Estrogens and Progestin Drugs Flashcards
Estrogen components:
Ethinyl estradiol
Mestranol
Progestin components: Desogestrel Norgestrel Drospirenone* Norethrindone
Oral Contraceptives - Daily pill
•Inhibit FSH & LH secretion (Inhibits ovulation)
•Thickens cervical mucus
•Thins endometrium
Levonorgestrel NORPLANT
Implanted Contraceptives (Subdermal silastic capsules)
•Inhibit FSH & LH secretion (Inhibits ovulation)
•Thickens cervical mucus
•Thins endometrium
Medroxyprogesterone DEPOPROVERA
Injected Contraceptives (Injected intramuscularly)
•Inhibit FSH & LH secretion (Inhibits ovulation)
•Thickens cervical mucus
•Thins endometrium
Estradiol & Norethrindone ORTHO EVRA
Patch Contraceptives
•Inhibit FSH & LH secretion (Inhibits ovulation)
•Thickens cervical mucus
•Thins endometrium
Levonorgestrel MIRENA
Drug Coated IUD Contraceptive
•Local: Thickens cervical mucus
•Systemic: inhibit FSH & LH secretion (Inhibits ovulation)
Local Effects > Systemic Effects
•Side Effects
As any progestin but less likely given low systemic concentration
(Low) potential for osteoporosis
Estradiol & Norethrindone NUVARING
Drug Impregnated Vaginal Ring Contraceptive
•Local: Thickens cervical mucus
•Systemic: inhibit FSH & LH secretion (Inhibits ovulation)
“Emergency Contraception”
Also known as Plan B Contraception Also known as Day After Contraception •Inhibit FSH & LH secretion (Inhibits ovulation) •Thickens cervical mucus •Thins endometrium
Estradiol Norethrindone Estradiol & Medroxyprogesterone Estradiol & Morethrindone Estradiol & Testosterone
Non Contraceptive Uses •Uses •Treatment of estrogen dependent tumors •Prevention/Treatment of osteoporesis •Prevention of cardiovascular pathologies occurrence and/or consequence in postmenopausal women: Stroke, MI •Prevention of uterine cancer •Restoration of sexual libido
Tamoxifen
Non Contraceptive Estrogen Receptor Antagonist
•Antagonist at estrogen receptors in breast (Prevents cell replication in tumors where estrogen induces tumor growth)
•Inactive at other estrogen receptors
•Use: Breast cancer
Raloxifene
Non Contraceptive Estrogen Receptor Agonist
•Agonist at estrogen receptors in bone (Promotes bone growth and Reduces bone resorption)
•Inactive at other estrogen receptors
•Use: Prevention & treatment of osteoporosis
Clomiphene
Non Contraceptive Estrogen Receptor Agonist
•Partial agonist at estrogen receptors in brain
Functionally antagonist
Prevents estrogen inhibition of GnRH secretion from hypothalamus
Induces GnRH secretion leading to follicle maturation and ovulation
•Inactive at other estrogen receptors
•Use: Treatment of anovulatory infertility
Mifepristone (RU486)
Non Contraceptive Progesterone Receptor Antagonist
•Antagonist at progesterone receptors
Prevents implantation of fertilized egg
Prevents critical progesterone maintenance of pregnancy
Induces endometrium break down
“Abortifacient”
•Use: Pregancy termination
Hydroxyprogesterone
Non Contraceptive Progesterone Receptor Agonists
•Agonist at progesterone receptors
•Mimics critical endogenous progesterone maintenance of pregnancy
•Use: Prolongs pregnancy
Prevents “spontaneous miscarriage”
Prevents premature labor
