estradiol/norgestimate (Rx)

Brand and Other Names:Cilest, Prefest
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Dosing & Uses

AdultPediatricGeriatric

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

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Interactions

Interaction Checker

and estradiol/norgestimate

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            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 (10)

              • 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.

              • 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.

              Minor (0)

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                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
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                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

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                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.

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                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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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.