Dosing & Uses
Dosage Forms & Strengths
drospirenone/estradiol
tablet
- 0.25mg/0.5mg
- 0.5mg/1mg
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
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

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
Warnings
Contraindications
Hypersensitivity
Undiagnosed abnormal genital bleeding
Known, suspected, or history of cancer of the breast
Known or suspected estrogen-dependent neoplasia
Active DVT, PE, or a history of these conditions
Active arterial thromboembolic disease (for example, stroke and MI), or history of these conditions
Renal impairment
Known liver impairment or disease
Adrenal insufficiency
Known or suspected pregnancy
Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders
Known anaphylactic reaction, angioedema, or hypersensitivity
Cautions
Use caution in bone mineral density changes, current/history of depression, DM, HTN, hyperlipidemia, obesity, endometriosis, family history of breast cancer, 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
Do not use with conditions that predispose to hyperkalemia
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
Increased risk of ovarian cancer reported in women who used hormonal therapy for menopausal symptoms
Manage appropriately risk factors for arterial vascular disease (e.g., hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (e.g., personal history or family history of VTE, obesity, and systemic lupus erythematosus)
A 2 to 4-fold increase in risk of gallbladder disease requiring surgery in postmenopausal women receiving estrogens reported
Retinal vascular thrombosis reported in patients receiving estrogens; discontinue medication pending examination if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine; if examination reveals papilledema or retinal vascular lesions, estrogens should be discontinued
There are, possible risks that may be associated with use of progestins with estrogens compared to estrogen-alone regimens, including a possible increased risk of breast cancer, adverse effects on lipoprotein metabolism (e.g., lowering HDL, raising LDL), and impairment of glucose tolerance
In patients with pre-existing hypertriglyceridemia, estrogen therapy may be associated with elevations of plasma triglycerides leading to pancreatitis and other complications
Estrogens may be poorly metabolized in patients with impaired liver function; exercise caution in patients with a history of cholestatic jaundice associated with past estrogen use or with pregnancy; in the case of recurrence, discontinue medication
Patients dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased doses of thyroid replacement therapy; these patients should have their thyroid function monitored in order to maintain their free thyroid hormone levels in an acceptable range
Use caution in individuals with severe hypocalcemia
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.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
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