Esterified Estrogens and Methyltestosterone
Tablet · Oral
Uses
5- Indication ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE HALF STRENGTH 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.) ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE HALF STRENGTH HAVE NOT BEEN SHOWN TO BE EFFECTIVE FOR ANY PURPOSE DURING PREGNANCY AND ITS USE MAY CAUSE SEVERE HARM TO THE FETUS.
Dosage and administration
6- Recommended Dose Usual Dosage Range ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE HALF STRENGTH 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. 7- Recommended route of administration: 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.
Contraindications
8- 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. 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 and precautions
9- Warnings and Precautions Associated with Estrogens 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. 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. 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 as in the case of oral contraceptives the increased risk appeared after two years of use. 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. 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. 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. An increased risk of post- surgery thromboembolic complications has also been reported in users of oral contraceptives. 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, 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 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. 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. 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 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. 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-alkylandrogens 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. Drug-induced jaundice is reversible when the medication is discontinued.
Side effects
10- Undesirable 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: 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. Breasts. Tenderness, enlargement, secretion. Gastrointestinal. Nausea, vomiting. Abdominal cramps, bloating. Cholestatic jaundice Skin. Chloasma or melasma which may persist when drug is discontinued. Erythema multiforme. Erythema nodosum. Hemorrhagic eruption. Loss of scalp hair. Hirsutism. Eyes. Steepening of corneal curvature. Intolerance to contact lenses. CNS. Headache, migraine, dizziness. Mental depression. Chorea. Miscellaneous. Increase or decrease in weight. Reduced carbohydrate tolerance. Aggravation of porphyria. Edema. Changes in libido. Associated with Methyltestosterone A. Endocrine and Urogenital. 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. Skin and Appendages: Hirsutism, male pattern of baldness, and acne. Fluid and Electrolyte Disturbances: Retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates. Gastrointestinal: Nausea, cholestatic jaundice, alterations in liver function test, rarely hepatocellular neoplasms, and peliosis hepatis. Hematologic: Suppression of clotting factors, II, V, VII, and X, bleeding in patients on concomitant anticoagulant therapy, and polycythemia. Nervous System: Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia. Metabolic: Increased serum cholesterol. Miscellaneous: Inflammation and pain at site of intramuscular injection or subcutaneous implantation of testosterone containing pellets, stomatitis with buccal preparations, and rarely anaphylactoid reactions.
Drug interactions
D. Drug Interactions 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. Oxyphenbutazone. Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone. Insulin. In diabetic patients the metabolic effects of androgens may decrease blood glucose and insulin requirements.
Pregnancy
G. Pregnancy Teratogenic Effects. Pregnancy Category X (see CONTRAINDICATIONS ).
Overdosage
11- Overdose and Treatment 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
1- Product Name: Esterified Estrogens and Methyltestosterone Tablets 2- Name and Strength of the active Ingredient (s) Each tablet contains: Esterified Estrogens, USP......0.625 mg Methyltestosterone, USP........1.25 mg 3- Product Description Physical properties light green, capsule-shaped, oral tablet
How supplied
12- Packaging and storage condition ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE TABLETS Half Strength in bottles of 100. ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE TABLETS Half Strength Green, capsule-shaped, oral tablet. 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.] Rx only
Patient information
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.
Label text from the FDA structured product label by STATUS PROJECTS PRIVATE LIMITED (revised Jan 21, 2026). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Estrogens, Esterified in 18 products
- Methyltestosterone in 18 products
Esterified Estrogens and Methyltestosterone NDC products (18)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 53746-077 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | Amneal Pharmaceuticals of New York LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 53746-078 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | Amneal Pharmaceuticals of New York LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 62559-149 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | ANI Pharmaceuticals, Inc. | UNAPPROVED DRUG OTHER · DEA CIII |
| 62559-150 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | ANI Pharmaceuticals, Inc. | UNAPPROVED DRUG OTHER · DEA CIII |
| 72162-2393 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | Bryant Ranch Prepack | UNAPPROVED DRUG OTHER · DEA CIII |
| 72162-1748 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | Bryant Ranch Prepack | UNAPPROVED DRUG OTHER · DEA CIII |
| 72162-1747 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | Bryant Ranch Prepack | UNAPPROVED DRUG OTHER · DEA CIII |
| 63629-1979 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | Bryant Ranch Prepack | UNAPPROVED DRUG OTHER · DEA CIII |
| 63629-1980 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | Bryant Ranch Prepack | UNAPPROVED DRUG OTHER · DEA CIII |
| 63629-9178 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | Bryant Ranch Prepack | UNAPPROVED DRUG OTHER · DEA CIII |
| 71335-2951 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | Bryant Ranch Prepack | UNAPPROVED DRUG OTHER · DEA CIII |
| 51293-640 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | ECI Pharmaceuticals LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 51293-639 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | ECI Pharmaceuticals LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 69315-284 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | Leading Pharmaceuticals, LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 69315-283 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | Leading Pharmaceuticals, LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 58657-408 | Estrogens, Esterified 1.25 mg/1; Methyltestosterone 2.5 mg/1 Tablet | Method Pharmaceuticals, LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 58657-407 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | Method Pharmaceuticals, LLC | UNAPPROVED DRUG OTHER · DEA CIII |
| 84346-450 | Estrogens, Esterified .625 mg/1; Methyltestosterone 1.25 mg/1 Tablet | STATUS PROJECTS PRIVATE LIMITED | UNAPPROVED DRUG OTHER · DEA CIII |
Frequently asked questions
What is Esterified Estrogens and Methyltestosterone used for?
5- Indication ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE HALF STRENGTH 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…
What are the side effects of Esterified Estrogens and Methyltestosterone?
10- Undesirable 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: Genitourinary… See the full label for the complete list.
Who makes Esterified Estrogens and Methyltestosterone?
Esterified Estrogens and Methyltestosterone is listed by 7 labelers in the FDA NDC directory, including Amneal Pharmaceuticals of New York LLC, ANI Pharmaceuticals, Inc., Bryant Ranch Prepack, ECI Pharmaceuticals LLC.