Estratest FS
Esterified Estrogens and Methyltestosterone · Tablet · Oral
Uses
INDICATIONS AND USAGE ESTRATEST H.S. AND ESTRATEST F.S. are indicated in the treatment of: Moderate to severe vasomotor symptoms associated with the menopause in those patients not improved by estrogens alone. (There is no evidence that estrogens are effective for nervous symptoms or depression without associated vasomotor symptoms, and they should not be used to treat such conditions.) ESTRATEST H.S. AND ESTRATEST F.S. HAVE NOT BEEN SHOWN TO BE EFFECTIVE FOR ANY PURPOSE DURING PREGNANCY AND ITS USE MAY CAUSE SEVERE HARM TO THE FETUS (SEE BOXED WARNING).
Dosage and administration
1. Given cyclically for short-term use only: For treatment of moderate to severe vasomotor symptoms associated with the menopause in patients not improved by estrogen alone. The lowest dose that will control symptoms should be chosen and medication should be discontinued as promptly as possible. Administration should be cyclic (e.g., three weeks on and one week off). Attempts to discontinue or taper medication should be made at three- to six month intervals. 2. Usual Dosage Range: 1 tablet of ESTRATEST F.S. or 1 to 2 tablets of ESTRATEST H.S. daily as recommended by the physician. Treated patients with an intact uterus should be monitored closely for signs of endometrial cancer and appropriate diagnostic measures should be taken to rule out malignancy in the event of persistent or recurring abnormal vaginal bleeding.
Contraindications
Estrogens should not be used in women with any of the following conditions: 1. Known or suspected cancer of the breast except in appropriately selected patients being treated for metastatic disease. 2. Known or suspected estrogen-dependent neoplasia. 3. Known or suspected pregnancy (See Boxed Warning). 4. Undiagnosed abnormal genital bleeding. 5. Active thrombophlebitis or thromboembolic disorders. 6. A past history of thrombophlebitis, thrombosis, or thromboembolic disorders associated with previous estrogen use (except when in treatment of breast malignancy). Methyltestosterone should not be used in: 1. The presence of severe liver damage. 2. Pregnancy and in breast-feeding mothers because of the possibility of masculinization of the female fetus or breast-fed infant.
Warnings
Associated with Estrogens 1. Induction of malignant neoplasms. Long term continuous administration of natural and synthetic estrogens in certain animal species increases this frequency of carcinomas of the breast, cervix, vagina, and liver. There is now evidence that estrogens increase the risk of carcinoma of the endometrium in humans (See Boxed Warning). At the present time there is no satisfactory evidence that estrogens given to postmenopausal women increase the risk of cancer of the breast, 18 although a recent long-term follow-up of a single physician's practice has raised this possibility. 18a Because of the animal data, there is a need for caution in prescribing estrogens for women with a strong family history of breast cancer or who have breast nodules, fibrocystic disease, or abnormal mammograms. 2. Gallbladder disease. A recent study has reported a 2 to 3-fold increase in the risk of surgically confirmed gallbladder disease in women receiving postmenopausal estrogens,18 similar to the 2-fold increase previously noted in users of oral contraceptives. 19-24a In the case of oral contraceptives the increased risk appeared after two years of use. 24 3. Effects similar to those caused by estrogen-progesterone oral contraceptives. There are several serious adverse effects of oral contraceptives, most of which have not, up to now, been documented as consequences of postmenopausal estrogen therapy. This may reflect the comparatively low doses of estrogen used in postmenopausal women. It would be expected that the larger doses of estrogen used to treat prostatic or breast cancer or postpartum breast engorgement are more likely to result in these adverse effects, and, in fact, it has been shown that there is an increased risk of thrombosis in men receiving estrogens for prostatic cancer and women for postpartum breast engorgement. 20-23 a. Thromboembolic disease. It is now well established that users of oral contraceptives have an increased risk of various thromboembolic and thrombotic vascular diseases, such as thrombophlebitis, pulmonary embolism, stroke, and myocardial infarction. 24-31 Cases of retinal thrombosis, mesenteric thrombosis, and optic neuritis have been reported in oral contraceptive users. There is evidence that the risk of several of these adverse reactions is related to the dose of the drug. 32-33 An increased risk of postsurgery thromboembolic complications has also been reported in users of oral contraceptives. 