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Esterified Estrogens / Methyltestosterone

Pronunciation: ess-TER-ih-fide ESS-truh-janz/METH-ill-tess-TAHS-ter-ohn
Class: Estrogen and androgen combination

Trade Names

Estratest
- Tablets 1.25 mg esterified estrogens and 2.5 mg methyltestosterone

Estratest HS
- Tablets 0.625 mg esterified estrogens and 1.25 mg methyltestosterone

Pharmacology

Esterified Estrogens

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.

Slideshow: Flashback: FDA Drug Approvals 2013

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.

Contraindications

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 Administration

Adults

PO Usual dose range is 1 tablet ( Estratest ) or 1 to 2 tablets ( Estratest HS ) daily.

General Advice

Administer without regard to meals. Administer with food if GI upset occurs.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F).

Drug Interactions

Anticoagulants (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.

Adverse Reactions

CNS

Headache; migraine; dizziness; mental depression; chorea; changes in libido; anxiety; generalized paresthesia.

Dermatologic

Chloasma; melasma; erythema multiforme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; hirsutism; male pattern baldness; acne.

EENT

Steepening of corneal curvature; intolerance to contact lenses.

GI

Nausea; vomiting; abdominal cramps; bloating.

Genitourinary

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).

Hematologic

Suppression of clotting factors II, V, VII, and X; polycythemia.

Hepatic

Cholestatic jaundice; alterations in LFTs; hepatocellular neoplasms (rarely); peliosis hepatitis (rarely).

Metabolic

Increase or decrease in weight; reduced carbohydrate tolerance; edema; retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates; increased serum cholesterol.

Miscellaneous

Aggravation of porphyria; anaphylactoid reactions.

Precautions

Monitor

Baseline examinations

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.


Pregnancy

Category X .

Lactation

Undetermined.

Elderly

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.

Depression

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.

Fluid retention

Use with careful observation when conditions that might be affected by fluid retention are present (eg, asthma, cardiac or renal dysfunction, epilepsy).

Gallbladder disease

Risk of gallbladder disease may increase in women receiving postmenopausal estrogens.

Glucose tolerance

A worsening of glucose tolerance has been observed. Diabetic patients should be carefully monitored while receiving estrogens.

Hepatic conditions

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.

Hypercalcemia

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.

Minimum dose

Ensure that attempts are made to discontinue or taper the medication at 3 to 6 mo intervals.

Surgery/Immobilization

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.

Thromboembolic disease

Risk of various thromboembolic and thrombotic vascular diseases (eg, pulmonary embolism, stroke, MI, retinal thrombosis) are increased.

Uterine bleeding

Certain patients may develop abnormal uterine bleeding.

Uterine leiomyomata

Preexisting uterine leiomyomata may increase in size during estrogen use.

Overdosage

Symptoms

Nausea, withdrawal bleeding.

Patient Information

  • 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.

Copyright © 2009 Wolters Kluwer Health.

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