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estradiol (Rx)Brand and Other Names:Estrace, Vivelle-Dot, more...Vagifem, Delestrogen, DepoEstradiol, Divigel, Elestrin, Alora, Estrace Cream, Estrace Vaginal, Estraderm Transdermal, Estring, estradiol intravaginal, estradiol topical, Estradot, Estrasorb, Estrogel, Evamist, Femtrace, Femring, Menostar, Minivelle, Vivelle, Climara

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

gel

  • 0.06%
  • 0.1%

injectable solution

  • 5mg/mL
  • 10mg/mL
  • 20mg/mL
  • 40mg/mL

tablet

  • 0.45mg (as acetate)
  • 0.5mg
  • 0.9mg (as acetate)
  • 1mg
  • 1.5mg
  • 2mg

transdermal patch

  • 0.025mg
  • 0.0375mg
  • 0.05mg
  • 0.06mg
  • 0.075mg
  • 0.1mg

topical emulsion

  • 4.35mg/1.74g (0.25%)

vaginal cream

  • 0.01%

vaginal ring

  • 0.05mg/24hr
  • 0.1mg/24hr

vaginal tablet

  • 10mcg
  • 25mcg
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Vulvar and Vaginal Atrophy in Menopause

Estrace: 1-2 mg PO once daily for 3 weeks, followed by 1 week off

Valerate: 10-20 mg IM q4weeks

Femring: 0.05 mg intravaginally; ring should remain in place for 3 months; increase dose to 0.1 mg if necessary

EstroGel: 1.25 g/day 3 weeks on, 1 week off

Alora, Climara Vivelle-Dot, Estraderm: Use transdermally and follow product-specific directions

Prevention of osteoporosis: 0.5 mg PO once daily for 3 weeks, followed by 1 week off

Metastatic breast cancer: 10 mg PO q8hr for 3 months

Prostate cancer: 1-2 mg PO q8hr for ≥3 months

Hypoestrogenism from Castration, Hypogonadonism, or Ovarian Failure

PO (Estrace): 1-2 mg PO qDay; titrate to use minimal effective dose

Transdermal (Alora, Estraderm, Climara, Vivelle-Dot, Minivelle): Use transdermally and follow product-specific directions

Valerate: 10-20 mg IM q4week

Metastatic Breast Cancer

Estrace: 10 mg PO 3 times daily

Hypoestrogenism

Cypionate: 1.5-2 mg IM every 4 weeks

Osteoporosis

PO (Estrace): 0.5 mg/day for 23 days of 28 day cycle used in clinical studies

Transdermal (Alora, Menostar, Estraderm, Vivell-Dot, Minivelle): Follow product specific directions

Vasomotor Symptoms Associated with Menopause

Estrace: 1-2 mg/day 3 weeks on, 1 week off

Valerate: 10-20 mg IM q3-4weeks

Cypionate: 1-5 mg IM q3-4weeks

Estrasorb: 3.48 g of emulsion applied qDay in the morning

Elestrin: 0.87 g/day gel applied at the same time each day; use patient's response to adjust dose

Divigel: 0.25 g/day gel; adjust dose based on patient response

EstroGel: 1.25 g/day gel applied at the same time each day

Prostate Cancer

Estrace: 1-2 mg PO three times daily

Valerate: 30 mg IM or more q1-2weeks

Estrogen Replacement in Turner Syndrome (Orphan)

Orphan indication sponsor

  • Ascend Therapeutics, Inc, 607 Herndon Parkway, Suite 110, Herndon, VA 21070

Safety and efficacy not established

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Interactions

Interaction Checker

estradiol and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Anxiety

            Abdominal cramping

            Amenorrhea

            Bloating

            Breakthrough bleeding

            Breast enlargement

            Breast tenderness

            Delayed ejaculation

            Depression

            Dry mouth

            Headache

            Hypertension

            Impotency

            Influenza

            Leukorrhea

            Melasma

            Muscle cramps

            Nausea

            Nervousness

            Peripheral edema

            Polydipsia

            Pruritus

            Rash

            Swelling

            Skin irritation and redness at application site (transdermal)

            Spotting

            Syncope

            Toothache

            Vaginal discomfort, vaginal erosion, vaginal ulceration, adherence of the vaginal ring to the vaginal wall (Estring)

            Vomiting

            Weight changes

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            Warnings

            Black Box Warnings

            Increased risk of endometrial cancer

            • Close clinical surveillance of all women taking estrogens is important
            • Risk of endometrial cancer increases with use of unopposed estrogens; adding progestin to estrogen therapy may reduce risk of endometrial hyperplasia, a precursor to endometrial cancer;
            • Adequate diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding

            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 embolism (PE), and deep vein thrombosis (DVT) in postmenopausal women (50-79 years) during 5.6 years of treatment with daily PO conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) in comparison with placebo
            • Estrogens alone: Substudy of WHI study reported increased risk of stroke and DVT in postmenopausal women (50-79 years) during 6.8 years of treatment with PO conjugated estrogens (0.625 mg/day) alone in comparison with placebo