34-35 If feasible, estrogen should be discontinued at least 4 weeks before surgery of the type associated with an increased risk of thromboembolism, or during periods of prolonged immobilization. While an increased rate of thromboembolic and thrombotic disease in postmenopausal users of estrogens has not been found, 18-36 this does not rule out the possibility that such an increase may be present or that subgroups of women who have underlying risk factors or who are receiving relatively large doses of estrogens may have increased risk. Therefore estrogens should not be used in persons with active thrombophlebitis or thromboembolic disorders, and they should not be used (except in treatment of malignancy) in persons with a history of such disorders in association with estrogen use. They should be used with caution in patients with cerebral vascular or coronary artery disease and only for those in whom estrogens are clearly needed. Large doses of estrogen (5 mg esterified estrogens per day), comparable to those used to treat cancer of the prostate and breast, have been shown in a large prospective clinical trial in men 37 to increase the risk of nonfatal myocardial infarction, pulmonary embolism and thrombophlebitis. When estrogen doses of this size are used, any of the thromboembolic and thrombotic adverse effects associated with oral contraceptive use should be considered a clear risk. b. Hepatic adenoma. Benign hepatic adenomas appear to be associated with the use of oral contraceptives. 38-40 Although benign and rare, these may rupture and may cause death through intra-abdominal hemorrhage. Such lesions have not yet been reported in association with other estrogen or progestogen preparations but should be considered in estrogen users having abdominal pain and tenderness, abdominal mass, or hypovolemic shock. Hepatocellular carcinoma has also been reported in women taking estrogen-containing oral contraceptives. 39 The relationship of this malignancy to these drugs is not known at this time. c. Elevated blood pressure. Increased blood pressure is not uncommon in women using oral contraceptives. There is now a report that this may occur with use of estrogens in the menopause 41 and blood pressure should be monitored with estrogen use, especially if high doses are used. d. Glucose tolerance. A worsening of glucose tolerance has been observed in a significant percentage of patients of estrogen-containing oral contraceptives. For this reason, diabetic patients should be carefully observed while receiving estrogens. 4. Hypercalcemia. Administration of estrogens may lead to severe hypercalcemia in patients with breast cancer and bone metastases. If this occurs, the drug should be stopped and appropriate measures taken to reduce the serum calcium level. Associated with Methyltestosterone In patients with breast cancer, androgen therapy may cause hypercalcemia by stimulating osteolysis. In this case the drug should be discontinued. Prolonged use of high doses of androgens has been associated with the development of peliosis hepatis and hepatic neoplasms including hepatocellular carcinoma. (See PRECAUTIONS – Carcinogenesis). Peliosis hepatis can be a life-threatening or fatal complication. Cholestatic hepatitis and jaundice occur with 17-alpha-alkylated androgens at a relatively low dose. If cholestatic hepatitis with jaundice appears or if liver function tests become abnormal, the androgen should be discontinued and the etiology should be determined.
Precautions
Associated with Estrogens A. General Precautions 1. A complete medical and family history should be taken prior to the initiation of any estrogen therapy. The pretreatment and periodic physical examinations should include special reference to blood pressure, breasts, abdomen, and pelvic organs, and should include a Papanicolaou smear. As a general rule, estrogen should not be prescribed for longer than one year without another physical examination being performed. 2. Fluid retention– Because estrogens may cause some degree of fluid retention, conditions which might be influenced by this factor such as asthma, epilepsy, migraine, and cardiac or renal dysfunction, require careful observation. 3. Certain patients may develop undesirable manifestations of excessive estrogenic stimulation, such as abnormal or excessive uterine bleeding, mastodynia, etc. 4. Oral contraceptives appear to be associated with an increased incidence of mental depression. 24 Although it is not clear whether this is due to the estrogenic or progestogenic component of the contraceptive, patients with a history of depression should be carefully observed. 5. Preexisting uterine leiomyomata may increase in size during estrogen use. 6. The pathologist should be advised of estrogen therapy when relevant specimens are submitted. 7. Patients with a past history of jaundice during pregnancy have an increased risk of recurrence of jaundice while receiving estrogen-containing oral contraceptive therapy. If jaundice develops in any patient receiving estrogen, the medication should be discontinued while the cause is investigated. 8. Estrogens may be poorly metabolized in patients with impaired liver function and they should be administered with caution in such patients. 9. Because estrogens influence the metabolism of calcium and phosphorus, they should be used with caution in patients with metabolic bone diseases that are associated with hypercalcemia or in patients with renal insufficiency. 10. Because of the effects of estrogens on epiphyseal closure, they should be used judiciously in young patients in whom bone growth is not complete. 