How is ethinyl estradiol metabolized?
Metabolism: Steroidal estrogens, including estradiol, are metabolized primarily in the liver, where they are conjugated with sulfate and glucuronide. Because of the rapid metabolism, nonesterified forms of estrogen, including estradiol, must usually be administered daily.
How is the oral contraceptive pill metabolised?
After absorption, ethinyl estradiol (EE) undergoes first-pass metabolism in the liver by cytochrome P450 (CYP) 3A4. 3 CYP3A4 is responsible for most drug interactions, as it metabolizes more than 80% of all drugs affected by CYP.
How long does ethinyl estradiol stay in your system?
EE is a long-acting estrogen, with a nuclear retention of about 24 hours.
Where is birth control metabolized?
The reason that happens is that these drugs speed up the liver’s metabolism, which makes the liver metabolize the hormones in the birth control faster.
Are oral contraceptives inhibitors or inducers?
Less well appreciated, oral contraceptive steroids may themselves modify the metabolism and pharmacological activity of various other drugs (e.g., anticoagulants, benzodiazepines, beta-blockers, caffeine, corticosteroids, and tricyclic antidepressants); in this respect the oral contraceptives are acting as enzyme …
How does ethinyl estradiol affect the body?
ethinyl estradiol and levonorgestrel also causes changes in your cervical mucus and uterine lining, making it harder for sperm to reach the uterus and harder for a fertilized egg to attach to the uterus. Ethinyl estradiol and levonorgestrel is used as contraception to prevent pregnancy.
Do oral contraceptives affect metabolism?
Oral contraceptives also affect carbohydrate metabolism, primarily through the activity of progestin. Studies have demonstrated insulin resistance, rises in plasma insulin, and relative glucose intolerance by means of curve analysis of glucose tolerance tests.
Does metabolism affect birth control?
Both the estrogens and the progestins in OCs cause biochemical alterations which have metabolic consequences. Changes in glucose, lipid, and protein metabolism suggest that the dosage of both estrogens and progestins should be minimized as much as possible.
What is the pharmacokinetic profile of ethinyl estradiol and triazolam?
Pharmacokinetic profiles for ethinyl estradiol and for a single oral dose of triazolam (0.125 mg) were obtained the day before initiation of treatment with modafinil (200 mg for 7 days, followed by 400 mg for 21 days) or placebo (28 days).
How is ethinyl estradiol metabolized in the body?
Ethinyl estradiol is also extensively metabolized, both by oxidation and by conjugation with sulfate and glucuronide. Sulfates are the major circulating conjugates of ethinyl estradiol and glucuronides predominate in urine. The primary oxidative metabolite is 2-hydroxy ethinyl estradiol, formed by the CYP3A4 isoform of cytochrome P450.
What is the difference between norethindrone and ethinyl estradiol?
administered norethindrone ( 1). Norethindrone acetate and ethinyl estradiol are subject to first-pass metabolism after oral dosing, resulting in an absolute bioavailability of approximately 64% for norethindrone and 43% for ethinyl estradiol ( 1-3). Distribution
What is the absolute bioavailability of norethindrone acetate and ethinyl estradiol?
Norethindrone acetate and ethinyl estradiol are subject to first-pass metabolism after oral dosing, resulting in an absolute bioavailability of approximately 64% for norethindrone and 43% for ethinyl estradiol ( 1-3). Distribution Volume of distribution of norethindrone and ethinyl estradiol ranges from 2 to 4 L/kg (1-3