Classes
DEA Class; Rx
Common Brand Names; Premarin
- Estrogen Derivatives
conjugated estrogens, vaginal (Rx)
- Classes: Estrogen Derivatives
Description
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.
Indications
Indicated in Atrophic Vaginitis and Kraurosis Vulvae
Treats symptom of vulvar and vaginal atrophy due to menopause
Contraindications
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
Adverse Effects
- 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
Warnings
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 and Lactation
Pregnancy category: X
Lactation: Use controversial; estrogens are excreted into breast milk in small quantities; use with caution
Maximum Dosage
Dependent on indication for therapy.
Dependent on indication for therapy.
Dependent on indication for therapy.
Not indicated in prepubescent females.
How supplied
Conjugated Estrogens
tablet
- 0.3mg
- 0.45mg
- 0.625mg
- 0.9mg
- 1.25mg
powder for injection
- 25mg