11. Certain endocrine and liver function tests may be affected by estrogen-containing oral contraceptives. The following similar changes may be expected with larger doses of estrogen: a. Increased sulfobromophthalein retention. b. Increased prothrombin and factors VII, VIII, IX and X; decreased antithrombin 3: increased norepinephrine induced platelet aggregability. c. Increased thyroid binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by PBI, T4 by column, or T4 by radioimmunoassay. Free T3 resin uptakes is decreased, reflecting the elevated TBG; free T4 concentration is unaltered. d. Impaired glucose tolerance. e. Decreased pregnanediol excretion. f. Reduced response to metyrapone test. g. Reduced serum folate concentration. h. Increased serum triglyceride and phospholipid concentration. B. Information for the Patient See Patient Package Insert. C. Pregnancy Category X See CONTRAINDICATIONS and Boxed WARNING. D. Nursing Mothers As a general principle, the administration of any drug to nursing mothers should be done only when clearly necessary since many drugs are excreted in human milk. Associated with Methyltestosterone A. General Precautions 1. Women should be observed for signs of virilization (deepening of the voice, hirsutism, acne, clitoromegaly, and menstrual irregularities). Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. Such virilization is usual following androgen use at high doses. 2. Prolonged dosage of androgen may result in sodium and fluid retention. This may present a problem, especially in patients with compromised cardiac reserve or renal disease. 3. Hypersensitivity may occur rarely. 4. PBI may be decreased in patients taking androgens. 5. Hypercalcemia may occur. If this does occur, the drug should be discontinued. B. Information for the Patient The physician should instruct patients to report any of the following side effects of androgens: Women: Hoarseness, acne, changes in menstrual periods, or more hair on the face. All Patients: Any nausea, vomiting, changes in skin color of ankle swelling. C. Laboratory Tests 1. Women with disseminated breast carcinoma should have frequent determination of urine and serum calcium levels during the course of androgen therapy (see WARNINGS). 2. Because of the hepatotoxicity associated with the use of 17-alpha-alkylated androgens, liver function tests should be obtained periodically. 3. Hemoglobin and hematocrit should be checked periodically for polycythemia in patients who are receiving high doses of androgens. D. Drug Interactions 1. Anticoagulants C-17 substituted derivatives of testosterone, such as methandrostenolone, have been reported to decrease the anticoagulant requirements of patients receiving oral anticoagulants. Patients receiving oral anticoagulant therapy require close monitoring, especially when androgens are started or stopped. 2. Oxyphenbutazone. Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone. 3. Insulin. In diabetic patients the metabolic effects of androgens may decrease blood glucose and insulin requirements. E. Drug/Laboratory Test Interferences Androgens may decrease levels of thyroxine-binding globulin, resulting in decreased T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged, however, and there is no clinical evidence of thyroid dysfunction. F. Carcinogenesis Animal Data. Testosterone has been tested by subcutaneous injection and implantation in mice and rats. The implant induced cervical-uterine tumors in mice, which metastasized in some cases.
Side effects
Associated with Estrogens (See Warnings regarding induction of neoplasia, adverse effects on the fetus, increased incidence of gallbladder disease, and adverse effects similar to those of oral contraceptives, including thromboembolism). The following additional adverse reactions have been reported with estrogenic therapy, including oral contraceptives: 1. Genitourinary system. Breakthrough bleeding, spotting, change in menstrual flow. Dysmenorrhea. Premenstrual-like syndrome. Amenorrhea during and after treatment. Increase in size of uterine fibromyomata. Vaginal candidiasis. Change in cervical erosion and in degree of cervical secretion. Cystitis-like syndrome. 2. Breasts. Tenderness, enlargement, secretion. 3. Gastrointestinal. Nausea, vomiting. Abdominal cramps, bloating. Cholestatic jaundice. 4. Skin. Chloasma or melasma which may persist when drug is discontinued. Erythema multiforme. Erythema nodosum. Hemorrhagic eruption. Loss of scalp hair. Hirsutism. 5. Eyes. Steepening of corneal curvature. Intolerance to contact lenses. 6. CNS. Headache, migraine, dizziness. Mental depression. Chorea. 7. Miscellaneous. Increase or decrease in weight. Reduced carbohydrate tolerance. Aggravation of porphyria. Edema. Changes in libido. Associated with Methyltestosterone 1. Female : The most common side effects of androgen therapy are amenorrhea and other menstrual irregularities, inhibition of gonadotropin secretion, and virilization, including deepening of the voice and clitoral enlargement. The latter usually is not reversible after androgens are discontinued. When administered to a pregnant woman androgens cause virilization of external genitalia of the female fetus. 2. Skin and Appendages : Hirsutism, male pattern of baldness, and acne. 3. Fluid and Electrolyte Disturbances : Retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates. 4. Gastrointestinal : Nausea, cholestatic jaundice, alterations in liver function test, rarely hepatocellular neoplasms, and peliosis hepatis (see WARNINGS). 5. Hematologic : Suppression of clotting factors, II, V, VII, and X, bleeding in patients on concomitant anticoagulant therapy, and polycythemia. 6. Nervous System: Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia. 7. Metabolic : Increased serum cholesterol. 8. Miscellaneous : Inflammation and pain at site of intramuscular injection or subcutaneous implantation of testosterone containing pellets, stomatitis with buccal preparations, and rarely anaphylactoid reactions.
