ESTROPIPATE

ESTROPIPATE
(es-troe-pi'pate)
Ogen, Ortho-Est
Classifications: hormone; estrogen;
Therapeutic: estrogen; female hormone replacement therapy (hrt)

Prototype: Estradiol
Pregnancy Category: X

Availability

0.625 mg, 1.25 mg, 2.5 mg, 5 mg tablets; 1.5 mg/g cream

Action

Water-soluble preparation of pure crystalline estrone. Estrone is one-third less active at the cellular level than estradiol, the principal premenopausal estrogen. Due to increased risk of serious complications from extended use, estrogen HRT or estrogen-progestin HRT should be prescribed for the shortest duration possible consistent with the treatment goals of postmenopausal symptoms.

Therapeutic Effect

Replaces estrogen in postmenopausal women relieving symptoms of menopause.

Uses

Atrophic vaginitis, kraurosis vulvae, and abnormal bleeding (hormonal imbalance); also female hypogonadism, primary ovarian failure, vasomotor symptoms associated with menopause, and as palliative therapy of prostatic carcinoma.

Contraindications

Estrogen hypersensitivity; breast cancer; vaginal cancer; endometrial hyperplasia; history of thromboembolic disease; known or suspected pregnancy (category X); lactation.

Cautious Use

Hypertension; gallbladder disease; diabetes mellitus; heart failure; kidney dysfunction; seizure disorders.

Route & Dosage

Menopause, Atrophic Vaginitis, Kraurosis Vulvae
Adult: PO 0.75–6 mg/d for 21 d each month; adjust to lowest level that gives symptom control Intravaginal 2–4 g of cream once/d in a cyclic regimen

Female Hypogonadism, Primary Ovarian Failure, Female Castration
Adult: PO 1.5–9 mg/d in 1–3 divided doses for 21 d, followed by an 8–10-d drug-free period

Administration

Oral
  • Give with food or fluid of patient's choice.
Intravaginal
  • Apply vaginal cream using calibrated dosage applicator dispensed with drug. Squeeze tube of cream to force sufficient amount into applicator so that number on plunger indicating prescribed dose is level with top of barrel.
  • Store at 15°–30° C (59°–86° F) in tightly closed containers unless otherwise directed.

Adverse Effects (≥1%)

CNS: Headache, dizziness, depression, libido changes. CV: Thromboembolic disorders, edema, hypertension. GI: Nausea, vomiting, diarrhea, bloating, cholestatic jaundice. Urogenital: Mastodynia, spotting, changes in menstrual flow, dysmenorrhea, amenorrhea. Metabolic: Reduced carbohydrate tolerance, fluid retention. Other: Leg cramps, intolerance to contact lenses.

Interactions

Drug: Carbamazepine, phenytoin, rifampin decrease estrogen levels because they increase its metabolism; may enhance steroid effects of corticosteroids; may decrease anticoagulant effects of oral anticoagulants. Herbal: St. John's wort may decrease blood levels. Dong quai, red clover, black cohosh, and saw palmetto may have additive hormonal effects.

Pharmacokinetics

Absorption: Absorbed with some metabolism occuring in GI tract. Some systemic absorption from vaginal administration. Metabolism: In GI tract and liver. Half-Life: 4–18.5 h.

Nursing Implications

Assessment & Drug Effects

  • See nursing implications under estradiol.
  • Monitor for and report breakthrough vaginal bleeding.
  • Assess for relief of menopausal symptoms.
  • Lab tests: Monitor serum phosphatase levels with prostate cancer.

Patient & Family Education

  • Do not use tampons while on vaginal cream therapy.
  • Intravaginal administration: For self-administration, wash hands well before and after application, and avoid contact of denuded areas with the cream.
  • Do not use tampons while on vaginal cream therapy. Pull plunger out of barrel and wash applicator in warm soapy water after use. Do not place plunger in hot or boiling water.
  • Note: Sudden discontinuation of vaginal cream after high dosage or prolonged use may evoke withdrawal bleeding.
  • Review patient package insert (PPI).

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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