated anesthetics can also prolong the QT interval.
Desipramine: (Minor) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like desipramine. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may also prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations).
Deutetrabenazine: (Major) Avoid coadministration of degarelix with deutetrabenazine due to the risk of reduced efficacy of degarelix. Deutetrabenazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin-releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval. Deutetrabenazine may prolong the QT interval, but the degree of QT prolongation is not clinically significant when deutetrabenazine is administered within the recommended dosage range.
Dexmedetomidine: (Moderate) Concomitant use of dexmedetomidine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Dextromethorphan; Quinidine: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents such as class IA antiarrhythmics. Class IA antiarrhythmics (disopyramide, procainamide, and quinidine) are associated with QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Disopyramide: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents such as class IA antiarrhythmics. Class IA antiarrhythmics (disopyramide, procainamide, and quinidine) are associated with QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Dofetilide: (Major) Coadministration of dofetilide and degarelix is not recommended as concurrent use may increase the risk of QT prolongation. Dofetilide, a Class III antiarrhythmic agent, is associated with a well-established risk of QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Dolasetron: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving dolasetron as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Dolasetron has been associated with a dose-dependent prolongation in the QT, PR, and QRS intervals on an electrocardiogram.
Dolutegravir; Rilpivirine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving rilpivirine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Supratherapeutic doses of rilpivirine (75 to 300 mg/day) have caused QT prolongation.
Donepezil: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving donepezil as concurrent use may increase the risk for QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Donepezil; Memantine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving donepezil as concurrent use may increase the risk for QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Doxepin: (Minor) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like doxepin. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may also prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations).
Dronedarone: (Contraindicated) Because of the potential for torsade des pointes (TdP), the use of degarelix with dronedarone is contraindicated. Dronedarone administration is associated with a dose-related increase in the QTc interval. The increase in QTc is approximately 10 milliseconds at doses of 400 mg twice daily (the FDA-approved dose) and up to 25 milliseconds at doses of 1600 mg twice daily. Although there are no studies examining the effects of dronedarone in patients receiving other QT prolonging drugs, coadministration of such drugs may result in additive QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Droperidol: (Major) Droperidol should not be used in combination with any drug known to have potential to prolong the QT interval, such as degarelix. If coadministration cannot be avoided, use extreme caution; initiate droperidol at a low dose and increase the dose as needed to achieve the desired effect. Droperidol administration is associated with an established risk for QT prolongation and torsade de pointes (TdP). Some cases have occurred in patients with no known risk factors for QT prolongation and some cases have been fatal. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Efavirenz: (Moderate) Consider alternatives to efavirenz when coadministering with degarelix. QTc prolongation has been observed with the use of efavirenz. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Efavirenz; Emtricitabine; Tenofovir Disoproxil Fumarate: (Moderate) Consider alternatives to efavirenz when coadministering with degarelix. QTc prolongation has been observed with the use of efavirenz. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate: (Moderate) Consider alternatives to efavirenz when coadministering with degarelix. QTc prolongation has been observed with the use of efavirenz. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Eliglustat: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving eliglustat as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Eliglustat is predicted to cause PR, QRS, and/or QT prolongation at significantly elevated plasma concentrations.
Emtricitabine; Rilpivirine; Tenofovir alafenamide: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving rilpivirine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Supratherapeutic doses of rilpivirine (75 to 300 mg/day) have caused QT prolongation.
Emtricitabine; Rilpivirine; Tenofovir Disoproxil Fumarate: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving rilpivirine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Supratherapeutic doses of rilpivirine (75 to 300 mg/day) have caused QT prolongation.
Encorafenib: (Major) Avoid coadministration of encorafenib and degarelix due to QT prolongation. If concurrent use cannot be avoided, monitor ECGs for QT prolongation and monitor electrolytes; correct hypokalemia and hypomagnesemia prior to treatment. Encorafenib is associated with dose-dependent prolongation of the QT interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Entrectinib: (Major) Avoid coadministration of entrectinib with degarelix due to the risk of QT prolongation. Entrectinib has been associated with QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Eribulin: (Major) ECG monitoring is recommended if eribulin is administered with degarelix. Eribulin has been associated with QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Erythromycin: (Major) Concomitant use of degarelix and erythromycin increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Escitalopram: (Moderate) Concomitant use of escitalopram and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Esterified Estrogens; Methyltestosterone: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Fingolimod: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving fingolimod as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Fingolimod initiation results in decreased heart rate and may prolong the QT interval. Fingolimod has not been studied in patients treated with drugs that prolong the QT interval, but drugs that prolong the QT interval have been associated with cases of TdP in patients with bradycardia.
Flecainide: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like flecainide. Flecainide is a Class IC antiarrhythmic associated with a possible risk for QT prolongation and/or torsade de pointes (TdP); flecainide increases the QT interval, but largely due to prolongation of the QRS interval. Although causality for TdP has not been established for flecainide, patients receiving concurrent drugs that have the potential for QT prolongation may have an increased risk of developing proarrhythmias. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Fluconazole: (Moderate) Concomitant use of fluconazole and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Fluoxetine: (Moderate) Concomitant use of fluoxetine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Fluphenazine: (Major) Avoid coadministration of degarelix with fluphenazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Fluphenazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Fluphenazine is also associated with a possible risk for QT prolongation. Theoretically, fluphenazine may increase the risk of QT prolongation if coadministered with other drugs that have a risk of QT prolongation.
Fluvoxamine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving fluvoxamine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. QT prolongation and torsade de pointes (TdP) has been reported during fluvoxamine post-marketing use.
Foscarnet: (Major) Avoid use of foscarnet with degarelix due to the potential for Both QT prolongation and torsade de pointes (TdP) as these have been reported during postmarketing use of foscarnet. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Fostemsavir: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Supratherapeutic doses of fostemsavir (2,400 mg twice daily, four times the recommended daily dose) have been shown to cause QT prolongation. Fostemsavir causes dose-dependent QT prolongation.
Gemifloxacin: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving gemifloxacin as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Gemifloxacin may also prolong the QT interval in some patients. The maximal change in QTc interval occurs approximately 5 to 10 hours following oral administration of gemifloxacin. The likelihood of QTc prolongation may increase with increasing dose of the drug; therefore, the recommended dose should not be exceeded especially in patients with renal or hepatic impairment where the Cmax and AUC are slightly higher.
Gemtuzumab Ozogamicin: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving gemtuzumab ozogamicin and degarelix together as concurrent use may increase the risk of QT prolongation. If these agents are used together, obtain an ECG and serum electrolytes prior to the start of gemtuzumab and as needed during treatment. Although QT interval prolongation has not been reported with gemtuzumab, it has been reported with other drugs that contain calicheamicin. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Gilteritinib: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving gilteritinib and degarelix as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Gilteritinib has also been associated with QT prolongation.
Glasdegib: (Major) Avoid coadministration of glasdegib with degarelix due to the potential for additive QT prolongation. If coadministration cannot be avoided, monitor patients for increased risk of QT prolongation with increased frequency of ECG monitoring. Glasdegib therapy may result in QT prolongation and ventricular arrhythmias including ventricular fibrillation and ventricular tachycardia. QTc prolongation has also been reported with the use of degarelix.
Granisetron: (Moderate) Consider whether the benefits of androgen deprivation therapy (i.e., degarelix) outweigh the potential risks in patients receiving granisetron as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy may prolong the QT/QTc interval. Granisetron has been associated with QT prolongation.
Halogenated Anesthetics: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like halogenated anesthetics. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Halogenated anesthetics can also prolong the QT interval.
Haloperidol: (Major) Avoid coadministration of degarelix with haloperidol due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Haloperidol can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. QT prolongation and torsade de pointes (TdP) have also been observed during haloperidol treatment. Excessive doses (particularly in the overdose setting) or IV administration of haloperidol may be associated with a higher risk of QT prolongation.
