Desogestrel: Mechanism of Action
Desogestrel is a hormonal agent used for contraception, hormone replacement therapy, or the management of menstrual and gynecological disorders.
Hormonal contraceptives suppress ovulation and alter reproductive tract conditions through progestin and/or estrogen receptor actions.
How It Works
Hormonal contraceptives contain synthetic progestins (±ethinylestradiol) acting on the hypothalamic-pituitary-gonadal (HPG) axis. Progestins bind progesterone receptors (PR-A and PR-B), suppressing GnRH pulsatility → reduced LH and FSH secretion → ovulation suppression. Combined OCP also uses estrogen to suppress FSH-driven follicular development. Additional mechanisms: cervical mucus thickening (reducing sperm penetration), endometrial thinning (reducing implantation potential), and altered fallopian tube motility. Different progestins vary in receptor affinity: drospirenone is anti-androgenic with anti-mineralocorticoid activity; levonorgestrel has mild androgenic activity.
Receptor / Target Profile
- •Progesterone receptors (PR-A, PR-B) — primary target; ovulation suppression
- •GnRH receptor (hypothalamic) — indirect suppression via negative feedback
- •Androgen receptor (AR) — varies: drospirenone anti-androgenic; levonorgestrel mildly androgenic
- •Glucocorticoid receptor — modest affinity for some progestins
- •Mineralocorticoid receptor — drospirenone has anti-mineralocorticoid (anti-aldosterone) activity
Pharmacokinetics
Onset of Action
Ovulation suppression: within 7 days if initiated day 1–5 of cycle; cervical mucus changes within 48 hours
Half-Life (t½)
Ethinylestradiol: ~24 hours; Levonorgestrel: ~24 hours; Drospirenone: ~30 hours; Desogestrel (active metabolite etonogestrel): ~30 hours
Oral bioavailability: ethinylestradiol ~45%; levonorgestrel ~100%; drospirenone ~76%. Extensive first-pass hepatic metabolism. Enterohepatic recirculation of ethinylestradiol. Depot medroxyprogesterone (IM) provides 3-month contraception via slow release.
Conditions Treated with Desogestrel
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