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Estrogen and Progestin

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Presentation on theme: "Estrogen and Progestin"— Presentation transcript:

1 Estrogen and Progestin
Oral Contraceptives Estrogen and Progestin

2 What we will be talking about today
Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives Estrogen and Progestin Types of Oral Contraceptives Future of Oral Contraceptives

3 Hormones = “chemical messenger from one cell to another”
4 classes of Hormones Amine Derived Hormones Peptide Hormones Steroid Hormones Lipid and Phospholipid Hormones -derived from cholesterol -primarily produced in adrenal cortex or gonads Types of Steroid Hormones Anabolic steroids Corticosteroids Sex hormones Major steps in Steroid Hormone Binding cholesterol

4 Interaction of Hormones with Surface Proteins

5 Ovulation Follicular phase Ovulation Phase
LH and FSH concentrations increase due to GnRH Follicular growth Antrum fluid volume increases Blister forms in ovary Ovulation Phase Follicle released from ovary  secretes estrogen Corpus lueteum triggers release of progesterones and estrogens

6 Ovulation

7 History of Oral Contraceptives
1937- discovery of effects of progesterone on ovulation 1940’s- Russell Marker isolates progesterone from Mexican yams 1951- Luis Miramontes synthesizes 1st progestin 1960- FDA approves “the pill” st oral contraceptive put on drug market 1965- number one form of birth control Late 1970’s- FDA mandated warning that indicated oral contraceptives carried risks of cancer and blood clots

8 Uses of Oral Contraceptives
Primary Use Prevent pregnancy Secondary Uses Heavy or irregular menstruation Endometriosis polycystic ovary syndrome dysfunctional uterine bleeding

9 What’s in “The Pill” 20-40 micrograms ethinyl estradiol (synthetic form of estrogen) Varying amounts of either levonorgestrel or norethindrone as the progestagen component Types of Regimens 21-day or 28-day pack

10 Combined mode of action of estrogen and progestin
Prevents ovulation Thickens mucous in cervix Thins endometrium

11 Gonadotropin Releasing Hormone (GnRH)
Synthesized by hypothalamus Stimulates anterior pituitary gland to release FSH and LH A decapetide (contains 10 amino acids) pGlu-His-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 secretion begins at puberty Primary Effects secretion of estrogen and progesterone in females secretion of testosterone in males

12 Estrogen Primary female sex hormone Roles of estrogen:
To develop secondary female sex characteristics Thicken the endometrium Regulate menstrual cycle Regulation Production of estrogen regulated by Follicle Stimulating hormone (FSH) and Luetinizing hormone (LH), both produced in the anterior lobe of the pituitary gland Hypothalamus→GnRH→ Pituitary→FSH→Follicle→Estrogens

13 Naturally occurring estrogens
Estradiol Estriol Estrone

14 Conversion of testosterone to estradiol
Testosterone Estradiol

15 Synthetic Estrogens

16 Estrogen Receptors Two types of Receptors ER alpha ER beta
Mode of Action- 1) Estrogen passes through phospholipid bilayer 2) Ligand binds in hydrophobic region of receptor forming cap over ligand binding pocket 3) Estrogen and ER complex bind to estrogen response element in the nucleus to initiate transcription 4) Translation creates proteins which target various organs and processes in the female body

17 Progesterone synthetic form of progesterone Produced by Adrenal glands
Gonads Brain Placenta (only during pregnancy) Regulation- stimulated by the production of LH Hypothalamus→GnRH→ Pituitary→LH→Corpus luteum→Progesterone Primary Effect- prepares uterus for implantation by the proliferation of endometrium; prepares body for pregnancy Natural progesterone- destroys digestive system when consumed orally ALL oral contraceptives contain progestin, synthetic form of progesterone

18 Conversion of pregnenolone to progesterone
pregnenolone progesterone

19 Progestins Types Role Binding 1) C19- derived from testosterone
2) C21- derived from progesterone Role in adequate doses it inhibits ovulation Makes your body think that it is pregnant Reduces levels of FSH and LH Binding Interacts with progesterone receptors either by entering cells through phospholipid bilayer or by interacting with surface proteins

20 Structure of Progestins

21 Brands of Oral Contraceptives
Loestrin Lo/Ovral Mircette ModiCo Necon N.E.E. Nelova Nordette Norethin Norinyl Ortho-Cept Ortho-Cyclen Alesse Brevicon Cyclessa Demulen Desogen Estrostep Genora Intercon Jenest Levlen Levlite Levora Ortho-Novum Ortho Tri-Cyclen Ovcon Ovral Tri-Levlen Tri-Noriny Triphasil Trivora Zovia

22 Side Effects of Oral Contraceptives
Changes in: Weight Sexual desire Vaginal discharge Menstrual flow Breast size Blood pressure complexion Other Common side effects: Breakthrough bleeding Nausea headaches Urinary tract infection Depression Gum inflammation

23 Future of Oral Contraceptives
Researchers continually trying to minimize adverse side effects of oral contraceptives Pharmaceutical companies have to compete with latest forms of contraception Contraceptive vaccines Vaginal rings Intrauterine Contraception Cervical caps Transdermal patch Implants and injectables

24 References

25 Thank you

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