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All price changes →Reluren
Rx40 mg+1 mg+0.5 mg • Tablet
Indications & Uses
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.
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.
Dosage Reference
Reference Information Only
Dosages shown are general references from official sources. Always consult your doctor or pharmacist for personalized dosing.
Adults:
Rule out pregnancy before starting this medicine, and stop any hormonal contraceptives before you begin. The dose of Relugolix + Estradiol + Norethindrone is one tablet by mouth once daily.
If you miss a dose, take it as soon as you can on the same day. Then go back to your usual time the next day.
If you can't avoid using an oral P-gp inhibitor at the same time, take this tablet at least 6 hours before the P-gp inhibitor.
Safety and effectiveness in pediatric patients have not been established.
Side Effects
The most common side effects, seen in more than 3% of people, are hot flush, hyperhidrosis or night sweats, uterine bleeding, alopecia and decreased libido.
Cautions & Contraindications
Warnings & Precautions
Thromboembolic disorders and vascular events: stop Relugolix + Estradiol + Norethindrone if an arterial or venous thrombotic, cardiovascular or cerebrovascular event occurs. Bone loss: the tablet can lower Bone Mineral Density (BMD), and the loss may not be completely reversible. Depression, mood disorders and suicidal ideation: patients should be told to see a doctor if they have new depression, anxiety or other mood changes, or if these get worse. Risk of early pregnancy loss: Relugolix + Estradiol + Norethindrone can cause early pregnancy loss, so women should be advised to use effective non-hormonal contraception.
Contraindications
Don't use this medicine if you have a high risk of arterial or venous thrombotic or thromboembolic disorder, if you are pregnant, or if you have known osteoporosis. It is also not for people who have or have had breast cancer or other hormone sensitive malignancies, or who have known hepatic impairment or disease. Avoid it with undiagnosed abnormal uterine bleeding, and with known hypersensitivity to relugolix, estradiol or norethindrone acetate.
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.
Overdose
Taking too much of an estrogen and progestin medicine, which includes the combination of relugolix, estradiol and norethindrone, may cause nausea, vomiting, breast tenderness, abdominal pain, drowsiness, fatigue and withdrawal bleeding. If an overdose happens, supportive care is recommended. It isn't known how much relugolix, estradiol or norethindrone hemodialysis removes from the body.
⚠️ In an emergency call 999 or go to the nearest hospital emergency department.
Storage
Keep this medicine in a cool, dry place where the temperature stays below 30°C. Protect it from light and moisture. As with all medicines, keep it out of reach of children.
Drug Interactions
Common questions about Reluren 40 mg+1 mg+0.5 mg
What is Reluren 40 mg+1 mg+0.5 mg Tablet?
Reluren 40 mg+1 mg+0.5 mg Tablet is a medicine that contains Relugolix + Estradiol + Norethindrone. It is made by Renata PLC. It belongs to the Gonadotropin-releasing hormone (GnRH) antagonist group of medicines.
What is Reluren used for?
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.
What are the side effects of Reluren?
The most common side effects, seen in more than 3% of people, are hot flush, hyperhidrosis or night sweats, uterine bleeding, alopecia and decreased libido.
Can I take Reluren during pregnancy or while 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. Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
What happens if I take too much Reluren?
Taking too much of an estrogen and progestin medicine, which includes the combination of relugolix, estradiol and norethindrone, may cause nausea, vomiting, breast tenderness, abdominal pain, drowsiness, fatigue and withdrawal bleeding. If an overdose happens, supportive care is recommended. In an emergency call 999 or go to the nearest hospital emergency department.
How should I store Reluren?
Keep this medicine in a cool, dry place where the temperature stays below 30°C. Protect it from light and moisture.
Can I take other medicines with Reluren?
Some medicines can interact with Relugolix + Estradiol + Norethindrone, for example: Relugolix, Estradiol. Tell your doctor or pharmacist about every medicine you take.
Is there a cheaper medicine with the same ingredient?
Reluren is already among the lowest-priced brands of Relugolix + Estradiol + Norethindrone at this strength.
Do I need a prescription for Reluren?
Reluren is a prescription (Rx) medicine. Take it as your doctor advises.