Esterified Estrogens

Description

DESCRIPTION Esterified estrogens is a mixture of the sodium salts of the sulfate esters of the estrogenic substances, principally estrone, that are of the type excreted by pregnant mares. It contains the concomitant component, 17α-estradiol. The content of total esterified estrogens is not less than 90 percent and not more than 110 percent of the labeled amount. Esterified estrogens contain not less than 75 percent and not more than 85 percent of sodium estrone sulfate, and not less than 6 percent and not more than 15 percent of sodium equilin sulfate, in such proportion that the total of these two components is not less than 90 percent, all percentages being calculated on the basis of the total esterified estrogens content. Inactive Ingredients: Ethyl cellulose, fragrances, hydroxypropyl cellulose, hypromellose 2910, lactose, magnesium stearate, methylcellulose, polyethylene glycol, sodium bicarbonate, shellac, starch, stearic acid, titanium dioxide, and vanillin. Dyes in the form of aluminum lakes are contained in each tablet strength as follows: 0.3 mg Tablet: FD&C Yellow No. 6, D&C Yellow No. 10. 0.625 mg Tablet : FD&C Yellow No. 6, D&C Yellow No. 10. 1.25 mg Tablet: FD&C Yellow No. 6, D&C Yellow No. 10, FD&C Blue No. 1. 2.5 mg Tablet: D&C Red No. 30.

What Is Esterified Estrogens Used For?

INDICATIONS AND USAGE Menest is indicated in the: 1. Treatment of moderate to severe vasomotor symptoms associated with the menopause. 2. Treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with the menopause. When prescribing solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered. 3. Female hypogonadism. 4. Female castration. 5. Primary ovarian failure. 6. Breast cancer (for palliation only) in appropriately selected women and men with metastatic disease. 7. Prostatic carcinoma - palliative therapy of advanced disease.

Dosage and Administration

DOSAGE AND ADMINISTRATION When estrogen is prescribed for a postmenopausal woman with a uterus, a progestin should also be initiated to reduce the risk of endometrial cancer. A woman without a uterus does not need progestin. Use of estrogen, alone or in combination with a progestin, should be with the lowest effective dose and for the shortest duration consistent with treatment goals and risks for the individual woman. Patients should be reevaluated periodically as clinically appropriate (e.g., 3-month to 6-month intervals) to determine if treatment is still necessary (See Boxed Warnings and WARNINGS .) For women who have a uterus, adequate diagnostic measures, such as endometrial sampling, when indicated, should be undertaken to rule out malignancy in cases of undiagnosed persistent or recurring abnormal vaginal bleeding. Patients should be started at the lowest dose. 1. Given cyclically for short term use only: For treatment of moderate to severe vasomotor symptoms, or moderate to severe symptoms of vulvar and vaginal atrophy associated with the menopause. Administration should be cyclic (e.g., 3 weeks on and 1 week off). USUAL DOSAGE RANGES: Vasomotor symptoms – 1.25 mg daily. If the patient has not menstruated within the last 2 months or more, cyclic administration is started arbitrarily. If the patient is menstruating, cyclic administration is started on day 5 of bleeding. Moderate to severe symptoms of vulvar and vaginal atrophy – 0.3 mg to 1.25 mg or more daily, depending upon the tissue response of the individual patient. Administer cyclically. 2. Given cyclically: Female hypogonadism; female castration; primary ovarian failure. USUAL DOSAGE RANGES: Female hypogonadism – 2.5 to 7.5 mg daily, in divided doses for 20 days, followed by a rest period of 10 days' duration. If bleeding does not occur by the end of this period, the same dosage schedule is repeated. The number of courses of estrogen therapy necessary to produce bleeding may vary depending on responsiveness of the endometrium. If bleeding occurs before the end of the 10 day period, begin a 20 day estrogen-progestin cyclic regimen with Menest (esterified estrogens tablets), 2.5 to 7.5 mg daily in divided doses, for 20 days. During the last 5 days of estrogen therapy, give an oral progestin. If bleeding occurs before this regimen is concluded, therapy is discontinued and may be resumed on the fifth day of bleeding. Female castration and primary ovarian failure – 1.25 mg daily, cyclically. Adjust dosage upward or downward according to severity of symptoms and response of the patient. For maintenance, adjust dosage to lowest level that will provide effective control. 3. Given chronically: Inoperable progressing prostatic cancer — 1.25 to 2.5 mg three times daily. The effectiveness of therapy can be judged by phosphatase determinations as well as by symptomatic improvement of the patient. Inoperable progressing breast cancer in appropriately selected men and postmenopausal women. (See...