Hydrochlorothiazide, HCTZ; Methyldopa: (Major) Avoid coadministration of degarelix with methyldopa due to the risk of reduced efficacy of degarelix. Methyldopa can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Hydroxychloroquine: (Major) Concomitant use of hydroxychloroquine and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Hydroxyzine: (Moderate) Concomitant use of hydroxyzine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Ibutilide: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like ibutilide. Ibutilide administration can cause QT prolongation and torsade de pointes (TdP); proarrhythmic events should be anticipated. The potential for proarrhythmic events with ibutilide increases with the coadministration of other drugs that prolong the QT interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Iloperidone: (Major) Avoid coadministration if iloperidone with degarelix due to the risk of QT prolongation; the efficacy of degarelix may also be reduced. Iloperidone has been associated with QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval. Additionally, iloperidone can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Imipramine: (Minor) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like imipramine. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may also prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations).
Inotuzumab Ozogamicin: (Major) Avoid coadministration of inotuzumab ozogamicin with degarelix due to the potential for additive QT interval prolongation and risk of torsade de pointes (TdP). If coadministration is unavoidable, obtain an ECG and serum electrolytes prior to the start of treatment, after treatment initiation, and periodically during treatment. Inotuzumab has been associated with QT interval prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Isoflurane: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like halogenated anesthetics. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Halogenated anesthetics can also prolong the QT interval.
Itraconazole: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving itraconazole as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Itraconazole has also been associated with prolongation of the QT interval.
Ivosidenib: (Major) Avoid coadministration of ivosidenib with degarelix due to an increased risk of QT prolongation. If concomitant use is unavoidable, monitor ECGs for QTc prolongation and monitor electrolytes; correct any electrolyte abnormalities as clinically appropriate. An interruption of therapy and dose reduction of ivosidenib may be necessary if QT prolongation occurs. Prolongation of the QTc interval and ventricular arrhythmias have been reported in patients treated with ivosidenib. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Ketoconazole: (Contraindicated) Avoid concomitant use of ketoconazole and androgen deprivation therapy (i.e., degarelix) due to an increased risk for torsade de pointes (TdP) and QT/QTc prolongation.
Lansoprazole; Amoxicillin; Clarithromycin: (Major) Avoid coadministration of clarithromycin with degarelix. Clarithromycin is associated with an established risk for QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Lapatinib: (Moderate) Monitor for evidence of QT prolongation if lapatinib is administered with degarelix. Lapatinib has been associated with concentration-dependent QT prolongation; ventricular arrhythmias and torsade de pointes (TdP) have been reported in postmarketing experience with lapatinib. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Lefamulin: (Major) Avoid coadministration of lefamulin with degarelix as concurrent use may increase the risk of QT prolongation. If coadministration cannot be avoided, monitor ECG during treatment. Lefamulin has a concentration dependent QTc prolongation effect. The pharmacodynamic interaction potential to prolong the QT interval of the electrocardiogram between lefamulin and other drugs that effect cardiac conduction is unknown. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Lenvatinib: (Major) Avoid coadministration of lenvatinib with degarelix due to the risk of QT prolongation. Prolongation of the QT interval has been reported with lenvatinib therapy. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Levofloxacin: (Moderate) Concomitant use of levofloxacin and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Levoketoconazole: (Contraindicated) Avoid concomitant use of ketoconazole and androgen deprivation therapy (i.e., degarelix) due to an increased risk for torsade de pointes (TdP) and QT/QTc prolongation.
Lithium: (Moderate) Concomitant use of lithium and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Lofexidine: (Major) Monitor ECG if lofexidine is coadministered with degarelix due to the potential for additive QT prolongation. Lofexidine prolongs the QT interval. In addition, there are postmarketing reports of torsade de pointes. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Loperamide: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving loperamide as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. At high doses, loperamide has been associated with serious cardiac toxicities, including syncope, ventricular tachycardia, QT prolongation, torsade de pointes (TdP), and cardiac arrest.
Loperamide; Simethicone: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving loperamide as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. At high doses, loperamide has been associated with serious cardiac toxicities, including syncope, ventricular tachycardia, QT prolongation, torsade de pointes (TdP), and cardiac arrest.
Lopinavir; Ritonavir: (Major) Avoid coadministration of lopinavir with degarelix due to the potential for additive QT prolongation. If use together is necessary, obtain a baseline ECG to assess initial QT interval and determine frequency of subsequent ECG monitoring, avoid any non-essential QT prolonging drugs, and correct electrolyte imbalances. Lopinavir is associated with QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Lorcaserin: (Major) Avoid coadministration of degarelix with lorcaserin due to the risk of reduced efficacy of degarelix. Lorcaserin can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Loxapine: (Major) Avoid coadministration of degarelix with loxapine due to the risk of reduced efficacy of degarelix. Loxapine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Macimorelin: (Major) Avoid concurrent administration of macimorelin with drugs that prolong the QT interval, such as degarelix. Use of these drugs together may increase the risk of developing torsade de pointes-type ventricular tachycardia. Sufficient washout time of drugs that are known to prolong the QT interval prior to administration of macimorelin is recommended. Treatment with macimorelin has been associated with an increase in the corrected QT (QTc) interval. