Estropipate (Piperazine Estrone Sulfate)

A to Z Drug Facts

 Action 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.

 Indications 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.

 Route/Dosage

Vasomotor Symptoms

ADULTS: PO 0.625 to 5 mg/day given cyclically.

Female Hypogonadism, Female Castration, Primary Ovarian Failure

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

Osteoporosis

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

Atrophic Vaginitis, Kraurosis Vulvae

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

 Interactions

Antidepressants, tricyclic: Estrogens may alter effects and increase toxicity of these agents. Barbiturates, rifampin: May decrease estropipate concentration. Corticosteroids: An increase in the pharmacologic and toxicologic effects of corticosteroids may occur. Hydantoins: Loss of seizure control or decreased estrogenic effects may occur.

 Lab Test Interferences Endocrine and liver function test results may be affected; possible decreased PT and increased platelet aggregability; increased thyroid-binding globulin and total T₄; impaired glucose tolerance; decreased serum folate concentration; increased serum triglyceride and phospholipid concentrations; increased corticosteoid binding globulin and sex-hormone binding globulin; increased plasma HDL concentrations; reduced LDL cholesterol concentrations; increased triglyceride levels.

 Adverse Reactions

CV: Thrombosis; thrombophlebitis; increased BP; pulmonary embolism; MI. CNS: Headache; migraine; dizziness; depression; insomnia; anxiety; emotional lability. DERM: 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. GU: Increased risk of endometrial carcinoma; breakthrough bleeding; dysmenorrhea; amenorrhea; vaginal candidiasis; premenstrual-like syndrome; increased size of uterine fibromyomata; hemolytic uremic syndrome; urinary tract infection; vaginitis; vaginal discomfort/pain; cystitis; dysuria; genital pruritus; urinary incontinence. HEPA: Cholestatic jaundice. META: Hyperglycemia; hypercalcemia. RESP: Upper respiratory tract infection; sinusitis; rhinitis; pharyngitis; flu-like symptoms; allergy; bronchitis; chest pain. OTHER: 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. Calcium and phosphorus metabolism: Use drug with caution in patients with metabolic bone diseases. Fluid retention: Use drug with careful observation when conditions that might be affected by this factor are present (eg, asthma, cardiac or renal dysfunction, epilepsy). Gallbladder disease: Risk of gallbladder disease may increase in women receiving postmenopausal estrogens. Hepatic function impairment: Metabolism may be impaired; use drug with caution. 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.

 Administration/Storage

• Administer vaginal cream high in vagina (about  length of applicator).
• Give tablets with meal to decrease GI upset.

 Assessment/Interventions

• Obtain patient history, including drug history and any known allergies.
• Include in physical assessments BP measurements, and examination of breasts, abdomen and pelvic organs. Review results of Pap test, which should be conducted at least annually.
• Monitor blood sugar in diabetic patients and report changes to health care provider.
• Be alert for changes in liver function test results and possible decreased PT.

 Patient/Family Education

• 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 physician: 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 < 15/day because of increased risk of cardiovascular complications.
• Remind patient to have Pap smear every 6–12 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.

Books@Ovid
Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts