Generic
Degarelix
2 brands available in the market
At a glance
Degarelix is a gonadotropin-releasing hormone (GnRH) antagonist used for the treatment of advanced hormone-dependent prostate cancer.
Description
Degarelix is a selective GnRH antagonist that competitively and reversibly binds to pituitary GnRH receptors, thereby rapidly reducing the release of gonadotrophins (LH and FSH), and thereby reducing testosterone secretion by the testes. Unlike GnRH agonists, GnRH antagonists do not induce a LH surge with subsequent testosterone surge/tumour stimulation after the initiation of treatment.
Indications
- Advanced hormone-dependent prostate cancer
Therapeutic class
Drugs affecting (inhibiting) gonadotrophin
Pharmacological class
GnRH Antagonist
Pharmacology
Degarelix is a selective GnRH antagonist that competitively and reversibly binds to pituitary GnRH receptors, thereby rapidly reducing the release of LH and FSH, and thereby reducing testosterone secretion by the testes. Unlike GnRH agonists, GnRH antagonists do not induce a LH surge with subsequent testosterone surge/tumour stimulation.
Mechanism of action
Degarelix blocks GnRH receptors in the pituitary gland, reducing LH and FSH secretion, which decreases testosterone production in the testes, slowing or stopping prostate cancer cell growth.
Dosage
Adult: Loading dose: 240 mg (as 2 separate injections of 120 mg each SC). Maintenance: 80 mg once every 28 days SC, starting 28 days after the initial dose.
Administration
This medicine is given as a subcutaneous injection (in the abdominal area) by a healthcare professional. Kindly do not self administer. Injection site should vary periodically.
Missed dose
If you miss a dose of Degarelix, please consult your doctor.
Side effects
Common: Injection site reactions (pain, swelling, redness), weight gain, hot flashes, increased liver enzymes, low sexual desire, erectile dysfunction.
Other: Transient chills, fever or flu-like illness.
Precautions & warnings
QT prolongation may occur; caution with class IA and III antiarrhythmics, methadone, moxifloxacin, and antipsychotics. Caution while driving (dizziness, blurred vision, drowsiness). Inform doctor if diabetic or have heart, kidney or liver problems. Avoid use in pregnancy and lactation.
Contraindications
Hypersensitivity; Pregnancy; Lactation.
Drug interactions
Class IA (disopyramide) and class III (amiodarone) antiarrhythmics, antipsychotics, methadone, moxifloxacin: Increased risk of QT prolongation.
Food interactions
Caution is advised when consuming alcohol with Degarelix (may worsen hot flashes). Please consult your doctor.
Use in pregnancy
Pregnancy Category X. Degarelix is highly unsafe during pregnancy. Studies on pregnant women and animals have shown significant harmful effects to the developing baby.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Information regarding the use of Degarelix during breastfeeding is not available. Please consult your doctor.
Pediatric use
There is no relevant use in children and adolescents.
Geriatric use
No dose adjustment is necessary for elderly patients.
Renal / hepatic impairment
Renal impairment: Mild-moderate (GFR >50 mL/min): No dose adjustment; <50 mL/min: Use caution. Severe kidney disease: limited information.
Hepatic impairment: Mild-moderate: No dose adjustment; Severe: Safety and efficacy not established; use caution.
Overdose effects
There is no clinical experience with the effects of an acute overdose. In the event of overdose, monitor patient and give appropriate supportive treatment.
Storage conditions
Store at 25°C. Chemical and physical in-use stability has been demonstrated for 2 hours at 25°C.
Chemical structure
Degarelix