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Maprotiline: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving maprotiline as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Maprotiline has been reported to prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations). Cases of long QT syndrome and torsade de pointes (TdP) tachycardia have been described with maprotiline use, but rarely occur when the drug is used alone in normal prescribed doses and in the absence of other known risk factors for QT prolongation. Limited data are available regarding the safety of maprotiline in combination with other QT-prolonging drugs.
Mefloquine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving mefloquine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. There is evidence that the use of halofantrine after mefloquine causes a significant lengthening of the QTc interval. Mefloquine alone has not been reported to cause QT prolongation.
Methadone: (Major) The need to coadminister methadone with drugs known to prolong the QT interval like degarelix should be done with extreme caution and a careful assessment of treatment risks versus benefits. Methadone is considered to be associated with an increased risk for QT prolongation and torsades de pointes (TdP), especially at higher doses (greater than 200 mg/day; averaging about 400 mg/day in adults). Laboratory studies, both in vivo and in vitro, have demonstrated that methadone inhibits cardiac potassium channels and prolongs the QT interval. Most cases involve patients being treated for pain with large, multiple daily doses of methadone, although cases have been reported in patients receiving doses commonly used for maintenance treatment of opioid addiction. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Methyldopa: (Major) Avoid coadministration of degarelix with methyldopa due to the risk of reduced efficacy of degarelix. Methyldopa can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Methyltestosterone: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Metoclopramide: (Major) Avoid coadministration of degarelix with metoclopramide due to the risk of reduced efficacy of degarelix. Metoclopramide can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Metronidazole: (Moderate) Concomitant use of metronidazole and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Midostaurin: (Major) Consider interval assessments of the QT interval by EKG if midostaurin is taken concurrently with degarelix. QT prolongation was reported in patients who received midostaurin in clinical trials. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Mifepristone: (Major) Concomitant use of mifepristone and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Mirtazapine: (Moderate) Concomitant use of mirtazapine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Mobocertinib: (Major) Concomitant use of mobocertinib and androgen deprivation therapy (i.e., degarelix) increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Molindone: (Major) Avoid coadministration of degarelix with molindone due to the risk of reduced efficacy of degarelix. Molindone can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Moxifloxacin: (Major) Avoid coadministration of moxifloxacin with degarelix as concurrent use may increase the risk of QT prolongation and torsade de pointes (TdP). Quinolones have been associated with a risk of QT prolongation. Although extremely rare, TdP has been reported during postmarketing surveillance of moxifloxacin. These reports generally involved patients with concurrent medical conditions or concomitant medications that may have been contributory. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Nilotinib: (Major) Avoid the concomitant use of nilotinib and degarelix; significant prolongation of the QT interval may occur. Sudden death and QT prolongation have been reported in patients who received nilotinib therapy. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Nortriptyline: (Minor) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like nortriptyline. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may also prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations).
Ofloxacin: (Moderate) Concomitant use of ofloxacin and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Olanzapine: (Major) Avoid coadministration of degarelix with olanzapine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Olanzapine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Limited data, including some case reports, suggest that olanzapine may also be associated with a significant prolongation of the QTc interval.
Olanzapine; Fluoxetine: (Major) Avoid coadministration of degarelix with olanzapine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Olanzapine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Limited data, including some case reports, suggest that olanzapine may also be associated with a significant prolongation of the QTc interval. (Moderate) Concomitant use of fluoxetine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Olanzapine; Samidorphan: (Major) Avoid coadministration of degarelix with olanzapine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Olanzapine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Limited data, including some case reports, suggest that olanzapine may also be associated with a significant prolongation of the QTc interval.
Ondansetron: (Major) Concomitant use of ondansetron and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary. Do not exceed 16 mg of IV ondansetron in a single dose; the degree of QT prolongation associated with ondansetron significantly increases above this dose.
