degarelix

Contraindicated in:

Previous hypersensitivity.

Use Cautiously in:

Severe renal impairment;
Severe hepatic impairment;
Previous history of cardiovascular disease including congenital long QT syndrome, electrolyte abnormalities, or HF, or concurrent use of class IA or class III antiarrhythmics (may ↑ the risk of QT prolongation);
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may be more sensitive to drug effects.

Adv. Reactions/Side Effects ⬆ ⬇

CV: QT interval prolongation

Derm: ↑sweating

Endo: hot flashes, gynecomastia, pituitary gonadal suppression

GI: ↑liver enzymes, diarrhea, nausea

GU: ↓fertility, erectile dysfunction, testicular atrophy

Local: injection site reactions

Metab: weight gain

MS: ↓bone density

Neuro: dizziness, headache, insomnia, weakness

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with class IA antiarrhythmics, including procainamide and quinidine, or class III antiarrhythmics, including amiodarone or sotalol, may ↑ risk of QT interval prolongation and serious arrhythmias.

Availability ⬆ ⬇

Powder for SUBQ injection: 80 mg/vial; 120 mg/vial

Route/Dosage ⬆ ⬇

SC (Adults ): 240 mg initially (given as two injections of 120 mg each) (loading dose), followed by maintenance dose of 80 mg every 28 days.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Reversibly binds to gonadotropin-releasing hormone receptors in the pituitary gland, causing a decrease in the release of gonadotropins and testosterone.

Therapeutic effects:

Decreased spread of prostate cancer.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: gnrh antagonist

Pharmacokinetics ⬆ ⬇

Absorption: Rapid release initially, then slow release from depot formed after SUBQ administration.

Distribution: Distributed throughout total body water.

Metabolism/Excretion: 70–80% undergoes hepatic metabolism and biliary excretion, most metabolites excreted in feces; 20–30% excreted unchanged in urine.

Half-Life: 53 days.

Time/Action Profile ⬆ ⬇

(↓ in testosterone levels)

ROUTE	ONSET	PEAK	DURATION
SC	within 1 wk	2 wk	1 mo

Patient/Family Teaching ⬆ ⬇

Explain purpose of medication to patient. Instruct patient to notify health care professional if an injection is missed. Advise patient to read Patient Informationbefore starting and with each Rx refill in case of changes.
Inform patient of possible side effects (hot flashes, flushing, increased weight, decreased sex drive, erectile dysfunction). Advise patient that redness, swelling, and itching at injection site are usually mild and self-limiting and should decrease within 3 days.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Rep: May impair fertility in males.

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Indications ⬇

Contraind./Precautions ⬆ ⬇