esterified estrogens, Estratab (discontinued); Menest
Omudhome Ogbru, PharmD
Omudhome Ogbru, PharmD
Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.
Medical and Pharmacy Editor:
GENERIC NAME: esterified estrogens
BRAND NAME: Estratab (Discontinued in the USA); Menest
DRUG CLASS AND MECHANISM: Esterified estrogens are a mixture of several estrogens, a type of female hormone. Estrogens cause growth and development of female sex organs and the maintenance of sex characteristics, including growth of underarm and pubic hair and shaping of body contours and skeleton. Estrogens also increase secretions from the cervix and promote growth of the inner lining of the uterus (endometrium).
GENERIC AVAILABLE: Yes
PREPARATIONS: Tablets: 0.3, 0.625, 1.25, and 2.5 mg.
STORAGE: Tablets should be stored between 2 C (36 F) and 30 C (86 F).
PRESCRIBED FOR: Esterified estrogens are prescribed for the treatment of the common symptoms associated with menopause (for, example, hot flashes and vaginal dryness), dysfunctional (excessive and painful) uterine bleeding, female castration, female hypogonadism (reduced production of female hormones by the ovaries), prostate cancer, and breast cancer.
DOSING: The dose for menopause and related conditions is 0.3 to 1.25 mg daily for 3 weeks then 1 week off. Female hypogonadism is treated with 2.5 to 7.5 mg daily for 20 days then 10 days off. Breast cancer is treated with 10 mg three times daily for at least 3 months and the dose for prostate cancer is 1.25 to 2.5 mg 3 times daily.
DRUG INTERACTIONS: Estrogens increase the liver's ability to manufacture proteins that are required for blood to clot. Therefore, patients receiving warfarin (Coumadin), which reduces clotting ("thins" the blood) by inhibiting the production of proteins required for clotting, should receive clotting tests if an estrogen is added to their treatment. If blood clots too easily, the dose of warfarin may need to be increased.
Rifampin, barbiturates, carbamazepine (Tegretol), griseofulvin, phenytoin (Dilantin) and primidone can increase the elimination of estrogen by enhancing the liver's ability to metabolize (destroy) it. Use of these drugs may result in a reduction of the beneficial effects of estrogens. Conversely, drugs such as erythromycin, ketoconazole (Nizoral), itraconazole (Sporanox), and ritonavir (Norvir) may reduce the elimination of estrogens by the liver and lead to increased levels of estrogens in the blood. Grapefruit juice also may increase levels of estrogen by increasing the absorption of estrogens from the intestine. Increased levels of estrogens in the blood may result in more estrogen-related side effects.
PREGNANCY: Estrogens should not be used during pregnancy because of an increased risk of fetal abnormalities.
NURSING MOTHERS: Estrogens are secreted in milk and cause unpredictable effects in the infant. Therefore, they generally should not be used during breastfeeding.
SIDE EFFECTS: Among the most common endocrine side effects are breakthrough bleeding or spotting, loss of periods, or excessively prolonged periods, breast pain, breast enlargement, and changes in sexuality (increase or decrease in libido).
Estrogens also may cause gallstones, hepatitis, migraine headaches, and fluid retention (swelling of the lower legs). Melasma (tan or brown patches) may develop on the forehead, cheeks, or temples. These may persist even after the estrogen is stopped. Estrogens may cause an increase in the curvature of the cornea, and, therefore, patients with contact lenses may develop intolerance to their lenses.
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