Osilodrostat: (Moderate) Monitor ECGs in patients receiving osilodrostat with degarelix. Osilodrostat is associated with dose-dependent QT prolongation. QTc prolongation has been reported with the use of degarelix. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Osimertinib: (Major) Avoid coadministration of degarelix with osimertinib if possible due to the risk of QT prolongation and torsade de pointes (TdP). If concomitant use is unavoidable, periodically monitor ECGs for QT prolongation and monitor electrolytes; an interruption of osimertinib therapy with dose reduction or discontinuation of therapy may be necessary if QT prolongation occurs. Concentration-dependent QTc prolongation occurred during clinical trials of osimertinib. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Oxaliplatin: (Major) Monitor ECGs and electrolytes in patients receiving oxaliplatin and degarelix concomitantly; correct electrolyte abnormalities prior to administration of oxaliplatin. QT prolongation and ventricular arrhythmias including fatal torsade de pointes have been reported with oxaliplatin use in postmarketing experience. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Oxandrolone: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Oxymetholone: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Ozanimod: (Major) In general, do not initiate ozanimod in patients taking degarelix due to the risk of additive bradycardia, QT prolongation, and torsade de pointes (TdP). If treatment initiation is considered, seek advice from a cardiologist. Ozanimod initiation may result in a transient decrease in heart rate and atrioventricular conduction delays. Ozanimod has not been studied in patients taking concurrent QT prolonging drugs; however, QT prolonging drugs have been associated with TdP in patients with bradycardia. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Pacritinib: (Major) Concomitant use of pacritinib and androgen deprivation therapy (i.e., degarelix) increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Paliperidone: (Major) Avoid coadministration of paliperidone with degarelix due to the potential for additive QT prolongation and risk of torsade de pointes (TdP); the efficacy of degarelix may also be reduced. Paliperidone has been associated with QT prolongation; torsade de pointes and ventricular fibrillation have been reported in the setting of overdose. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval. Additionally, paliperidone can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Panobinostat: (Major) Use of panobinostat with degarelix is not recommended due to the risk of QT prolongation. If concomitant use is unavoidable, frequently monitor ECGs for QT prolongation. Prolongation of the QT interval has been reported with panobinostat. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Pasireotide: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving pasireotide as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. QT prolongation has occurred with pasireotide at therapeutic and supra-therapeutic doses.
Pazopanib: (Major) Coadministration of pazopanib and other drugs that prolong the QT interval like degarelix is not advised. If concomitant use is unavoidable, closely monitor the patient for QT interval prolongation. Pazopanib has been reported to prolong the QT interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Pentamidine: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents. Systemic pentamidine has been associated with QT prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Perphenazine: (Major) Avoid coadministration of degarelix with perphenazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Perphenazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Perphenazine is also associated with a possible risk for QT prolongation. Theoretically, perphenazine may increase the risk of QT prolongation if coadministered with other drugs that have a risk of QT prolongation.
Perphenazine; Amitriptyline: (Major) Avoid coadministration of degarelix with perphenazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Perphenazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Perphenazine is also associated with a possible risk for QT prolongation. Theoretically, perphenazine may increase the risk of QT prolongation if coadministered with other drugs that have a risk of QT prolongation.
Pimavanserin: (Major) Avoid coadminsitration of pimavanserin with degarelix due to additive QT effects and increased risk of cardiac arrhythmia. Pimavanserin prolongs the QT interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Pimozide: (Contraindicated) Because of the potential for torsade de pointes (TdP), use of degarelix with pimozide is contraindicated; the efficacy of degarelix may also be reduced. Pimozide is associated with a well-established risk of QT prolongation and TdP. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval. Additionally, pimozide can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Pitolisant: (Major) Avoid coadministration of pitolisant with degarelix as concurrent use may increase the risk of QT prolongation. Pitolisant prolongs the QT interval. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Ponesimod: (Major) In general, do not initiate ponesimod in patients taking degarelix due to the risk of additive bradycardia, QT prolongation, and torsade de pointes (TdP). If treatment initiation is considered, seek advice from a cardiologist. Ponesimod initiation may result in a transient decrease in heart rate and atrioventricular conduction delays. Ponesimod has not been studied in patients taking concurrent QT prolonging drugs; however, QT prolonging drugs have been associated with TdP in patients with bradycardia. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Posaconazole: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving posaconazole as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Posaconazole has been associated with prolongation of the QT interval as well as rare cases of torsade de pointes.
Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supp

