sodium 13-methyl-17-oxo-3-sulfonatooxy-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[ a] phenanthrene
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Absorption Well absorbed from GI tract. The tablets slowly release the drug over several hours.
Distribution Bound to sex hormone–binding globulin and albumin. Widely distributed and generally found in higher concentration in the sex hormone target organs. Crosses the placenta.
Metabolism Partially metabolized by CYP3A4. Metabolized in the liver and undergoes enterohepatic recirculation. Estradiol is converted reversibly to estrone, and both can be converted to estriol (major urinary metabolite).
Elimination Estradiol, estrone, and estriol are excreted in the urine along with glucuronide and sulfate conjugates.
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Corticosteroids (eg, prednisone) Increased pharmacologic and toxicologic effects of corticosteroids may occur.
Hydantoins (eg, phenytoin) Loss of seizure control or decreased estrogenic effects may occur.
Inducers of CYP3A4 (eg, barbiturates [eg, phenobarbital], bosentan, carbamazepine, modafinil, rifampin, St. John's wort, topiramate) May reduce plasma estrogens, resulting in a decrease in therapeutic effects and changes in uterine bleeding profile.
Inhibitors of CYP3A4 (eg, azole antifungal agents [eg, itraconazole, ketoconazole], grapefruit juice, macrolide antibiotics [eg, clarithromycin, erythromycin], ritonavir) May elevate estrogen plasma levels, resulting in increased adverse reactions.
Thyroid hormones (eg, levothyroxine) Serum free thyroxine concentrations may be decreased, increasing serum thyrotropin concentrations and the need for thyroid hormone.
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