![]() ![]() Table 1: Mean (SD) Pharmacokinetic Parameters of Amethyst™ Over a 28-Day Dosing Period Levonorgestrel Levonorgestrel and ethinyl estradiol concentrations did not increase from days 14 to 28, but did increase from days 1 to 28. The plasma concentrations of levonorgestrel and ethinyl estradiol reached steady-state by approximately day 14. Ethinyl estradiol is rapidly and almost completely absorbed from the gastrointestinal tract but, due to first-pass metabolism in gut mucosa and liver, the bioavailability of ethinyl estradiol is between 38% and 48%.Ī summary of the single dose and multiple dose levonorgestrel and ethinyl estradiol pharmacokinetic parameters for 18 women under fasting conditions is provided in Table 1. However, literature indicates that levonorgestrel is rapidly and completely absorbed after oral administration (bioavailability about 100%) and is not subject to first-pass metabolism. No specific investigation of the absolute bioavailability of Amethyst™ in humans has been conducted. Although the primary mechanism of this action is inhibition of ovulation, other alterations include changes in the cervical mucus (which increase the difficulty of sperm entry into the uterus) and the endometrium (which reduce the likelihood of implantation). ![]() ![]() Related/similar drugs norethindrone, levonorgestrel, medroxyprogesterone, Depo-Provera, Provera, Mirena CLINICAL PHARMACOLOGY Mode of ActionĬombination oral contraceptives act by suppression of gonadotropins. ![]()
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