Usual Adult Dose for Uterine Fibroids

One capsule orally twice a day

• Morning capsule contains elagolix 300 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg
• Evening capsule contains elagolix 300 mg

Duration of therapy: 24 months

Comments:

• Rule out pregnancy prior to starting therapy or start therapy within 7 days from the onset of menses.
• Take capsules twice a day at approximately the same time each day.
• Duration of use should be limited to 24-months due to risk of bone loss.

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

Renal Dose Adjustments

No adjustment recommended

Liver Dose Adjustments

Contraindicated in women with any hepatic impairment or disease

Precautions

US BOXED WARNING(S): THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS

• Estrogen and progestin combinations increase the risk of thrombotic or thromboembolic disorders including pulmonary embolism, deep vein thrombosis, stroke and myocardial infarction, especially in women at increased risk for these events
• This drug is contraindicated in women with current or a history of thrombotic or thromboembolic disorders and in women at increased risk for these events, including women over 35 years of age who smoke and women with uncontrolled hypertension

CONTRAINDICATIONS:

• Known anaphylactic reaction, angioedema, or hypersensitivity to this drug or any of its components
• Women at high risk of arterial, venous thrombotic, or thromboembolic disorders including:
• over 35 years of age who smoke
• a current or history of deep vein thrombosis or pulmonary embolism
• vascular disease (e.g., cerebrovascular disease, coronary artery disease, peripheral vascular disease)
• thrombogenic valvular or thrombogenic rhythm diseases of the heart (for example, subacute bacterial endocarditis with valvular disease, or atrial fibrillation)
• inherited or acquired hypercoagulopathies
• uncontrolled hypertension
• headaches with focal neurological symptoms or women over 35 years having migraine headaches with aura
• Pregnancy; exposure early in pregnancy may increase the risk of early pregnancy loss
• Osteoporosis (risk of further bone loss)
• A current or history of breast cancer or other hormonally sensitive malignancies, and those with increased risk for hormonally sensitive malignancies
• Known hepatic impairment or disease
• Undiagnosed abnormal uterine bleeding
• Concomitant use of inhibitors of organic anion transporting polypeptide (OATP)1B1 that are known or expected to significantly increase elagolix plasma concentrations

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

Consult WARNINGS section for additional precautions.

Dialysis

No adjustment recommended

Other Comments

Administration advice:

• Take orally twice a day at approximately the same time each day
• May take with or without food

MISSED DOSE: If a dose is missed, take within 4 hours of the time it would have been taken and then take the next dose at the usual time; if more than 4 hours have elapsed since the dose should have been taken, skip the missed dose and take the next dose at the usual time

PACKAGING:

• Product is packaged for use in weekly blister packs; morning capsules are white and yellow (EL300 AM) and formulated with elagolix 300 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg; evening capsules are white and light blue (EL300 PM) and contain elagolix 300 mg/capsule
• Unused medication should be disposed of via a take-back program or following FDA instructions for disposing of medication in household trash; capsules should not be flushed.

General:

• Supplementary calcium and vitamin D may be beneficial if dietary intake of calcium and vitamin D is not adequate.

Monitoring:

• Monitor blood pressure
• Blood glucose monitoring may need to be performed more frequently in women with prediabetes and diabetes
• Monitor lipid levels

Patient advice:

• Patients should be instructed to read the US FDA-approved patient labeling (Medication Guide).
• Patients should understand the use of combination estrogen and progestin may increase the risk of thromboembolic disorders and if symptoms of heart attack, stroke, or blood clot develop, this drug should be stopped and they should seek immediate medical attention.
• Patients should understand that changes in menstrual bleeding during therapy may reduce the ability to recognized pregnancy; if pregnancy is suspected a pregnancy test should be performed and if pregnancy is confirmed, therapy should be discontinued.
• Patients should be advised to use non-hormonal contraception during therapy and for 28 days after stopping this drug.
• Patients should be instructed to report any signs or symptoms of liver injury such as jaundice, any changes or worsening in depression, or other mood changes.
• Patients should understand there is a risk of bone loss and adequate calcium and vitamin D intake should be encouraged.
• Patients should be advised to dispose of unused medication via a take-back option if possible. Otherwise, follow FDA instructions for disposing of in household trash (www.fda.gov/drugdisposal); do not flush down the toilet.