Myfembree

— THERAPEUTIC CATEGORIES —
  • Endometriosis
  • Menorrhagia

Myfembree Generic Name & Formulations

General Description

Relugolix 40mg, estradiol 1mg, norethindrone acetate 0.5mg; per tab.

Pharmacological Class

GnRH antagonist + estrogen + progestin.

How Supplied

Tabs—28

Manufacturer

Generic Availability

NO

Myfembree Indications

Indications

Moderate to severe pain associated with endometriosis in premenopausal women.

Limitations of Use

Limit use to 24 months due to the risk of continued bone loss, which may not be reversible.

Myfembree Dosage and Administration

Adult

Exclude pregnancy and discontinue hormonal contraceptives prior to initiating. Start as early as possible after onset of menses but no later than 7 days after menses has started. Take at same time each day. 1 tab once daily.

Children

Not established.

Myfembree Contraindications

Contraindications

High risk of arterial, venous thrombotic, or thromboembolic disorder (eg, smokers or migraineurs over 35 years of age, history of DVT or PE, vascular disease, thrombogenic valvular disease, atrial fibrillation, subacute bacterial endocarditis, hypercoagulopathies, uncontrolled hypertension, headaches with focal neurologic symptoms). Pregnancy. Osteoporosis. Hepatic impairment or disease. Breast cancer or other hormonally-sensitive malignancies. Undiagnosed abnormal uterine bleeding.

Myfembree Boxed Warnings

Boxed Warning

Thromboembolic disorders. Vascular events.

Myfembree Warnings/Precautions

Warnings/Precautions

Increased risk of thrombotic or thromboembolic disorders. Discontinue immediately if thrombotic, cardiovascular or cerebrovascular event occurs or is suspected or if sudden unexplained loss of vision. Discontinue if gallbladder disease or jaundice occurs, and at least 4–6 weeks prior to surgery associated with increased risk of thromboembolism or during periods of immobilization. Risk of decrease in bone mineral density (BMD). Assess BMD at baseline and periodically thereafter. Consider treatment benefits/risks in those with a history of low-trauma fracture or other risk factors for osteoporosis or bone loss; supplementation with calcium and Vit.D may be beneficial. Perform breast exams and regular mammography. Discontinue if a hormonally-sensitive malignancy develops. Evaluate if new onset or worsening depression, anxiety, other mood changes occur. Monitor BP; discontinue if significant rise occurs. History of cholestatic jaundice associated with prior estrogen use or with pregnancy. Risk of uterine fibroid prolapse or expulsion in women with known or suspected submucosal uterine fibroids. Monitor lipid levels; consider discontinuing if hypertriglyceridemia or hypercholesterolemia worsens. Diabetes. Prediabetes. Hypothyroidism. Hypoadrenalism. Reduced ability to recognize pregnancy. Perform pregnancy testing if suspected; discontinue if confirmed. Advise women of reproductive potential to use effective non-hormonal contraception during and for 1 week after discontinuation. Nursing mothers.

Myfembree Pharmacokinetics

See Literature

Myfembree Interactions

Interactions

Avoid concomitant use with hormonal contraceptives. Potentiated by oral P-gp inhibitors: avoid; if unavoidable, take Myfembree first, separate dosing by at least 6hrs; monitor for adverse reactions. Antagonized by combined P-gp and strong CYP3A inducers (eg, rifampin): avoid. May affect levels of thyroid-binding globulin, corticosteroid-binding globulin, coagulation factors, sex hormone binding globulin, lipids, glucose.

Myfembree Adverse Reactions

Adverse Reactions

Vasomotor symptoms, uterine bleeding, alopecia, decreased libido; for endometriosis: also headache, mood disorders, nausea, toothache, back pain, decreased sexual desire and arousal, arthralgia, fatigue, dizziness; uterine expulsion or prolapse, menorrhagia, cholecystitis, pelvic, pain, bone loss, elevated hepatic transaminase, elevated lipids, hypertension, depression-related adverse reactions, mood changes, hypersensitivity reactions (discontinue if occurs).

