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Conjugated Estrogens

    DEA Class; Rx

    Common Brand Names; Premarin

    • Estrogen Derivatives

    conjugated estrogens, vaginal (Rx)

    Brand and Other Names:Premarin Vaginal Cream
    • Classes: Estrogen Derivatives

    Estrogen mixture of the water soluble salts of sulfate esters from estrone, equilin, 17 alpha-dihydroequilin, and other related steroids
    Traditional product derived from pregnant equine urine; other products are synthesized from yam and soy plants (synthetic conjugated estrogens, A) and plant-derived (synthetic conjugated estrogens, B)
    Different conjugated estrogen products are not bioequivalent, but there are no data that ‘natural’ estrogens are more or less efficacious or safe than ‘synthetic’ estrogens.

    Indicated for treatment of moderate to severe vasomotor symptoms (hot flashes) of menopause and/or related genitourinary symptoms including atrophic vaginitis, vulvar atrophy (kraurosis vulvae), or dyspareunia, whether menopause is natural or surgical (e.g., due to oophorectomy).
    For postmenopausal osteoporosis prophylaxis.
    For treatment of premenopausal females with estrogen deficiency due to hypogonadism.
    For treatment of hypoestrogenism due to primary ovarian failure.
    For the short-term treatment of abnormal or dysfunctional uterine bleeding caused by hormonal imbalance in the absence of organic pathology.
    For the palliative treatment of breast cancer that has metastasized, in appropriately selected men or women.
    For the palliative treatment of advanced inoperable prostate cancer.

    Indicated in Atrophic Vaginitis and Kraurosis Vulvae

    Treats symptom of vulvar and vaginal atrophy due to menopause

    Known anaphylactic reaction or angioedema

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

    Active or history of breast cancer

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

    Liver disease, liver tumors

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

    Estrogen-dependent neoplasia

    Undiagnosed abnormal vaginal bleeding

    • Abdominal pain (15-17%)
    • Back pain (13-14%)
    • Breast enlargement
    • Breast tenderness (7-12%)
    • Headache (26-32%)
    • Arthralgia (7-14%)
    • Pharyngitis (10-12%)
    • Sinusitis (6-11%)
    • Diarrhea (6-7%)
    • Depression (5-8%)
    • Dizziness (4-6%)
    • Nervousness (2-5%)
    • Flatulence (6-7%)
    • Vaginitis (5-7%)
    • Leukorrhea (4-7%)
    • Leg cramps (3-7%)
    • Increased cough (4-7%)
    • Pruritus (4-5%)
    • Amenorrhea
    • Breakthrough bleeding
    • Corneal curvation change
    • Melasma
    • Spotting
    • Vaginal moniliasis
    • Weight changes

    Use caution in diabetes mellitus, hyperlipidemias, hypertension, hypothyroidism, advanced age, hepatic or renal impairment, uterine leiomyomata, porphyria, patients with defects of lipoprotein metabolism, hypertriglyceridemia, ovarian cancer, systemic lupus erhythematosus, exacerbation of endometriosis or other conditions, smoking, diseases exacerbated by fluid retention

    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)

    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

    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

    Discontinue if any of the following develop: Jaundice, signs of venous thromboembolism, visual problems (may cause contact lens intolerance), massive blood pressure increase, major surgery or prolonged immobilization occurring in 4 weeks, new migraine, depression

    Women with protein C or S deficiency (inherited thrombophilia), may have increased risk of venous thromboembolism

    Do not use with conditions that predispose to hyperkalemia

    Conditions exacerbated by fluid retention (asthma, epilepsy, migraines, cardiac or renal dysfunction)

    Pregnancy category: X

    Lactation: Use controversial; estrogens are excreted into breast milk in small quantities; use with caution

    Adults

    Dependent on indication for therapy.

    Elderly

    Dependent on indication for therapy.

    Adolescents

    Dependent on indication for therapy.

    Children

    Not indicated in prepubescent females.

    Conjugated Estrogens

    tablet

    • 0.3mg
    • 0.45mg
    • 0.625mg
    • 0.9mg
    • 1.25mg

    powder for injection

    • 25mg