Estrogens and Progestins

Question 1

Two cells of steroidogenesis in females

regulatory molecules (2)?

Answer 1

Theca

Granulosa

gonadotropins, LH and FSH

Question 2

Steroidogenesis regulated by what?

Answer 2

feedback regulation

Question 3

Estrogen and Progesterone exert what types of feedback?

Answer 3

both NEGATIVE AND POSITIVE

Positive occurs MID-OVARIAN CYCLE (day 14)

Question 4

Phases of Menstrual Cycle

associated hormones (2)? What does each control?

Answer 4

Follicular - estrogen rises, low amplitude LH secretion

Ovulation - estrogen induced gonadotropin surge

Luteal - rise in estrogen and progesterone,

progesterone controls DIFFERENTIATION

Estrogen controls PROLIFERATION

Question 5

Endogenous steroids bind to?

Answer 5

INTRACELLULAR RECEPTORS - modulate transcriptional activity

AGONISTS/ANTAGONISTS COMPETE FOR INTRACELLULAR SITES

Question 6

Estrogen effects - HPG Axis? Endometrium? Metabolic? Development? Menstrual cycle?

Answer 6

feedback regulation on HPG axis

proliferation of endometrium

Good cholesterol effects
Anti-resorptive for bone
Increase plasma proteins from liver
Increase coagulation factors, decrease anti-thrombin

Ovary, fallopian tubes, uterus, vagina, breast development

FOLLICULAR PHASE of cycle

Question 7

Progesterone effects - - HPG Axis? Endometrium? Metabolic? Development? Menstrual cycle? Cervical Glands?

Answer 7

feedback regulation on HPG axis

DIFFERENTIATION of endometrium, decrease uterine contraction

Bad cholesterol effects
Increase fasting glucose

Ovary, fallopian tubes, uterus, vagina, breast development

LUTEAL PHASE of cycle

INCREASE CERVICAL MUCOUS VISCOSITY

Question 8

Natural steroidal estrogens

Answer 8

Estradiol
Estrone
Estriol

Conjugated equine estrogens

Question 9

Synthetic steroidal estrogens

Chemical modification has what effect?

Answer 9

Ethinyl estradiol
Mestranol

INCREASES HALF-LIFE

ethinyl group - DECREASES 1st PASS EFFECT

Question 10

Dosing of natural vs synthetic

Answer 10

HIGHER DOSAGE FOR NATURAL ESTROGENS

Question 11

Estrogen therapy in hypogonadism goals

Answer 11

promote development of female sex characteristics

Question 12

Estrogen therapy in hormone replacement goals

Answer 12

HPG axis - feedback on gonadotropins
Endometrium proliferation
Anti-resorption of bone
Development

maintain bone density, suppress hot flashes, suppress urogenital atrophy

Question 13

Estrogen Risks and Benefits

Answer 13

increased risk of coronary heart disease, stroke, PE, invasive breast cancer

decreased risk of colorectal cancer, hip fracture

Question 14

Estrogen therapy in contraception goals

Answer 14

NEGATIVE FEEDBACK PRESSURE ON HPG AXIS

progestins are not as effective

Question 15

Estrogen therapy in acne treatment

Answer 15

may suppress steroidogenesis

increase SHBG production in liver - DECREASING FREE TESTOSTERONE

ESTROGENIC COMPONENT, not progestin component suppresses acne

Question 16

Adverse effects of estrogen

Answer 16

breast tenderness
endometrial hyperplasia
increased blood coagulation

nausea, cholestasis, migraine, cancer, bloating

Question 17

Progestin use as contraceptive

Answer 17

alone or in combination with estrogen

negative feedback on HPG axis

Increases cervical mucous viscosity

Question 18

Mechanisms of Progestin use in Hormone replacement therapy, dysmenorrhea, and endometriosis

Answer 18

HRT - decrease risk of endometrial hyperplasia

Dysmenorrhea - decrease endometrial mass, decrease prostaglandin production

Endometriosis - decrease proliferation

Question 19

Adverse Effects of progestins

Adverse related to 19-nor compounds

Answer 19

breakthrough bleeding

impaired glucose tolerance

changes in lipid metabolism

19-Nor compounds – acne, hirsutism

Question 20

Mechanism of Action of Birth control

Answer 20

suppress LH and FSH

Alter cervical mucous

Alter endometrium

Question 21

Oral pill - hormones?
Injectable?
Implantable?
IUD?
Transdermal?
Vaginal Ring?

Answer 21

oral - estrogens and progestins or progestins alone

injectable - estrogens and progestins or progestins alone

implantable - progestins alone

IUD - progestins + copper

Transdermal - estrogens and progestins

Vaginal ring - estrogens and progestins

Question 22

Emergency contraception effectiveness

Answer 22

Combined - 25% failure

Progestin only - 12% failure

Question 23

Contraceptive Hormone Adverse Effects - 3 categories? Name some from each

Answer 23

Mild - nausea, mastalgia, breakthrough bleecding, edema, headache, withdrawal bleeding, serum protein changes

Moderate - breakthrough bleeding, weight gain, skin pigmentation, acne, hirsutism, vaginal infections, amenorrhea

Severe - thromboembolic disease, MI, cerebrovascular disease, GI, depression, cancer?

Question 24

Non-contraceptive benefits of hormone birth control

Answer 24

reduced ovarian/endometrial cancer

reduce dysmenorrhea, endometriosis

decrease ectopic pregnancy

decrease benign breast disease

increase Hb concentrations

Suppress acne/hirsutism

Question 25

Contraindications of estogen containing contraceptives

Answer 25

known or suspected breast cancer or female reproductive tract cancer

thromboembolic disorders

liver disease

history of CV disease

smokers aged 35 and older

Question 26

Interactions of contraceptives

Answer 26

HIV agents, anti-convulsants, St. Johns Wort - INDUCE METABOLISM

Anti-biotics LOWER EFFECTIVENESS