lements): (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved): (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Primaquine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving primaquine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Primaquine is associated with QT prolongation.
Procainamide: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents such as class IA antiarrhythmics. Class IA antiarrhythmics (disopyramide, procainamide, and quinidine) are associated with QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Prochlorperazine: (Major) Avoid coadministration of degarelix with prochlorperazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Prochlorperazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Prochlorperazine is also associated with a possible risk for QT prolongation. Theoretically, prochlorperazine may increase the risk of QT prolongation if coadministered with other drugs that have a risk of QT prolongation.
Promethazine: (Major) Avoid coadministration of degarelix with promethazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Promethazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Promethazine, a phenothiazine, is associated with a possible risk for QT prolongation.
Promethazine; Dextromethorphan: (Major) Avoid coadministration of degarelix with promethazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Promethazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Promethazine, a phenothiazine, is associated with a possible risk for QT prolongation.
Promethazine; Phenylephrine: (Major) Avoid coadministration of degarelix with promethazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Promethazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Promethazine, a phenothiazine, is associated with a possible risk for QT prolongation.
Propafenone: (Major) Concomitant use of propafenone and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Protriptyline: (Minor) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like protriptyline. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may also prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations).
Quetiapine: (Major) Concomitant use of quetiapine and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Quinidine: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents such as class IA antiarrhythmics. Class IA antiarrhythmics (disopyramide, procainamide, and quinidine) are associated with QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Quinine: (Major) Avoid concurrent use of quinine with degarelix due to the risk of QT prolongation. Quinine has been associated with QT prolongation and rare cases of torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Quizartinib: (Major) Concomitant use of quizartinib and androgen deprivation therapy (i.e., degarelix) increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Ramelteon: (Major) Avoid coadministration of degarelix with ramelteon due to the risk of reduced efficacy of degarelix. Ramelteon can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Ranolazine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving ranolazine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Ranolazine is associated with dose- and plasma concentration-related increases in the QTc interval. Although there are no studies examining the effects of ranolazine in patients receiving other QT prolonging drugs, coadministration of such drugs may result in additive QT prolongation.
Ribociclib: (Major) Avoid coadministration of ribociclib with degarelix due to an increased risk for QT prolongation and torsade de pointes (TdP). Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Ribociclib; Letrozole: (Major) Avoid coadministration of ribociclib with degarelix due to an increased risk for QT prolongation and torsade de pointes (TdP). Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Rilpivirine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving rilpivirine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Supratherapeutic doses of rilpivirine (75 to 300 mg/day) have caused QT prolongation.
Risperidone: (Major) Avoid coadministration of degarelix with risperidone due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Risperidone can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, risperidone has been associated with a possible risk for QT prolongation and/or torsade de pointes (TdP), primarily in the overdose setting. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Romidepsin: (Moderate) Consider monitoring electrolytes and ECGs at baseline and periodically during treatment if romidepsin is administered with degarelix as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Romidepsin has been reported to prolong the QT interval.
Saquinavir: (Major) Avoid administering saquinavir boosted with ritonavir concurrently with other drugs that may prolong the QT interval like degarelix. If no acceptable alternative therapy is available, perform a baseline ECG prior to initiation of concomitant therapy and carefully follow monitoring recommendations. Saquinavir boosted with ritonavir increases the QT interval in a dose-dependent fashion, which may increase the risk for serious arrhythmias such as torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Selpercatinib: (Major) Monitor ECGs more frequently for QT prolongation if coadministration of selpercatinib with degarelix is necessary due to the risk of additive QT prolongation. Concentration-dependent QT prolongation has been observed with selpercatinib therapy. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Sertraline: (Moderate) Concomitant use of sertraline and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP. The degree of QT prolongation associated with sertraline is not clinically significant when administered within the recommended dosage range; QT prolongation has been described at 2 times the maximum recommended dose.
Sevoflurane: (Major) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like halogenated anesthetics. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Halogenated anesthetics can also prolong the QT interval.
Siponimod: (Major) In general, do not initiate treatment with siponimod in patients receiving degarelix due to the potential for QT prolongation. Consult a cardiologist regarding appropriate monitoring if siponimod use is required. Siponimod therapy prolonged the QT interval at recommended doses in a clinical study. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Sodium Stibogluconate: (Moderate) Concomitant use of sodium stibogluconate and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Solifenacin: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving solifenacin as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Solifenacin has been associated with dose-dependent prolongation of the QT interval. Torsade de pointes (TdP) has been reported with postmarketing use, although causality was not determined.
