ESTROGENS, CONJUGATED
(ess'tro-jenz)
C.E.S.  , Cenestin, Enjuvia, Premarin, Progens
Classifications: hormones & synthetic substitutes; estrogens
Prototype: Estradiol
Pregnancy Category: X
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0.3 mg, 0.45 mg, 0.625 mg, 0.9 mg, 1.25 mg, 2.5 mg tablets; 25 mg injection; 0.625 mg vaginal cream
Short-acting estrogen mixture of conjugated estrogens including sodium estrone sulfate and sodium equilin sulfate.
Binds to intracellular receptors that stimulate DNA and RNA to synthesize proteins responsible for effects of estrogen.
Atrophic vaginitis, kraurosis vulvae, and abnormal bleeding (hormonal imbalance); also female hypogonadism, primary ovarian
failure, vasomotor symptoms associated with menopause; to retard progression of osteoporosis and as palliative therapy of
breast and prostatic carcinomas.
Postcoital contraceptive.
Breast cancer; known or suspected pregnancy (category X), lactation.
Hypertension; gallbladder disease; diabetes mellitus; heart failure; liver or kidney dysfunction, history of thromboembolic
disease.
Menopause, Osteoporosis, Atrophic Vaginitis, Kraurosis Vulvae
Adult: PO 0.3–1.25 mg/d for 21 d each month, adjust to lowest level that gives symptom control ( 0.625
mg/d) IV/IM 25 mg, repeated in 6–12 h if needed Topical 2–4 g of cream/d
Female Hypogonadism
Adult: PO 2.5–7.5 mg/d in 1–3 divided doses for 20 d, followed by a 10 d rest period
Postcoital Contraception
Adult: PO 30 mg/d in divided doses for 5 consecutive days beginning within 72 h of coitus
Breast Cancer
Adult: PO 10 mg t.i.d. for at least 3 mo
Prostatic Cancer Palliation
Adult: PO 1.25–2.5 mg t.i.d.
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Oral
- Give cyclically except when used for treatment of postpartum breast engorgement and for palliation of cancer. Cyclic regimen
is to dose for 3 wk followed by 1 wk off.
Topical
- Use calibrated dosage applicator dispensed with the cream.
Intramuscular
- Reconstitute by first removing approximately 5 mL of air from the dry-powder vial, then slowly inject the supplied diluent
to the vial by aiming it at the side of the vial. Gently agitate to dissolve but DO NOT SHAKE.
- Use within a few hours of reconstitution.
| Intravenous PREPARE: Direct: Reconstitute as for IM injection.
ADMINISTER: Direct: Give slowly at a rate of 5 mg/min. Estrogen solution is compatible with D5W and NS and may be added to IV tubing just distal
to the needle if necessary.
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- Store ampule and reconstituted solution at 2°–8° C (38°–46° F) and protected from light; stable
for 60 d. Discard precipitated or discolored solution.
CNS: Headache, dizziness, depression, libido changes. CV: Thromboembolic disorders, 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.
Drug: barbiturates, carbamazepine, phenytoin, rifampin decrease estrogen effect by increasing its metabolism; oral anticoagulants may decrease hypoprothrombinemic effects; interfere with effects of bromocriptine; may increase levels and toxicity of cyclosporine, tricyclic antidepressants, theophylline; decrease effectiveness of clofibrate.
Absorption: Rapid absorption from GI tract; readily absorbed through skin and mucous membranes (including vaginal mucosa); slow absorption
from IM injections. Distribution: Distributed throughout body tissues, especially in adipose tissue; crosses placenta, excreted in breast milk. Conjugated estrogens
are bound primarily to albumin. Metabolism: Metabolized primarily in liver to glucuronide and sulfate conjugates of estradiol, estrone, and estriol. Elimination: Excreted in urine. Half-Life: 4–18 h.
Assessment & Drug Effects
- See additional 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.
- Monitor bone density annually when used for osteoporosis prophylaxis.
Patient & Family Education
- Be aware of importance of taking drug exactly as prescribed: Specifically, do not omit, increase, or decrease doses without
advice of physician.
- 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.
- Notify physician promptly of adverse symptoms.
- Risk of blood clot formation is high with morning after pill. Know signs of thrombophlebitis (see Appendix F).
- Review package insert to ensure understanding of estrogen therapy.
- Do not breast feed while taking this drug.
1%)
Prototype drug