Dosing & Uses
Dosage Forms & Strengths
estradiol/norgestimate
tablet
- Pink: 1mg (15 tabs)
- White: 1mg/0.09mg (15 tabs)
Hormone Replacement Therapy
1 pink tablet PO qDay for 3 days
Followed by 1 white tab PO qDay for 3 days, then repeat
Other Indications & Uses
Treatment of moderate to severe vasomotor symptoms in menopause with an intact uterus, prevention of osteoporosis in postmenopausal women with an intact uterus, vulvar and vaginal atrophy in women with an intact uterus
Off-label: postmenopausal hypercholesterolemia
Not recommended
Hormone replacement therapy
1 pink tablet PO qDay for 3 days
Followed by 1 white tab PO qDay for 3 days, then repeat
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (1)
- darunavir
darunavir will decrease the level or effect of norgestimate by unspecified interaction mechanism. Avoid or Use Alternate Drug.
Monitor Closely (12)
- albiglutide
norgestimate decreases effects of albiglutide by pharmacodynamic antagonism. Use Caution/Monitor. Oral contraceptives may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.
- atazanavir
atazanavir, norgestimate. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Atazanavir may increase or decrease levels of norgestimate. Use alternatives if available.
- carbamazepine
carbamazepine will decrease the level or effect of norgestimate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Advise patients to use alternative contraceptive method during coadministration; continue alternative contraception for 28 days after discontinuing therapy to ensure contraception reliability
- clobazam
clobazam will decrease the level or effect of norgestimate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Clobazam is a weak CYP3A4 inducer; effectiveness of hormonal contraceptives may be diminished when given concurrently with clobazam. Additional non-hormonal forms of contraception are recommended.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF, norgestimate. Other (see comment). Modify Therapy/Monitor Closely. Comment: Increases norgestimate levels and may result in insulin resistance, dyslipidemia, acne, and venous thrombosis; decreases ethinyl estradiol levels that may result in decreased efficacy.
- lamotrigine
norgestimate will decrease the level or effect of lamotrigine by increasing hepatic clearance. Use Caution/Monitor. Combination oral contraceptives have been shown to significantly decrease plasma concentrations of lamotrigine, likely due to induction of lamotrigine glucuronidation.
- liraglutide
norgestimate decreases effects of liraglutide by pharmacodynamic antagonism. Use Caution/Monitor. Oral contraceptives may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.
- maraviroc
norgestimate increases levels of maraviroc by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity.
- metformin
norgestimate decreases effects of metformin by pharmacodynamic antagonism. Use Caution/Monitor.
- mifepristone
mifepristone decreases effects of norgestimate by pharmacodynamic antagonism. Use Caution/Monitor. Backup contraceptive method recommended.
- siltuximab
siltuximab, norgestimate. Other (see comment). Use Caution/Monitor. Comment: CYP450 activity in the liver is down regulated by infection and inflammation stimuli including cytokines (eg, IL-6); inhibition of IL-6 by siltuximab may restore CYP450 enzymatic activity; caution if coadministered with CYP substrates that have a narrow therapeutic index.
- warfarin
norgestimate increases effects of warfarin by unspecified interaction mechanism. Use Caution/Monitor.
Minor (0)
Adverse Effects
Frequency Not Defined
Common
- Headache
- Breast pain
- Abdominal pain
- Back pain
- URI
- Influenza-like symptoms
Less common
- Cardiovascular disease
- Deep vein thrombosis
- Hypertension
- Breast cancer
- Endometrial neoplasia
- Gallbladder disease
Warnings
Black Box Warnings
Cardiovascular risks
- Estrogens with and without progestins should not be used to prevent cardiovascular disease
- Estrogens plus progestins: Women’s Health Initiative (WHI) Estrogen Plus Progestin substudy reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis (DVT) in postmenopausal women (aged 50-79 yr) during 5.6 yr of treatment with daily PO conjugated estrogens (CE 0.625 mg) combined with medroxyprogesterone acetate (MPA 2.5 mg) compared with placebo
- Estrogens alone: The estrogen alone substudy of the WHI Study reported increased risks of stroke and DVT in postmenopausal women (aged 50-79 yr) during 6.8 yr of treatment with oral conjugated estrogens (0.625 mg/day) alone compared with placebo
Dementia risks
- Estrogens with and without progestins should not be used to prevent dementia
- Women's Health Initiative Memory Study (WHIMS), a substudy of the WHI study, reported increased risk of developing probable dementia in postmenopausal women aged 65 yr or older during 4 yr of treatment w/ daily CE 0.625 mg combined with MPA 2.5 mg, compared with placebo
- Estrogens alone: A substudy of the WHIMS reported an increased risk of developing probable dementia in postmenopausal women aged 65 yr or older during 5.2 yr of treatment with conjugated estrogens 0.625 mg alone compared with placebo
- Unknown whether these findings apply to younger postmenopausal women
Dose & Duration
- In the absence of comparable data, these risks should be assumed to be similar for other doses of CE and MPA and other combinations and dosage forms of estrogens and progestins
- Because of these risks, estrogens with or without progestins should be prescribed at lowest effective dose and for shortest duration consistent with treatment goals and individual risks
Contraindications
Hypersensitivity
Pregnancy
Estrogen-dependent neoplasia
Current/history of: DVT/PE, arterial thromboembolic disease, breast cancer, liver disease/tumours
Undiagnosed abnormal vaginal bleeding
Jaundice with previous OCP use
Porphyria
History of pruritus gravidarum, pemphigoid gestationis, deterioration of otosclerosis or idiopathic jaundice during pregnancy
Untreated endometrial hyperplasia
Cautions
Bone mineral density changes, current/history of depression, DM, HTN, hyperlipidemia, hypertriglyceridemia, obesity, endometriosis, family history of breast cancer and DVT/PE, smoking, epilepsy, migraine, renal impairment, severe hypocalcemia, ovarian cancer
Discontinue if the following develop: jaundice, visual problems, 4-6 wk before major surgery, any symptoms of VTE, massive BP increases, unusually severe migraines or first-time migraines, depression
Increased risk of post-op thromboembolic complications
Conditions exacerbated by fluid retention (eg, asthma, migraine, cardiac/renal dysfunction, epilepsy)
Patients on warfarin/oral anticoagulants: Estrogens increase thromboembolic risk; increase in anticoagulant dose may be warranted
History of migraine with aura
Cholelithiasis
Risk of developing dementia
Monitor blood pressure
Pregnancy & Lactation
Pregnancy Category: X
Lactation: enters breast milk; use with caution
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
See estradiol combos for further details
Mechanism of Action
Estradiol: endogenous estrogen; reduces the release of gonadotropin-releasing hormone from hypothalamus, reduces release of LH and FSH from pituitary gland; increases synthesis of DNA, RNA, and various proteins in target tissues. Estrogen replacement reduces elevated levels of estrogen and progesterone LH and FSH in postmenopausal women
Norgestimate: Progestin; inhibits secretion of gonadotropins from pituitary gland; prevents follicular maturation and ovulation, stimulates growth of mamary tissues
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Formulary
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