Generic
Relugolix + Estradiol + Norethindrone
3 brands available in the market
At a glance
Relugolix + Estradiol + Norethindrone is used for the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women. Relugolix acts as a GnRH receptor antagonist, estradiol reduces bone loss, and norethindrone protects the uterus.
Description
Relugolix is a non-peptide GnRH receptor antagonist that binds to pituitary GnRH receptors, reducing LH and FSH release, decreasing estradiol and progesterone concentrations, and reducing fibroid-associated bleeding. Estradiol reduces bone resorption and resultant bone loss. Norethindrone protects the uterus from adverse endometrial effects of unopposed estrogen.
Indications
- Management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women
Therapeutic class
Gonadotropin-releasing hormone (GnRH) antagonist
Pharmacological class
GnRH Antagonist + Estrogen + Progestin
Pharmacology
Relugolix blocks pituitary GnRH receptors, reducing LH and FSH release, decreasing estradiol and progesterone levels, and reducing fibroid-associated bleeding. Estradiol prevents bone loss, and norethindrone protects the endometrium from unopposed estrogen effects.
Mechanism of action
Controls fibroid-associated bleeding by blocking GnRH receptors and reducing hormone levels.
Dosage
Adult Dose (Oral):
- 1 tablet once daily
- Exclude pregnancy and discontinue hormonal contraceptives prior to initiation
- Missed dose: Take as soon as possible on the same day; resume regular dosing the next day
- With P-gp inhibitors: Take this tablet at least 6 hours before the P-gp inhibitor
Administration
- Take at approximately the same time each day
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as possible on the same day; resume regular dosing the next day; do not double the dose.
Side effects
Common Side Effects (>3%):
- Hot flush
- Hyperhidrosis or night sweats
- Uterine bleeding
- Alopecia
- Decreased libido
Precautions & warnings
- Discontinue if arterial or venous thrombotic, cardiovascular, or cerebrovascular event occurs
- Bone mineral density decrease may not be completely reversible
- Depression, mood changes, suicidal ideation: Seek medical attention for new or worsening symptoms
- Risk of early pregnancy loss; use non-hormonal contraception
Contraindications
- High risk of arterial, venous thrombotic or thromboembolic disorder
- Pregnancy
- Known osteoporosis
- Current or history of breast cancer or other hormone-sensitive malignancies
- Known hepatic impairment or disease
- Undiagnosed abnormal uterine bleeding
- Hypersensitivity to relugolix, estradiol, or norethindrone acetate
Drug interactions
- P-gp inhibitors: Increase AUC and Cmax of relugolix; risk of adverse reactions
- P-gp + strong CYP3A inducers: Decrease AUC and Cmax of relugolix, estradiol, and/or norethindrone; may decrease therapeutic effects
- Grapefruit juice: May increase plasma concentrations of CYP3A4 substrates
Food interactions
It is not known whether it is safe to consume alcohol with Relugolix + Estradiol + Norethindrone.
Use in pregnancy
Use in Pregnancy: May cause early pregnancy loss; discontinue if pregnancy occurs; do not use.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No data on presence in human milk; detected in animal milk; do not use during breastfeeding.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Not applicable for elderly patients (premenopausal women).
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed; consult your doctor.
Hepatic Impairment: Contraindicated in hepatic impairment or disease; consult your doctor.
Overdose effects
Overdose: Nausea, vomiting, breast tenderness, abdominal pain, drowsiness, fatigue, withdrawal bleeding; treatment: supportive care; removal by hemodialysis unknown.
Storage conditions
Store in a cool (below 30°C) and dry place, away from light and moisture; keep out of reach of children.
Chemical structure
Relugolix + Estradiol + Norethindrone