Esterified Estrogens / Methyltestosterone
Pronunciation: ess-TER-ih-fide ESS-truh-janz/METH-ill-tess-TAHS-ter-ohn
Class: Estrogen and androgen combination
- Tablets 1.25 mg esterified estrogens and 2.5 mg methyltestosterone
- Tablets 0.625 mg esterified estrogens and 1.25 mg methyltestosterone
Promotes growth and development of female reproductive system and secondary sex characteristics; affects release of pituitary gonadotropins; inhibits ovulation and prevents postpartum breast engorgement; conserves calcium and phosphorous and encourages bone formation; overrides stimulatory effects of testosterone.Methyltestosterone
Promotes growth and development of male reproductive organs; maintains secondary sex characteristics; increases protein anabolism; decreases protein catabolism.
Indications and Usage
Treatment of moderate to severe vasomotor symptoms associated with the menopause in patients not improved by estrogens alone.
Known or suspected cancer of the breast except in appropriately selected patients being treated for metastatic disease; known or suspected estrogen-dependent neoplasia; known or suspected pregnancy; undiagnosed abnormal genital bleeding; active thrombophlebitis or thromboembolic disorders; past history of thrombophlebitis, thrombosis, or thromboembolic disorders associated with previous estrogen use except when treating breast malignancy. In addition, methyltestosterone should not be used in the presence of severe liver damage, pregnancy, and breast-feeding mothers because of the possibility of masculinization of the female fetus or breast-fed infant.
Dosage and AdministrationAdults
PO Usual dose range is 1 tablet ( Estratest ) or 1 to 2 tablets ( Estratest HS ) daily.
Administer without regard to meals. Administer with food if GI upset occurs.
Store tablets at controlled room temperature (59° to 86°F).
Drug InteractionsAnticoagulants (eg, Coumadin)
The hypoprothrombinemic effect of oral anticoagulants is potentiated by 17-alkyl androgens. Oral anticoagulant dose requirements will be reduced. Estrogens affect several coagulation and fibrinolysis tests and at high doses, could increase the risk of thromboembolism. The benefit from oral anticoagulants could be diminished by estrogen.Insulin
Blood glucose may be reduced, decreasing the insulin requirements.Oxyphenbutazone
Serum levels of oxyphenbutazone may be elevated, increasing the risk of adverse reactions.
Laboratory Test Interactions
Increased sulfobromophthalein retention; increased prothrombin and factors VII, VIII, IX and X; decreased antithrombin; increased norepinephrine-induced platelet aggregability; impaired glucose tolerance; decreased pregnanediol excretion; increased thyroxine-binding globulin (TBG), leading to increased circulating total thyroid hormone as measured by protein bound iodine, T4 by column, or T4 by radioimmunoassay; free T3 resin uptake is decreased (reflecting the elevated TBG); reduced response to metyrapone test; reduced serum folate concentration; increase serum triglyceride and phospholipid concentrations.
Headache; migraine; dizziness; mental depression; chorea; changes in libido; anxiety; generalized paresthesia.
Chloasma; melasma; erythema multiforme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; hirsutism; male pattern baldness; acne.
Steepening of corneal curvature; intolerance to contact lenses.
Nausea; vomiting; abdominal cramps; bloating.
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 degree of cervical secretion; cystitis-like syndrome; breast tenderness, enlargement, and secretion; menstrual irregularities; inhibition of gonadotropin secretion and virilization (including deepening of voice and clitoral enlargement).
Suppression of clotting factors II, V, VII, and X; polycythemia.
Cholestatic jaundice; alterations in LFTs; hepatocellular neoplasms (rarely); peliosis hepatitis (rarely).
Increase or decrease in weight; reduced carbohydrate tolerance; edema; retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates; increased serum cholesterol.
Aggravation of porphyria; anaphylactoid reactions.
Ensure that breast, abdominal, and pelvic examination and Pap smear have been completed and documented before starting therapy.Adverse reactions
Notify health care provider if any of the following are noted: pain, swelling, redness or warmth in calves; sudden severe headache; visual disturbances; weakness or numbness of arms or legs; signs of liver dysfunction (eg, dark urine, jaundice); abdominal pain, tenderness, or swelling; nausea; vomiting; ankle swelling; hoarseness; acne; increased facial hair; signs of depression.
Category X .
Risk for development of prostatic hypertrophy or prostatic carcinoma may be increased.
Special Risk Patients
Use with caution in patients with impaired liver function, renal insufficiency, metabolic bone diseases associated with hypercalcemia, and in young patients in whom bone growth is not complete.
Carefully observe patients with history of depression.
Elevated blood pressure
Increased BP during estrogen replacement during menopause has been reported. Assess BP at beginning of therapy and periodically during treatment.
Use with careful observation when conditions that might be affected by fluid retention are present (eg, asthma, cardiac or renal dysfunction, epilepsy).
Risk of gallbladder disease may increase in women receiving postmenopausal estrogens.
A worsening of glucose tolerance has been observed. Diabetic patients should be carefully monitored while receiving estrogens.
Benign hepatic adenomas and hepatocellular carcinoma appear to be associated with oral contraceptive use. Prolonged use of high doses of androgens has been associated with peliosis hepatitis and hepatic neoplasms. Cholestatic hepatitis and jaundice have been reported. Patients with history of jaundice during pregnancy have an increased risk of recurrence while receiving estrogen-containing oral contraceptive therapy.
In patients with breast cancer or bone metastases, severe hypercalcemia has occurred with estrogen therapy.
Induction of malignant neoplasm
May increase risk of endometrial or other carcinomas. Ensure that a progestin is used to prevent endometrial hyperplasia in women with an intact uterus.
Ensure that attempts are made to discontinue or taper the medication at 3 to 6 mo intervals.
Ensure that, if feasible, therapy is discontinued at least 4 wk before surgery of the type associated with an increased risk of thromboembolism or during periods of prolonged immobilization.
Risk of various thromboembolic and thrombotic vascular diseases (eg, pulmonary embolism, stroke, MI, retinal thrombosis) are increased.
Certain patients may develop abnormal uterine bleeding.
Preexisting uterine leiomyomata may increase in size during estrogen use.
Nausea, withdrawal bleeding.
- Advise patient to read patient information leaflet before starting therapy and with each refill.
- Instruct patient to take as prescribed and not to change the dose or stop taking unless advised to do so by health care provider.
- Advise patient that medication can be taken without regard to meals, but to take with food if GI upset occurs.
- Instruct diabetic patient to monitor blood glucose more frequently when drug is started or dose is changed and to inform health care provider of significant changes in readings.
- Review nonhormonal modalities that help prevent osteoporosis: 1,500 mg/day of calcium; vitamin D supplementation; exercise.
- Instruct patient to report these symptoms to health care provider: pain in groin or calves; sharp chest pain or sudden shortness of breath; abnormal vaginal bleeding; breast lumps; sudden severe headache; dizziness or fainting; vision or speech problems; weakness or numbness of arms or legs; severe abdominal pain; yellowing of skin or eyes; abdominal pain, tenderness, or swelling; nausea, vomiting, or ankle swelling; hoarseness; acne; increased facial hair; or signs of depression.
- Teach patient proper method of breast self-examination.
- Advise patient that follow-up visits and examinations, including Pap smear, at least once a year will be required to monitor therapy and to keep appointments.
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