drospirenone/estradiol (Rx)

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Brand and Other Names:Angeliq

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

drospirenone/estradiol

tablet

  • 0.25mg/0.5mg
  • 0.5mg/1mg
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Hormone Replacement Therapy

1 tablet PO daily

Use the lowest dose that will control symptoms

Renal Impairment

Do not administer

Hepatic Impairment

Do not administer

Other Indications & Uses

Hormone replacement therapy for women with intact uterus: Treatment of menopause-associated hot flashes and vulvar/vaginal atrophy

Safety and efficacy not established

Hormone replacement therapy

1 tablet PO daily

Use the lowest dose that will control symptoms

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Interactions

Interaction Checker

and drospirenone/estradiol

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Breast pain (19%)

            Upper respiratory infection (19%)

            Abdominal pain (11%)

            1-10%

            Edema

            Peripheral edema

            Headache

            Accidental injury, back pain, pain in extremity

            Endometrial disorder

            Leukorrhea

            Vaginal hemorrhage

            Abdominal enlargement

            Flu syndrome

            Sinusitis

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            Warnings

            Contraindications

            Hypersensitivity

            Known anaphylactic reaction or angioedema

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

            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

            Hepatic/renal/adrenal impairment

            Cautions

            Bone mineral density changes, current/history of depression, DM, HTN, hyperlipidemia, obesity, endometriosis, family history of breast cancer and DVT/PE, smoking

            Discontinue if the following develop: jaundice, visual problems, 4-6 wk before major surgery, any symptoms of VTE, massive BP increase, unusually severe migraines or first-time migraines, depression

            Increased risk of post-op thromboembolic complications, arterial/venous thromboembolic disorder, hyperkalemia, exacerbation of endometriosis

            Consider monitoring serum potassium concentrations during first month of dosing in high-risk patients who take strong CYP3A4 inhibitors long-term and concomitantly

            Conditions exacerbated by fluid retention (eg, asthma, migraine, cardiac/renal dysfunction, epilepsy)

            Patients on warfarin/oral anticoagulants: oestrogens increase thromboembolic risk; increase in anticoagulant dose may be warranted

            History of migraine with aura

            Cholelithiasis

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

            Consider topical vaginal products when used solely for vulvovaginal atrophy

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            Pregnancy & Lactation

            Pregnancy Category: contraindicated in pregnancy

            Lactation: enters breast milk/not recommended

            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

            Estradiol: Endogenous estrogen; reduces the release of gonadotropin-releasing hormone from hypothalamus, reduces release of luteinizing hormone (LH) and follicle stimulating hormone (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

            Drospirenone: Progestin; spironolactone analog with antimineralocorticoid and antiandrogenic activity

            Pharmacokinetics

            Half-Life elimination: 36-42 hr (drospirenone)

            Vd: 4.2 L/kg (drospirenone)

            Metabolism: Hepatic

            Bioavailability: 76-85% (drosperidone)

            Metabolites: Inactive

            Excretion: Urine, feces

            Peak plasma time

            • Drospirenone: 1 hr
            • Estradiol: 6-8 hr

            Peak plasma concentration

            • Drospirenone: 13-24 ng/mL
            • Estradiol: 34-54 pg/mL

            Protein bound

            • Drospirenone: 97% bound to serum proteins (not SHBG or corticosteroid binding globulin)
            • Estradiol: 98% (37% to globulin and 61% to albumin)
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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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