Myfembree Clinical Trials

See Literature

Myfembree Note

Not Applicable

Myfembree Patient Counseling

See Literature

Myfembree Generic Name & Formulations

General Description

Relugolix 40mg, estradiol 1mg, norethindrone acetate 0.5mg; per tab.

Pharmacological Class

GnRH antagonist + estrogen + progestin.

How Supplied

Tabs—28

Manufacturer

Generic Availability

NO

Myfembree Indications

Indications

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

Limitations of Use

Limit use to 24 months due to the risk of continued bone loss, which may not be reversible.

Myfembree Dosage and Administration

Adult

Exclude pregnancy and discontinue hormonal contraceptives prior to initiating. Start as early as possible after onset of menses but no later than 7 days after menses has started. Take at same time each day. 1 tab once daily.

Children

Not established.

Myfembree Contraindications

Contraindications

High risk of arterial, venous thrombotic, or thromboembolic disorder (eg, smokers or migraineurs over 35 years of age, history of DVT or PE, vascular disease, thrombogenic valvular disease, atrial fibrillation, subacute bacterial endocarditis, hypercoagulopathies, uncontrolled hypertension, headaches with focal neurologic symptoms). Pregnancy. Osteoporosis. Hepatic impairment or disease. Breast cancer or other hormonally-sensitive malignancies. Undiagnosed abnormal uterine bleeding.

Myfembree Boxed Warnings

Boxed Warning

Thromboembolic disorders. Vascular events.

Myfembree Warnings/Precautions

Warnings/Precautions

Increased risk of thrombotic or thromboembolic disorders. Discontinue immediately if thrombotic, cardiovascular or cerebrovascular event occurs or is suspected or if sudden unexplained loss of vision. Discontinue if gallbladder disease or jaundice occurs, and at least 4–6 weeks prior to surgery associated with increased risk of thromboembolism or during periods of immobilization. Risk of decrease in bone mineral density (BMD). Assess BMD at baseline and periodically thereafter. Consider treatment benefits/risks in those with a history of low-trauma fracture or other risk factors for osteoporosis or bone loss; supplementation with calcium and Vit.D may be beneficial. Perform breast exams and regular mammography. Discontinue if a hormonally-sensitive malignancy develops. Evaluate if new onset or worsening depression, anxiety, other mood changes occur. Monitor BP; discontinue if significant rise occurs. History of cholestatic jaundice associated with prior estrogen use or with pregnancy. Risk of uterine fibroid prolapse or expulsion in women with known or suspected submucosal uterine fibroids. Monitor lipid levels; consider discontinuing if hypertriglyceridemia or hypercholesterolemia worsens. Diabetes. Prediabetes. Hypothyroidism. Hypoadrenalism. Reduced ability to recognize pregnancy. Perform pregnancy testing if suspected; discontinue if confirmed. Advise women of reproductive potential to use effective non-hormonal contraception during and for 1 week after discontinuation. Nursing mothers.

Myfembree Pharmacokinetics

See Literature

Myfembree Interactions

Interactions

Avoid concomitant use with hormonal contraceptives. Potentiated by oral P-gp inhibitors: avoid; if unavoidable, take Myfembree first, separate dosing by at least 6hrs; monitor for adverse reactions. Antagonized by combined P-gp and strong CYP3A inducers (eg, rifampin): avoid. May affect levels of thyroid-binding globulin, corticosteroid-binding globulin, coagulation factors, sex hormone binding globulin, lipids, glucose.

Myfembree Adverse Reactions

Adverse Reactions

Vasomotor symptoms, uterine bleeding, alopecia, decreased libido; for endometriosis: also headache, mood disorders, nausea, toothache, back pain, decreased sexual desire and arousal, arthralgia, fatigue, dizziness; uterine expulsion or prolapse, menorrhagia, cholecystitis, pelvic, pain, bone loss, elevated hepatic transaminase, elevated lipids, hypertension, depression-related adverse reactions, mood changes, hypersensitivity reactions (discontinue if occurs).

Myfembree Clinical Trials

See Literature

Myfembree Note

Not Applicable

Myfembree Patient Counseling

See Literature

Images