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

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