Overdosage
Numerous reports of ingestion of large doses of estrogen-containing oral contraceptives by young children indicate that serious ill effects do not occur. Overdosage of estrogen may cause nausea, and withdrawal bleeding may occur in females. There have been no reports of acute overdosage with the androgens.
Description
DESCRIPTION ESTRATEST F.S.: Each light green, oval-shaped, biconvex tablet debossed with "640" on one side and scripted "E" on other side contains: 1.25 mg of Esterified Estrogens, USP and 2.5 mg of Methyltestosterone, USP. ESTRATEST H.S.: Each dark green, oval-shaped, biconvex tablet debossed with "639" on one side and scripted "E" on other side contains: 0.625 mg of Esterified Estrogens, USP and 1.25 mg of Methyltestosterone, USP. Esterified Estrogens Esterified Estrogens, USP 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. Esterified Estrogens contain not less than 75.0 percent and not more than 85.0 percent of sodium estrone sulfate, and not less than 6.0 percent and not more than 15.0 percent of sodium equilin sulfate, in such proportion that the total of these two components is not less than 90.0 percent. Methyltestosterone Methyltestosterone, USP is an androgen. Androgens are derivatives of cyclopentano-perhydrophenanthrene. Endogenous androgens are C-19 steroids with a side chain at C-17, and with two angular methyl groups. Testosterone is the primary endogenous androgen. Fluoxymesterone and methyltestosterone are synthetic derivatives of testosterone. Methyltestosterone is a white to light yellow crystalline substance that is virtually insoluble in water but soluble in organic solvents. It is stable in air but decomposes in light. Methyltestosterone structural formula: ESTRATEST F.S. TABLETS contain the following inactive ingredients: Anhydrous Lactose, Colloidal Silicon Dioxide, D&C Yellow #10, FD&C Blue #1, FD&C Yellow #6, Magnesium Stearate, Microcrystalline Cellulose, Polyethylene Glycol, Polyvinyl Alcohol, Sodium Bicarbonate, Sodium Citrate, Talc, and Titanium Dioxide. ESTRATEST H.S. TABLETS contain the following inactive ingredients: Anhydrous Lactose, Colloidal Silicon Dioxide, D&C Yellow #10, FD&C Blue #1, FD&C Blue #2, Magnesium Stearate, Microcrystalline Cellulose, Polyethylene Glycol, Polyvinyl Alcohol, Sodium Bicarbonate, Sodium Citrate, Talc, and Titanium Dioxide. ab03b87f-figure-01
How supplied
HOW SUPPLIED ESTRATEST F.S. in bottles of 100. ESTRATEST F.S. light green, oval-shaped, biconvex tablet debossed with "640" on one side and scripted "E" on other side. Contains: 1.25 mg of Esterified Estrogens, USP and 2.5 mg of Methyltestosterone, USP. ESTRATEST H.S. in bottles of 100. ESTRATEST H.S. dark green, oval-shaped, biconvex tablet debossed with "639" on one side and scripted "E" on other side. Contains: 0.625 mg of Esterified Estrogens, USP and 1.25 mg of Methyltestosterone, USP. Store at 20°-25°C (68°-77°F); excursions permitted to 15°-30°C (59°-86°F). [See USP Controlled Room Temperature.]
Label text from the FDA structured product label by Method Pharmaceuticals (revised Mar 10, 2025). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Estrogens, Esterified in 1 product
- Methyltestosterone in 1 product
Estratest FS NDC products (1)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 58657-417 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | Method Pharmaceuticals | UNAPPROVED DRUG OTHER · DEA CIII |
Frequently asked questions
What is Estratest FS used for?
INDICATIONS AND USAGE ESTRATEST H.S. AND ESTRATEST F.S. are indicated in the treatment of: Moderate to severe vasomotor symptoms associated with the menopause in those patients not improved by estrogens alone. (There is no evidence that estrogens are effective for nervous symptoms or depression without associated vasomotor symptoms, and they should not be used to treat such conditions.) ESTRATEST…
What are the side effects of Estratest FS?
Associated with Estrogens (See Warnings regarding induction of neoplasia, adverse effects on the fetus, increased incidence of gallbladder disease, and adverse effects similar to those of oral contraceptives, including thromboembolism). The following additional adverse reactions have been reported with estrogenic therapy, including oral contraceptives: 1. Genitourinary system. Breakthrough… See the full label for the complete list.
Who makes Estratest FS?
Estratest FS is listed by 1 labeler in the FDA NDC directory, including Method Pharmaceuticals.