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Estradiol / Norethindrone / Relugolix Dosage

Medically reviewed by Last updated on Jun 30, 2021.

Applies to the following strengths: 1 mg-0.5 mg-40 mg

Usual Adult Dose for Menstrual Disorders

1 tablet orally once a day
Total duration of therapy: 24 months

Use: For the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women

Renal Dose Adjustments

Data not available

Liver Dose Adjustments

Liver dysfunction or disease: Contraindicated


  • The use of estradiol in patients with liver dysfunction is expected to increase the exposure of estradiol and increase the risk of estradiol-related side effects.

Dose Adjustments

Concomitant Use with Oral P-gp Inhibitors: Use should be avoided.

  • If concomitant use is unavoidable, this drug should be administered first, and dosing should be separated by at least 6 hours.



  • THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS: Estrogen and progestin combination products (including this drug) increase the risk of thrombotic or thromboembolic disorders (including pulmonary embolism, deep vein thrombosis, stroke, myocardial infarction), especially in women at increased risk for these events. This drug is contraindicated in women with current or history of thrombotic or thromboembolic disorders and in women at increased risk for these events (including women over 35 years of age who smoke, women with uncontrolled hypertension).

Women with high risk of arterial, venous thrombotic, or thromboembolic disorders; examples include women over 35 years of age who smoke, and women who are known to have:current or history of deep vein thrombosis or pulmonary embolismvascular disease (e.g., cerebrovascular disease, coronary artery disease, peripheral vascular disease)thrombogenic valvular or thrombogenic rhythm diseases of the heart (e.g., subacute bacterial endocarditis with valvular disease, atrial fibrillation)inherited or acquired hypercoagulopathiesuncontrolled hypertensionheadaches with focal neurological symptoms or migraine headaches with aura if over 35 years of ageWomen who are pregnantWomen with known osteoporosis (due to risk of further bone loss)Women with current or history of breast cancer or other hormone-sensitive malignancies, and with increased risk for hormone-sensitive malignanciesWomen with known hepatic impairment or diseaseWomen with undiagnosed abnormal uterine bleedingWomen with known anaphylactic reaction, angioedema, or hypersensitivity to any active component or to any of the ingredients

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.


Data not available

Other Comments

Administration advice:

  • Before starting this drug, exclude pregnancy.
  • Before starting this drug, discontinue hormonal contraception.
  • Start this drug as early as possible after the onset of menses but no later than 7 days after menses has started.
  • Administer at about the same time each day, with or without food.
  • If using an oral P-gp inhibitor, administer this drug first and separate dosing by at least 6 hours.

Storage requirements:
  • Store at 15C to 30C (59F to 86F).

  • Each tablet contains estradiol 1 mg, norethindrone acetate 0.5 mg, and relugolix 40 mg.
  • Limitations of Use: Use of this drug should be limited to 24 months due to the risk of continued bone loss which may not be reversible.
  • The impact of bone mineral density (BMD) decreases on long-term bone health and future fracture risk in premenopausal women is unknown.

  • Cardiovascular: Blood pressure in patients with well-controlled hypertension
  • General: For pregnancy (before starting therapy, if pregnancy suspected)
  • Metabolic: Blood glucose in patients with diabetes or prediabetes; lipid levels
  • Musculoskeletal: BMD by dual-energy x-ray absorptiometry (DXA) scan (at baseline and periodically thereafter)

Patient advice:
  • Read the US FDA-approved patient labeling (Patient Information).
  • If a dose is missed, take it as soon as possible the same day and then resume regular dosing the next day at the usual time; if you do not remember until the next day, do not take the missed dose. Do not take 2 doses at once to make up for a missed dose.
  • Supplementary calcium and vitamin D may be beneficial if dietary intake is not adequate; do not take oral iron supplementation at the same time as calcium and vitamin D.
  • Seek immediate medical attention for suicidal ideation and behavior; promptly seek medical attention for new onset/worsening depression, anxiety, or other mood changes.
  • Promptly seek medical attention if signs/symptoms develop that may reflect liver injury (e.g., jaundice, right upper abdominal pain).
  • Contact physician if severe bleeding and/or cramping occurs during therapy.
  • Patients of childbearing potential: Use effective nonhormonal contraception during therapy and for 1 week after the last dose; discontinue this drug if pregnancy is confirmed.
  • Contact health care provider if concerned about change to your hair.
  • Dispose of unused medication properly; do not flush it down the toilet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.