Sorafenib: (Major) Avoid coadministration of sorafenib with degarelix due to the risk of additive QT prolongation. If concomitant use is unavoidable, monitor electrocardiograms and correct electrolyte abnormalities. An interruption or discontinuation of sorafenib therapy may be necessary if QT prolongation occurs. Sorafenib is associated with QTc prolongation. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Sotalol: (Major) Concomitant use of sotalol and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Sunitinib: (Moderate) Monitor for evidence of QT prolongation if sunitinib is administered with degarelix. Sunitinib can prolong the QT interval. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Tacrolimus: (Moderate) Consider ECG and electrolyte monitoring periodically during treatment if tacrolimus is administered with degarelix as concurrent use may increase the risk of QT prolongation. Tacrolimus may prolong the QT interval and cause torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Tamoxifen: (Moderate) Concomitant use of tamoxifen and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Telavancin: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving telavancin as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Telavancin has been associated with QT prolongation.
Testosterone: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
Tetrabenazine: (Major) Avoid concurrent use of tetrabenazine with degarelix due to the potential for additive QT prolongation; the efficacy of degarelix may also be reduced. Tetrabenazine causes a small increase in the corrected QT interval (QTc). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval. Additionally, tetrabenazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Thioridazine: (Contraindicated) Because of the potential for torsade de pointes (TdP), use of degarelix with thioridazine is contraindicated; the efficacy of degarelix may also be reduced. Thioridazine is associated with a well-established risk of QT prolongation and TdP. Thioridazine is considered contraindicated for use along with agents that may prolong the QT interval and increase the risk of TdP, and/or cause orthostatic hypotension. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval. Additionally, thioridazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Thiothixene: (Major) Avoid coadministration of degarelix with thiothixene due to the risk of reduced efficacy of degarelix. Thiothixene can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Tolterodine: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving tolterodine as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tolterodine has been associated with dose-dependent prolongation of the QT interval, especially in poor CYP2D6 metabolizers.
Toremifene: (Major) Avoid coadministration of degarelix with toremifene if possible due to the risk of additive QT prolongation. If concomitant use is unavoidable, closely monitor ECGs for QT prolongation and monitor electrolytes; correct hypokalemia or hypomagnesemia prior to administration of toremifene. Toremifene has been shown to prolong the QTc interval in a dose- and concentration-related manner. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Trandolapril; Verapamil: (Major) Avoid coadministration of degarelix with verapamil due to the risk of reduced efficacy of degarelix. Verapamil can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Trazodone: (Major) Concomitant use of trazodone and degarelix increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Avoid concomitant use if possible, especially in patients with additional risk factors for TdP. Consider taking steps to minimize the risk for QT/QTc interval prolongation and TdP, such as electrolyte monitoring and repletion and ECG monitoring, if concomitant use is necessary.
Triclabendazole: (Moderate) Concomitant use of triclabendazole and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Trifluoperazine: (Major) Avoid coadministration of degarelix with trifluoperazine due to the risk of reduced efficacy of degarelix; QT prolongation may also occur. Trifluoperazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog. Additionally, androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Trifluoperazine is also associated with a possible risk for QT prolongation. Theoretically, trifluoperazine may increase the risk of QT prolongation if coadministered with other drugs that have a risk of QT prolongation.
Trimipramine: (Minor) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving other QT prolonging agents like trimipramine. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may also prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations).
Valbenazine: (Major) Avoid concurrent use of degarelix with valbenazine due to the risk of reduced efficacy of degarelix. Valbenazine can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Vandetanib: (Major) Avoid coadministration of vandetanib with degarelix due to an increased risk of QT prolongation and torsade de pointes (TdP). If concomitant use is unavoidable, monitor ECGs for QT prolongation and monitor electrolytes; correct hypocalcemia, hypomagnesemia, and/or hypomagnesemia prior to vandetanib administration. An interruption of vandetanib therapy or dose reduction may be necessary for QT prolongation. Vandetanib can prolong the QT interval in a concentration-dependent manner; TdP and sudden death have been reported in patients receiving vandetanib. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Vardenafil: (Moderate) Concomitant use of vardenafil and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Vemurafenib: (Major) Avoid vemurafenib in patients receiving medications known to prolong the QT interval such as degarelix. Vemurafenib has been shown to prolong the QT interval in a concentration-dependent manner; the ECG changes occurred within the first month of treatment. Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Venlafaxine: (Moderate) Concomitant use of venlafaxine and androgen deprivation therapy (i.e., degarelix) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Consider taking steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, especially in patients with additional risk factors for TdP.
Verapamil: (Major) Avoid coadministration of degarelix with verapamil due to the risk of reduced efficacy of degarelix. Verapamil can cause hyperprolactinemia, which reduces the number of pituitary gonadotropin releasing hormone (GnRH) receptors; degarelix is a GnRH analog.
Voclosporin: (Moderate) Concomitant use of voclosporin and degarelix may increase the risk of QT prolongation. Consider interventions to minimize the risk of progression to torsades de pointes (TdP), such as ECG monitoring and correcting electrolyte abnormalities, particularly in patients with additional risk factors for TdP. Voclosporin has been associated with QT prolongation at supratherapeutic doses. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.
Vonoprazan; Amoxicillin; Clarithromycin: (Major) Avoid coadministration of clarithromycin with degarelix. Clarithromycin is associated with an established risk for QT prolongation and torsade de pointes (TdP). Androgen deprivation therapy (i.e., degarelix) may also prolong the QT/QTc interval.
Voriconazole: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving voriconazole as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Voriconazole has been associated with QT prolongation and rare cases of torsade de pointes.
Vorinostat: (Moderate) Consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients receiving vorinostat as concurrent use may increase the risk of QT prolongation. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval. Vorinostat therapy is associated with a risk of QT prolongation.
Ziprasidone: (Major) Concomitant use of ziprasidone and degarelix should be avoided due to the potential for additive QT prolongation. Clinical trial data indicate that ziprasidone causes QT prolongation; there are postmarketing reports of torsade de pointes (TdP) in patients with multiple confounding factors. Androgen deprivation therapy (i.e., degarelix) may prolong the QT/QTc interval.

