Relugolix + Estradiol + Norethindrone
Indications
Relugolix with estradiol and norethindrone is used to manage heavy menstrual bleeding caused by uterine leiomyomas (fibroids) in women who have not yet reached menopause.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
This tablet combines three medicines: relugolix, estradiol (E2) and norethindrone acetate (NETA). Relugolix is a non-peptide GnRH receptor antagonist. It binds competitively to the GnRH receptors in the pituitary gland, and this lowers the release of Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH). As a result, the serum levels of the ovarian sex hormones estradiol and progesterone fall, and the bleeding linked to uterine fibroids is reduced.
Estradiol works by binding to nuclear receptors found in estrogen-responsive tissues. In this tablet, the added estradiol may limit the rise in bone resorption, and the bone loss that follows, which can happen when circulating estrogen drops with relugolix alone.
Progestins such as norethindrone work by binding to nuclear receptors found in progesterone-responsive tissues. In this tablet, norethindrone may protect the uterus from the possible harmful effects of unopposed estrogen on the endometrium.
Pregnancy & Breastfeeding
Animal studies and the way this medicine works suggest that Relugolix + Estradiol + Norethindrone may cause early pregnancy loss. If pregnancy happens during treatment, stop the tablet.
No data exist on whether relugolix or its metabolites pass into human milk, what effect they may have on a breastfed child, or whether they change milk production. Relugolix was found in the milk of lactating rats, and when a drug appears in animal milk, it is likely to appear in human milk too.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.