estrogens esterified (Rx)

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Brand and Other Names:Estrogens, Esterified, Menest

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 0.3mg
  • 0.625mg
  • 1.25mg
  • 2.5mg
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Menopause, Atrophic Vaginitis, Kraurosis Vulvae

0.3-1.25 mg PO qDay (3 weeks on, 1 week off)

Female Hypogonadism

2.5-7.5 mg PO qDay in divided doses (20 days on, 10 days off)

Female Castration/Primary Ovarian Failure

1.25 mg PO qDay in cyclic regimen

Breast Cancer

10 mg PO q8hr for 3 months (minimum)

Prostate Cancer

1.25-2.5 mg PO q8hr

Other Indications & Uses

Vasomotor symptoms associated with menopause

Palliative treatment of metastatic inoperable breast cancer in men & postmenopausal women

Palliative treatment of prostate cancer

Safety & efficacy not established

Menopause, atrophic vaginitis, kraurosis vulvae

0.3-1.25 mg PO qDay (3 weeks on, 1 week off)

Breast cancer

10 mg PO q8hr for 3 months (minimum)

Prostate cancer

1.25-2.5 mg PO q8hr

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Interactions

Interaction Checker

and estrogens esterified

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

            Common

            • Edema, peripheral edema
            • Headache
            • Melasma
            • Breast enlargement, breast tenderness
            • Bloating
            • Nausea
            • Vomiting

            Less common

            • Depression
            • Amenorrhea
            • Breakthrough bleeding
            • Spotting
            • Weight changes
            • Corneal curvation change
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            Warnings

            Black Box Warnings

            Estrogens increase risk of endometrial cancer

            • Close clinical surveillance of all women taking estrogens is important
            • 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
            • There is no evidence that the use of "natural" estrogens results in a different endometrial risk profile than synthetic estrogens at equivalent estrogen doses

            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 year) during 5.6 yr of treatment w/ daily PO conjugated estrogens (CE 0.625 mg) combined w/ medroxyprogesterone acetate (MPA 2.5 mg) compared with placebo
            • Estrogens alone: A substudy of the WHI Study reported increased risk for stroke and DVT in postmenopausal women (aged 50-79 yr) during 6.8 year 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 with daily CE 0.625 mg combined w/ 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 & dosage forms of estrogens & progestins
            • Because of these risks, estrogens with or without progestins should be prescribed at lowest effective dose & for shortest duration consistent w/ treatment goals and individual risks

            Contraindications

            Documented hypersensitivity

            Active or history of breast cancer

            Arterial thromboembolic disease (stroke, MI), thrombophlebitis, DVT/PE, thrombogenic valvular disease

            Estrogen-dependent neoplasia, liver disease, liver tumors

            Uncontrolled hypertension

            Diabetes mellitus with vascular involvement

            Jaundice with prior oral contraceptive use

            Undiagnosed abnormal genital bleeding

            Cautions

            Diabetes mellitus, endometriosis, hyperlipidemias, HTN, hypothyroidism, liver impairment, uterine leiomyomata, smoking, porphyria, patients with defects of lipoprotein metabolism, hypertriglyceridemia, hypothyroidism, ovarian cancer, exacerbation of endometriosis or other conditions

            Conditions exacerbated by fluid retention (asthma, epilepsy, migraine etc)

            Hypercalcemia may occur in patients with breast cancer and bone metastases

            Long-term postmenopausal estrogen treatment has been associated with an increased risk of breast cancer, MI, stroke, DVT, PE, and dementia

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

            Concomitant warfarin, oral anticoagulants: estrogens increase risk of thromboembolic disorders; may need to increase anticoagulant dose

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            Pregnancy & Lactation

            Pregnancy Category: X

            Lactation: Controversial; estrogens are excreted into breast milk in small quantities, use 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

            Mixture of sodium salts and sulfate esters of estrogenic substances, principally estrone sodium sulfate; reduces LHRH release from hypothalamus, reduces gonadotropin release from pituitary; increase synthesis of DNA, RNA, and various proteins in target tissues

            Pharmacokinetics

            Protein Bound: 50-80%

            Metabolism: Principally and rapidly in liver and undergoes extensive first-pass metabolism to less active products such as estriol; kidneys, gonads, and muscle tissues may be involved in metabolism to some extent

            Metabolites: Estriol

            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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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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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.
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            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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