How Supplied

Firmagon Subcutaneous Inj Pwd F/Sol: 80mg, 120mg

Maximum Dosage
Adults

240 mg subcutaneously.

Geriatric

240 mg subcutaneously.

Adolescents

Safety and efficacy have not been established.

Children

Safety and efficacy have not been established.

Mechanism Of Action

Degarelix is a gonadotropin-releasing hormone (GnRH) receptor antagonist. Degarelix binds reversibly to the anterior pituitary GnRH receptor thereby reducing luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. This results in an immediate and sustained decrease in the testosterone concentration without the initial stimulation of the hypothalamic-pituitary-gonadal axis. Testosterone suppression to castrate concentrations (0.5 ng/mL) is achieved within 1 to 3 days of administration.

Pharmacokinetics

Degarelix is administered by subcutaneous injection. It is approximately 90% bound to plasma proteins in vitro. The volume of distribution after IV (greater than 1 liter/kg) or subcutaneous (greater than 1,000 liters) administration indicates that degarelix is distributed throughout total body water. It is metabolized via peptide hydrolysis in the hepatobiliary system. No quantitatively significant metabolites were detected in plasma samples after subcutaneous administration. Degarelix exhibits biphasic elimination, with a median terminal half-life of approximately 53 days due to the very slow release of degarelix from the depot formed at injection sites. The clearance of degarelix is about 9 liters/hour after subcutaneous administration to prostate cancer patients. Approximately 20% to 30% of a given dose is renally excreted, with about 70% to 80% excreted as peptide fragments in the feces.
 
Affected cytochrome P450 isoenzymes or transporters: None

Subcutaneous Route

After subcutanous administration, a depot is formed from which degarelix is slowly released into circulation reaching a mean peak plasma concentration (Cmax) of 26.2 ng/mL (CV 83%) within 2 days. The mean AUC is 1,054 ng x day/mL (CV 35%). The pharmacokinetics of degarelix are linear over a dose range of 120 mg to 140 mg; the pharmacokinetic behavior is strongly influenced by its concentration in the injection solution.

Pregnancy And Lactation
Pregnancy

The safety and efficacy of degarelix have not been established in females. Although there are no adequately controlled studies in pregnant women, degarelix can cause fetal harm or death when administered during pregnancy based on its mechanism of action and animal studies. Women who are pregnant or who become pregnant while receiving degarelix should be apprised of the potential hazard to the fetus. An increase in early postimplantation loss occurred when degarelix was given to rabbits during early organogenesis at approximately 0.02% of the clinical loading dose based on body surface area (BSA) and to female rats at approximately 0.036% of the loading dose based on BSA. Embryofetal lethality and abortion occurred when degarelix was given to rabbits during mid and late organogenesis at approximately 0.05% of the loading dose based on BSA. An increase in the number of minor skeletal abnormalities and variants occurred in the offspring of female rats given degarelix during mid and late organogenesis at approximately 0.36% of the loading dose based on BSA.

The safety and efficacy of degarelix have not been established in females. Due to the potential for serious adverse reactions in nursing infants from degarelix, advise women to discontinue breast-feeding during treatment. It is not known whether degarelix is present in human milk, although many drugs are excreted in human milk.