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Trade Names:
Ogen
- Tablets 0.625 mg
- Tablets 1.25 mg
- Tablets 2.5 mg sodium estrone sulfate

Trade Names:
Ortho-Est
- Tablets 0.625 mg
- Tablets 1.25 mg sodium estrone sulfate

Mechanism of Action

Pharmacology

Promotes growth and development of female reproductive system and secondary sex characteristics; affects release of ovulation and prevents postpartum breast engorgement; conserves calcium and phosphorous and encourages bone formation; overrides stimulatory effects of testosterone.

Pharmacokinetics

Absorption

Well absorbed from the GI tract.

Distribution

Largely bound to sex hormone-binding globulin and albumin. Crosses the placenta.

Metabolism

Undergoes first-pass metabolism. Metabolic conversion occurs primarily in the liver, but also at local target tissue sites. Also undergoes enterohepatic recirculation.

Elimination

A certain portion is excreted into the bile and then reabsorbed from the intestine. Excreted in the urine as conjugates.

Indications and Usage

Management of moderate to severe vasomotor symptoms associated with menopause; female hypogonadism, female castration, primary ovarian failure, and atrophic conditions caused by deficient endogenous estrogen production; prevention and treatment of osteoporosis.

Contraindications

Breast cancer; estrogen-dependent neoplasia; undiagnosed abnormal genital bleeding; thrombophlebitis or thromboembolic disorders associated with previous estrogen use; known or suspected pregnancy.

Dosage and Administration

Dosage is calculated as estrone sulfate.

PO 0.625 to 5 mg/day given cyclically.

PO 1.25 to 7.5 mg/day for 3 wk followed by 8- to 10-day drug-free period.

PO 0.625 mg/day for 25 days of 31-day cycle.

PO 0.625 to 5 mg/day. Give cyclically. Intravaginal 2 to 4 g/day. Give cyclically.

Drug Interactions

Estrogens may alter effects and increase toxicity of these agents.

May decrease estropipate concentration.

An increase in the pharmacologic and toxicologic effects of corticosteroids may occur.

Loss of seizure control or decreased estrogenic effects may occur.

Laboratory Test Interactions

Endocrine and LFT results may be affected; possible decreased PT and increased platelet aggregability; increased thyroid-binding globulin and total T ₄ ; impaired glucose tolerance; decreased serum folate concentration; increased serum triglyceride and phospholipid concentrations; increased corticosteroid binding globulin and sex-hormone binding globulin; increased plasma HDL concentrations; reduced LDL cholesterol concentrations; increased triglyceride levels.

Adverse Reactions

Cardiovascular

Thrombosis; thrombophlebitis; increased BP; pulmonary embolism; MI.

CNS

Headache; migraine; dizziness; depression; insomnia; anxiety; emotional lability.

Dermatologic

Chloasma; melasma; erythema nodosum/multiforme; scalp hair loss; hirsutism; urticaria; dermatitis; skin hypertrophy; pruritus.

EENT

Intolerance to contact lenses.

GI

Nausea; vomiting; abdominal cramps; bloating; colitis; acute pancreatitis; diarrhea; dyspepsia; flatulence; gastritis; gastroenteritis; enlarged abdomen; hemorrhoids.

Genitourinary

Increased risk of endometrial carcinoma; breakthrough bleeding; dysmenorrhea; amenorrhea; vaginal candidiasis; premenstrual-like syndrome; increased size of uterine fibromyomata; hemolytic uremic syndrome; UTI; vaginitis; vaginal discomfort/pain; cystitis; dysuria; genital pruritus; urinary incontinence.

Hepatic

Cholestatic jaundice.

Metabolic

Hyperglycemia; hypercalcemia.

Respiratory

Upper respiratory tract infection; sinusitis; rhinitis; pharyngitis; flu-like symptoms; allergy; bronchitis; chest pain.

Miscellaneous

Increase or decrease in weight; edema; changes in libido; breast tenderness; acute intermittent porphyria; vaginal bleeding; hypersensitivity reactions; back pain; arthritis; arthralgia; hot flushes; otitis media; toothache.

Precautions

Pregnancy

Category X .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Hepatic Function

Metabolism may be impaired; use drug with caution.

Calcium and phosphorus metabolism

Use drug with caution in patients with metabolic bone diseases.

Cardiovascular and other risks

Compared with placebo, increased risks of MI, stroke, deep vein thrombosis, pulmonary emboli, and invasive breast cancer were reported in postmenopausal women during 5 yr of treatment with conjugated equine estrogens combined with medroxyprogesterone acetate. Other combinations of estrogens and progestins were not studied; however, in the absence of comparable data, assume these risks to be similar.

Fluid retention

Use drug with careful observation when conditions that might be affected by this factor are present (eg, asthma, cardiac or renal function impairment, epilepsy).

Gallbladder disease

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

Induction of malignant neoplasms

May increase risk of endometrial or other carcinomas.

Familial hyperlipoproteinemia

May be associated with massive elevations of plasma triglycerides.

Uterine leiomyomata

Preexisting uterine leiomyomata may increase in size.

Unopposed estrogen administration (eg, without progesterone)

Increases risk of uterine cancer. Therefore, when using estrogens on long-term basis in a woman with intact uterus, consider cyclic therapy with progesterone (eg, estrogen on days 1 to 25 of mo with progesterone added for last 12 days) or daily coadministration of estrogen plus progesterone on daily basis. In a woman without uterus, use of cyclic therapy and/or therapy with progesterone is not necessary.

Overdosage

Symptoms

Nausea, withdrawal bleeding in women.

Patient Information

• Caution patient that this medication must not be taken during pregnancy or when pregnancy is possible. Advise patient to use reliable form of birth control while taking this drug.
• 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; or severe depression.
• Advise patient to stop smoking or to reduce number of cigarettes smoked to less than 15/day because of increased risk of cardiovascular complications.
• Remind patient to have Pap smear every 6 to 12 mo while undergoing therapy.
• Teach patient proper method of breast self-examination.
• Advise patient to avoid prolonged exposure to sunlight or other sources of UV light. Sunscreens and protective clothing should be used until tolerance is determined.