            Dementia risks

            • Estrogens with and without progestins should not be used to prevent dementia
            • Women's Health Initiative Memory Study (WHIMS), substudy of WHI study, reported increased risk of developing probable dementia in postmenopausal women ≥65 years during 4 years of treatment with daily PO conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) in comparison with placebo
            • Estrogens alone: Substudy of WHIMS reported increased risk of developing probable dementia in postmenopausal women ≥65 years during 5.2 years of treatment with conjugated estrogens (0.625 mg/day) alone in comparison with placebo
            • Unknown whether these findings apply to younger postmenopausal women

            Breast cancer

            • The WHI estrogen plus progestin substudy also demonstrated an increased risk of invasive breast cancer; estrogens with or without progestins should be prescribed at the lowest doses and for the shortest duration

            Dose & duration

            • In the absence of comparable data, these risks should be assumed to be similar for other doses of conjugated estrogens and medroxyprogesterone acetate, as well as for 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

            Unintentional secondary exposure to transdermal products

            • Breast budding, breast masses in prepubertal females, and gynecomastia in prepubertal males have been reported after unintentional secondary exposure

            Contraindications

            Documented hypersensitivity

            Known anaphylactic reaction or angioedema with topical emulsion

            Known protein C, protein S, or antithrombin deficiency or other known thrombophilic disorder

            Active or previous breast cancer

            Arterial thromboembolic disease (stroke, myocardial infarction [MI]), thrombophlebitis, DVT/PE, thrombogenic valvular disease

            Estrogen-dependent neoplasia

            Uncontrolled hypertension, diabetes mellitus with vascular involvement, jaundice with previous oral contraceptive (OC) use

            Undiagnosed abnormal vaginal bleeding

            Liver disease, liver tumors

            Porphyria (Vagifem)

            Cautions

            Severe anaphylactic reactions including hives , pruritus, swollen lips-tong-face, respiratory compromise, abdominal pain, vomiting during transdermal treatment reported

            Family history of breast cancer or DVT/PE; current or previous depression, endometriosis, diabetes mellitus, hypertension, bone mineral density changes, renal or hepatic impairment, bone metabolic disease, systemic lupus erythematosus; conditions exacerbated by fluid retention (eg, migraine, asthma, epilepsy)

            Discontinue if the following develop: Jaundice, visual problems (may cause contact lens intolerance), any signs of venous thromboembolism, migraine with unusual severity, significang blood pressure increase, severe depression, increased risk of thromboembolic complications after surgery

            Discontinue 4 weeks before major surgery or prolonged immobilization

            Patients on warfarin or other oral anticoagulants (increase in anticoagulant dose may be warranted)

            Some studies link OC use with increased risk of breast cancer, whereas other studies have not shown any change in risk; risk depends on conditions where naturally high hormone levels persist for long periods, including early-onset menstruation (<12 years), late-onset menopause (>55 years), first child after age 30 years, nulliparity

            Increased risk of cervical cancer with OC use; however human papillomavirus (HPV) remains main risk factor for this cancer; evidence suggests long-term (≥5 years) use of OCs may be associated with increased risk

            Increased risk of liver cancer with OC use; risk increases with longer duration of use

            Hypercalcemia may occur in patients with breast cancer or bone metastases

            Exogenous estrogens may exacerbate symptoms of angioedema in women with hereditary angioedema

            Angioedema involving eye/eyelid, face, larynx, pharynx, tongue and extremity (hands, legs, ankles, and fingers) with or without urticaria reported; discontinue therapy permanently if angioedema occurs

            Femring is more potent than Estring and should be used with progesterone therapy to prevent endometrial hyperplasia

            Caution regarding unintentional exposure in children (see Black Box Warnings)

            Risk of endometrial cancer increases with use of unopposed estrogens (see Black Box Warnings)

            An increased risk of invasive breast cancer reported with estrogen plus progestin in WHI substury; estrogens with or without progestins should be prescribed at lowest doses and for shortest duration

            There is no evidence that the use of "natural" estrogens results in different endometrial risk profile from use of synthetic estrogens at equivalent estrogen doses

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            Pregnancy & Lactation

            Pregnancy category: X

            Lactation: Drug 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

            Mechanism of Action

            Endogenous estrogen; reduces release of gonadotropin-releasing hormone and luteinizing hormone-releasing hormone from hypothalamus; reduces gonadotropin release from pituitary; increases synthesis of DNA, RNA, and various proteins in target tissues

            Absorption

            Readily absorbed through GI tract, skin, mucous membrane

            Onset: PO, 2-4 weeks; transdermal, 4 hr

            Duration: Estradiol valerate, 7-8 days; estradiol cypionate, 11 days

            Distribution

            Widely distributed

            Protein bound: To globulin and albumin

            Elimination

            Half-life: 1.5-5 hr (IM); 4 hr (transdermal)

            Excretion: Mainly in urine (as conjugates with small amount of unchanged drug); most estrogens are also excreted in bile and undergo enterohepatic recycling

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            Images

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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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