Side Effects (Adverse Reactions)

ADVERSE REACTIONS See Boxed Warnings , WARNINGS and PRECAUTIONS . The following additional adverse reactions have been reported with estrogens and/or progestin therapy. 1. Genitourinary system Changes in vaginal bleeding pattern and abnormal withdrawal bleeding or flow; breakthrough bleeding; spotting; dysmenorrhea, increase in size of uterine leiomyomata; vaginitis, including vaginal candidiasis; change in amount of cervical secretion; changes in cervical ectropion; ovarian cancer; endometrial hyperplasia; endometrial cancer; premenstrual like syndrome, amenorrhea during and after treatment; cystitis like syndrome. 2. Breasts Tenderness, enlargement, pain, nipple discharge, galactorrhea; fibrocystic breast changes; breast cancer. 3. Cardiovascular Deep and superficial venous thrombosis; pulmonary embolism; thrombophlebitis; myocardial infarction; stroke; increase in blood pressure. 4. Gastrointestinal Nausea, vomiting; abdominal cramps, bloating; cholestatic jaundice; increased incidence of gall bladder disease; pancreatitis, enlargement of hepatic hemangiomas. 5. Skin Chloasma or melasma, that may persist when drug is discontinued; erythema multiforme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; hirsutism; pruritus, rash. 6. Eyes Retinal vascular thrombosis; steepening of corneal curvature; intolerance to contact lenses. 7. Central nervous system Headache; migraine; dizziness; mental depression; chorea; nervousness; mood disturbances; irritability; exacerbation of epilepsy, dementia. 8. Miscellaneous Increase or decrease in weight; reduced carbohydrate tolerance; aggravation of porphyria; edema; arthalgias; leg cramps; changes in libido; urticaria, angioedema, anaphylactoid/anaphylactic reactions; hypocalcemia; exacerbation of asthma; increased triglycerides.

Contraindications

CONTRAINDICATIONS Menest should not be used in women with any of the following conditions: 1. Undiagnosed abnormal genital bleeding. 2. Known, suspected, or history of cancer of the breast except in appropriately selected patients being treated for metastatic disease. 3. Known or suspected estrogen-dependent neoplasia. 4. Active deep vein thrombosis, pulmonary embolism or a history of these conditions. 5. Active or recent (e.g., within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction). 6. Liver dysfunction or disease. 7. Menest should not be used in patients with known hypersensitivity to its ingredients. 8. Known or suspected pregnancy. There is no indication for Menest in pregnancy. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins from oral contraceptives inadvertently during early pregnancy. (See PRECAUTIONS .)

Pregnancy and Breastfeeding

F. PREGNANCY Menest should not be used during pregnancy. (See CONTRAINDICATIONS .)

G. NURSING MOTHERS Estrogen administration to nursing mothers has been shown to decrease the quantity and quality of the milk. Detectable amounts of estrogens have been identified in the milk of mothers receiving this drug. Caution should be exercised when Menest is administered to a nursing mother.

Overdosage

OVERDOSAGE Serious ill effects have not been reported following acute ingestion of large doses of estrogen-containing drug products by young children. Overdosage of estrogen may cause nausea and vomiting, and withdrawal bleeding may occur in females.

How Supplied

HOW SUPPLIED Tablets: 0.3 mg yellow, film-coated oblong tablet imprinted with M72 100's: NDC 61570-072-01 0.625 mg orange, film-coated oblong tablet imprinted with M73 100's: NDC 61570-073-01 1.25 mg green, film-coated oblong tablet imprinted with M74 100's: NDC 61570-074-01 2.5 mg pink, film-coated oblong tablet imprinted with M75 50's: NDC 61570-075-50 Do not store above 25°C (77°F).