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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.

Indications
  • Management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women
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.

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
Side effects

Common Side Effects (>3%):

  • Hot flush
  • Hyperhidrosis or night sweats
  • Uterine bleeding
  • Alopecia
  • Decreased libido
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.

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
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.

Relugolix + Estradiol + Norethindrone — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.