sound asleep [50:<50 mL/minute. 1 7 (See Renal Impairment under Cautions.) Geriatric Patients No dosage adjustment required. 1 (See Geriatric Use under Cautions.) Cautions for Degarelix Acetate Contraindications Known hypersensitivity to degarelix or any ingredient in the formulation. 1 Women who are or may become pregnant; not indicated for use in women. 1 (See Fetal/Neonatal Morbidity and Mortality and also see Pregnancy under Cautions.) Warnings/Precautions Fetal/Neonatal Morbidity and Mortality May cause fetal harm; teratogenicity and embryolethality demonstrated in animals. 1 7 (See Contraindications under Cautions.) Prolongation of QT Interval Prolongation of QT c F interval reported. 1 2 7 Long-term androgen deprivation therapy prolongs QT interval. 1 6 Consider whether benefits of androgen deprivation therapy outweigh potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, or CHF and in patients receiving class IA (e.g., procainamide, quinidine) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents. 1 Laboratory Monitoring Periodically measure PSA concentrations to monitor response to the drug. 1 If serum PSA concentrations increase, measure serum testosterone concentrations. 1 Laboratory Test Interferences Degarelix therapy suppresses pituitary gonadal system; may affect results of diagnostic tests of pituitary gonadotropic and gonadal functions performed during and after therapy. 1 Decrease in Bone Mineral Density Possible decrease in bone mineral density (BMD) with long-term androgen deprivation therapy. 1 7 Antibody Formation Development of antibodies to degarelix reported; safety and efficacy of the drug not affected by antibody formation. 1 6 Specific Populations Pregnancy Category X. 1 (See Fetal/Neonatal Morbidity and Mortality and also see Contraindications under Cautions.) Lactation Not known whether distributed into milk. 1 Not indicated for use in women. 1 (See Contraindications under Cautions.) Pediatric Use Safety and efficacy not established in pediatric patients. 1 7 Geriatric Use No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out. 1 (See Geriatric Patients under Dosage and Administration.) Hepatic Impairment Patients with hepatic impairment were excluded from clinical study in prostate cancer. 1 7 No dosage adjustment required in patients with mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment. 1 Not studied in patients with severe hepatic impairment; use with caution in such patients. 1 Reduced degarelix exposure in patients with mild or moderate hepatic impairment. 1 (See Special Populations under Pharmacokinetics.) Monitor testosterone concentrations monthly in patients with hepatic impairment until medical castration achieved; thereafter, consider monitoring testosterone concentrations every other month. 1 Renal Impairment Insufficient data in patients with moderate renal impairment, and not studied in patients with severe renal impairment; use with caution in patients with Cl cr> <50 mL/minute because 20 30% of a given dose is excreted unchanged in urine. 1 7 (See Renal Impairment under Dosage and Administration.) Pharmacokinetics not studied in patients with renal impairment. 1 (See Special Populations under Pharmacokinetics.) Common Adverse Effects Injection site reactions (e.g., pain, erythema, swelling, induration, nodule), 1 hot flashes, 1 weight gain, 1 increased transaminase and γ-glutamyltransferase (γ-glutamyltranspeptidase, GGT, GGTP) concentrations, 1 hypertension, 1 back pain, 1 fatigue, 1 chills, 1 arthralgia, 1 constipation, 1 urinary tract infection. 1 Interactions for Degarelix Acetate No formal drug interaction studies to date. 1 7 Not a substrate, inducer, or inhibitor of CYP isoenzyme or P-glycoprotein transport systems. 1 Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes Clinically important pharmacokinetic interactions with drugs affecting or metabolized by CYP isoenzymes unlikely. 1 7 Drugs Affecting or Affected by the P-glycoprotein Transport System Clinically important pharmacokinetic interactions with drugs affecting or affected by the P-glycoprotein transport system unlikely. 7 Degarelix Acetate Pharmacokinetics Absorption Bioavailability Forms a depot at injection site following sub-Q administration from which drug is slowly released into circulation. 1 Peak plasma concentrations generally occur within 2 days following sub-Q administration of a single 240-mg dose at a concentration of 40 mg/mL. 1 6 Pharmacokinetic behavior strongly influenced by concentration of drug in injection solution. 1 Onset Medical castration achieved within 7 days. 1 Special Populations Pharmacokinetics not affected by age, weight, or race. 1 Exposure to degarelix reduced by 10 or 18% in patients with mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment, respectively, compared with individuals with normal hepatic function. 1 (See Hepatic Impairment under Cautions.) Pharmacokinetics not studied in patients with renal impairment; however, a population pharmacokinetic analysis suggests that mild renal impairment (Cl cr of 50 80 mL/minute) has no clinically important effect on concentrations of degarelix or testosterone. 