CONJUGATED ESTROGENS

AbsorptionConjugated estrogens are water-soluble and are absorbed from the gastrointestinal tract after release from the drug formulation. The Conjugated Estrogens Tablets release CE slowly over several hours. Table 2 summarizes the mean pharmacokinetic parameters for unconjugated and CE following administration of 1 × 0.625 mg and 1 × 1.25 mg tablets to healthy postmenopausal women. Food effect: The pharmacokinetics of Conjugated Estrogens Tablets 0.45 mg and 1.25 mg tablets were assessed foll...

14.1 Effects on Vasomotor Symptoms In the first year of the Health and Osteoporosis, Progestin and Estrogen (HOPE) Study, a total of 2,805 postmenopausal women (average age 53.3 ± 4.9 years) were randomly assigned to one of eight treatment groups of either placebo or CE, with or without MPA. Efficacy for vasomotor symptoms was assessed during the first 12 weeks of treatment in a subset of symptomatic women (n = 241) who had at least seven moderate to severe hot flushes daily, or at least 50 moderate to severe hot flushes during the week before randomization. Conjugated Estrogens Tablets (0.3 m...

The following serious adverse reactions are discussed elsewhere in labeling:

• Cardiovascular Disorders [see Boxed Warning , Warnings and Precautions (5.1) ]
• Malignant Neoplasms [see Boxed Warning , Warnings and Precautions (5.2) ] Most common adverse reactions (≥5%) are: abdominal pain, asthenia, pain, back pain, headache, flatulence, nausea, depression, insomnia, breast pain, endometrial hyperplasia, leucorrhea, vaginal hemorrhage, and vaginitis. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS...

Conjugated Estrogens Tablets therapy is contraindicated in individuals with any of the following conditions:

• Undiagnosed abnormal genital bleeding [see Warnings and Precautions (5.2) ]
• Breast cancer or a history of breast cancer except in appropriately selected patients being treated for metastatic disease [see Warnings and Precautions (5.2) ]
• Estrogen-dependent neoplasia [see Warnings and P...

• Estrogens increase the risk of gallbladder disease ( 5.4 )
• Discontinue estrogen if severe hypercalcemia, loss of vision, severe hypertriglyceridemia or cholestatic jaundice occurs ( 5.5 , 5.6 , 5.10 , 5.11 )
• Monitor thyroid function in patients on thyroid replacement therapy ( 5.12 , 5.19 ) 5.1 Cardiovascular Disorders An increased risk of stroke and DVT has been reported with estrogen-alone therapy. An increased risk of PE, DVT, stroke and MI has been reported with estrogen plus progestin...

7 DRUG INTERACTIONS Data from a single-dose drug-drug interaction study involving CE and MPA indicate that the pharmacokinetic disposition of both drugs is not altered when the drugs are coadministered. No other clinical drug-drug interaction studies have been conducted with CE. Inducers and/or inhibitors of CYP3A4 may affect estrogen drug metabolism ( 7.1 ) 7.1 Metabolic Interactions In vitro and...