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Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation...

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Oral Oral Contraceptives Contraceptives Estrogen and Progestin
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Page 1: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

Oral Oral ContraceptivesContraceptivesEstrogen and Progestin

Page 2: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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What we will be What we will be talking about todaytalking about today

• Hormones

• Ovulation

• History of Oral Contraceptives

• Uses of Oral Contraceptives

• Estrogen and Progestin

• Types of Oral Contraceptives

• Future of Oral Contraceptives

Page 3: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Hormones Hormones = “chemical messenger from one cell to another”

4 classes of Hormones• Amine Derived Hormones• Peptide Hormones• Steroid Hormones• Lipid and Phospholipid Hormones

Steroid 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

• http://highered.mcgraw-hill.com/sites/0072437316/student_view0/chapter47/animations.html#

cholesterol

Page 4: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Interaction of Hormones Interaction of Hormones with Surface Proteinswith Surface Proteins

Page 5: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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OvulationOvulation• Follicular 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

Page 6: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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OvulationOvulation

Page 7: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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History of Oral History of Oral ContraceptivesContraceptives

• 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”• 1963- 1st 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

Page 8: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Uses of Oral Uses of Oral ContraceptivesContraceptives

• Primary Use– Prevent pregnancy

• Secondary Uses– Heavy or irregular menstruation– Endometriosis– polycystic ovary syndrome – dysfunctional uterine bleeding

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What’s in “The Pill”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

Page 10: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Combined mode of Combined mode of action of estrogen and action of estrogen and

progestinprogestin• Prevents ovulation• Thickens mucous in cervix• Thins endometrium

Page 11: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Gonadotropin Gonadotropin Releasing Hormone Releasing Hormone

(GnRH)(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

Page 12: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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EstrogenEstrogen• 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

Page 13: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Naturally occurring Naturally occurring estrogensestrogens

Estradiol

Estrone

Estriol

Page 14: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Conversion of Conversion of testosterone to testosterone to

estradiolestradiol

Testosterone Estradiol

Page 15: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Synthetic EstrogensSynthetic Estrogens

Page 16: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Estrogen ReceptorsEstrogen ReceptorsTwo types of Receptors• ER alpha• ER beta

Mode of Action-1) Estrogen passes through

phospholipid bilayer2) 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

Page 17: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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ProgesteroneProgesterone• 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

Page 18: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Conversion of Conversion of pregnenolone to pregnenolone to

progesteroneprogesterone

pregnenolone progesterone

Page 19: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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ProgestinsProgestins

• Types1) 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

Page 20: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Structure of Structure of ProgestinsProgestins

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Brands of Oral Brands of Oral ContraceptivesContraceptives

• Alesse• Brevicon• Cyclessa• Demulen • Desogen • Estrostep • Genora• Intercon• Jenest • Levlen • Levlite• Levora

• Loestrin• Lo/Ovral• Mircette• ModiCo • Necon • N.E.E. • Nelova• Nordette • Norethin• Norinyl• Ortho-Cept • Ortho-Cyclen

• Ortho-Novum • Ortho Tri-Cyclen• Ovcon• Ovral• Tri-Levlen• Tri-Noriny • Triphasil • Trivora• Zovia

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Side Effects of Oral Side Effects of Oral ContraceptivesContraceptives

• 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

Page 23: Oral Contraceptives Estrogen and Progestin. 2 What we will be talking about today Hormones Ovulation History of Oral Contraceptives Uses of Oral Contraceptives.

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Future of Oral Future of Oral ContraceptivesContraceptives

• 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

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ReferencesReferences• http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a601

050.html• http://en.wikipedia.org/wiki/Estrogen• http://users.rcn.com/jkimball.ma.ultranet/BiologyPages/S/Sex

Hormones.html• http://www.emc.maricopa.edu/faculty/farabee/biobk/BioBookR

EPROD.html• http://en.wikipedia.org/wiki/Gonadotropin_releasing_hormone• http://www.contraceptiononline.org/slides/slide01.cfm?

q=progestin+chemical+structures&dpg=1• http://users.rcn.com/jkimball.ma.ultranet/BiologyPages/H/

Hormones.html• http://www.contraceptiononline.org/contrareport/

article01.cfm?art=93• http://users.rcn.com/jkimball.ma.ultranet/BiologyPages/G/

G_Proteins.html

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Thank youThank you


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