1 (See Renal Impairment under Cautions.) Distribution Extent Distributed throughout total body water. 1 Not known whether distributed into milk. 1 (See Contraindications under Cautions.) Plasma Protein Binding Approximately 90%. 1 Elimination Metabolism Subjected to peptide hydrolysis during passage through the hepatobiliary system; mainly excreted as peptide fragments in feces. 1 6 No substantial metabolites detected in plasma following sub-Q administration. 1 Not a substrate, inducer, or inhibitor of CYP isoenzyme or P-glycoprotein transport systems. 1 Elimination Route Excreted in urine (20 30%) as unchanged drug; 70 80% of administered dose presumably excreted via hepatobiliary system. 1 6 Half-life Eliminated in a biphasic manner; median terminal half-life of about 53 days following sub-Q administration of a 240-mg dose at a concentration of 40 mg/mL. 1 6 Stability Storage Parenteral Powder for Injection 25 C (may be exposed to 15 30 C). 1 Reconstituted solution: Use within one hour following addition of sterile water for injection to lyophilized powder. 1 Actions Synthetic GnRH antagonist. 1 2 6 Immediately, competitively, and reversibly binds to and blocks GnRH receptors in the pituitary, thereby reducing release of gonadotropins (i.e., LH, FSH) and, consequently, testosterone without initial stimulation of hypothalamic-pituitary-gonadal axis and associated testosterone surge. 1 2 3 4 5 6 Exhibits low histamine-releasing potential compared with other GnRH antagonists; no signs of immediate- or late-onset systemic allergic reactions reported. 2 3 4 5 Advice to Patients Importance of instructing patients to carefully read the manufacturer s patient information before initiating therapy and each time the prescription is refilled. 1 Importance of understanding frequency and duration of treatment and required monitoring procedures. 1 Risk of hot flashes, flushing of the skin, increased weight, decreased sex drive, and difficulties with erectile function. 1 Risk of redness, swelling, and itching at the injection site; usually mild, self-limiting, and decrease within 3 days. 1 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription (e.g., antiarrhythmic agents) and OTC drugs and herbal supplements, as well as any concomitant illnesses (e.g., CHF, electrolyte abnormalities, hepatic or renal impairment). 1 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Degarelix Acetate Routes Dosage Forms Strengths Brand Names Manufacturer Parenteral For injection, for subcutaneous use only 80 mg (of degarelix) Firmagon Ferring 120 mg (of degarelix) Firmagon Ferring AHFS DI Essentials. Copyright 2017, Selected Revisions October 16, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. Ferring Pharmaceuticals Inc. Firmagon (degarelix acetate) for injection prescribing information. Parsippany, NJ; 2009 Feb. 2. Klotz L, Boccon-Gibod L, Shore ND et al. The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer. BJU Int . 2008; 102:1531-8. [PubMed 19035858] 3. Anderson J. Degarelix: a novel gonadotropin-releasing hormone blocker for the treatment of prostate cancer. Future Oncol . 2009; 5:433-43. [PubMed 19450172] 4. Gittelman M, Pommerville PJ, Persson BE et al. A 1-year, open label, randomized phase II dose finding study of degarelix for the treatment of prostate cancer in North America. J Urol . 2008; 180:1986-92. [PubMed 18801505] 5. Van Poppel H, Tombal B, de la Rosette JJ et al. Degarelix: a novel gonadotropin-releasing hormone (GnRH) receptor blocker--results from a 1-yr, multicentre, randomised, phase 2 dosage-finding study in the treatment of prostate cancer. Eur Urol . 2008; 54:805-13. [PubMed 18538469] 6. . Degarelix (firmagon) for prostate cancer. Med Lett Drugs Ther . 2009; 51:82-3. [PubMed 19838145] 7. Ferring Pharmaceuticals Inc., Parsippany, NJ: Personal communication. Next Interactions Print this page Add to My Med List More about degarelix Side Effects During Pregnancy Dosage Information Drug Interactions Support Group En Español 5 Reviews Add your own review/rating Drug class: gonadotropin-releasing hormone antagonists Consumer resources Degarelix Degarelix Subcutaneous (Advanced Reading) Professional resources Degarelix (Wolters Kluwer) Other brands: Firmagon Related treatment guides Prostate Cancer> ]} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only X Pregnancy Category Not for use in pregnancy N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Gonadotropin-releasing hormone antagonists Hormones / antineoplastics Related Drugs Prostate Cancer estradiol , Premarin , Estrace , bicalutamide , Casodex , Eligard , Xtandi , Zytiga , leuprolide , Taxotere , Lupron Depot , conjugated estrogens , docetaxel , Firmagon , Trelstar , enzalutamide , Zoladex , abiraterone , degarelix , Menest , flutamide , flax , Delestrogen , More... 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