Overview
11 DESCRIPTION ORIAHNN consists of two capsules: one to be taken orally in the morning (AM) and one to be taken orally in the evening (PM). The AM capsule is white and yellow and contains 300 mg elagolix (equivalent to 310.4 mg of elagolix sodium), 1 mg estradiol, and 0.5 mg norethindrone acetate.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action ORIAHNN combines elagolix and estradiol/norethindrone acetate (E2/NETA), a combination of estrogen and progestin. Elagolix is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of elagolix 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. E2 acts by binding to nuclear receptors that are expressed in estrogen-responsive tissues.
Indications
- 1 INDICATIONS AND USAGE ORIAHNN is indicated for the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women. Limitation of Use: Use of ORIAHNN should be limited to 24 months due to the risk of continued bone loss, which may not be reversible [see Dosage and Administration ( 2.1 ) and Warnings and Precautions ( 5.2 ) ] . ORIAHNN is a combination of elagolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, estradiol, an estrogen, and norethindrone acetate, a progestin, indicated for the management of heavy menstrual bleeding...
Common Doses
- 300 mg
- 1 mg
- 0.5 mg
Dosage
2 DOSAGE AND ADMINISTRATION One capsule (elagolix 300 mg, estradiol 1 mg, norethindrone acetate 0.5 mg) in the morning and one capsule (elagolix 300 mg) in the evening for up to 24 months. ( 2.1 ) 2.1 Important Dosing Information Exclude pregnancy before starting ORIAHNN or start ORIAHNN within 7 days from the onset of menses [see Use in Specific Populations ( 8.1 ) and ( 8.3 ) ] . The recommended dosage of ORIAHNN is: ○ One elagolix 300 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg capsule in the morning (AM), and ○ One elagolix 300 mg capsule in the evening (PM).
Black Box Warning
WARNING: THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS Estrogen and progestin combinations, including ORIAHNN, 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 [see Warnings and Precautions ( 5.1 )] . ORIAHNN 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 [see...
Contraindications
- 4 CONTRAINDICATIONS ORIAHNN is contraindicated in women: With a high risk of arterial, venous thrombotic, or thromboembolic disorders [see Boxed Warning and Warnings and Precautions ( 5.1 ) ] . 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 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...
Side Effects
- 6 ADVERSE REACTIONS The following serious adverse reactions are discussed elsewhere in labeling: Thromboembolic Disorders and Vascular Events [see Warnings and Precautions ( 5.1 ) ] Bone Loss [see Warnings and Precautions ( 5.2 ) ] Suicidal Ideation, Suicidal Behavior, and Exacerbation of Mood Disorders [see Warnings and Precautions ( 5.4 ) ] Hepatic Transaminase Elevations [see Warnings and Precautions ( 5.5 ) ] Elevated Blood Pressure [see Warnings and Precautions ( 5.6 ) ] Effects on Carbohydrate and Lipid Metabolism [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS See full prescribing information for a list of clinically important drug interactions. ( 7 ) 7.1 Potential for ORIAHNN to Affect Other Drugs Elagolix (a component of ORIAHNN) is: A weak to moderate inducer of cytochrome P450 (CYP3A). Co-administration with ORIAHNN may decrease plasma concentrations of drugs that are substrates of CYP3A. A weak inhibitor of CYP2C19. Co-administration with ORIAHNN may increase plasma concentrations of drugs that are substrates of CYP2C19 (see Table 3). An inhibitor of efflux transporter P-glycoprotein (P-gp).