Oriahnn Generic Name & Formulations
Legal Class
Rx
General Description
Elagolix 300mg, estradiol 1mg, norethindrone acetate 0.5mg; per cap; with elagolix 300mg; cap.
Pharmacological Class
GnRH antagonist + estrogen + progestin.
How Supplied
Caps—56 (14 weekly blister packs x 4)
Manufacturer
Generic Availability
NO
Mechanism of Action
Elagolix inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Elagolix treatment results in dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased blood concentrations of the ovarian sex hormones estradiol and progesterone and reduces bleeding associated with uterine fibroids. Estradiol binds to nuclear receptors that are expressed in estrogen-responsive tissues, which may reduce the increase in bone resorption and resultant bone loss that can occur due to a decrease in circulating estrogen from elagolix alone. Norethindrone acetate binds to nuclear receptors that are expressed in progesterone-responsive tissues, which may protect the uterus from the potential adverse endometrial effects of unopposed estrogen.
Oriahnn 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.
Oriahnn Dosage and Administration
Adult
Exclude pregnancy prior to starting or begin within 7 days from onset of menses. Take at same time each day. AM: 1 cap (300mg/1mg/0.5mg) daily. PM: 1 cap (300mg) daily.
Children
Not established.
Oriahnn 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. Concomitant OATP1B1 inhibitors that are known or suspected to potentiate elagolix.
Oriahnn Boxed Warnings
Boxed Warning
Thromboembolic disorders. Vascular events.
Oriahnn Warnings/Precautions
Warnings/Precautions
Increased risk of thrombotic or thromboembolic disorders. Discontinue if thrombotic, cardiovascular or cerebrovascular event, unexplained visual changes, 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. Gallbladder disease. History of cholestatic jaundice associated with prior estrogen use or with pregnancy. 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 to use non-hormonal contraception during and for 28 days after discontinuation. Nursing mothers.
Oriahnn Pharmacokinetics
Distribution
Plasma protein bound: 80% (elagolix); 98% (estradiol); 97% (norethindrone).
Elimination
Elagolix: fecal (90%), renal (<3%).
Half-life: 5.9 hours ± 2.1 (elagolix); 14.5 hours ± 6.6 (estradiol); 9.2 hours ± 4.0 (norethindrone).
Oriahnn Interactions
Interactions
See Contraindications. May potentiate P-gp substrates (eg, digoxin; monitor), CYP2C19 substrates (eg, omeprazole; limit doses to ≤40mg daily). May antagonize CYP3A substrates. Antagonizes oral midazolam, rosuvastatin: consider increasing their doses. May be antagonized by strong CYP3A inducers. May be potentiated by strong CYP3A inhibitors, rifampin: not recommended. May affect levels of thyroid-binding globulin, corticosteroid-binding globulin, coagulation factors, sex hormone binding globulin, lipids, glucose.
Oriahnn Adverse Reactions
Adverse Reactions
Hot flushes, headache, fatigue, metrorrhagia; bone loss, elevated hepatic transaminase, elevated lipids, hypertension, depression-related adverse reactions, mood changes, alopecia.
Oriahnn Clinical Trials
See Literature
Oriahnn Note
Notes
To enroll patients in the Pregnancy Exposure Registry: call (833) 782-7241 or visit www.bloompregnancyregistry.com.
Oriahnn Patient Counseling
See Literature
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