Sex Hormones

Question 1

Estrogen is produced by

Answer 1

developing ovarian follicles

Question 2

Which are the natural Estrogens

Answer 2

17-B Estradial
Estrone
Estriol

Question 3

Metabolism of Natural Estrogens

Answer 3

Large 1st pass hepatic metabolism
short T1/2

Question 4

What is a Natural Estrogen

Answer 4

most potent and principal Estrogen secreted by ovary

Question 5

Which are the Synthetic Estrogens

Answer 5

Ethinyl Estradial
Mestranol

Question 6

Metabolism of Synthetic Estrogens

Answer 6

less 1st pass metabolism
much longer T1/2

Question 7

How are Estrogens transported

Answer 7

by binding to SHBG(binds NE more) and Albumin

Question 8

Action of Synthetic Estrogens

Answer 8

Decr. GNRH from hypothalamus–> decr. FSH and LH release

Question 9

Metabolic effects of Estrogen

Answer 9

Bone mass: decr. activity of osteolcasts–> decr. bone resorption
Lipid M: incr. in trigs and HDL, decr. in cholesterol and LDL
Carbohydrate M: can impair glucose tolerance and induce insulin resistance
Protein M
Blood: decr. Antithrombin III levels=incr risk of blood clots and thrombosis
CVS: causes arteriolar vasoldilation
Skin: decr. sebum production

Question 10

AEs of Estrogen

Answer 10

NV
Fullness and tenderness of breast
Oedema
Migraine
Reactive/exacerbate Endometriosis
Gallbladder disease
Thromboembolis
Carcinogenic actions: endometrial+breast cancer
Glucose intolerance
Post menopausal uterine bleeding

Question 11

Uses of HRT

Answer 11

used to treat symptoms associated with meonopause

Question 12

Effects of Menopause

Answer 12

marked decr. in Ovarian Estrogen production–> low serum [Estradiol] + vasmotor symptoms like hot flashes

Question 13

What is a combined continuous HRT

Answer 13

progestin given daily with estrogen to prevent Endomterial proliferation and avoids bleeding

Question 14

What is a combined Sequential HRT

Answer 14

Progestin added for the last 10-14 days of the cycle to produce endometrial shedding and withdrarwal bleeding

Question 15

Indications of Estrogen Therapy

Answer 15

Osteoporosis: prevents bone loss
Urogenital Atrophy: dryness and itching of vagina, painful intercourse and urination, sudden/unexpected incontinence
Vasomotor symptoms: hot flushes, chilly sensations inappriopriate sweating and paresthias

Question 16

HRT CIs

Answer 16

Breast cancer
Past DVT or Pulmonary embolism: incr. risk of blood clotting bcos it decr. Antithrobin III
Active liver disease

Question 17

Cautions in HRT

Answer 17

Diabetes
Hypercholesterolaemia
Hypertension

Question 18

Indications of Estrogen Monotherapy

Answer 18

ONLY for women who had a Hysterectomy as progesterone unfavourably alters HDL:LDL ration

Question 19

Preparations of Estrogen Monotherapy

Answer 19

Conjugated estrogens
Estradiol
Estriol
Estrone

Question 20

Admin of Estrogen Monotherapy

Answer 20

Transdermal patch
SC implants
Vaginal Pessaries: oil based
Rings
Topical gel applications like sprays, patchs

Question 21

Which admin route of Estrogen bypassess 1st pass effect

Answer 21

Parenteral admin

Question 22

Which are the selective Estrogen Receptor Modulators

Answer 22

TTCR
Tamoxifen
Toremifene
Raloxifene
Clomiophen

Question 23

Activity of SERMs

Answer 23

have tissue selective activity
–> are Estrogenic on bone BUT have Anti-Estrogenic effects in Breast tissue

Question 24

Indications of Tamoxifen & Toremifene

Answer 24

Estrogen-dependent Breast cancer

Question 25

Effects of Tamoxifen & Toremifene

Answer 25

decr. total cholesterol and LDL No incr. in HDL and Trigs Incr. risk of DVT and pulmonary embolism

Question 26

Estrogenic effects of Tamoxifen & Toremifene

Answer 26

Estrogenic on bone, in blood and in Endometrium

Question 27

AEs of Tamoxifen & Toremifene

Answer 27

Hot flushes Vagial dryness/discharge Cataracts Nasuea

Question 28

Indications of Raloxifene

Answer 28

Prevention and Treatment of Osteoporosis

Question 29

Effects of Raloxifene

Answer 29

decr total Cholesterol Decr. LDL No effect on HDL

Question 30

Raloxifene have no effects on

Answer 30

breast tissue and endometrium Vasmotor symptoms

Question 31

Raloxifene is an agonist in

Answer 31

bone: distal sites and spinal column

Question 32

AEs of Raloxifene

Answer 32

Hot flushes Leg cranps Incr. risk of DVT and Pulmonary Embolism

Question 33

Estrogenic effects of Raloxifene

Answer 33

Estrogenic on bone and in blood

Question 34

Name an Antiestrogen

Answer 34

Clomiphene

Question 35

Indications of Clomiphene

Answer 35

treatment of infertility --> inhibits Estrogen Rs in Hypothalamus --> triggers PG to incr FSH+LH=initiation of ovulation

Question 36

Clomiphene is used in conjunction with

Answer 36

hCG

Question 37

Clomiphene acts as an

Answer 37

SERM: Selective Estrogen Receptor Modulator

Question 38

AEs of Clomiphene

Answer 38

Ovarian Hyperstimulation Incr. incidence of multiple births Ovarian Cysts Blurred vision Acidic mucous Hot flushes

Question 39

What is Tibolone

Answer 39

agent that acts as an agonist at Estrogen Rs

Question 40

Activity of Tibolone

Answer 40

Estrogenic Progestogenic Weak Androgenic

Question 41

Indications of Tibolone

Answer 41

HRT Endometriosis Breast cancer

Question 42

Tibolone relieves

Answer 42

Hot flushes insomnia vaginal dryness Prevents bone loss

Question 43

Tibolone is an Anti-Estrogenic at

Answer 43

Endometrium: has less stimulatory effects

Question 44

Name an Estrogen Receptor Antagonist/Downregulator

Answer 44

Fulvestrant

Question 45

Indications of Fulvestrant

Answer 45

hormone receptor positive or metasttatic cancer

Question 46

MOA of Estrogen Synthesis inhibitors

Answer 46

Continuous admin of long acting GNRH agonists--> inhibit ovarian synthesis of Estrogen

Question 47

Indications of Estrogen Synthesis inhibitors

Answer 47

Endometriosis Uterine Fibroids

Question 48

What is Aromatase

Answer 48

Enzyme that converts androgens to Estrogen

Question 49

MOA of Non-steroidal Aromatase Inhibitors

Answer 49

Decr. Estrogen by inhibiting Aromatase enzyme=decr. breast cancer risk *also inhibit testosterone conversion to Estradiol

Question 50

Which are the Non-steroidal Aromatase Inhibitors

Answer 50

Anastrozole Letrozole Exemestane

Question 51

Effects of Non-steroidal Aromatase Inhibitors

Answer 51

lead to Hypoestrogenic states

Question 52

AEs of Non-steroidal Aromatase Inhibitors

Answer 52

Insomnia vaginal dryness hot flushes