REMS
Contraindicated in:
Women >35 yr who smoke
;Current or history of deep vein thrombosis or pulmonary embolism
;Cerebrovascular disease, cardiovascular disease, or peripheral vascular disease
;Subacute bacterial endocarditis with valvular disease or atrial fibrillation
;Inherited or acquired hypercoagulopathies
;Uncontrolled hypertension
;Headaches with focal neurological symptoms or migraine headaches with aura if >35 yr
;Use Cautiously in:
CV: DEEP VEIN THROMBOSIS, edema, hypertension, MI
Derm: hot flush, hyperhidrosis, night sweats, alopecia
Endo: hyperglycemia
GI: ↑liver enzymes, cholecystitis, diarrhea, dyspepsia, nausea
GU: ↓libido, amenorrhea, uterine bleeding, uterine fibroid expulsion/prolapse, vulvovaginal dryness
MS: ↓bone mineral density, arthralgia
Neuro: headache, anxiety, depression, dizziness, fatigue, irritability, STROKE, SUICIDAL THOUGHTS/BEHAVIORS
Resp: PULMONARY EMBOLISM
Misc: BREAST CANCER, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)
Drug-drug:
Therapeutic Classification: hormones
Pharmacologic Classification: gnrh antagonist, estrogens, progestins
Relugolix
Absorption: 12% absorbed following oral administration.
Distribution: Unknown.
Half-Life: 61 hr.
Estradiol
Absorption: Well absorbed following oral administration.
Distribution: Widely distributed to tissues.
Half-Life: 16.6 hr.
Norethindrone
Absorption: Rapidly absorbed following oral administration.
Distribution: Widely distributed to tissues.
Half-Life: 89 hr.
(plasma concentrations)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO (relugolix) | unknown | 2 hr | unknown |
| PO (estradiol) | unknown | 7 hr | unknown |
| PO (norethindrone) | unknown | 1 hr | unknown |
Advise patient to notify health care provider immediately if signs and symptoms of thromboembolism (leg pain or swelling; sudden shortness of breath; double vision; bulging of eyes; sudden blindness; pain or pressure in chest, arm, or jaw; sudden, severe headache; weakness or numbness in arm or leg; trouble speaking) occur.