Top Gene Interactions
- Metabolism: Hepatic. Quantitatively, the major metabolic pathway for ethinyl estradiol, both in rats and in humans, is aromatic hydroxylation, as it is for the natural estrogens. Half Life: 36 +/- 13 hours
- Uses/Sources: For treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.
- Symptoms: Symptoms of overdose include nausea and vomiting, and withdrawal bleeding may occur in females. The FDA label includes a black box warning that states that combination oral contraceptives with ethinyl estradiol should not be used in women over 35 years old who smoke due to the increased risk of serious cardiovascular side effects.
- Route of Exposure: Rapid and complete absorption follows oral intake of ethinyl estradiol (bioavailability 43%).
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: Oral, mouse LD<sub>50</sub>: 1737 mg/kg.
Mechanism of Action
|Target Name||Mechanism of Action||References|
Estrogen receptor beta
Cytochrome P450 3A5
Nuclear receptor subfamily 1 group I member 2
Sodium-dependent serotonin transporter
Sodium-dependent dopamine transporter
Sodium-dependent noradrenaline transporter
Cytochrome P450 2C9
Cytochrome P450 2C19
Nuclear receptor subfamily 1 group I member 3
Cytochrome P450 2C18
Cytochrome P450 2J2
Bile acid receptor