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Alternatives (2)Cheaper & Alternative Brands (40 mg+1 mg+0.5 mg)
Same active generic (Relugolix + Estradiol + Norethindrone), same form (Tablet), exact same strength (40 mg+1 mg+0.5 mg)
Clinical Prescribing Information
Medical monograph and safety information for healthcare professionals & patients.Indications & Clinical Uses
This is indicated for the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women.
Dosage & Administration
Exclude pregnancy and discontinue hormonal contraceptives prior to this initiation. Orally one tablet once daily. In case of missed dose, need to take as soon as possible the same day and then resume regular dosing the next day at the usual time. If concomitant use of oral P-gp inhibitors is unavoidable, need to take this tablet at least 6 hours before taking the P-gp inhibitor.
Safety and effectiveness of in pediatric patients have not been established.
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.
Known hypersensitivity to relugolix, estradiol or norethindrone acetate.
Side Effects & Adverse Reactions
Most common adverse reactions (incidence >3%) are: Hot flush, Hyperhidrosis or night sweats, Uterine bleeding, Alopecia, Decreased libido.
Warnings & Precautions
Thromboembolic disorders and vascular events
: Discontinue this tablet, if an arterial or venous thrombotic, cardiovascular or cerebrovascular event occurs.
Bone Loss
: Decreases in Bone Mineral Density (BMD) that may not be completely reversible.
Depression, mood disorders and suicidal ideation
: Advise patients to seek medical attention for new onset or worsening depression, anxiety or other mood changes.
Risk of early pregnancy loss
: Can cause early pregnancy loss. Advise women to use effective non-hormonal contraception.
Pharmacology & Mechanism of Action
This tablet is a combination of relugolix, estradiol (E2) and norethindrone acetate (NETA). Relugolix is a non-peptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby reducing the release of Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH), leading to decreased serum concentrations of the ovarian sex hormones estradiol and progesterone and reduced bleeding associated with uterine fibroids. Estradiol acts by binding to nuclear receptors that are expressed in estrogen-responsive tissues. As a component of this tablet, the addition of exogenous estradiol may reduce the increase in bone resorption and resultant bone loss that can occur due to a decrease in circulating estrogen concentrations from relugolix alone. Progestins such as norethindrone act by binding to nuclear receptors that are expressed in progesterone-responsive tissues. As a component of this tablet, norethindrone may protect the uterus from the potential adverse endometrial effects of unopposed estrogen.